The invention discloses compositions, compounds, apparatuses and methods of using them to study bone mineralization and identify agents that regulate bone mineralization. Methods of using bone mineralization gene profiles and signatures for compound screening and research are also disclosed. Reagents for modulating ...
The present invention broadly relates to the synergistic attenuation of vesicular stomatitis virus (VSV). More particularly, the invention relates to the identification of combined mutation classes which synergistically attenuate the pathogenicity of VSV vectors in mammals and immunogenic compositions thereof.
...
The present application provides methods of modulating immune responses by using IL-22 in combination with at
least one of IL-17A, IL-17F, or IL-23 or by using an IL-22 antagonist, such as an antibody or a soluble receptor or a binding protein,
in combination with an antagonist of at least one of IL-17A, IL-17F, o...
Compounds of formula 1 or a pharmaceutically acceptable salt thereof are provided: I where R1 through R7 are defined herein. The compounds of formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.
The present application provides human antibodies and antigen binding fragments thereof that specifically bind to the human interleukin-21 receptor (IL-21R). The antibodies can act as antagonists of IL-21R activity, thereby modulating immune responses in general, and those mediated by IL-21R in particular. The discl...
This invention relates to the use bazedoxifene (l-[4-(2-azepan-l-y]-ethoxy)-benzyl]-2-(4-hydroxy-pheny])-3-methyl- lH-indol-5-ol) in the treatment or inhibition of osteoporosis and osteopenia related to aromatase inhibitor therapy.
The present invention provides a method for inhibiting mannitol-induced aggregation of a protein in a liquid formulation by increasing the protein concentration to an amount greater than 50 mg/ml. The present invention also provides methods for storing and preparing a liquid formulation containing mannitol and a pro...
The invention discloses novel intermediates in the production of Medrogestone (6,17a-dimethylpregna-4,6-diene-3', 20-dione) and pharmaceutical composition containing them.
The invention provides truncated biologically active ADAMTS polypeptides, particularly those with hyalectenase activity, and more particularly those with aggrecanase activity, that exhibit greater stability and homogeneity and higher expression yields than their full-length counterparts. The invention also provides ...
Semi-solid compositions comprising metaflumizone, a gelling agent and a non-aqueous solvent. The semi-solid compositions of this invention may be topically administered to animals, and are useful for preventing or treating, ectoparasitic infestations in warm-blooded animals for prolonged periods of time.
...
This invention provides a compound of formulae (I) or (II) having the structure or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflamma...
The present invention is directed to fused-aryl and heteroaryl derivatives of formula I, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointe...
This invention provides compounds of the formula wherein
A", X and Y are defined in the specification. These compounds are useful as
antibacterial agents.
Antigenic isolates and vaccines for Infectious Bursal Disease Virus include variants of the molecular Group 6 family of IBDV isolates, in particular the 28-1 isolate.
PROGESTERON RECEPTO ANTAGONIST CONTRACEPTIVE REGIMENS AND KITS A method of contraception is provided which involves delivery of 21 to 27 consecutive days of one or more PR antagonists in the absence of a progestin, estrogen, or other steroidal compound, followed by 1 to 7 days without any active agent. Also describe...
The invention describes an immunogenic composition for inducing an immune response to human immunodeficiency virus (HIV) in a vertebrate host, said immunogenic composition comprising: a) a first DNA plasmid comprising a single transcriptional unit comprising a nucleotide sequence that encodes an HIV gag-pol fusion p...
An oral, liquid pharmaceutical composition is provided. The composition comprises phenylephrine and substantially aldehyde-free polyethylene glycol. The composition has phenylephrine stability compatible with the stability required for commercial preparations. Optionally, the composition may comprise one or more add...
The present invention is directed to selective dopamine reuptake inhibitors, including (-)-l-(3,4-dichlorophenyl)-3-azabicyclo[3,1.0]hexane,(-)-l-(4methylphenyl)-3-azabicyclo [3.1.0]hexane, mazindol, methylphenidate, and l-[2[bis(4-fluoro phenyl)methoxy]ethyl]-4-(-3-phenylpropyl)piperazine, and methods of their use ...
The present invention is directed to racemic 1 -(3,4-dichlorophenyl)-3 -azabicyclo[3.1.0]hexane, (+)-l-(3,4-dichlorophenyl)-3 -
azabicyclo[3.1.O]hexane, racemic l-(4-methylphenyl)-3-
azabicyclo[3.1.0]hexane, and (+)-l-(4-methyiphenyl)-3-
azabicyclo[3.1.0]hexane, and methods of their use for treating certain ne...
The present invention provides compositions and methods useful for purifying recombinant myelin-associated glycoprotein (MAG) and fragments thereof. In particular, the invention provides a one-step purification method for MAG and MAG fragments. Novel forms of human recombinant MAG protein are also disclosed in addit...
Process for the preparation of l-[cyano (phenyl) methylj cyclohexanol compounds of general formula (I) in which R! is hydrogen, (C1-4) alkyl or (C1-4) alkoxy, wherein a compound uf general formula (II) in which Ri is as defined above, is reacted with cyclohcxanonc, the reaction being carried out in the presence of a...
An oral, highly bioavailable unit dosage form of O-desmethylvenlafaxine succinate (DVS) having a delayed release
of at least about one hour and a sustained release over multiple hours to provide a total release of greater than about 85 % within about
12 to about 14 hours is described. In one embodiment, the superb...
The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar- (R) 2-SO2-X and sulfonamides of Formula Ar-(R)2-SO2- NR4R5, where the constituent variables are as defined herein, that are useful as intermediates in the preparation of pharmaceuticals. The sulfonyl halides are...
The present application provides methods of purifying Aβ binding proteins having a Fc region, for example, anti-Aβ antibodies or antibody fusions, by adsorbing the Aβ binding protein to a Fc binding agent, such as, for example, Protein A or Protein G, followed by a wash with a divalent cation salt buffer to remove i...
Formulations are described that are suitable for storage of proteins, such as antibodies, over a relatively broad range of protein concentrations, pH, and buffer types. Also described are methods of storing a protein and methods of identifying a suitable formulation for storage of a specific protein. In general, a f...
The present invention is directed to a crystalline polymorph of pipindoxifene hydrochloride monohydrate, compositions containing the same, preparations thereof, and uses thereof.
The present invention is directed to racemic l-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, (+)-1 -(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, racemic 1 -(4-methylphenyl)-3-azabicyclo[3.1 .0]hexane, and (+)- l-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane, and methods of their use for treating certain nervous sy...
Methods and compositions for inhibiting interleukin-21 (IL-21)/IL-21 receptor (MU-1) activity using antagonists of IL-21 or IL-21 receptor ("IL-21R" or "MU-1"), are disclosed. IL-21 /IL-21 R antagonists can be used to induce immune suppression in vivo, e.g., for treating, ameliorating or preventing autoimmune "or in...
Pyrrole-oxindole derivatives useful as progesterone receptor antagonists, and methods for preparing the same, are provided. Pharmaceutical compositions containing these derivatives are described, as is the use thereof in contraception and hormone-related conditions.
The present invention relates to methods for synthesizing compounds useful as 5HT2C agonists or partial agonists, derivatives thereof, and to intermediates thereto.
The present invention provides a ß-lactam antibiotic such as cefepime and a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
Progesterone receptor modulators of formula (I), or a pharmaceutically acceptable salt thereof, Formula (I); wherein R1, R2, R3, R4, R5,
R6 and R7 are as defined herein. These compounds are useful for contraception and hormone replacement therapy. Also provided are products containing these compounds.
...
The use of compounds of formula (I), or a pharmaceutically acceptable salt thereof, (I) wherein R1, R2, R3, R4, R5, R6 and R7, are as defined herein, for contraception, hormone replacement therapy, synchronizing estrus, treating dysmenorrhea, treating dysfunctional uterine bleeding, treating uterine myometrial fibro...
A method of generating synthetic metabolites OF CCI-779 is provided. Five novel CCI-779 derivatives are described, as are methods of using these derivatives for detecting CCI-779 metabolites in samples.
Pyrrole-oxindole derivatives useful as progesterone receptor antagonists are provided. Pharmaceutical compositions these derivatives are described, as is the use thereof in contraception and .hormone-related conditions
The present invention is directed to a crystalline polymorph of pipindoxifene hydrochloride monohydrate, compositions containing the same, preparations thereof, and uses thereof
Compounds of the structure (I) are described, wherein R1, R2, R5, R6, V, X, Y, Z and Q are described herein, or a pharmaceutically acceptable salt, tautomer, metabolite or prodrug thereof. These compounds are useful for treating a variety of hormone-related conditions including contraception, treating or preventing ...
A method of treating obesity, cardiovascular diseases, and disorders of insulin metabolism in a subject, comprising administering to the subject a therapeutically effective amount of a GDF-8 inhibitor, and a therapeutically effective amount of at least one other therapeutic agent which treats the targeted syndrome.
...
The present invention provides methods of decreasing the frequency of emergence, decreasing the level of resistance, and delaying the emergence of a treatment-resistant Hepatitis C viral infection, by administering to a subject, either in combination or in series, an inhibitor of the Hepatitis C RNA-dependent RNA po...
A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
This invention provides estrogen receptor modulators of formula I, having the structure (I) wherein Q1 Q2, R1, R2 R2a, R3 R3a, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.
An implantable catheter or shunt (24) for draining fluid from a body cavity. The catheter or shunt body has a wall structure (28) that carries one or more therapeutic agents (26) in a manner enabling release of the therapeutic agent from the wall structure in situ after surgical implantation of the catheter or shunt...
A method of inducing an antigen-specific immune response in a mammalian subject includes the steps of administering
to the subject an effective amount of a first composition comprising a DNA plasrnid comprising a DNA sequence encoding
an antigen undet the cuntrol of regulatoty sequences directing expression thereo...
This invention relates to aggrccanasc polypeptides and aggrecanase polypeptide/ligand complexes, crystals of aggrecanase
and aggrecanase polypeptide/ligand complexes, and related methods and software systems.
This invention provides estrogen receptor modulators having the structure: (I) wherein R1, R2, R3, R4, Q, n, R9, R10, R11, and RH have been defined in the specification; or a pharmaceutically acceptable salt thereof. The invention further provides methods for the preparation and use of the compounds.
...
The present invention relates generally to phenanthridine carbonyl compositions such as substituted phenanthridine carbonyl phenols and methods of using them.
The invention relates to systems and methods for producing proteins of interest. The invention employs genetically-engineered animal or plant cells that have modified protein folding or processing capacities. In one aspect, the invention features genetically-engineered cells comprising one or more recombinant exp...
This invention provides 6H-[l]benzopyrano[4,3-b]quinoline compounds having the formula I: The invention further provides compositions including the compounds, methods for the use of the compounds, and the methods of preparation of the compounds.
The invention is directed to a process of synthesizing compouds of formula (VI), wherein R1, R9, R3, R4 and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) ...
A novel salt of O-desmethylvenlafaxine, O-desmethylvenlafaxine formate, is provided. Pharmaceutical compositions, dosage forms and methods of use are also provided.
The present invention relates to a pharmaceutical composition for modulating differentiation, development and activity of T-helper cell or cell population as herein described, comprising IL-21 or IL-21 modulators selected from an IL-21 antagonist of the kind such as herein described in the range of from 0.1 to 99.0%...
The present invention provides transdermal drug delivery devices (i. e., patches) comprising O-desmethylvenlafaxine
(ODV), a selective serotonin and norepinephrine re-uptake inhibitor, or a pharmaceutically acceptable salt thereof, which, among
other, offer the advantage of eliminating or reducing the adverse side...
wherein substitutions at R1 - R13, m and Y are set forth in the specification.
The invention is directed to a method of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the formula:
A vaccine composition and method which is effective in preventing or ameliorating Avian Influenza Virus infection is set forth herein. The vaccine contains at least two inactivated strains of avian influenza virus, wherein the combined haemoagglutinin (HA) total is at least about 256 HA/dose of the vaccine compositi...
The present invention is directed to a thermal covering that delivers consistent therapy to a portion of a user"s hand-wrist area, is easy to use and apply to the body, and is securely positionable on the body. The thermal covering can be entirely disposable after one use. The thermal covering can also have a dispos...
A serum-free insect cell culture medium is described which provides improvements in the maximum cell density supported and replication of insect viruscs within these cells, at a significantly lower cost than commercially available media. An improved method for preparing a lipid emulsion which is easy to scale and wh...
Disclosed herein is the use of LXR agonists
for preventing and treating osteoarthritis as well as methods of delecting an osteoarthritic phenotype in a subject and methods of identifying an LXR ligand capable of
reducing an osteoarthritic effect in cartilage.
The present invention relates to, among other embodiments, protein complexes which include tumor necrosis factor alpha (TNF-<) and/or tumor necrosis factor alpha receptor (TNFR). Preferably, the complexes comprise at least one polypeptide selected from the group consisting of: NF-KB activating kinase (NAK), RasGAP3,...
The present invention provides a safe and effective vaccine composition against West Nile virus disease. An immunogenically active component of West Nile virus or plasmid DNA, an adjuvant such as a metabolizable oil, and a pharmacologically
acceptable carrier are formulated into an immunizing vaccine. The invention...
The invention provides the use of a combination of an mTOR inhibitor such as a rapamycin and an antimetabolite antineoplastic agent such as gemcitabine or fluorouracil in the treatment of neoplasms.
Compounds of Formula I, wherein R1-R8 are defined herein are provided, together with
pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these
compounds for inhibiting beta amyloid production and for the prevention and treatment of
Alzheimer's Disease and Down's syndrome are...
The present invention provides a compound of formula (I) and the use thereof for the
treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
R is methyl or ethyl;
R' and R" are independently alkyl of 1 to 3 carbon atoms, or R' and R", taken together with the nitrogen to which they are attached, can form a 5 or 6 membered saturated ring which may optionally contain an additional heteroatom selected from NR'", O or S(O)n; n is 0-2; and R"' is hydrogen ...
Nucleic acid molecules modified to enhance recombinant protein, e.g., antibody, expression and/or reduce or eliminate mis-spliced and/or intron read-through (IRT) byproducts are disclosed. The invention also provides methods for producing proteins devoid of mis-spliced and/or intron read-through by-products by the u...
Compositions and methods for treating autoimmune diseases are described. In particular, the use of B cell depleting agents and cytotoxic drug/B cell depleting agent conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LC...
