The present invention provides anti-N3pGlu Aß antibodies or antigen-binding fragment thereof. In addition the present invention provides the use of the anti-N3pGlu Aß antibodies or antigen-binding fragment thereof for the treatment of Alzheimers disease.
The invention is a pharmaceutical composition of human insulin or insulin analog that includes citrate, treprostinil and stabilizing agents, that has faster pharmacokinetic and/or pharmacodynamic action than commercial formulations of existing insulin analog products and that is stable for commercial use.
...
The present disclosure relates to antibodies that bind human programmed cell death 1 ligand 1 (PD-L1 ), useful for treating solid and hematological tumors alone and in combination with chemotherapy and other cancer therapeutics. Said antibodies have specific variable chain sequences. According to the experimental re...
The present invention relates to a c-Met inhibitor (disclosed herein) or a pharmaceutically acceptable salt thereof useful in treating cancer mediated by activity of c-Met receptors.
The present invention provides glucagon and GLP 1 co agonist compounds that are useful in the treatment of type 2 diabetes obesity nonalcoholic fatty liver disease (NAFLD) and/or nonalcoholic steatohepatitis (NASH). P 20637
The present invention provides 3-indazoyl-4-pyridylisothiazoles or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and methods of using the same, as well as processes for preparing the same, and intermediates thereof.
The present invention provides compounds of the formula below: where A X and R1 R6 are as described herein a pharmaceutical salt thereof and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt ...
The present invention relates to compounds with an extended duration of action at the glucagon receptor as compared to native glucagon. Specifically provided are glucagon receptor agonists with modifications to the structure of native glucagon introduced to selectively agonize the glucagon receptor over an extended ...
The present invention provides a compound of the formula below or a pharmaceutical salt thereof methods of treating diabetes using the compound and a process for preparing the compound.
Monoclonal antibodies to human tau aggregate compositions comprising such tau antibodies and methods of using such tau antibodies for the treatment of neurodegenerative diseases including Alzheimer s disease Progressive Supranuclear Palsy and Pick s disease.
The present invention provides a compound of the formula:
or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carriér, diluent, or excipient; and methods for treating physiological disorders, particula...
The compound, ((3-2-amino-1,2-dioxoethyl)-2-ethyl-l-(phenylmethyl)-1H-indol-4-yl)oxy)acetic acid morpholino-N-ethyl ester, is disclosed together with its use as a highly bioavailable indole compound for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
...
The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and pro...
The invention provides the use of a compound of the(Figure Remove)
R: is hydrogen, Q-C4 alkyl, bromo, fluoro, chloro or iodo;
or a pharmaceutically-acceptable salt thereof for the manufacture of a medicament for immunosuppressive therapy of the human or animal body.
The present invention relates to certain benzimidazole compounds of Formula I, or pharmaceutically acceptable salts thereof, that inhibit Janus kinase 1 (JAKI), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat certain types of cancer.
This invention provides a process to prepare 10,11-(optionally substituted)methanodibenzosuberane derivatives. The invention also provides an intermediate in this process.
A pharmaceutical delivery apparatus with an automatic syringe retraction following a manually controlled injection. The apparatus includes a housing, a syringe carriage, a medication-filled syringe held within the carriage, the syringe needle tip being
5 disposed within the housing when the carriage is in a first ...
The present invention includes a method for decreasing hot flashes in a human female by administering fluoxetine to that female.
Another aspect of the invention is a method for decreasing hot flashes in a human female undergoing raloxifene administration by
administrating fluoxetine to that female. Another aspect ...
The present disclosure provides animal feed supplements comprising a therapeutically effective amount of monensin and a solvent wherein the supplement is a solution. The disclosure also provides food compositions comprising a therapeutically effective amount of monensin a solvent and an animal feed methods of admini...
The present invention discloses various parenteral
pharmaceutical formulations, which comprise: a monomeric
insulin analog, zinc, protamine, and phenolic derivative.
The analog formulations provide a prolonged duration of
action. A process for preparing insulin analog-protamine
formulations is also described.