This invention provides compound of formulae I or II having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined in the specification or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in t...
Compounds of formula (I) or pharmaceutically acceptable salts thereof
are provided:
Wherein:
A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms;
R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the gr...
The present invention is directed to benzothiadiazolylphenylalkylamine derivatives of formula I:
or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake includi...
Disclosed are compounds of Formula I:
wherein R1, R2, R3, R4, and X, are defined hereinbefore in the specification, which can
i
be useful in the treatment of autoimmune and inflammatory diseases, and processes for producing said compounds.
The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-3,5-dihydro-phenylimidazol-4-one compound of formula I
The present invention also provides methods for the use thereof to inhibit secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles.
The present invention is directed to substituted propylamine derivatives of formula I:
or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, va...
The present invention discloses an isolated nucleic acid molecule encoding a human liver X
receptor alpha (LXRα) variant polypeptide selected from the group consisting of:
(a) an isolated nucleic acid molecule encoding SEQ ID NO: 6, 8, 17, or 19;
(b) an isolated nucleic acid molecule encoding an amino acid sequen...
The present invention provides improved methods for the reduction or removal of protein impurities from a
complex cellular Streptococcus pneumoniae lysate or centrate comprising serotype 3 polysaccharides
involving steps relating to post-lysis heating or pH adjustment. In certain methods, the lysate is heated for ...
Separation methods,
for example, to isolate a recombinant
protein, are disclosed. The methods
include forming a solid containing a
first cation and a first anion in a medium
containing a protein, and separating the
solid from the protein.
The present invention relates to novel methods for the preparation of glutamic acid derivatives and intermediates
thereof, and such compounds prepared by the novel methods.
A process for the preparation of a pharmaceutical composition comprising
bringing into association:
a) a pain treating effective amount of at least one compound having the formula (I):
wherein:
R1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenylalkyl of 7 to 12 carbon atoms;
R2 is hydrogen, alkyl of 1 to 6 c...
Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided:
which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophreni...
The present invention concerns production of a compound of the formula (I) or a pharmaceutically acceptable salt thereof by a process which utilizes the cyclization of a compound of the formula (II) where Ar, Y, R1, RY, R2, and m are as defined herein.
The invention relates to metabolites of certain [l,4]diazepmo[6,7,l-i~]quinoline derivatives and methods of preparation and use thereof. Specifically, the invention relates to compounds of formula I wherein the various substituents are defined herein. The invention also provides pharmaceutical compositions including...
The present teachings relate to the field of anti-inflammatory substances, and more particularly to the preparation of compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, the present teachings provide methods for preparing compounds for treating selectin-medi...
The present invention provides a stable veterinary oral composition which comprises one or more surfactants, a water-miscible solvent, optionally an oil and an effective amount of each of a benzimidazole antihelmintic compound, such as triclabendazole and a macrocyclic lactone, such as moxidectin. Said composition i...
This invention relates to methods for rationally designing cell culture media for use in cell cultures, e.g., cell cultures employed in polypeptide production; cell culture media designed with the disclosed methods; methods of producing a polypeptide of interest, e.g., an antibody, using such media; polypeptides pro...
Methods for synthesizing tetrahydroquinoline-containing compounds of formula (II) are provided, along with synthetic intermediates and products associated with such methods.
Methods for treating and preventing anxiety, anxiety-related disorders, schizophrenia and schizophrenia-related disorders are described herein wherein said methods comprise the administration of oxytocin receptor agonists, of formula 1 , or a pharmaceutically acceptable salt thereof: 1 wherein: G1 is (I) of formula ...
The invention provides compounds of formula
(I) and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.
Methods of producing a protein in cell culture comprising an anti-senescence compound, such as the antioxidant carnosine, are provided. According to teachings of the present invention, cells grown in a cell culture medium comprising an anti-senescence compound exhibit increased viability and productivity. Furthermor...
The present invention relates to methods for synthesizing compounds useful as 5HT2C agonists or partial agonists, derivatives thereof, and to intermediates E thereto.
The present invention is directed to a method for treating bone or bone marrow infections, joint infection or infection of the tissues surrounding the joint by administration of the antibiotic tigecycline alone or in combination with a rifamycin antibiotic. In a preferred embodiment the bone or bone marrow infection...
Disclosed herein are nucleic acid and polypeptide sequences of mutated KCNQ5 potassium channels which lack
responsiveness to the potassium channel activator retigabine. Also disclosed herein are methods and kits related to the use of the
aforementioned mutated KCNQ5 potassium channels.
The present invention is directed to bi-layer tablets comprising at least one estrogen in a first layer and a therapeutic agent in a second layer, and processes for their preparation.
Osteogenic proteins are delivered via an injectable solid rod or hardenable paste. The formulation comprises a calcium phosphate material, an osteogenic protein, and optional additives and active ingredients such as a bone resorption inhibitor. Methods of making injectable pharmaceutical compositions and methods of ...
The present invention provides methods, systems and equipment for the prognosis and treatment of renal cell carcinoma (RCC) or other solid tumors. Genes prognostic of clinical outcomes of a solid tumor can be identified according to the present invention. The expression profiles of these genes in peripheral blood...
Compound of formula (I) and (II) are provided wherein X is an alkali metel or a basic amine moitey; R1is alkyl
cycloalkyl, -CH2-cycloalkyl, pyridinyl, phenyl or benzyl, the rings of these groops being optionally substituted; R2
is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH2,cycloalkyl, -NH2- or -NO...
The invention provides methods for preparing pharmaceutical formulations for injection such that upon injection the
formulation does not cause erythrocyte agglutination, hemolysis, and/or cell shrinkage. To prevent agglutination, a pharmaceutical
formulation ready for injection needs to have a sufficient ionic str...
The invention provides sugar-containing compositions suitable for use in coating solid preparations such as tablets, pills, granules and grains. Methods of using such coatings are provided, as are solid dosage forms coated with the compositions. In some embodiments, the methods provide sugar coated tablets comprisin...
This invention provides baffles
(10) for use in coating pans (50) within coating
apparatus, and methods of manufacturing the baf-
fles (10). The invention further provides methods
of coating pharmaceutical formulations using the
baffles (10) and coating pans (50) of the present
invention.
...
The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a CNS disorder related to or affected by the 5-HT6 receptor.
A combination of temsirolimus and herceptin in the treatment of cancer is provided. A combination of temsirolimus
and HKI-272 is provided. A combination of herceptin and HKI-272 is also provided. Regimens and kits for treatment of metastatic
breast cancer, containing herceptin, temsirolimus and/or HKI-272, optiona...
Compounds of formula (1) or pharmaceutically acceptable salts thereof are provided Formula (1) which are agonists and partial agonists of the 2c subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as s...
The present invention relates to solid dosage formulations that include ERβ-selective ligands that contain benzoxazole, and processes for manufacture of said formulations, more particularly to novel formulations and processes for manufacture of formulations containing the ERβ-selective ligand, ERB-041.
...
The present invention provides solid dosage formulations of benzoxazole-containing ErB-selective ligands, and processes for their manufacture, more particularly to novel formulations, and processes for their manufacture, that contain the ERB-selective ligand, ERB-041.
This invention provides a method of treating pain in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula (I): where R1 is H, alkyl or phenylalkyl; R2 is H, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together as Z are -CH2CH2-...
Infant formula compositions are provided which comprise 3.2mg/L to 15.4mg/L of CMP; 1.8 mg/L to 11.0mg/L of UMP; 1.8 mg/L to 8.0 mg/L of GMP; 0. 1 mg/L to 2.2 mg/L of IMP; and 2.5 mg/L to 13.2 mg/L of AMP.
The present invention is directed to phenylpiperazine cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal a...
This invention relates to the application of hydroxyapatite chromatography to the purification of at least one antibody from a preparation containing high molecular weight aggregates. Further, this invention relates to an integration of ceramic hydroxyapatite chromatography into a combination chromatographic protoco...
The present invention provides method for the treatment, amelioration or prevention of a neurodegenerative disorder in a patient in need thereof which comprises administering to said patient an effective amount of a 5-hydroxytryptamine-6 agonist.
This invention relates to extended release pharmaceutical dosage forms for orally delivering drugs to mammals, e.g., humans. More particularly, this invention concerns dosage forms of water soluble drugs such as venlafaxine, enantiomeric (R or S) forms of venlafaxine, metabolites of venlafaxine such as 0-desmethyl v...
This invention relates to an extended release tableted dosage formulation of the antidepressant venlafaxine hydrochloride or an optical form thereof having improved bioavailability.
The present invention is directed to substituted N-heterocycle derivatives of formula (I), compositions containing these derivatives, and their use in the manufacture of a medicament for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexu...
A scalable process for the preparation of a rapamycin 42-ester by reacting a rapamycin 42-ester boronate with a diol
and purifying crude rapamycin 42-esler by recrystallization and treatment with a diol is provided. Also provided is a method for
isolating and purifying a rapamycin 42-ester boronate from mother liq...
Pantoprazole sodium multiparticulates are described which avoid sticking to nasogastric and gastronomy tubes. The pantoprazole multiparticulates have a spheroid core of pantoprazole or an enantiomer thereof, or a salt thereof , a surfactant, and a disintegrant; a sub coat which is comprised of hydroxypropyl
methylc...
The present invention provides compounds of the following structure, wherein R1-R9, R15, and n are defined herein. These compounds are useful in treating neurological disorders or complications due to stroke or head injury, and as neuroprotective and neuroregenerative agents.
The present invention provides an amino-imidazolone compound of formula I
Also provided are compositions and methods for the use thereof to inhibit (3-secretase (BACE) and treat p-amyloid deposits and neurofibrillary tangles.
Processes are disclosed for preparing substituted aryl cycloalkanol derivatives, particularly chiral substituted aryl cycloalkanol derivatives of the general formula:
A process for the enantio selective synthesis of an (S)- or (R)- l-[2- dimethylamino)-!-(methoxyphenyl)ethyl]cyclohexanol and analogues or salt thereof are described. The method involves the steps of (a) reacting an (S) or (R) 4- benzyloxazolidinone with a mixed anhydride of a methyoxyphenylacetic acid under conditi...
This invention relates to methods and pharmaceutical compositions for
providing estrogen replacement therapy in perimenopausal, menopausal, and
postmenopausal women through the continuous administration of conjugated
estrogens.
The specification discloses materials and methods for screening and identifying reagents, which modulate Norrin
activity as it relates to Wnt pathway signaling. Preferably, agents identified thereby modulate bone remodeling and/or lipid levels,
and can be Norrin mimetics and Norrin agonists, as well as other agoni...
This invention provides compounds of the formula: wherein A", X and Y are defined in the specification. These compounds are useful as antibacterial agents.
The present invention relates to biaryl sulfonamides of the formula 1: wherein: R<1> is H or Cl-.C6 a]kyl; R<2> is H, C I -C6 alkyl, (CH2)nR<2" >, phenyl, or benzyl; n is 0-6; R<2">is aryl, heteroaryl, cycloalkyl, or heterocycloalkyl; R <3> is, independently with respect to each occurrence, H, halogen, OC(halogen)3,...
There is provided a process for the preparation of substituted amino alcohols HO-(CH2)n-NR<1>R<2> from haloalcohols HO-(CH2)n-X, where X is Cl, Br or I, bz reaction with an amine HNR<1>R<2>, in water as solvent at a temperature range of about 20 DEG C to about 90 DEG C optionally in the presence of a catalytic amoun...
The present invention provides novel isolated BFI-P0169 polynucleotides and polypeptidcs encoded by the
BFLP0169 polynucleolides. Also provided are the antibodies that immunospecifically bind to a BFLP0 169 polypeptide or any
derivative (including fusion derivative), variant, mutant or fragment of the BFLP0169 pol...
The present invention provides a 2-amino-5-piperidinylimidazolone compound
of formula I
The present invention also provides methods and compositions for the
inhibition of ß-secretase (BACE) and the treatment of ß-amyloid deposits and
neurofibrillary tangles.
The present invention relates to lyophilized compositions of a triazolopyrimidine compound, or a hydrate thereof,
or a pharmaceutically acceptable salt of Compound I or hydrate thereof; solutions useful in preparing said lyophilized compositions;
methods for preparing such compositions; methods of reconstituting t...
Certain adducts and dinners of 6-[(substituted)phenyl]triazolopyrimidine compounds or pharmaceutically acceptable
salts thereof, and compositions containing said compounds orpharmaceutically acceptable salts thereof, wherein said compounds are
anti-cancer agents useful for the treatment of cancer in mammals, are d...
The invention provides microemulsion pharmaceutical compositions comprising pharmaceutical actives which are hydrotropes that facilitate formation of microemulsions. The invention further provides methods of making the compositions and utilization of the compositions in liquid fill soft shell capsules including caps...
The present invention relates to compositions comprising excipients or solubilizing agents for proteins. The invention
relates to the discovery that a peptide derived from the N-terminus extension of the T266 isoform of rhBMP2 has properties that
enhance the solubility of proteins. The invention also relates to me...
A method of preparing a rapamycin composition having increased potency is provided. The method involves selecting a rapamycin compound having less than 1.5% oxidative and hydrolytic rapamycin impurities and formulating the selected
rapamycin with an antioxidant and optional excipients.
Disclosed herein are methods of treating at least one bacterial infection, such as lower gastrointestinal infections,
comprising orally administering a pharmaceutical composition comprising tigecycline. The composition can take solid or liquid
forms, such as solutions, dispersions, or solid forms comprising tigecy...
Novel sodium channel nucleic acids and polypeptides are disclosed herein. Methods of using the novel nucleic acids and polypeptides are also disclosed.
The present invention provides processes for the preparation of substituted naphthyl indole derivatives of formula (I) that can be used as inhibitors of plasminogen activator inhibitor- 1 (PAI-I) . In certain embodiments of the invention, the processes involve reactions that include one or more of an Oppenauer oxida...
The present invention provides CCI-779 polymorph Form II. This invention also provides processes for preparing CCI-779 pofymorph Form II and pharmaceutical compositions including CCI-779 polymorph Form II.
Methods for agents useful for treating asthma are disclosed. The methods include screening for agents that inhibit the producfion of a PKC-Θ protein, as well as for agents that inhibit the kinase activity of a PKC-Θ protein, or a functional fragment thereof, wherein such agents are useful for treating asthma. The me...
The present invention provides methods and compositions for use in the treatment, prevention, and/or alleviation of
drug abuse and/or its symptoms. In particular, the invention demonstrates that compositions comprising compounds of formula (I)
are useful in such treatment revention and/or alleviation: formula (I) ...
Methods and compositions are provided for treating sexual dysfunction, e.g., sexual dysfunction associated with
drug treatment, using 5-HT1A receptor antagonists.
The present invention provides a method for suppressing protein aggregation in a liquid formulation during freeze-thaw by including sorbitol in the liquid formulation. The present invention also provides methods for storing and preparing a liquid formulation containing a protein and sorbitol such that the presence o...
The instant invention discloses a method of isolating CLCA1 in vitro comprising: contacting a fluid with a specific binding partner of CLCA1 such that a complex between CLCA1 and the specific binding partner forms; isolating the complex of CLCA1 and the specific binding partner of CLCA1 from said fluid; and disrupti...
The invention provides a purified oxepane isomer of 42-O-(2-hydroxy)ethyl-rapamycin (SDZ-RAD Isomer C), a
chemical process for its preparation, as well as pharmaceutical compositions and packs containing SDZ-RAD Isomer C and methods
for its use as an immunosuppressive, anti-inflammatory, antifungal, antiproliferat...
The present invention is directed to monohydrate and anhydrate crystal forms of 2-(3- fluoro-4-hydroxyphenyl)-7-vinyl-l,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.
The invention provides a multivitamin and mineral nutritional supplement composition comprising at least one polyvalent metal and at least one oxidizable vitamin with substantially improved resistance to reactions that lead to darkening and /or spotting and reactions that may reduce the potency of oxidizable vitamin...
The present invention relates to processes for the preparation of substituted benzoxazole compounds, and in particular
2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl- benzoxazol-5-ol. The processes include the vinylation of a substituted benzoxazole
compound having an appropriate substitutable moiety.
...
The present invention
provides processes for the purification of
substituted benzoxazole compounds of
formla (I), and in particular 2-(3-fluoro-4-hydroxy-phenyl)
-7-vinyl-benzooxazol-5-ol.
The processes include recrystallizing the
compound from a solution comprising
acetone and acetonitrile; treating the crud...
The present invention relates to novel tigecycline compositions with improved stability in both solid and solution
states and processes for making these compositions. These compositions comprise tigecycline, a suitable carbohydrate, and an acid
or buffer.
This invention is directed to methods of preparing 4-substituted quinoline compounds as intermediates in the manufacture of receptor tyrosine kinase inhibitors and intermediate compounds used in the methods thereof, wherein the 4-substituted quinoline compound has the general formula (I); and wherein substitutions a...
The present invention is directed to crystal and amorphous forms of the 5-HT1A receptor antagonist 4-cyano-N-{(2R)-2-[4-(2,3-dihydro-benzo[ 1,4]dioxin-5-yl)-piperazin-1 -yl]-propyl}-N-pyridin-2-yl-benzamide hydrochloride, as well as compositions thereof and methods of using the same. (I)
...
Crystalline polymorph forms of Gonadotropin Releasing Hormone receptor antagonists, including cry!|bll0e polymorphs of quinoxaline dihydrohalide dihydrates, in particular crystalline polymorphs of 6-({4-[2-(4-tert-butylphenyl)-IH-benzimidazol-4-yl]-piperazin-l- yl}methyl)-quinoxaline dihydrochloride dihjdr...
The instant invention concerns processes for the production of pyrrole-2-carbonitriles such as l-methylpyrrole-2-carbonifirile. Such processes preferably comprise the steps of reacting a pyrrole with chlorosulfonyl isocyanate in the presence of a solvent and contacting the resulting product with a molar excess of an...
A process for the preparation of a compound of formula (I), wherein R1, and R2 are ortho or para substituents, independently
selected from the group consisting of hydrogen, hydroxyl, C1-C6 alkyl, C1-C6 alkoxy, C7-C9 aralkoxy, C2-C7 alkanoyloxy,
C1-C6 alkylmercapto, halo and trifluoromethyl; R3 is hydrogen or C1-C6...
The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.
Thioamide compounds, and specifically, thioamide pyrrole compounds, and preparation thereof are provided. These thioamide compounds can be used as progesterone receptor modulators, in contraception, and in the treatment of progesterone-related maladies (formula I).
The present invention is directed to bazedoxifene ascorbate, compositions containing the same, dispersions thereof, preparations thereof, and uses thereof.
A method for the regiospecific synthesis of rapamycin 42-ester derivatives is described. The method involves lipase-catalyzed acylation of 42 hydroxy rapamycin with an acyl donor such as a vinyl ester, an isopropenyl ester or an anhydride in a suitable organic solvent.
The present invention is directed to solid dispersions of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.
Methods for the synthesis of regiospecific rapamycin 42-hemiesters and regiospecific FK506 32-esters with di-carboxylic acids is described. The methods involve catalyzing the reaction between a rapamycin or a FK-506 and a dicarboxylic anhydride or a bifunctional activated ester of dicarboxylic acid with a lipase.
...
A method for rapamycin-specific labeling using rapI, rapM and/or, rapQ enzymes is described. Also are methods for generating crude enzyme extracts useful in the method of the invention. Uses of the specifically labeled rapamycin as diagnostic tools are provided.
Disclosed are proline-rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (proline-CCI-779) as well as a method for the regiospecific preparation of a rapamycin 42-ester or proline-rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (CCI-779 and proline-CCI-779) comprising the steps of: (a) reactin...
Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided: Formula (I) Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or op...
This invention provides estrogen receptor modulators of formula (I), having the structure (I) wherein R1, R2, R3, R4,
R5, R6, R7, R8, R9 and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Processes are described for preparing 42-pegylated rapamycins including reacting a rapamycin with an acylating agent in the presence of a lipase to form an acylated rapamycin and reacting the acylated rapamycin with a methoxy poly(ethylene glycol)
derivative in the presence of a base. Also described are processes f...
This invention provides a method of treating
pain in a mammal that includes administering to a mammal in need of such treatment a pain
treating effective amount of a compound of the formula (I): or a pharmaceutically acceptable
salt thereof, wherein each of R1, R2, R3, R4, R5, R6, n, and m is as defined and descr...
Compounds of formula (2) or pharmaceutically acceptable salts thereof are provided: wherein each of R1a, R2a, R3a, Ar, y, and m are as defined herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, are used to treat a v...
The invention provides a nutritional supplement and/or pharmaciutical composition for tableting comprising an embedded lubrication matrix. The embedded lubrication matrix comprises an oily liquid finely dispersed in an oil insoluble material. A method of lubricating a nutritional supplement or pharmaceutical composi...
The present invention is directed to crystalline forms of the 5-HT2C agonist {[(2R)-7-(2,6-dichlorophenyl)-5-fluoro-2,3-dihydro-1-benzofuran-2-yl]methyl}amine hydrochloride, as well as compositions, processes of preparation, and uses thereof.
The present invention provides novel insecticidal animal ear tags, neck collars or pendants, and a method for controlling insects in a homeothermic animal.
A process for reducing the protein content and preserving the capsular polysaccharide content in a com||l cellular Streptococcus pneumoniae lysate broth prior to purification is described. Utilizing pH reduction after cellular lysis has resulted in a purified polysaccharide that consistently meets the protein specif...
Compounds of formula (I) are provided: formula (I), wherein each of R1, R2, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of melatoninergic receptors. The compounds, and compositions containing the compounds, can be used to treat melatoninergic...
Micronized tanaproget, purified tanaproget Form I, and micronized, purified tanaproget Form I are provided. Also provided are compositions containing one or more of the prepared tanaproget forms, methods of using one or more of the prepared tanaproget forms, and kits containing one or more of the prepared tanaproget...
This invention provides methods and pharmaceutical compositions for modulating bladder function, and in particular for maintaining bladder control or treating urinary incontinence, by using the compounds of this general formula (I).
FAST PERFUSION SYSTEM AND PATCH CLAMP TECHNIQUE UTILIZING AN INTERFACE CHAMBER SYSTEM HAVING HIGH THROUGHPUT AND LOW VOLUME REQUIREMENTS
A system for carrying out fast perfusion for the patch clamp techniques useful in studying the effect of compounds on ion transfer channels in biological tissue is disclosed. The ...
The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, and magnesium stearate; or can contain microcrystalline cellulose, croscarmellose sodium, sodiu...
Therapeutic combinations useful in the treatment or prevention of depression or other mood disorders, comprising a compound of Formula (1), or a pharmaceutically acceptable salt thereof, wherein each of R1, R2, R3, R4, R5, R6, n, and m are as defined and described herein and one or more antidepressants.
...
Therapeutic combinations useful in the treatment or prevention of psychotic disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of psychotic disorders are provided. Such compounds are of formula (I) or a pharmaceutically acceptable salt thereof, wh...
The present invention is directed to a pliable package (5) which includes a flexible liquid storage reservoir (40) having a funnel-shaped outlet passageway (50) leading to an opening. The
package also includes a reinforced tear resistant tab portion (30) that may prevent accidental discharge of liquid when the tab ...
The present invention relates to methods for the prevention and treatment of conditions arising from local estrogen deficiency, such as dyspareunia, vulvar atrophy, vaginal atrophy, vaginal dryness, vulvar itching, vaginal itching, vulvar burning, vaginal burning, vulvar dystrophy, atrophic vaginitis or menopausal s...
The present invention relates to a stable, antiparasitic, non-aqueous pour-on parasiticidal composition which comprises an effective amount of amitraz, optionally a macrocyclic lactone, a stabilizer and a carrier system having no active hydroxyl group.
The invention provides a novel assay system for detecting the presence, concentration and binding activity of GPIbα in a biological sample. The method for determining the presence of GPIbα in a biological sample comprises: (a) providing a substance comprising GPIbα; (b) contacting the substance from step (a) with a ...
The present invention relates to a method for treating premenstrual dysphoric disorder through administration of at least one progestin and at least one estrogen to a female subject for at least (100) days.
High load concentrate compositions comprising metaflumizone, an optional bridging agent, a surfactant, and a suitable carrier solvent. These compositions may be topically administered to animals, and are useful for preventing or treating ectoparasitic infestations in warm-blooded animals for prolonged periods of tim...
Methods of screening for agents for treating asthma are provided. The methods involve screening for agents that decrease the production or activity of a RegIII protein that has been discovered herein to play a role in producing the symptoms and pathological complications involved in asthma. Methods of treating asthm...
Crystalline solid forms of tigecycline, Form I, Form II, Form III, Form IV, and Form V, compositions comprising
these crystalline solid forms, and processes for preparing these crystalline solid forms are described herein.
High load concentrate compositions comprising metaflumizone, a substantially water-insoluble anti-parasitic
macrolide compound,such as moxidectin, an optional bridging agent, a surfactant, and a suitable carrier solvent are prepared.
These compositions may be topically administered to animals, and are useful for p...
This invention relates to extended dosing regimens for the selective estrogen receptor modulator bazedoxifene (1-[4-(2-azepan-l-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1h-indol-5-ol).
Solid dosage formulations are provided for a compound having the formula: (I) R2 = Cl, F, Br,CH3, CF3, SCH3, NHCH3, NO2, CN, OH, OC1 - C6 alkyl, substituted OC1 - C6 alkyl or a prodrug or a pharmaceutically ...
A method of selectively preparing a chiral 2S-amino alcohol useful in preparation of an amide sulfonated or acylated
with alkyl, substituted aryl or substituted heteroaryl is described. The method involves reacting a di-tert-butyl diazene-1,2-di-
carboxylate with a (4S)-4-benzyl-3-[(S)-trifluoromethyl - alkyl subs...
This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLA2α). In some embodiments, the inhi...
Methods of formulating proteins at high concentration in protein solutions, wherein the protein solutions lack or have reduced liquid-liquid phase separation are described. Such protein solutions are substantially dear and substantially hoinoge-lious. Additionally, methods of concentrating and purifying proteins usi...
The present invention relates to crystalline forms of the 5-HT1A binding agent 6-methoxy-8-[4-(1-(5-fluoro)-quinolin
-8-yl-piperidin-yl-piperazin-1-yl]-quinoline, as well as pharmaceutical compositions thereof, and methods of use thereof.
The present invention relates to hydrochloric acid salt and crystalline forms of the 5-HT1A binding agent
6-methoxy-8-[4-(1-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-1-yl]-quinoline, as well as pharmaceutical compositions
thereof, and methods of use thereof.
The present invention relates to 4-oxo-l,3,8-triaza-spiro[4.5]decanes which are useful as Kvl.5 potassium channel inhibitors providing atrial-selective antiarrhythmic activity. The present invention further relates to compositions and method s for treating atrial-selective antiarrhythmia.
Lyophilized CCI-779 formulations and solutions useful for preparing freeze-dried CCI-779 formulations composed of CCI-779 and a solvent selected from dimethylsulfoxide, acelonilrile, ethanol, isopropanol or t-butyl alcohol are described. Also provided are the methods of preparing the lyophilized CC1-7 79 formulation...
Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (alsoknown as premenstrual syndrome), attention deficit disorder ...
The present invention provides a compound of Formula (I), pharmaceu-tical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.
Disclosed are methods of producing a cytokine antagonist polypeptide by co-expressing the cytokine antagonist polypeptide with a nucleic acid encoding a complexing polypeptide for the cytokine antagonist polypeptide.
The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
Fusion proteins comprising a Receptor for Advanced Glycation End Products Ligand Binding Element (RAGE-LBE) and an immunoglobulin element are disclosed. Also disclosed are fusion proteins comprising a RAGE-LBE and a dimerization domain. Also disclosed are nucleic acids encoding such fusion proteins and methods for u...
Methods for producing proteins, for example, recombinant meningococcal 2086 proteins, using fed-batch fermentation with continuous input of an inducer after achieving a threshold parameter, and optionally continuous input of a carbon source, for example, a constant rate input, to improve protein yields, as well as h...
Methods for determining if test compounds are able to modulate the interaction between adrogen receptor and beta-
catenin are disclosed. Methods for the determining whether a test compound selectively modulates an adrogen receptor signaling
pathway over a beta-catenin-Wnt signaling pathway or a beta-catenin-Wnt si...