...
The present invention provides a compound or a pharmaceutically acceptable salt or hydrate and a pharmaceutical composition containing said compound or a pharmaceutically acceptable salt or hydrate useful as a Notch pathway signaling inhibitor for the treatment of cancer
ABSTRACT This invention provides a single dose oral formulation of spinosad for the extended control of a C. infestation on a cat at a predictable dose of spinosad that is suitable for administration once every 30 days (. one month). The invention also provides methods of using the formulation of spinosad.
...
The invention provides certain azetidinyloxyphenylpyrrolidine compounds particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.
The present invention provides certain imidazole carboxamide derivatives, pharmaceutical compositions thereof, methods of using the same for preparing a medicament useful in the treatment of conditions associated with the mGlur2 receptor, such as depression and anxiety, and processes of the following Formula (I) for...
The present invention provides novel trimethylammonium compounds of the Formula: (I) methods of making these compounds methods of using the compounds for preparation of tau imaging agents and preparation of tau imaging agent formulations.
The present invention provides a method of treating a cognitive or neurodegenerative disease comprising administering to a patient in need of such treatment an effective amount of a compound of the formula I or a pharmaceutically acceptable salt thereof; in combination with an effective amount of an anti N3pGlu Abet...
The present invention provides compounds of Formula I or a pharmaceutical salt thereof; methods of treating osteoarthritis and the pain associated with osteoarthritis using the compounds; and processes for preparing the compounds.
The present invention provides a novel compound of the formula: methods of making this compound, methods of using this compound for tau imaging, and preparations of tau imaging formulations.
The present invention is directed to a compound of the formula
or a pharmaceutically acceptable salt thereof; and also to compounds of formula I:
or a pharmaceutically acceptable salt thereof.
The present invention provides 1 2 benzothiazole compounds particularly useful in the treatment of diabetic nephropathy and other chronic kidney disorders and other diabetic complications.
The present invention provides compounds of Formula 1 or a pharmaceutically acceptable salts thereof where R X A E and G are as described herein methods of preparing the compounds and use of the compounds to treat pain and/or inflammation.
The present invention provides thieno[2 3 c]pyrrol 4 one compounds that inhibit activity of extracellular signal regulated kinase (ERK) and may be useful in the treatment of cancer.
A locking assembly for a medication dispensing device including a housing a drive member a medication cartridge having a barrel holding medication between a movable plunger and a septum and a dose delivery mechanism for controlling the advancement of the drive member. The locking assembly in one form includes a lock...
The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I uses of compounds of Formula I and method of using compounds of Formula I.
The present invention provides compounds of the formula wherein R is selected from the group consisting of H and CH; R is selected from the group consisting of H and CH; R is selected from the group consisting of H C C alkyl O(CH)SOCH O(CH)OCH O(CH)C(CH)OH CN and OCF; or a pharmaceutical salt thereof methods of trea...
3332The present invention provides a compound of the Formula: wherein X is selected from the group consisting of R is selected from the group consisting of H and CH; R1 is selected from the group consisting of H CH F Cl OCH C(O)OH C(O)NH or a pharmaceutically acceptable salt thereof.
The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The prese...
The present invention provides compounds of Formula (I) below: and analogues thereof where the various substituent groups R1 R2 R3 R4 R5 A and X are described herein; or a pharmaceutical salt thereof; a method of treating a condition such as hypertriglyceridemia and a process for preparing the compounds.
...
The present invention relates to dual incretin peptide mimetic compounds that agonize receptors for both human glucose dependent insulinotropic polypeptide (GIP) and glucagon like peptide 1 (GLP 1) and may be useful for treating type 2 diabetes mellitus (T2D).
The present invention provides compounds of Formula I or a pharmaceutical salt thereof methods of treating hypertriglyceridemia using the compounds; and a process for preparing the compounds.
Monoclonal antibodies are provided that selectively bind human hepcidin-25 and are characterized as having high affinity for human hepcidin-25 and strong human mature hepcidin neutralizing properties. The antibodies of the invention are useful therapeutically for increasing serum iron levels, reticulocyte count, red...