A chewable pharmaceutical composition comprising phenylephrine, artificial sweetener, and a substantially aldehyde-free matrix is provided. The composition has phenylephrine stability suitable for a typical commercial product with a two year shelf life. A method of manufacture of the composition and a method of use ...
An improved system for large scale production of glycoproteins in cell culture is provided. In accordance with the present invention, cells expressing a glycoprotein are grown in media that contain manganese at a concentration of between approximately 10 and 600 nM. The use of such a system allows production of a gl...
A process for preparing a compound of formula I
wherein:
one of A and B denotes hydrogen and the other an optionally substituted fused
tricyclic heteroaryl group;
X is S or O;
R5 is H, C1 -C6 alkyl, C5 - C6 cycloalkyl, or CHR3OCOC1-C6alkyl; and
R3 is hydrogen, C1-C6 alkyl, C5 - C6 cycloalkyl, optionally substi...
This invention provides
substituted indole compounds of the general
formula: (I) and pharmaceutically acceptable
salt forms thereof, and methods for using the
compounds as inhibitors of the activity of
various phospholipase enzymes, particularly
phospholipase A2 enzymes, and for the medical
treatment, prevent...
The present invention provides materials and methods for treatment of diseases involving aberrant B-cell activity,
using a CD20-specific binding molecule, in particular, antibodies or antigen binding fragment thereof. The compositions disclosed
herein is useful for the treatment and diagnosis of B-cell disorders, ...
Members of the TGF-β superfamily and peptide fragments based on member proteins are employed to purify solutions containing member proteins or as therapeutics.
Highly selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agoraphobia, post traumatic st...
The instant invention discloses a method of preparing O-desmethylvenlafaxine
which comprises reacting venlafaxine with a high molecular weight alkane, arylalkyl or
arene thiolate anion in a hydroxylic or ethereal solvent, or mixture thereof, to provide O-
desmethylvenlafaxine.
The disclosure provides novel molecules related to growth and differentiation factor-8 (GDF-8), in particular mouse and humanized antibodies, and antibody fragments, including those that inhibit GDF-8 activity and signaling in vitro and/or in vivo. The disclosure also provides methods for diagnosing, treating, ameli...
The present invention is directed to formulations of bazedoxifene acetate that have reduced polymorph conversion,
compositions containing the same, preparations thereof, and uses thereof.
This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in
peri menopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated
estrogens and medroxyprogesterone acetate.
This invention provides compounds of Formula I having the structure
where RI, R2, R3 and A are defined in the specification or a pharmaceutically acceptable salt thereof useful as antibacterial agents. Compounds according to Formula (II):
where Q, R4, R5, and R6 and A are defined in the specification are useful a...
The present invention provides topical compositions comprising O-desmethylvenlafaxine (ODV), a selective serotonin and norepinephrine re-uptake inhibitor, or a pharmaceutically acceptable salt thereof. In certain embodiments, the inventive
topical formulations contain one or more percutaneous/permucosal absorption ...
Methods for the treatment
of neuropsychiatric disorders such
as anxiety are disclosed. The methods
involve modulating the expression of the
angiotensin IV receptor or modulating
the biological activity of the angiotensin
IV receptor by utilizing antagonists to the
receptor. Also disclosed are methods for
ide...
The invention relates to, for example, novel formulations and methods for the delivery of 4-cyano-N-{(2R)-2-[4-
(2,3-dihydro-benzo[l ,4]dioxin-5-yl)-piperazin-l -yl]-propyl)-N- pyridin-2-yl-benzamide, pharmaceutically acceptable salts thereof,
structurally related compounds and/or metabolites; as well as to use of...
A stick lip balm with efficacious amounts of natural moisturizer and organoleptic/sensory attributes of lip feel associated with moisturizers and emollients is provided. The lip balm of the invention comprises at least 90% botanically derived materials and can be formed into a stick sufficiently robust to substantia...
A process for the preparation of 4-hydroxythieno[2,3-b]pyridine-5-carbonitriles, which can be useful for the preparation of protein kinase inhibitors, is provided.
The present invention relates to 8-Hydroxyquinoline Compounds; compositions comprising an 8-Hydroxyquinoline Compound; and methods for treating or preventing a metalloproteinase-related disorder, such as, an arthritic disorder, osteoarthritis, malignant neoplasm, rheumatoid arthritis, asthma, chronic obstructive pul...
A method and apparatus for optimizing the primary drying step of a lyophilization cycle of a biological or pharmaceutical
material. In one aspect, the invention is a method for lyophilizing a material comprising the steps of calculating a designed
primary drying cycle for the material based on a product temperatu...
Methods for reducing the opalescent appearance of a protein preparation by modifying the ionic strength of the preparation, as well as compositions, e.g., pharmaceutical compositions, of concentrated protein with decreased opalescence are disclosed. Purification methods which monitor and/or reduce the salt concentra...
The present invention provides novel isolated
compounds characterized as metabolites or derivatives of desmethylvenlafaxine including hydroxy DV metabolites, hydroxy DV-glucuronide metabolites, N-oxide DV metabolites, and benzyl hydroxy-DV metabolites. The invention includes pharmaceutical compositions comprising a...
Compounds of formula (I) or pharmaceutically acceptable salts
thereof are provided where at least one of R2 or R3 is not hydrogen. The compounds
of the present invention arc N-methyl-D-aspartate (NMDA) receptor antagonists
and are useful in treating a variety of conditions present in a mammal
that benefit from i...
This invention relates to modulating bone-related activity in a subject by modulating Ror molecules. The invention further relates to compositions and methods for the screening, diagnosis and development of therapies for bone-related disorders.
This invention provides estrogen receptor modulators
having the structure formula (I): wherein R1 to R6 and R8 are
as defined in the specification; or a pharmaceutically acceptable salt
thereof.
This invention is directed to a
method of selectively acylating a compound of
formula (II): (II), wherein: R1 is NO2, -N+R33,
trihalomethyl, -CN, -SO3H, -CO2H, -CO2 R3,
-CHO and -COR3, wherein R3 is C1-C6, alkyl,
C1-C6 haloalkyl, C3-C12 cycloalkyl, C6-C12 aryl,
C2-C9 heteroaryl, or C1-C9 heterocycloalkyl;
com...
The present invention provides novel isolated BFLP1698 polynucleotides and polypeptides encoded by the BFLP1698 polynucleotides. Also provided are the antibodies that immunospecifically bind to a BFLP1698 polypeptide or any derivative (including fusion derivative), variant, mutant, or fragment of the BFLP1698 polype...
Methods of adapting cells, e.g., mammalian cells, to a cell culture process are provided. When the adapted cells are
genetically modified and used for protein production, they exhibit beneficial characteristics, such as being able to attain higher cell
densities and/or achieve a higher overall yield of the produce...
This invention provides estrogen receptor modulators of formula: (1). having the structure wherein. R1, R2, R3, R4, R5 and R6 are as defined in the specification, or a N-oxide thereof or a pharmaceutically acceptable salt thereof or a prodrug thereof.
The present invention relates to Neisseria ORF2086 proteins, crossreactive immunogenic proteins which can be isolated from nesserial strains or prepared recombinantly, including immunogenic portions thereof, biological equivalents thereof, antibodies that immunospecifically bind to the foregoing and nucleic acid seq...
The present invention is directed to tablet-in-tab let compositions comprising one or more estrogens in a first layer and a therapeutic agent in a second layer, and processes for their preparation
A method of contraception is provided which involves delivery of 21 to 27 consecutive days of a progestin such as tanaproget in the absence of an estrogen or other steroidal compound, followed by 1 to 7 days without an effective amount of an active agent. Also described is a pharmaceutically useful kit to facilitate...
An immunogenic composition having 13 distinct polysaccharide-protein conjugates and optionally, an aluminum-based adjuvant, is described. Each conjugate contains a capsular polysaccharide prepared from a different serotype of Streptococcus pneumoniae (1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F) conjugated...
An immunogenic composition having 13 distinct polysaccharide-protein conjugates and optionally, an aluminum-based adjuvant, is described. Each conjugate contains a capsular polysaccharide prepared from a different serotype of Streptococcus pneumoniae (1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F) conjugated...
The invention provides methods and systems for predicting or evaluating protein-ligand coupling specificities. A pattern recognition model can be trained by selected sequence segments of training proteins which have a specified ligand coupling specificity. Each selected sequence segment is believed to include amino ...
An immunogenic composition having 13 distinct polysaccharide-protein conjugates and optionally, an aluminum-based adjuvant, is described. Each conjugate contains a capsular polysaccharide prepared from a different serotype of Streptococcus pneumoniae (1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F) conjugated...
This invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof that are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, t...
The present application provides methods of purifying polypeptides having a Fc igion. for example, antibodies or antibody fusions, by adsorbing the polypeptides to a c binding agent, such as, for example. Protein A or Protein G, followed by a wash with divalent cation salt buffer to remove impurities and subsequent ...
A formulation for a animal vaccines is provided. The vaccine formulation contains a stabilizer component and a viral immunogen. The stabilizer component includes a substantially TSE/BSE-safe animal-based protein and a vegetable-based protein. The stabilizer component provides for the stabilization of a vaccine throu...
A pharmaceutical composition comprising a human interleukin-11 ("IL- 11") polypeptide, wherein said composition comprises: a therapeutically effective amount of a polypeptide as herein described with the amino acid sequence of a human IL-11 polypeptide; at least one binder, as described herein, at a concentration of...
Cyclic peptides and peptidomimetics are provided that bind to and/or modulate activities associated with Trk receptors, including processes associated with the growth and repair of the central nervous system (e.g., neuronal growth and survival, axonal growth, neurite outgrowth and synaptic plasticity). Cyclic peptid...
A method of automated determination of saccharide concentration is provided herein. The method includes preparing one or more saccharide standards and one or more diluted polysaccharide test samples, transferring a portion of the one or more saccharide standards and the one or more diluted polysaccharide test sample...
The present invention provides methods of treating an autoimmune pathology in a mammal, comprising administering an agent with estrogen receptor a agonist activity in particular a selective estrogen receptor modulator. to the mammal in an amount sufficient to decrease production of Til-1 and/or TII-2 cytokines. Also...
Compounds of formula (I) wherein n is an integer from 1-3; X is N, CH, provided that when X is N, n is 2 or 3; R is alkyl of 1 to 3 carbon atoms; R1 is 2,4-diCI, 5-OMe; 2,4-diCI; 3,4,5-triOMe; 3-CI, 5-OMe; 2-Me, 5-OMe; 2,4-di-Me; 2,4-diMe-5-OMe, 2,4-diCI, 5-OEt; R2 is alkyl of 1 to 2 carbon atoms, and pharmaceutical...
Devices and methods that provide consistent skin side temperature comprising a primary insulative material disposed on a skin side of a thermal source; wherein the device provides a rate of change in temperature of less than about 0.8 are disclosed. Also included are methods of providing improved skin health, and me...
The present invention provides a method for treating, inhibiting the progression of, or eradicating polycystic kidney disease of in a patient in need thereof which comprises providing to said patient an effective amount of a TACE inhibitor compound in combination with an effective amount of a Src kinase inhibitor , ...
The present invention describes a process for preparing N-substituted phthalimides of Formula: (I) which are widely useful as intermediates in the preparation of organic compounds such as pharmaceuticals.
The present invention provides a process for the preparation of 6-[(substituted) phenyl]-triazolopyrimidine dicarboxylic acid salt and as a hydrated salt having the structural formula (I) wherein: R<1> is CF3 or C2F5; R<2> is H or C1-C3 alkyl; n is an integer of 2, 3, or 4; X is Cl or Br; R<3> and R<4> are each inde...
The present invention is directed to methods of producing conjugates of peptide immunogens with protein/polypep-tide carrier molecules, which are useful as immunogens, wherein peptide immunogens are conjugated to protein carriers via activated functional groups on amino acid residues of the carrier or of the optiona...
The invention pertains to pharmaceutical compositions of ZosynΦ having substantially free or reduced levels of galactomannan and processes to prepare said pharmaceutical compositions.
A multiparticulale O-desmethylvenlafaxine (ODV) succinate or formate is described. Methods of treating depression
and reducing the gastrointestinal side-effects of ODV are also described.
Use of animal models of neurodegenerative disorders for establishment of preclinical diagnostic and therapeutic indices, and for screening methods to identify effective preclinical therapies.
The present invention provides processes for the preparation of arylalkylsulfonyl halides and heteroarylalkylsufonyl halides of Formula: Ar-R-SO2-X, that are useful as intermediates in the preparation of pharmaceuticals.
This invention relates to processes for the preparation of 4-dimethylamino-but-2-
enoic acid [4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl]-amide
(EKB-569) and to compounds useful in the preparation of EKB-569.
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention discloses a pharmaceutical combination for enhanced induction of remission in a
patient having acute leukemia or myelodysplastic syndrome comprising (a) an anti-CD33
cytotoxic conjugate, wherein the cytotoxin in the anti-CD33 cytotoxic conjugate is selected from
the group consisting of a calicheamic...
The present invention provides compositions of Ig fusion proteins, especially compositions including an Ig fusion
protein, a bulking agent, a disaccharide, a surfactant, and a buffer. In one aspect, these compositions are stable under long-term
storage or at least one freeze/thaw cycle. The invention also provides...
This invention relates to the application of hydroxyapatite chromatography to the purification of at least one antibody
from a preparation containing high molecular weight aggregates. Further, this invention relates to an integration of ceramic
hydroxyapatite chromatography into a combination chromatographic proto...
This invention relates to a novel PTH gene. The invention further relates to methods of screening, diagnosis and development of therapies for bone related disorders.
Compounds of the Formula (I), wherein X is N, CH n
is an integer from 1-3; and R' and R are independently, alkyl of 1 to 3
carbon atoms, and pharmaceutically acceptable salts thereof, with the
proviso that when n is 1, X is not N; are useful for inhibiting vascular
permeability caused by disease, injury, or oth...
Methods for purifying rapamycin are described. Methods for measuring particle quality, median particle size, and
crystallinity of samples containing rapamycin or a derivative thereof are also provided.
The present invention provides processes and intermediates for the preparation of aminoethoxybenzyl alcohols of Formula (I) useful in the production of pharmaceutically useful compounds. Formula (I)
A serum-free insect cell culture medium is described which provides improvements in the maximum cell density supported and replication of insect viruses within these cells, at a significantly lower cost than commercially-available media. An improved method for preparing a lipid emulsion which is easy to scale and wh...
The invention pertains to treatment of bacterial infections with tigecycline and cardiac insufficiency with digoxin by coadministration to a human in need thereof.
Disclosed are compositions and methods for modulating hemichannel function in a cell, tissue or organ. The invention also relates to useful screens for detecting such compounds, particularly those capable of modulating connexin phosphorylation. Further provided are therapeutic mehtods for preventing or treating co...
The present invention provides method for making a compound of formula (1) comprising the steps of reacting compounds of formulas (2) and (3) to produce a compound of formula (4) wherein R1, R2, R3, R4 and R5 are defined as described herein. The compound of formula (4) is then converted to the compound of formula (1...
The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
The present invention provides a stable composition which comprises a non-hydroxyl-group-containing solvent mixture comprising N.N-diethyl-m-toluamide and ϝ-hexalactone, optionally with dimethyl sulfoxide, eucalyptol and 1-methoxy-2-propyl acetate; and an effective amount of each of amitraz and at least one a...
A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
The present invention relates to a method for treating thermoregulatory disorders by administering compounds and compositions of compounds which by modulating 5HT levels activate the 5HT2a receptor. The invention also relates to therapy using 5HT1a antagonists and SRIs in combination and pharmaceutical compositions ...
Processes are provided for preparing novel 4-substituted N-{2-[4-(2,3-dihydro-benzo[1,4]dioxin-5-yl)-piperazin-1-yl]propyl}-N-pyridin-2-yl-benzamide derivatives having the formula (III):
wherein R1 is cyano, nitro, trifluoromethyl or halogen, and pharmaceutically acceptable acid addition salts thereof, which com...
The present invention relates to thiazolo-naphthyl acids of the formula (I) and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders.
A process for the preparation of cyclohexanol derivatives of formula (11 by reacting a compound of formula (II) with a compound of formula (III) in the presence of a base catalyst of formula (IV) or (V). In the above formula, R1-R9 ,A, B, X and p have lghe meanings given in the specification.
This invention discloses an antineoplastic combination comprising an antineoplastic
effective amount of a combination of CCI-779 and an aromatase inhibitor.
Protein formulations and methods for reducing the viscosity of a protein formulation are provided. The method for
reducing the viscosity of a protein formulation comprises adding a viscosity reducing agent, such as calcium chloride or magnesium
chloride to the protein formulation.
Disclosed herein are pharmaceutical compositions comprising tigecycline for oral administration. The composition
can comprise tigecycline having at least one enteric coating.
The present invention provides formulations for maintaining the stability of polypeptides, in particular, therapeutic antigen-binding polypeptides such as antibodies and the like, for example, anti-A&bgr; antibodies. The formulations generally include an antioxidant in a sufficient amount as to inhibit by-product fo...
The present invention provides compounds of the following structure, wherein R1, R2, R4, R4, R6, R7, and R15 are defined above: These compounds are useful in treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; prol...
Estrogen receptor ligands, estrogen receptor polypeptide/ligand complexes, crystals of estrogen receptor polypeptide/ligand complexes, and related methods and software systems are disclosed
This invention provides compounds of Formula (I);
wherein: R1 is a moiety selected from the group:
n is an integer of 1 or 2; R2 is selected from hydrogen, amino, -NR6R7, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms o...
The invention is related to findings that IL-17F-mediated inflammation of airway passages may be mediated via signaling through IL-17R on the baso lateral surface of human respiratory epithelial cells. Thus, the present invention provides isolated and purified IL-17F or IL-17R polynucleotides and polypeptides. The p...
The present invention provides methods, systems and equipment for prognosis or evaluation of treatment of solid tumors. Gene markers that are prognostic of solid tumors can be identified according to the present invention. Each gene marker has altered expression patterns in PBMCs of solid tumor patients following in...
An apparatus, system, and method of irradiating fluent food products. The present invention utilizes a transmissive wall having a convex surface. A source of radiation is positioned on a side of the transmissive wall that is opposite the convex surface so that when the radiation source is emitting radiation ene...
The present invention provides a method for the treatment of a cognitive disorder such as Alzheimer's disease in a patient in need thereof which comprises providing to said patient a therapeutically effective amount of a combination of an acetylcholinesterase inhibitor and a 5-hydroxytryptamine-6 antagonist.
...
The present invention is directed to compounds of Formula 1: which are modulators of the 5-hydroxtryptamine-6 and 5-hydroxytryptamine-2A receptors and which are inhibitors of norepinephrine reuptake. The compounds of the invention, and pharmaceutical composition thereof, are useful in the treatment of disorders rela...
A CCI-779 oral dosage form is provided in which, after oral administration to a subject, the CCI-779 has a whole blood peak concentration (Cmax) of 5.4 ±1.8 ng/mL and an area under the curve (AUC) of about 66 ± about 22 ng-hr/ml and the sirolimus has a Cmax of 18.7 ± 9.6 ng/mL and an AUC of about 600 ± about 228 ng-...
CYCLOALKYLFUSED INDOLE, BENZOTHIOPHENE, BENZOFURAN AND INDENE DERIVATIVES
The present invention provides cyctoalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HT1A rec...
The present invention provides methods, systems and equipment for the prognosis, diagnosis and selection of treatment of AML or other types of leukemia. Genes prognostic of clinical outcome of leukemia patients can be identified according to the present invention. Leukemia disease genes can also be identified accord...
The present invention provides an azolylacylquanidine compound of formula I
The present invention also provides methods for the use thereof to inhibit β-secretase (BACE) and treat β-amyloid deposits and neurofibrillary tangles.
An infant formula composition is provided comprising a whey fraction wherein 40% or less of the total protein in said
fraction is alpha-lactalbumin and more than 8% of the total protein in said whey fraction is beta-lectoglobulin, with the proviso that
the percentage of alpha-lactalbumin in said whey fraction is g...
This invention relates to modulating Ror activity (e.g., Ror2 protein activity) and/or
14-3-3 β to affect bone formation or resorption. The invention further relates to compositions and methods for the screening, diagnosis and development of therapies for bone-related disorders such as osteoporosis and bone fractu...
This disclosure relates to LINGO-1 polypeptides,
LINGO-1 polypeptide/ligand complexes, crystals of LINGO-1
polypeptides, crystals of LINGO-1 polypeptide/ligand complexes,
and related methods and software systems.
The present application provides human antibodies and antigen binding fragments thereof that specifically bind to the human interleukin-22 (IL-22) and methods of using those antibodies, for example, in diagnosing, treating or preventing inflammatory disorders, autoimmune diseases, allergies, septic shock, infectious...
Methods, systems and equipment for diagnosing renal cell carcinoma (RCC) and other solid tumors. This invention
identifies numerous disease genes that are differentially expressed in the peripheral blood of patients having RCC or other solid
tumors relative to disease-free humans. These disease genes can be used a...
This invention is directed to compounds of formula (I): wherein R1, R2, X, and n are as defined herein, including all crystalline forms and pharmaceutically acceptable salts thereof, with the provisos that when X is CH2, n is 1, and R1 is -COOH, then R2 cannot be formula (A) wherein A is CH3-, CH3CH2- or a haloalkyl...
Methods to detect GDF-8 modulating agents in animals, including humans, are provided herein, including methods
to detect the presence of exogenous GDF-8 modulating agent such as a GDF-8 inhibitor in a biological sample. In particular, methods
to assess the presence and/or quantity of a GDF-8 modulating agent in a ...
This disclosure provides methods for the detection of antibodies to a GDF-8 modulating
agent such as, e.g., MYO-029, in a biological sample. Methods to detect an immune response to a GDF-8
modulating agent are also included. In particular, methods to assess an immune response in animals,
including humans, to a GD...
The present invention relates to aqueous formulations of ERβ selective ligands. In some embodiments, the formulations include an ERβ selective ligand, a solubilizer/complexant component, and a pH adjusting component. The invention further provides preparations of the formulations, and uses thereof.
...
Processes for the preparation of trifluoroalkyl
substituted N-(2-hydroxyalkyl) heteroarene- and benzene-sulphonamide derivatives of formula (I) or formula (II) (wherein the variables are as defined in the claims) are provided which
comprises reacting a trifluoroalkyl substituted amino alcohol, a sulphonyl chloride...
This invention describes processes for the convergent synthesis of calicheamicin derivatives of Formula (I)1 and similar analogs using bifunctional and trifunctional linker intermediates.
This invention describes novel methods of treating muscle damage, muscle wasting, muscle degeneration, muscle atrophy or reduced rates of muscle repair associated with various conditions such as muscular dystrophy, through the use of small-molecule PAI-1 inhibitors
Fusion proteins comprising a Receptor for Advanced Glycation End Products Ligand Binding Element (RAGE-LBE) and an immunoglobulin element are disclosed. Also disclosed are fusion proteins comprising a RAGE-LBE and a dimerization domain. Also disclosed are nucleic acids encoding such fusion proteins and methods for u...
The present disclosure relates to hernia repair and methods for stimulating growth of fascia tissue employing compositions comprising fibrous tissue inducing proteins. In a preferred embodiment, a surgical hernia mesh is impregnated with
rhBMP-12.
Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.
...
The present invention is directed to pharmaceutical formulations and tablet compositions of pharmacological active
agents of Formula (I) that are estrogen receptor modulators, and preparative processes thereof.
The invention provides methods for treating tendinopathy. The disorders treated or prevented include, for example tendinitis, tendonitis, tendinosis, paratendinitis, tenocynovitis, tendon overuse injury and trauma, peritendinitis, paratenonitis, or other tendon degenerative disorders. The disclosed therapeutic metho...
This invention provides methods and pharmaceutical compositions for treating cognitive disorders such as learning
disorders and ADD/ADHD, and other disorders.
Antibodies that bind specifically to receptor for advanced glycation end products (RAGE) and RAGE-binding fragments thereof are disclosed. Also disclosed are pharmaceutical compositions comprising such anti-RAGE antibodies and RAGE-binding antibody fragments thereof, and their use for treatment of RAGE related disea...
Compounds of formula I or pharmaceutically acceptable salts thereof are provided: wherein each of R1, R2, R3, R4, y, m, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions cont...
The present invention provides methods of screening for compositions useful for treating, ameliorating, or preventing fibrosis arid/or fibresis associated conditions by measuring: changes in the level(s) of IL-21. and/or IL-21 receptor (IL-21 R) (e.g., the. level of expression of IL-21 and/or 1L-21R protein and/or m...
This invention discloses method of treating or inhibiting cancer in a human having at least one of an Exon 19 del E746-A750 and/or an Exon 21 point mutation comprising administering to said human gefitinib and/or iressa alone or in combination with other cytotoxic agents or chemotherapeutic agents and an effective a...
Compounds of formula (I) are described herein which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. Formula (I), or pharmaceutically acceptable salts thereof, wherein each of R1 , R2 , R3 , R4 , Rx, Ry, and n are as defined herein. Such compounds, and compositions thereof, are useful...
This invention provides a method of treating functional gastrointestinal and genitourinary disorders in a mammal by administering to the mammal an effective amount of hydroxycycloalkane phenethylamine of the following structural formula (I) in which A is a moiety of the formula (II) where the dotted line represents ...
The present application provides human antibodies and antigen binding fragments thereof that specifically bind to the human interleukin-22 (IL-22). The antibodies can act as antagonists of IL-22 activity, thereby modulating immune responses in general, and those mediated by IL-22 in particular. The disclosed composi...
The present invention provides a composition comprising a compound of formula:(I) or a pharmaceutically acceptable salt thereof,
wherein each of R1, R2, R3, y, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin recept...
Therapeutic combinations useful in the treatment or prevention of psychotic disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of psychotic disorders are provided.
Compounds of formula I pr pharmaceutically acceptable salts thereof are provided: wherein each of R1, R1', R2, R3, R4, n, and Ar are as defined in the description which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be us...
Therapeutic combinations useful in the treatment or prevention of depression or other mood disorders, to pharmaceutical compositions containing said combinations, and to their use in the treatment or prophylaxis of depression or
other mood disorders are provided. Such compounds are of formula (I) or a pharmaceutica...
Methods of reducing aggregation of a protein or proteins in a formulation, and protein formulations having reduced aggregation properties are provided. The methods and formulations described herein maintain the biological activity of a protein and increase the shelf life of protein formulations.
...
The present invention relates to pyrazolo[1,5-a]pyrimidine derivatives, compositions comprising an effective amount of a pyrazolo[1,5-a]pyrimidine derivative and methods for treating or preventing cancer, comprising administering to a subject in need thereof an effective amount of a pyrazolo[1,5-a]pyrimidine derivat...
The present invention provides a compound of formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
Methods and compositions for stimulating
hair growth and inhibiting immune system activity by
administering BMPs are provided. The methods and
compositions can be used for treating or preventing
disorders resulting in loss of hair, as well as a wide range of
autoimmune disorders.
This invention provides methods and pharmaceutical compositions for modulating bladder function, and in particular for maintaining bladder control or treating urinary incontinence.
The invention features the use of whole blood samples or samples comprising peripheral blood mononuclear cells (PBMCs) for diagnosing or evaluating the progression or treatment of leukemia. Genes that are differentially expressed in un-fractionated PBMCs of leukemia patients, as compared to in disease-free humans or...
This invention provides methods and pharmaceutical compositions for treating cognitive disorders such as learning disorders, ADD/ADHD, and other disorders.
A method for treating a disease or disorder characterized by amyloid deposit of A-beta comprising administering to the subject a therapeutically effective amount of an antibody that binds specifically to RAGE and inhibits the binding of a RAGE binding partner.
An immunogenic composition having 13 distinct polysaccharide-protein conjugates and optionally, an aluminum-based adjuvant, is described. Each conjugate contains a capsular polysaccharide prepared from a different serotype of Streptococcus pneumoniae (1, 3, 4, 5, 6A, 6B, 7F, 9V, 14, 18C, 19A, 19F and 23F) conjugated...
The invention provides compositions containing polypeptides, including therapeutic polypeptides such as interleukin-11, that are suitable for oral administration.
Pharmaceutical compositions, containing micronized-tanaproget, or pharmaceutically acceptable salt thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, butylafced hydroxyanisole, povidone, and magnesium stearate,
are provided. In addition processes of manufacturing are described.
...
Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Foπn II, micronized tanaproget polymorph Form II, and processes for converting Form II to
tanaproget Form I are provided. Also provided are methods of contraception, hormone...