The present invention provides a combination therapy comprising the compound 4-[4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for use in the treatment of glioblastoma multiforme, a...
The present invention provides a combination therapy comprising the compound 4-[4-[4-(4-fluoro-3-trifluoromethyl-phenyl)-1-methyl-1H-imidazol-2-yl]-piperidin-1-yl]-1H-pyrazolo[3,4-d]pyrimidine, or a pharmaceutically acceptable salt thereof, and an EGFR inhibitor for use in the treatment of glioblastoma multiforme, a...
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine:
where A is C(H)= or -N= and R1-7 are as defined herein.
The invention provides certain 3 substituted 6 (pyridinylmethoxy) pyrrolopyridine compounds particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat Parkinsons disease Formula (I).
As ORL-1 receptor antagonist of the formula I, its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful; in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have als...
The present invention provides the compound l (3 3 Dimethylbutyl) 3 (2 fluoro 4 methyl 5 (7 methyl 2 (methylamino)pyrido[2 3 d]pyrimidin 6 yl)phenyl)urea or a pharmaceutically acceptable salt thereof that inhibits Raf and therefore may be useful in treating cancer.
The present invention provides novel tetrasubstituted pyridine hedgehog pathway antagonists of the following formula I (I) or a pharmaceutically acceptable salt thereof, wherein: X is C-R1 or N; R1 is hydrogen, fluoro or cyano; R2 is formula II (II), piperidinyl, or gem di-F-substituted cyclohexyl; R3 is methyl or t...
Provided are monoclonal antibodies and antigen-binding fragments thereof that bind to, and inhibit the activity of human FPN1, and which are effective in maintaining or increasing the transport of iron out of mammalian cells and/or maintaining or increasing the level of serum iron, reticulocyte count, red blood cell...
The present invention provides amino pyrazole compounds useful in the treatment of chronic myeloproliferative disorders and various cancers. E.e. glioblastoma, breast cancer, multiple myeloma, prostate, cancer, and leukemias.
Bispecific antibodies are provided that specifically bind both Tumor Necrosis Factor alpha (TNFa) and Interleukin 17 (IL 17). The bispecific antibodies of the invention are useful for treating various autoimmune diseases including Rheumatoid Arthritis (RA) Psoriatic Arthritis (PsA) and Ankylosing Spondylitis (AS).
...
The present invention provides novel mGlu2 agonists useful in the treatment of bipolar disorder, schizophrenia, depression, and generalized anxiety disorder. The novel agonists are represented by the formula.
This invention relates to pyrazole compounds or pharmaceutically acceptable salts thereof. Compounds of this invention are inhibitors of methionine aminopeptidase 2 (MetAP2) and dipeptidyl peptidase 4 (DPP 4). MetAP2 is a metalloproteinase that cleaves initiator methionine from nascent peptide emerging from the ribo...
This invention provides compounds of formula (I) : or a pharmaceutically acceptable salt thereof as inhibitors of diacylglycerol acyltransferase 1 (DGAT-1); as well as a method for treating obesity, a method for treating diabetes, and a pharmaceutical composition.
A dispensing device for dispensing medication from a medication container. The
dispensing device includes a housing, a drive member engageable with the
medication container, at least one first ramp surface fixed relative to the housing,
a driver movable within the housing to move the drive member for forcing
med...
The invention provides certain azetidinyloxyphenylpyrrolidine compounds particularly compounds of formula I wherein R is hydrogen or methyl and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat overactive bladder.
A delay mechanism for an automatic injection device having a housing and a medication filled syringe. The delay mechanism includes a shuttle a follower a damping compound at least one biasing member and a biased plunger element. When moved in the device housing from a first location to a second location the biased p...
Crystalline R-2-(4-cyclopropanesulfonyl-phenyl)-N-pyrazin-2-yl-3-(tetrahydropyran-4-yl)-propionamide and methods of its preparation and use are disclosed.