The present invention provides a substituted-dihydro[1,4]oxazino[2,3,4-hijindazole compound of formula I
Formula Removed
Wherein
X is a bond, O, S, NR or CONR;
m is 0 or an integer of 1;
R is H or an optionally substituted alkyl group;
R1 and R7 are each independently H or an optionally substituted alkyl...
The present invention relates to methods for preparing substituted 3-cyanoquinolines and intermediates obtained by the methods of the present invention. The methods of the invention comprise reacting an N-aryl-2-propanimide with phosphoryl chloride to produce the substituted 3-cyanoquinolines. The methods further co...
The present invention is directed to a method of synthizing compounds of formula (I):
wherein X, Z, V, R1, R3, R4, G2, n, x, y, and z are defined herein. This invention also includes a method of preparing acid compounds of formula (VII):
wherein R is H, and R4, x, y, and z are as defined herein and PG is a protect...
The invention provides methods for treating or preventing bone degenerative disorders. The disorders treated or prevented include, for example, osteopenia, osteomalacia, osteoporosis, osteomyeloma, osteodystrophy. Paget's disease, osteoge nesis imperfecta, and bone degenerative disorders associated with chronic rena...
The invention provides compounds of formula (1) or a pharmaceutically
acceptable salt thereof, wherein R, R1, R2, R3, and B are as defined in the accompanying
specification. Methods of making such compounds are also provided.
The invention provides compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R1, R2,
R3, A, and B are as defined in the accompanying specification. Methods of making such compounds are also provided.
The present invention provides compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, m and n are defined as described herein. The invention also provides methods of making the compounds of formula (I), and methods of treating inflammatory diseases, such as rheumatoi...
The invention provides novel inhibitory polynucleotides directed against IRES sequences. The invention also provides genetically engineered expression vectors, host cells, transgenic animals, and transgenic plants comprising the novel inhibitory
polynucleotides of the invention. The invention additionally provides ...
Disclosed are methods for high-throughput screening of cell lines for use in protein expression in certain pharmaceutical,
drug development, and biotechnological processes such that high productivity cell lines are identified for their ability to
produce both desired levels of protein expression and appropriate qu...
A process for preparing an encapsulated, extended release formulation of venlafaxine hydrochloride comprising incorporation of a therapeutically effective amount of spheroids comprised of venlafaxine hydrochloride, microcrystalline cellulose and hydroxypropyl methylcellulose coated with ethyl cellulose and hydroxypr...
The invention provides 6-chloro-5-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-2-pyrazin-2-yl-N-[(1 S)-2,2,2-trifluoro-1 -methylethyl]pyrimidin-4-amine hemifumarate which is a tubulin inhibitor useful in the treatment of cancer and processes of making said hemifumarate.
The invention is directed to methods of making substituted 3- cyanoquinolines, including compounds according to the following formula: (IV) The methods are amenable to large scale manufacture, avoid the use of chromatographic separations, and provide stable, high purity product more efficiently than in the prior art...
This invention relates to certain tricyclic 6-alkylidene penems which act as a inlribitor of class-D enzymes. Lacamases hydrolyze D-lactam antibiotics, and as such serve as the primary cause of bacterial resistance. The compounds of the present invention when combined with lactam antibiotics will provide an effect...
The present invention provides methods for systematically identifying genes and proteins and related pathways that maximize protein expression and secretion by expression profiling analysis. The present invention further provides methods for manipulating the identified genes and proteins to engineer improved cell li...
Methods of preparing and parifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
The present invention provides a method for the non-sedative treatment of noise phobia in a companion animal, particularly a dog, which comprises providing said animal with a therapeutically effective amount of N-methyl-N-[3-(3-methyl-1,2,4-triazolo-[4,3-b]pyridazin-6-yl)phenyl]acetamide or 7-(3-pyridyl)pyrazolo[1,5...
The present invention provides isolated and purified polynucleotides, polypeptides, and antibodies related to mammalian
(e.g., mouse and human) legumain and the novel legumain splice variant, ZB-I. The invention further relates to the use of these
isolated and purified polynucleotides, polypeptides, and antibodies...
Compositions containing micronized tanaproget, or a pharmaceutically acceptable salt thereof, and ethinyl estradiol and methods of preparing the same are provided. Also provided are kits containing the compositions, methods of contraception and hormone replacement therapy including administering a composition contai...
This invention provides pyrrolobenzodiazepine pyridine carboxamides selected from those of
Formula (1), which act as follicle stimulating hormone receptor antagonists. The invention also provides pharmaceutical compositions and methods of treatment utilizing the compounds of Formulae (1) and (2).
...
The present invention provides monoclonal antibodies for human TrkB. In certain embodiments the inventive antibodies bind and activate human TrkB. In certain embodiments the inventive antibodies are selective for human TrkB in that they do not bind (or activate) human TrkA or human TrkC. In some embodiments the inve...
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor wherein R1 to R5 has the meaning as herein before described.
This invention provides a compound of Formula (I) wherein S1, and S2 are each independently, hydrogen, alkyl, alkenyl, alkynyl, aralkyl, substituted or unsubstituted aryl, and S1, and S2 together with the nitrogen to which
they are attached form a nitrogen containing heteroaryl and a
pharmaceutically acceptable sa...
The present teachings provide compounds of formula I
and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by admini...
The present invention provides methods for production and purification of active chromoproteins produced by Actinomadura sp. 21G792. The chromoproteins are useful for developing pharmaceutical compositions and treating diseases such as cancer or bacterial infections.
The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agon f its. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression an...
The present invention provides a safe and effective process for the selective oxidation of a 5-0-protected-LLF-28249-a compound to the corresponding 23-keto compound of formula I
wherein R is a protecting group. The present invention also provides the use of the selective oxidation process in the manufacture of mox...
The present invention provides compositions and methods useful for detecting or treating asthma or other allergic
or inflammatory diseases. In one aspect, the methods of the present invention include inhibiting the activity or expression of a
component of an arginine metabolic pathway in tissues affected by asthma...
3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of usi...
The present Invention addresses an ongoing need in the art to improve the stability of immuoGENIC compositions such as polysaccharlde-protein conjugates and protein immunogens. The invention wroaaiy relates to novel formulations which stabilize and inhibit precipitation of immunogenic compositions. More particularly...
The present invention is directed to the identification of PBMC- and IBD- associated biomarkers that may be used
to diagnose inflammatory bowel disease, and optionally, distinguish between PBMCs isolated from a patient with Crohn's disease
and PBMCs isolated from a patient with ulcerative colitis. The present inve...
The present invention relates to solid dosage formulations containing conjugated estrogens and bazedoxifene, or a salt thereof. In some embodiments, the compositions include a core comprising conjugated estrogens, and at least one coating that comprises bazedoxifene, or a salt thereof.
This invention is directed to methods of preparing compounds of formula (I):comprising the step of reacting a compound of formula (II):with a reagent of formula POX3 and silica gel at a temperature greater than about 75°C, and wherein substitutions at X, PG, A, G, R1 and R4 are set forth in the specification.
...
The present invention relates to novel methods for the preparation of glutamic acid derivatives of formula (I) and intermediates thereof, and such compounds prepared by the novel methods wherein all the variables have meaning as herein before defined.
The present invention relates to compounds of the formula (I), which are modulators of metalloproteinase activity, and pharmaceutically acceptable salts thereof, wherein W is -C(O)-, -OC(O)-, -NHC(O)-, -C(O)O-, Or -C(O)NH-; R1 is phenyl, heteroaryl, biphenyl, bicyciic aryi, tricyclic aryl, bicyclic heteroaryl or tri...
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I
The present invention also provides methods for the use thereof to inhibit ß-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor wherein R1 to R has the meaning as herein before described.
Pharmaceutical compositions and compositions arc provided for treating cognitive disorders using synergistically effective amounts of 5-HT1A receptor antagonists and cognition enhancers.
The present invention relates to l-N-amino-2-imidazolidinones and derivatives, thereof which are effective as Kvl.5 potassium channel inhibitors providing atrial-selective antiarrhythmic agents. The present invention further relates to compositions comprising said Kvl.5 potassium channel inhibitors, and to methods f...
The present invention provides a 2-amino-5-cycloalkyl-hydantoin compound of formula I
(FORMULA REMOVED)
The present invention also provides methods and compositions for the inhibition of (3-secretase (BACE) and the treatment of p-amyloid deposits and neurofibrillary tangles.
Progesterone receptor modulators of formula (I), or a pharmaceutically acceptable salt thereof, Formula (I); wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, are useful for contraception and hormone replacement therapy are described. Also provided are products containing these compounds.
...
The present invention relates to oxazolo-naphthyl acids of the formula (I) and methods of using them to modulate PAI-1 expression and 6 to treat PAI-1 related disorders.
The present invention provides compounds of formula (I) and the use thereof for the treatment of central nervous system disorders related or affected by the 5-HT6 receptor.
The present
invention is directed to compounds
of formula (I): wherein R1 is
selected from the group consisting
of -C(O)R and (a), wherein
R6 and R7 are independently
selected from H, alkyl, cycloalkyl,
heterocycloalkyl, heteroaryl
or aryl, any of which may be
optionally substituted, G is
selected from H o...
Nutritional compositions are provided which comprise oligofructose, sialyllactose and probiotic bacteria, which are useful in the eradication of pathogenic microorganisms in the gastrointestinal tracts of patients.
A glucuronide metabolite of tigecycline, and its corresponding epimer, have been identified in humans treated with tigecycline. Mass spectral data have been used to identify these structures
Compounds of the formula: I are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric
disorder (also known as pre-menstrual syndrome), attention deficit diso...
The present invention relates to uses of proteins that bind MK2 to modulate
inflammation. More particularly, the invention relates to uses of proteins that bind
MK2 for treating condition that are related to inflammation. The invention is useful
for treating inflammatory conditions, particularly those in which a ...
A pharmaceutical composition for modulating differentiation, development and activity of a T cell or cell population as herein described, comprising IL-21 or IL-21 receptor [IL-21R] modulators of the kind such as herein described in the range of from 0.1 to 99.0% along with pharmaceutically acceptable carriers or ex...
The present invention relates to, among other embodiments, protein complexes which include tumor necrosis factor alpha (TNF-&agr;) and/or tumor necrosis factor alpha receptor (TNFR). Preferably, the complexes comprise at least one polypeptide selected from the group consisting of: NF-ĸB activating kinase (NAK...
The present invention provides an amino-pyridine compound of formula I
The present invention also provides methods for the use thereof to inhibit ß-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles:
The present invention is directed to a process for preparing
compounds of formula (I): wherein A, R -R , X, s, t, u, m and Z are defined herein, comprising the step of reacting a reagent of formula (II): in the
presence of Pd(O) metal with a compound of formula (III): or salts thereof.
Another aspect of this inve...
The disclosure provides novel antibodies against growth and differentiation
factor-8 (GDF-8) and bone morphogenetic protein-11 (BMP-11). In particular,
human antibodies and antibody fragments, including those that inhibit GDF-8 or
BMP-11 activity in vitro and/or in vivo, are encompassed. The disclosure also
prov...
The present invention provides formulations that achieve effective delivery of methylnallrexone compositions. The provided formulations are useful for preventing, treating delaying, diminishing or reducing the severity of side effects resulting from use of analgesic opioids.
The present invention provides a compound of formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
Novel purification processes for obtaining vesicular stomatitis virus (VSV) of improved purity from mammalian cell culture are described herein. More particularly, in certain embodiments, a process is described for purifying VSV from cell culture fluid of a mammalian cell culture infected with VSV, the process compr...
This invention relates to methods of using weak partitioning chromatography for the purification of a product from a
load fluid containing one or more impurities. Further, the invention relates to methods of weak partitioning chromatography defined
by operating conditions which cause a medium to bind least 1 mg of...
Methods for preparing oxindole and thio-oxindole compounds are provided, which compounds are useful as precursors to useful pharmaceutical compounds. Specifically provided are methods for preparing 5-pyrrole-3,3-oxindole compounds and 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-lH-indol-5-yl)-l-methyl-lH-pyrrole-2-ca...
The present teachings provide compounds of formula I
and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by admini...
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor wherein the variables R-1 to R5 are as herein before defined.
Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline
compositions, such as tigecycline compositions, prepared by these methods.
Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
Bicyclic 6-Alkylidene-penems as Class-D ß-Lactamases Inhibitors
This invention relates to certain bicyclic 6-alkylidene penems which act as a
inhibitor of class-D enzymes. ß-Lactamases hydrolyze ß-lactam antibiotics, and as
such serve as the primary cause of bacterial resistance. The compounds of the present
inv...
The present invention provides methods for preparing a compound of formula D
having activity as dopamine autoreceptor agonist and partial agonists at the postsynaptic dopamine
D2 receptor. This compound is useful for treating dopaminergic disorders, such as schizophrenia,
schizoaffective disorder, Parkinson's dis...
The present invention is directed to a method of preventing treating and/or inhibiting cancer using compounds of
formula (I): or a pharmaceutically acceptable salt thereof. This invention is also directed to pharmaceutical compositions containing
compounds of formula (I).
This invention is directed to a crystalline 4-[(2,4-dichloro-5- methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-l-piperazinyl)propoxy]-3- quinolinecarbonitrile monohydrate having an x-ray diffraction pattern wherein 20 angles (°) of significant peaks are at about: 9.19, 11.48, 14.32, 19.16, 19.45, 20.46, 21.29, 22.33,...
The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I
The present invention also provides methods for the use thereof to inhibit secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles
The present invention relates to processes for synthesizing piperazine-piperidine compounds, and compounds useful
as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. The processes also allow for safer and environmentally
tolerant production of these useful compounds.
...
The present invention relates to succinic acid salt forms of the 5-HT1A binding agent 6-melhoxy-8-[4-(l-(5-fluoro)-quinolin-8-yl-piperidin-4-yl)-piperazin-l-yl]-quinoline, as well as crystalline forms thereof, pharmaceutical compositions thereof, and methods of use thereof.
Cyclic peptides and peptidomimetics are provided that bind to and/or modulate activities associated with Trk recep
tors, including processes associated with the growth and repair of the central nervous system (e.g., neuronal growth and survival,
axonal growth, neurite outgrowth and synaptic plasticity). Cyclic pep...
The present invention provides methods for the treatment and/or prevention of thrombocytopenia including thrombocytopenia
associated with drug-induced liver damage and thrombocytopenia associated with drug-induced bone marrow destruction.
The methods of treatment of the invention include administration of interleu...
A method is described for predicting the relative solubility of a polypeptide using polyethylene glycol (PEG) based
volume exclusion precipitation. Different polypeptides can be tested for their solubilities relative to each other or relative to a
reference. A single polypeptide can be tested for its relative solu...
The present invention relates to Thiadiazale Compounds having, for examples the Formula; compositions comprising an effective dose of a Thiadiazole Compound; and methods treating or preventing a metalloproteinase- related disorder, such as, an arthritic disorder, osteoarthritis, cancer, rheumatoid arthritis, asthma,...
The invention relates to methods for isolating a producl and/or reducing turbidity and/or impurities from a load fluid comprising the product and one or more impurities by passing the load fluid through a medium, followed by at least one wash solution comprising arginine or an arginine derivative, and collccting the...
The present invention provides lyophilized formulations comprising methylnaltrexone, and processes for preparation
of provided formulations. Additionally provided are compositions and products containing the methylnaltrexone formulation,
as well as methods for producing formulations, compositions and products. Pr...
Methods of producing a protein in cell culture comprising an anti-senescence compound, such as the antioxidant carnosine, are provided. According to teachings of the present invention, cells grown in a cell culture medium comprising an anti-senescence compound exhibit increased viability and productivity. Furthermor...
Methods for producing infectious, non-segmented, negative-stranded RNA
viruses of the Order Mononegavirales are provided that involve coexpression of a viral
cDNA along with essential viral proteins, N, P, and L in a host cell transiently transfected
with an expression vector encoding an RNA polymerase. In altern...
The present invention is directed to assays for the detection of an anti-drug antibody in general and in particular to the detection of an anti-drug antibody wherein the drug has a carbohydrate moiety. The invention is also directed to assays for the detection of a drug in general and in particular to the detection ...
The present invention provides rapamycin polymorph Form II. This invention also provides processes for preparing rapamycin polymorph Form II and pharmaceutical compositions including rapamycin polymorph Form II.
The invention provides a method of treating of inhibiting the growth of cancerous tumour cells and associated diseases in a mammal in need thereof which comprises administering to said mammal an effective amount of a substituted triazolopyrimidine derivative or a pharmaceutically acceptable salt thereof and further ...
The present invention relates to immunogenic polypeptides isolated from Staphylococcus epidermidis. The invention also relates to polynucleotides encoding Staphylococcus epidermidis polypeptides and their use in immunogenic compositions. In addition, the invention relates to methods of inducing an immune response in...
The present invention provides isolated and purified polynucleotides and polypeptides related to the IL-17F signaling pathway. The invention also provides antibodies to IL-17F homodimers and IL-17A/IL-17F heterodimers, and methods of
isolating and purifying members of the IL-17 family, including IL-17A/IL-17F heter...
A combination product containing at least two active compounds, O- desmethylvenlafaxine or a pharmaceutically
acceptable salt thereof and bazedoxifene or a pharmaceutically acceptable salt thereof is described. Also described are methods of
making and using this combination product to treat a variety of conditions...
The present invention features mammalian expression systems with improved production yields, and method of using these systems to produce desired proteins. In one embodiment, the expression systems of the present invention comprise genetically-engineered mammalian host cells cultured in a medium that contains an eff...
This invention provides a method of treating pain
in a mammal that includes administering to a mammal in need of such treatment a pain treating effective amount of a compound of the formula I: or a pharmaceutically acceptable salt thereof, wherein each of R1, R2, R3, n, y, and Ar is as defined and described herein....
The present invention provides methods and compositions for use in the treatment, prevention, and/or alleviation of drug abuse and/or its symptoms. In particular, the invention demonstrates that compositions comprising compounds of formula I are useful in such treatment, prevention, and/or alleviation: or a pharmace...
A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
A process for the preparation of a compound of formula I, having the structure
wherein
R1 is alkenyl of 2-7 carbon atoms; wherein the alkenyl moiety is optionally substituted
with hydroxyl, -CN, halogen, trifluoroalkyl of 1-6 carbon atoms, trifluoroalkoxy
of 1-6 carbon atoms, -COR5, -CO2R5, -NO2, CONR5R6, NR5...
Methods and compositions for modulating interleukin-21 (IL-21 )/IL-21 receptor (MU-1) activity using agonists of IL-21 or IL-21 receptor ("IL-21R" or "MU-1"), are disclosed. IL-21/IL-21R agonists can be used by themselves or in combination with anti-inflammatory agents to treat, e.g., ameliorate, symptoms associated...
The present invention provides novel isolated and purified polynucleotides and polypeptides related to a novel ligand for glucocorticoid-induced TNF receptor (GITR). The invention also provides antibodies to the GITR ligand (GITRL). The present invention also is directed to novel methods for diagnosing, prognosing, ...
The present invention provides controlled release dosage formulations of compounds having the Formula (I) or pharmaceutically acceptable salts thereof, and in particular, aplindore. The dosage forms are useful, inter alia, for reducing side effects from administration of such compounds.
52
The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compou...
Compounds of Formula (I) or pharmaceutically acceptable salts thereof are provided: Formula (I) which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as s...
The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compou...
The present invention provides methods of coupling carbon-containing compounds using a transition metal or transition metal complex on a solid support. The solid support can include alkaline earth metal salts, including carbonate and sulfate salts. The transition metals can include palladium or nickel metal. The met...
The present invention relates to selective adrenergica2B antagonists alone, selective adrenergicalpha2B antagonists in combination with norepinephrine reuptake inhibitors (NRI)(as a single compound or as a combination of two or more compounds), or selective adrenergicalpha2B antagonists in combination with dual nore...
The present invention is directed to alkanoyl and cycloalkanoyl-amine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, nc gastrointesti...
A process for the reductive alkylation at the C-3 position of an indole compound in which the indole is treated with an aldehyde in the presence of a Lewis acid and a silicon hydride reducing agent. The process is useful for alkylating the C-3 position of indoles that contain acid-sensitive substituents at the N-1 p...
The present invention provides a method for producing a less-painful immunogenic composition of a hydrophobic protein in a pharmaceutically acceptable carrier suitable for administering to a mammal, comprising the steps of (a) solubilizing said hydrophobic protein with a zwitterionic detergent to make a first compos...
The present invention relates to methods of treating ADAMTS-S-associatcd diseases and particularly ostcoarlhritis comprising administering an agent capable an of modulating ADMATS-5 activity to a subject afflicted with the disease. The agent is preferably a biaryl sulfonamide compound. The invention is based, in par...
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula la: wherein, R1 is lower alky], substituted lower alkyl, phehyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, subst...
The invention is directed to an antiviral for administering to a mammalian host (e.g., a human) susceptible to paramyxovirus infection, particularly respiratory syncytial virus (RSV) infection. In certain embodiments, an antiviral molecule of the invention is a polypeptide, a chemokine polypeptide, a chemokine polyp...
This application presents the discovery that the Vitamin D3 receptor (VDR), a member of the nuclear hormone ligand-activated receptor superfamily, interacts with a MNAR, a scaffolding protein. This interaction results in the formation of a ternary complex between VDR, MNAR, and the Src or PI3 kinase families of tyro...
The present invention provides improved methods to lyophilize (freeze-dry) active ingredients such as proteins, nucleic acids and viruses The present methods improve the degree of excipient crystallization during lyophilization over prior methods. The improvement in excipient crystallization is based, in part, on a ...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
This invention provides estrogen receptor modulators of fomula (I), having the structure where R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification.
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein cab be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
This invention relates to, for example, novel formulations and methods for the delivery of 4-cyano-N-[(2R)-2-[4-(2,3-dihydro-benzo[ l,4]dioxin-5 yl)-pipcrazin-l-yl]-propyl ]-N-pyridin-2-ylbcnzamidc, pharmaceutically acceptable salts thereof, structurally related compounds and/or metabolites; as well as to use of the...
Processes for preparing N-aryl-piperazine derivatives of formula 1 particularly (R).4.cyano-N-[2-[|4-(2,3-dihydro-1,4-ben-zodioxan-5-yl)-1-piperazinyipropyl]-N-(2-pyridinyl)-benzamide are disclosed. Compositions comprising N-arylpiperazine derivatives and low levels of common impurities are also disclosed. In additi...
The present invention provides processes for the preparation of amino-aryl iodides wherein a micronized amino-aryl compound is reacted with an iodinating reagent.
Antigenic isolates and vaccines for Infectious Bursal Disease Virus include variants of the molecular Group 6 family of IBDV isolates, in particular the 28-1 isolate.
Anti-Lewis Y antibodies are described. Methods for preparing monomeric cytotoxic drug/carrier conjugates with a drug loading significantly higher than in previously reported procedures and with decreased aggregation and low conjugate fraction (LCF) are described. Cytotoxic drug derivative/antibody conjugates, compos...
PASSIVE TARGETING OF CYTOTOXIC AGENTS The present invention provides methods of treating cancer cells comprising administering to a patient in need thereof a therapeutically effective amount of a non-specific antibody conjugated to a cytotoxin, wherein the cancer cells do not express an antigen to which the non-spec...
The present invention provides a process for preparing a calicheamicin conjugate comprising removing glycosylation of a protein and reacting (i) an activated calicheamicin—hydrolyzable linker derivative and (ii) the deglycosylated protein. In one embodiment, the protein is an antibody, such as an anti-CD33 antibody ...
The present invention provides a safe and effective vaccine composition which comprises: an effective immunizing amount of an inactivated Ehrlichia canis bacterin; a pharmacologically acceptable carrier; and an immunogenically stimulating amount of an adjuvant system consisting essentially of an antibody response in...
The present invention is directed to phenylaminopropanol derivatives of formula 1: or a pharmaceutical ly acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symp...
Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrile groups, are provided.
An isolated, altered fibronectin-binding protein (Fnb) of S. aureus having at least one mutation in an amino acid selected from residues corresponding to Gin 103, Gin 105, Lysl57, Lys503, Lys620, Lys702, Lys762, Gln783 and Gln830 of FnbA of S. aureus strain ATCC49525 is described. Replacement of these reactive resid...
Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein The methods include mixing the compound of formula I and a solvent, adding a base to the solvent, and precipitating purified compound of formula, I
A three-dimensional structure of protein kinase C theta (PKCtheta) can be used in methods of designing an agent that interacts with PACtheta. The agent can be an inhibitor of PKCtheta activity.
The present invention features methods of using ADAMTS-8 proteins or their functional derivatives to cleave aggrecan or other proteoglycan molecules. The present invention also features methods for identifying ADAMTS-8 modulators that are capable of inhibiting or enhancing ADAMTS-8 proteolytic activities. In additio...
PERFUSION SYSTEM AND APPARATUS FOR AUTOMATED MULTICHANNEL PATCH-CLAMP RECORDINGS UTILIZING INSIDE-OUT WHOLE-CELL CONFIGURATION
A system and method for high throughput patch clamp measurements to study the effect of various chemicals on ion transfer channels is provided. One or more patch clamp configurations is est...
This invention provides compounds of Formula II: (I) wherein: R<1>, R<2> and X are defined hereinbefore in the specification, which are useful in the treatment of cancer, stroke, myocardial infarction, neuropathic pain, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoid arthritis, and transplant...
Compositions particularly useful as coatings for solid dosage forms of therapeutic agents are provided, as are solid dosage forms comprising such coalings, processes for preparing such solid dosage forms, and the products of those processes. The coating compositions generally provide excellent strength and resistanc...
The present invention provides a novel method of reducing protein misfolding and aggregation in the cell culture by growing the cell culture at a reduced temperature and/or reduced pH. As a result, the quality of the protein produced in the cell culture is greatly improved. Thus, the present invention facilitates im...
The present invention relates to indole oxime derivatives of formula (I) wherein: R1 is -OH, -OC1-C8 alkyl, or NH2; R2 and R3 are, independently, hydrogen, C1-C8 alkyl, -CH2-C3-C6 cycloalkyl, -CH2-pyridinyl, phenyl, or benzyl; R4 is hydrogen, C1-C8 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, phenyl, benzyl, hete...
The present invention relates to Dibenzonaphthyridine Derivatives of Formula I wherein R1 to R10 has meaning as herein before described, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subj...
The present invention provides a method of treating acute lung injuries, such as acute lung injury induced by peritonitis during sepsis, acute lung injury induced by intravenous bacteremia during sepsis, acute lung injury caused by smoke inhala-tion, acute lung injury occurring in a premature infant with deficiency ...
The present teachings relate to novel compounds of formula I: wherein the constituent variables are as defined herein. Compounds of the present teachings can act as antagonists of the mammalian adhesion proteins known as selectins. Methods for treating or preventing selectin-mediated disorders are provided, which in...
This invention relates to cinnoline-based modulators of Liver X receptors (LXRs) of
formula (I) wherein R2 is a ring containing residue, particularly a phenyl residue. These
compounds are useful in the treatment of cardiovascular diseases.
The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particu...
The present invention is based on the discovery that ξPKC expression is increased in the tissues of arthritis patients as compared to normal individuals. Accordingly, the present invention provides methods of diagnosing, prognosing, and monitoring the course of arthritis in a patient based on increased ξPKC gene ex...
The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
The present invention relates to Imidazolopyrimidine Analogs, of Formula lb methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods foT treating OT preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of...
Agents (e.g. antibodies and fragments thereof) that bind specifically to IL 13 and modulate the ability of IL 13 to interact with IL 13 receptors and signaling mediators are disclosed.
Synthetic methods are provided for production of compounds of the formula: (I) where R1g R2, R< RS, Re, R?, Ra, Rg, RIO, Rn, Ri2, RIS, and R14are as defined in the specification.
The present invention relates to recombinant raccoon poxvirus vectors that express the rabies virus glycoprotein gene at the hemagglutinin (ha) locus of the poxvirus genome or express the glycoprotein gene of the same or different rabies strains at the thymidine kinase (tk) and the hemagglutinin (ha) loci of the pox...
The present invention relates to Pyrazolopyrimidine Analogs, methods of making Pyrazolopyrimidine Analogs, compositions comprising a Pyrazolopyrimidine Analog, and methods for treating mTOR -related disorders comprising administering to a subject in need thereof an effective amount of a Pyrazolopyrimidine Analog. Th...