The present invention provides a compound of Formula (I): Formula (I) and methods for treating physiological disorders, particularly congestive heart failure, hypertension, diabetic nephropathy, or chronic kidney disease. The present inv ention relates to nonsteroidal mineralocpiticoid receptor antagonists.
...
The present invention provides an aminopyrazole compound, or a pharmaceutically acceptable salt thereof or a solvate of the salt, that inhibits Chk1 and is useful in the treatment of cancer.
The present invention relates to HDAC2 as a biological marker for treating cancer in a patient using Enzastaurin as a single agent or in combination with a Class I selective HDAC inhibitor.
This present invention relates to pharmacologically potent and stable human fibroblast growth factor 21 (FGF21) proteins pharmaceutical compositions comprising FGF21 proteins and methods for treating type 2 diabetes obesity dyslipidemia and/or metabolic syndrome using such proteins.
The present invention provides a compound of the Formula II: wherein A is: * R is CH3 CF or F; * R is H CH3 or F; * R is CH3 OCH OH F; R is OH or CH H; and * X is CH or N; These compounds are selective EP4 inhibitors and are useful for the treatment of inflammatory conditions such as arthritis.
...
The invention is a composition of human insulin or insulin analog that includes treprostinil and that has faster pharmacokinetic action than commercial formulations of existing insulin analog products.
An injection device for injecting a medicament includes a housing a dose setting member (20) movable to set a dose to be injected and a signal part (7). The signal part rotates from a first rotational position to a second rotational position to increase loading on a spring or spring arm when a dose is set due to rot...
1234The present invention provides a compound of Formula (III): wherein A is: Formula (A) (B) (C) (D) (E) or (F); and Z R R R and R are as defined herein or a pharmaceutically acceptable salt thereof.
The present invention is in the field of treatment of diabetes and relates to peptides that exhibit activity for both glucose-dependent insulinotropic peptide receptor (GIP-R) and glucagon-like peptide-1 receptor (GLP-1-R) and are selective over glucagon receptor (Gluc-R). Specifically provided are GIP analog...
The present invention provides a compound of the formula:
Formula (I)
or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating or preventing physiological disorders, partic...
Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above or a pharmaceutically acceptable salt thereof to an animal ...
1A TARP ?8 dependant AMPA receptor antagonist of the formula: wherein X is CH or N; A is; and R is as defined herein; its pharmaceutically acceptable salts uses and methods for its preparation are described.
An automatic injection apparatus including a delay mechanism for properly delivering medication prior to the needled syringe of the apparatus being retracted. In one form the delay mechanism includes a shuttle ( 170 ) for the syringe a follower ( 250 ) a locking member a damping compound between the follower and...
The present invention provides aldosterone synthase inhibitors of the formula (I): intermediates methods for their preparation pharmaceutical preparations and methods for their use.
The present invention provides a compound of the formula:
or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly congestive heart failure, ...
The invention provides human engineered antibodies, antigen-binding fragments thereof, that bind to, and inhibit the activity of, human DKK-1, and which are effective in treating diseases in which pathogenesis is mediated by DKK-1.
The present invention provides 6-substituted 2,3,4,5-tetrahydro-1Hbenzo[
d]azepines of Formula I as selective 5-HT2C receptor agonists for the treatment of
5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression,
and anxiety:............
The present invention provides human engineered calcitonin gene related peptide (CGRP) antibodies or antigen-binding fragment thereof. In addition the present invention provides the use of the human engineered calcitonin gene related peptide (CGRP) antibodies or antigen-binding fragment thereof for the treatment of...
The present disclosure provides animal feed supplements comprising a therapeutically effective amount of monensin,
a solvent, and a mineral mix, wherein the mineral mix is substantially free of monocalcium phosphate. In addition, the present dis -
closure provides processes of preparing animal feed supplements and...
A cartridge for a medication dispensing device which includes multiple septums. The cartridge includes a body and an axially shiftable piston in fluid-tight engagement with an interior surface of the body. The first septum covers a dispensing port that opens to an interior hollow of the body at a proximal location. ...
The present invention relates to a crystalline variable hydrate of (S)-(-3-pyridinecarboxamide 6-[4-[2-[[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]-2-methylpropyl]phenoxy])-hemi-succinate, a pharmaceutical formulation containing said salt and to methods for treating obesity and/or Type 2 diabetes using said sal...
The present invention relates to the field of diabetes. More particularly, the invention relates to PEGylated insulin lispro compounds that are PEGylated with high molecular weight poly(ethylene glycol), are highly soluble at physiological pH, have an extended duration of action, and characterized by pharmacokineti...
Monoclonal anti-myostatin antibodies that preferentially bind myostatin over GDF-11, have strong binding affinity to myostatin and are resistant to chemical degradation. The antibodies of the invention are useful for increasing muscle mass, increasing bone density, or for the treatment or prevention of various disor...
The present invention provides novel compounds of Formula (I) and (I(a)), or the pharmaceutically acceptable salt thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes fo...
The present invention provides a novel compound of Formula I,or a pharmaceutically acceptable salt thereof, having histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compo...
Methods for using TRL V6 as a biomarker for the risk of weight gain associated with treatment of a patient with a pharmaceutical agent as for example olanzapine.
The present invention encompasses isolated antibodies, or antigen-binding portions thereof, that specifically bind to the p19 subunit of IL-23. These antibodies, or antigen-binding portions thereof, are high affinity, neutralizing antibodies useful for the treatment of autoimmune disease.
Disclosed are glucagons-like peptide-1(GLP-1) compounds with modifications at one or more of the following positions: 7, 8, 12, 16, 18, 19, 20, 22, 25, 27, 30, 33, and 37. Methods of treating a subject in need of GLP-1 receptor stimulation using these GLP-1 compounds are also disclosed. (FIG). nil
...
Compounds and pharmaceutical compositions of Formula (I) by blockade of the CB1 receptors via an inverse agonism mechanism which are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics ...
The present invention relates to compounds of Formula I: pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and the use of such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
...
The present invention relates to compounds of the formula which are useful for treating conditions associated with mGluR3 receptors,
pharmaceutical compositions thereof, and methods of using the same.
The stereospecific synthesis of a glycopeptide using a triply orthogonal protection
scheme is described, in particular, the synthesis of N-acetylglucosaminyl- beta -[1,4]-
N-acetylmuramylmonopeptide and derivatives thereof. The glycopeptide is useful for
the preparation of GMDP and related compounds having a gluc...
The present invention relates to substituted benzopyran derivatives,stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor beta agonists. such agonists are useful for the treating estrogen recept...
The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising aa compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced ...
A neutralizing epitope is identified within amino acids 40-64 of the mature form of human myostatin. Antibodies that bind this epitope with high affinity preferentially bind GDF-8 over GDF-11 and may be chimeric, humanized or fully human antibodies, immunoconjugates of the antibodies or antigen-binding fragments the...
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compo...
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising com...
A compound according to formula II and the pharmaceutically acceptable salts thereof and the method of treating cancer in a patient in need thereof by administration of said compound.
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising com...
The present invention provides novel crystalline forms of {2-[l-(3,5-bistrifluoromethylbenzyl)-5-pyridin-4-yl-lH-[l,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone, compositions thereof, intermediates thereof, methods of using the same, processes for making the same, and processes for making intermediates...
The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. wherein: R1 hydrogen, hydroxy, halo, methyl, C1-C2 alkoxy, amino, or rnethylamino; R2 is hydrogen, halo, or cyano; R3 is hydrogen or halo;, R4 is hydrogen, ha...
The present invention provides glycopeptide antibiotic derivative compounds. These derivative compounds possess antibacterial activity against a wide variety of bacteria, including activity against vancomycin-resistant isolates. Methods of making and using these glycopeptide antibiotic derivative compounds are also ...
The present invention provides kinase inhibitors of Formula (I). Wherein R1, R2, X and Z are as described herein, or a pharmaceutically acceptable salt thereof.