This application relates to antibodies, e.g., humanized antibodies, and antigen-binding fragments thereof, that bind to interleukin-13 (IL-13), in particular, human IL-13, and their uses in regulating immune responses mediated by IL-13. The antibodies disclosed herein are useful in diagnosing, preventing, and/or tre...
The present invention provides a topical, high-dose, long-acting ectoparasiticide composition, kit and method for protecting against ectoparasite infestations in a warm-blooded animal for a period of greater than about 6 weeks.
The present invention relates to modified ADAMTS4 proteins having improved stability comparing to the Corresponding native, unmodified proteins. The modified ADAMTS4 proteins can be expressed and isolated in large quantities, thus allowing further characterization of the proteins, such as crystallographic and enzyme...
The present invention provides a chromoprotein produced by Actinomadura sp. 21G792, as well as amino acid and nucleic acid sequences of the apoprotein component of the chromoprotein and of components of the biosynthetic pathway for the chromophore. The present invention is useful for developing pharmaceutical compos...
The invention provides a DNA plasmid comprising: (a) a first transcriptional unit comprising a nucleotide sequence that encodes a first polypeptide operably linked to regulatory elements including a first promoter and a first polyadenylation signal; (b) a second transcriptional unit comprising a nucleotide sequence ...
The present invention relates to methods of making Gonadotropin Releasing Hormone ("GnRH") (also known as Leutinizing Hormone Releasing Hormone) receptor antagonists.
A shortened process for producing a solution containing substantially purified capsular polysaccharides from a cellular Streptococcus pneumoniae lysate broth is described. Ultrafiltering and diafiltering a clarified S. pneumoniae lysate followed by pH adjustment to less than 4.5, preferably about 3.5, precipitated a...
A polyketide synthase complex composed of polyketide synthase with 15 total modules, a non-ribosomal peptid synthetase with I module, and a cytochrome P450 hydroxylase is described. Also provided are novel Streptomyces species an methods of modified Streptomyces species. Further described are novel compounds, 36-ket...
The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ss-amyloid deposits or ss-amyloid levels in a patient.
The present invention provides compounds and methods for the use thereof to inhibit (3-secretase (BACE) and treat ß-amyloid deposits and neurofibrillary tangles.
Methods arc disclosed for separating and detecting bazedoxifenc acetate from pharmaceutical compositions containing a mixture of bazedoxifene acetate and one or more other components that produce X-Ray diffraction patterns having interfering peaks at or near the characteristic peaks for bazedoxifene acetate.
...
An improved system for large scale production of polypeptides in cell culture is provided. In accordance with the present invention, cells expressing a polypeptide of interest are grown in media that contain copper, glutamate or both. The use of such a system allows production of polypeptides in which misfolding and...
The present invention is directed to arylalkyl- and cycloalkylalkyl-piperazine derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastroi...
The present invention provides controlled release dosage formulations of compounds having the Formula (I) or pharmaceutically acceptable salts thereof, and in particular aplindore. The dosage forms are useful, inter alia, for reducing side effects from administration of such compounds.
Immunophilin ligands of general formula 1 wherein all the variables have meanings as herein before described, and their uses as modulators of calcium channel activity are disclosed. Screening, therapeutic and prophylactic methods for conditions associated with calcium channel dysfunction, e.g., neurodegenerative and...
This invention concerns a process for the preparation of benzofuran derivatives. In some aspects, these compounds are of formula I: wherein each of R1, R2, R3, and R4 is as defined herein.
Bone cement mixing systems and related methods are disclosed. The bone cement mixing systems can include a first chamber, a second chamber, and a passage fluidly connecting the first and second chambers. A first piston can be disposed in the first chamber, and a second piston can be disposed in the second chamber.
...
The present invention provides methods of treating inflammatory diseases/disorders in a subject by inhibiting/antagonizing
TREM-1 expression/activity/signal transduction and/or DAP12/TyroBP expression and/or activity. Methods of detecting
the presence of inflammatory disease in a subject by detecting TREM-1 and/o...
The invention provides a pharmaceutical composition comprising piperacillin, tazobactam, an aminocarboxylic acid, and a buffer in a sodium lactate diluent. The invention further relates to a method of treating a bacterial infection and an LR condition in a human which comprises administering to said human an effecti...
The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment, prevention or amelioration of a disease or disorder characterized by elevated ss-amyloid deposits or ss-amyloid levels in a patient
Micronized CCI-779 is described. This directly compressible rapamycin 42ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid provides a convenient and effective method to deliver therapeutic levels of CCI-779 to a patient.
The present invention is directed to phenylaminopropanol derivatives of formula (I): or a pharmaceutically acceptable salt thereof; wherein: the dotted line between Y and Z represents an optional double bond; the dotted line between the two R4 groups represents an optional heterocyclic ring of 4 to 6 ring atoms that...
The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, whereinR1, R2, R3, R4, R5, R6, R7, R8, m and n are defined as described herein. The invention also provides methods of making the compounds of formula (I), and methods of treating inflammatory diseases, such as rhe...
DIARYLSULFONE SULFONAMIDES AND USE THEROF
Compounds of Formula (I), or pharmaceutically acceptable salts thereof, are provided, which are modulators of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.
...
This invention provides an antineoplastic composition which comprisesrapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) and 4-dimethylamino-but-2-enoic acid [4-(3-chloro-4-fluoro-phenylamino)-3-cyano-7-ethoxy-quinolin-6-yl]-amide (EKB-569). The invention al...
The invention discloses a compound of the formula (I): wherein R, R1, R2, R3, R4, X1, X2, n1 and n2 are as defined in the specification an effective inhibitor of cytosolic phospholipase A2 and process for its preparation.
A process for making a vaccine composition which comprises: an immunogenically active component selected from the group consisting of a live attenuated, inactivated or killed whole or subunit West Nile virus, an antigen derived from said virus, plasmid West Nile virus DNA, plasmid with sequence inserts of sa...
The present invention provides an efficient method of preparing O-desmethylvenlafaxine.The method invlolves demthylating venlafaxinewith a high molecular weight alkane, arylalkyl or arene thiolae anion in ahydroxylic or ethereal solvent or a mixture of hydroxylic and etherealsolvents....
A biomass for producing antigen which comprises avian embryo particleswherein said particles are mechanically reduced in size to having a particle size ofabout 1.0 mm to 10.0 mm and wherein said particles are infected with an antigencapable of reproducing in an avian embryonic cell. Also pr...
A process for making an N1-(2’-pyridyl)-1,2-alkanediamine sulfamic acid of formula (II) by reacting a compound of formula (I) with NH2R’, wherein R and R’ are as defined in the specification. The invention also includes the compound of formula (II), and optical isomers thereof. The compound of formula (II) i...
The invention discloses a process for the stereoselective preparation of a compound of formula IIIwherein R and R' each independently represents a C1-C3 alkyl group; Ar represents dihydro-benzodioxinyl or benzodioxinyl, or phenyl optionally substituted with up to three substituents independently select...
The invention relates to the field of osteogenic proteins and pharmaceutical formulationsthereof. The invention is directed to the technical problem of local and systemic osteogenicprotein delivery, and particularly to the problem of delivering osteogenic proteins to the site ofbone defects...
Compounds of Formula I, wherein R1-R8 are defined herein are provided,together with pharmaceutically acceptable salts, hydrates, metabolites, and/orprodrugs thereof. Uses of these compounds for inhibiting beta amyloid productionand for the prevention and treatment of Alzheimer's Disease and...
Compounds of formula I or a pharmaceulically acceptable salt thereof are pro-vided: I where R1 through R7 are defined herein. The compounds of formula I are 5HT3c agonistsor partial agonists, and are useful for treating a variety of disorders.
The present invention provides a compound of formula (I) and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
Compounds of the Formula: are useful for thetreatment of depression ( including but not limited to majordepressive disorder, childhood depression and dysthymia). Anxiety,panic disorder, post-traumatic stress disorder, premenstrualdysphoric disorder (also known as premenstrual syndrome...
The present invention provides a compound of formula (I) and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
This invention provides compounds of Formula (1a) - (1f) wherein: X, R1 andR2 are defined hereinbefore in the specification, which are useful in the treatment ofcancer, stroke, osteoporosis, polycystic kidney disease, autoimmune disease, rheumatoidarthritis, and transplant rejection and pro...
The disclosure provides novel antibodies against growth and differentiationfactor-8 (GDF-8) and bone morphogenetic protein-11 (BMP-11). In particular,human antibodies and antibody fragments, including those that inhibit GDF-8 orBMP-11 activity in vitro and/or in vivo, are encompassed. The d...
Compounds of formula (I) and (II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, -CH2-cycloalkyl, pyridinyl, -CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, ...
The disclosure provides antibodies and antigen-binding fragments that can act as agonistsand/or antagonists of PD-1 (Programmed Death 1), thereby modulating immuneresponses in general, and those mediated by TcR and CD28. in particular. The disclosedcompositions may be used for example, in t...
This invention provides estrogen receptor modulators havingthe structure (I) where R1-R5 are as defined in the specification; or apharmaceutically acceptable salt thereof.
A process for making a compound of formula (I)in which process the compound HC=C- (CH2)n-NH2 is reactedwith the compound R1-SO2Cl to produce an intermediate compound, which intermediate compound is then reacted with thecompound of formula (II) to produce the compound of formula(...
This invention provides human LXR α variant polypeptides and nucleic acidsencoding such polypeptides. This invention also provides the therapeutic, diagnostic,and research utilities as well as the production of such polynucleotides andpolypeptides.
Recombinant lubricin molocolet and uses thereof. Novel recombinnat lubricin molecules and their cros lubricants,and adhesive agents and/or intra-articular supplement for e.g. syaovial joints. meniscus. tendon, periontum, perticudinon andpleora, are provide.
The present invention is directed to substituted aryl cycloalkanoyl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal a...
1- (1H- INDOL- 1-YL) -3- (METHYLAMINO) -1- PHENYLPROPAN-2-OL DERIVATIVES AND RELATED
COMPOUNDS AS MODULATORS OF THE MONOAMINE REUPTAKE FOR THE TREATMENT
VASOMOTOR SYMPTOMS (VMS)
present invention is directed to phenylaminopropanol derivatives of formulae (I), (II), and (III); or a pharmaceutically acceptable s...
Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF...
The present invention provides acompound of formula (I) and the use thereof forthe therapeutic treatment of disorders relating to oraffected by the 5-HT6 receptor.
This invention relates to methods and pharmaceutical compositions for providing hormone replacement therapy in perimenopausal, menopausal, and postmenopausal women through the continuous administration of combinations of conjugated estrogens and medroxyprogesterone acetate.
This invention provides compounds of Formula (I), having the structure where G1 G2, G3, G", A1, A2, Y1, Y2, L1, Z, e and f are defined herein, or a pharrnaceutically acceptable salt thereof, which are useful for treating or preventing cancer.
The present invention is directed to aryl sulfamide derivatives of formula I:
or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, includin...
Methods and compositions for reducing or inhibiting, or preventing or delaying the onset of, one or more symptoms
associated with an early and/or a late phase of an IL- 13-associated disorder or condition using IL-13 binding agents are disclosed.
Methods for evaluating the kinetics and/or efficacy of an IL-13 bin...
This invention relates to a 24 hour extended release dosage formulation and unit dosage form thereof of venlafaxine hydrochloride, an antidepressant, which provides better control of blood plasma levels than conventional tablet formulations which must be administered two or more times a day and further provi...
The invention relates to methods of treating a disease or condition, wherein expression or activity of soluble CLCA1 is up-regulated, by administering inhibitors of soluble CLCA1. The invention also relates to methods of isolating soluble CLCA1 from a bodily flnid.
[Class : 5] Pharamceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss Being Goods Falling In Class 5.
[Class : 5] Pharmaceutical Preparations Including Preparations To Treat Menopausal And Post Menopausal Conditions And For The Prevention And Treatment Of Osteoporosis Being Goods Falling In Class 5
[Class : 5] Pharmaceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss Being Goods Falling In Class 5.
[Class : 5] Pharmaceutical And Veterinary Preparations; Preparation For Treatment Of Diabetes Dietetic Substances Adapted For Medical Use Food For Babies Being Goods Falling In Lcass 5
[Class : 5] Veterinary Products And Preparations, Falling In Class 5.
Trade mark is likely to be removed due to non filing of Renewal request within prescribed time limit In case of any discripancy contact respective TM Registry.
[Class : 5] Medicinal And Pharmaceutical Preparations Falling In Class 5.
Trade mark is likely to be removed due to non filing of Renewal request within prescribed time limit In case of any discripancy contact respective TM Registry.
[Class : 5] Pharmaceutical Preparations Including Preparations To Treat Menopausal And Post Menopausal Conditions And For The Prevention And Treatment Of Osteoporosis Falling In Class 5.
[Class : 5] Medicinal And Pharmaceutical Preparations, Veterinary And Sanitary Substances; Infants And Invalds Foods, Plasters; Material For Bandaging, Materials For Stopping Teeth, Dental Wax, Disinfectants, Preparations For Killing Weeds And Destroying Vermin.
[Class : 5] Pharamceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss Being Goods Falling In Class 5.
[Class : 5] Pharmaceutical Preparations Being Sedatives Including Hypnotic Sedatives To Be Sold Only Under The Prescription Of A Registered Medical Practioner, Included In Class 5.
[Class : 5] Pharmaceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss Being Goods Falling In Class 5.
[Class : 5] Pharamceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss Being Goods Falling In Class 5.
[Class : 5] Pharmaceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss All Being Goods Falling In Class 5.
[Class : 5] Pharamceutical Preparations For Treating Symptoms Of Menopause And For The Prevention And Treatment Of Bone Loss Being Goods Falling In Class 5.
[Class : 5] Medicinal And Pharmaceutical Preparations, Veterinary And Sanitary Substances, Infants And Invalids Foods, Particularly A Food Specially Prepared For Infact Feeding, Milk Either Whole Or Filled Being Food For Infant And Invalids And Breast Milk Substitutes, Evaporated Or Condensed Milk In Liquid Or Powdered Form For Infants And Invalids, Medicinal And Surgical Pl...
[Class : 5] Pharmaceuticals Veterinary Preparations Preprarations For Treatment Of Diabetes Dietetic Substances Adpated For Medical Use Foods For Babies Being Goods Falling In Lcass 5