The present invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders.
The present invention relates to a melanin concentrating hormone antagonist compound
of formula (I); wherein Ar1, L1 R1, q, X, R2, R3, R4, and R5 are as defined, or a
pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment,
prevention or amelioration of symptoms associated with ob...
ABSTRACT
TGF-BETA BINDING COMPOSITIONS
The present invention provides very high affinity antibodies, or antigen-binding fragments thereof, that neutralize mature human TGF-&bgr;l, TGF-&bgr;2, and TGF-&bgr;3. The antibodies of the invention are useful for treating cell proliferative disorders in a mammal.
...
The present invention relates to novel, non-secosteroidal, phenyl-benzoxazole compounds
of Formula (I) wherein the variables R, R', RP, RP3, LP1, LP2, ZP, RB, RB', LXB and
ZXB are as hereinafter defined, their preparation, pharmaceutical compositions, and
methods of use.
A compound of the formula (I); wherein the variables X1 to x10, R1 to R7 including R3, E, W, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases ...
The present invention relates to glucagon-like-1 compounds fused to proteins that have the effect of extending the in vivo half-life of the peptides. These fusion proteins can be used to treat non-insulin dependent diabetes mellitus as well as a variety of other conditions.
The present invention is directed to compounds of the structural Formula: wherein: R1 is H or -C1-C3 alkyl; R2 is selected from the group consisting of -H, -C1-C4 alkyl, -C1-C3 alkyl-CF3, phenyl, and pyridinyl; and R3 is selected from the group consisting of -H, -C1-C4 alkyl, -C1-C3 alkyl-O-CH3, -CH2-cyclopropyl, -C...
A delay mechanism for staging the operation of an automatic injection apparatus to ensure medication contents are properly delivered prior to the needled syringe of the apparatus being retracted. In one form, the delay mechanism includes a shuttle, a follower, a locking member, a damping compound, and a driver and a...
The present invention relates to novel muteins of human fibroblast growth factor 21 with improved pharmaceutical properties. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells for the propagation of said nucleic acid sequences and the produ...
This present invention provides a composition that is suitable for administration to a human subject comprising an anti-Aβ antibody that is free of Aβpeptide or that has acceptably low levels thereof, free of non-human Aβ peptide or that has acceptably low levels thereof, or having an undetectable concentration of A...
Humanized and chimeric antibodies are provided that specifically bind human sclerostin and are characterized as having high affinity and strong neutralizing properties. The antibodies of the invention are useful for increasing bone mass, bone mineral density and bone strength and for the treatment of various disord...
The present invention provides dosing regimens for Propanoic Acid, 2-[4-[3-[2,5-
dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1H-1,2,4-triazol-3-yl]propyl]phenoxy]-2-
methyl- and compositions thereof. A further embodiment of the present invention is a
solid oral formulation of Propanoic Acid, 2-[4-[3-[2,5-dihydro-1-[...
The present invention provides novel crystalline forms of {2-[1-(3,5-bistrifluoromethylbenzyl)-5-pyridin-4-yl-1H-[1,2,3]triazol-4-yl]- pyridin-3-yl}-(2-chlorophenyl)-methanone, compositions thereof, intermediates thereof, methods of using the same, processes for making the same, and processes for making in...
The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising com...
The present invention relates to a method of treating cancer in a patient comprising administering an effective amount of a Survivin antisense oligonucleotide in combination with an effective amount of an additional anti-cancer agent.
The present invention provides a pro-inflammatory synthetic polysaccharide antigen (SPA), or a pharmaceutically acceptable salt thereof, comprising a TLR2 -targeting synthetic
peptidoglycan (PGN) moiety onto which a first epitope and a second epitope are each
covalently attached. The first epitope comprises one or...
The present invention relates to a selective estrogen receptor modulator of formula I or a
pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or
uterine leiomyoma/leiomyomata.
This invention relates to a series of tetracyclic derivatives, to processes for
their preparation, pharmaceutical compositions containing them, and their use
as therapeutic agents. In particular, the invention relates to tetracyclic
derivatives which are potent and selective inhibitors of cyclic guanosine 3',5'-
...
The present invention relates to a crystalline variable hydrate of (S)-(-3-pyridinecarboxamide 6-[4-[2-[[3-(9H-carbazol-4-yloxy)-2-hydroxypropyl]amino]-2-methylpropyl]phenoxy])-hemi-succinate, a pharmaceutical formulation containing said salt and to methods for treating obesity and/or Type 2 diabetes using said salt...
The present invention provides Compound (I): Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and methods for the treatment of inflammatory and immune disorder...
The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising com...
The invention provides a stable solution formulation comprising a therapeutically effective amount of a GLP-1-Fc fusion protein at about pH 6.5 in citrate buffer with polysorbate-80 and mannitol. The formulation is useful in treating diabetes and obesity as well as a variety of other conditions or disorders.
...
The present invention provides formulation parameters and manufacturing conditions for stable pharmaceutical compositions comprising N-{4-(2,2-dimethyl-propionyl)-(5R)-5-[(2-ethylamino-ethanesulfonylamino)-methyl]-5-phenyl-4,5-dihydro-[1,3,4]thiadiazol-2-yl}-2,2-dimeth yl-propionamide that minimize undesirable chira...
A pharmaceutical delivery apparatus including a housing, a syringe assembly, and a needle cap. The syringe assembly is plungeable relative to the housing from a first position, at which its needle tip is disposed within the housing, to a second position, at which its needle tip projects from the housing beyond the p...
The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HT2C receptor agonists for the treatment of 5-HT2C associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where R6 is -C=C-R10, -CH=CR11R11" , or -(C0-C8)alkyl-Ar...
Compound and pharmaceutical compositions of Forumla by blockade of the CB1 receptors via an inverse agonism mechanism, and are useful for reducing body weight in mammals, cognitive impairment associated with schizophrenia, mitigating treatment emergent weight gain observed during treatment with antipsychotics and ha...
Anti-myostatin antibodies are identified that are characterized as having high affinity and may be chimeric, humanized or fully human antibodies, immunoconjugates of the antibodies or antigen-binding fragments thereof. The antibodies of the invention are useful for increasing muscle mass, increasing bone density, or...
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compo...
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising com...
An article of manufacture comprising packaging prasugrel tablets, caplets, capsule or other solid form of prasugrel in an air and/or moisture impervious container under a positive liquid gas pressure.
The present invention relates to novel compounds, (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone benzoate, and (2-chlorophenyl)-[2-(2-hydroxy-2-pyridin-4-yl-vinyl)pyridin-3-yl]methanone toluate, which are useful intermediates for the preparation of the compound of Formula I: (I) The prese...
The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.
...
Anti-IL-17 antibodies are identified that are characterized as having a high affinity and
slow off rate for human IL-17. The antibodies of the invention may be chimeric,
humanized or fully human antibodies, immunoconjugates of the antibodies or antigen-
binding fragments thereof. The antibodies of the invention a...
The present invention relates to a melanin concentrating hormone antagonist compound of
formula I: wherein " " is absent or is optionally a bond; q is 1 or 2; R1 is independently
selected from hydrogen, -C1-C2 alkyl, halo, hydroxy, -C1-C2 haloalkyi, -C1-C3 alkoxy, cyano, -O-C3-C4 cycloalkyl, and -OC1-C2 haloalkyi;...
The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N- ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino...
The present invention discloses novel aryl oxazole compounds of Formula I (I), or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing and using such compounds. In another embodiment, the invention disclose pharmaceutical...
wherein me variables X) to X1, R1 to R7 including R3, E, q, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
...
This present invention provides a composition that is suitable for administration to a human subject comprising an anti-Abeta antibody that is free of Abeta peptide or that has acceptably low levels thereof, free of non-human Abeta peptide or that has acceptably low levels thereof, or having an undetectable concentr...
A medication dispensing apparatus with a spring-driven locking feature. The apparatus includes a drive member movable in a distal direction within a housing, and a fluid container with a movable piston that is advanceable by the drive member when such drive member is moved distally by a driving means. The apparatus ...
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl...
The invention provides a stable solution formulation comprising a GLP-1-Fc fusion at a pH between about pH 6 and about pH 8.5 analogs fused to specific IgG4-Fc derivatives. These formulations provide unexpected and considerably greater chemical stability than when compared to GLP-1-Fc fusions at a pH outside the des...
A pen delivery device and a procedure for administering parathyroid hormone is
provided to allow for the priming and injection of a single predetermined dose.
The method is a three-step method using visual indicators to set the priming and
injectable dose deliveries. The device is made of a minimal number of part...
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-CO-2-alkyl, heteroaryl-CO-2-alkyl, C3-C6 cycloalkylaryl-CO-2-alkyl or phenyl...
The present invention provides Compound (I):
or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and methods for the treatment of inflammatory and immune disorders compris...
The present invention is concerned with certain novel spiro substituted heterocyclic ring
derivatives. These compounds may be useful in the manufacture of pharmaceutical
compositions for treating disorders mediated by lipoxygenase. They may also be useful in
the manufacture of pharmaceutical formulations for the ...
A selective kappa opioid receptor antagonist having the Formula (I) useful for treating ethanol use disorder withdrawal and anxiety, and/or depression, or schizophrenia as independent comorbid conditions.
The present invention relates to a melanin concentrating hormone antagonist compound
of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a
pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment,
prevention or amelioration of symptoms associated with ...
The present invention is concerned with certain novel derivatives of Formula (I): wherein X and R1 to R10 are as described in the specification, and where either R5
is OH, -NRdORa or NRd-NRbRc, or R7 is -NRdORa or NRd-NRbRc, or C=R7R8 is C=NORa or
C=N-NRbRc, which may be useful in the manufacture of pharmaceutical...
The present invention relates to crystalline non-solvated 1-(4-2-piperidinylethoxy)phenoxy)-2-(4-methanesulfonylphenyl)-6-hydroxynaphthalene hydrochloride, useful as a selective estrogen receptor modulator.
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable
salts thereof which have glucagon receptors antagonist or inverse agonist activity, as well as
methods of using these compounds and intermediates and methods for preparing such
compounds. In another embodiment, the inven...
The present invention discloses novel compounds of Formula (I) or pharmaceutically
acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist
activity, as well as methods and intermediates for preparing such compounds. In another
embodiment, the invention discloses pharmaceutical comp...
This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical composition comprising, the compounds for treatment of
neurological disorders and psychiatric disorders.
ABSTRACT;
"SELECTIVE VPAC2 RECEPTOR PEPTIDE AGONISTS"
The present invention encompasses peptides that selectively activate the VPAC2 receptor and are useful in the treatment of diabetes.
The present invention discloses novel compounds of Formula (I) or pharmaceutically
acceptable salts thereof which have histamine-H3 receptor antagonist or inverse
agonist activity, as well as methods and intermediates for preparing such compounds.
In another embodiment, the invention discloses pharmaceutical comp...
The present invention is concerned with certain derivatives of Formula:(I). wherein R. R1 to R10
are as described in the specification, and at least one of CR5R6, or CR7R8, or CR9R10 is a an
optionally substituted azetidine ring or an optionally substituted oxetan ring, which may be
useful in the manufacture of p...
The present invention relates to a stabilized composition for reducing the risk of bone
fracture and increasing toughness or stiffness of bone at a site of potential for actual
trauma. Further, the invention also relates to methods for increasing the toughness and/or
stiffness of bond and/or reducing the likeliho...
An insoluble composition, comprising:
a) a protein selected from the group
consisting of insulin, insulin analog, and proinsulin;
b) a derivatized protein selected from the
group consisting of derivatized insulin, derivatized insulin
analog, and derivatized proinsulin;
c) a complexing compound;
d) a hexamer-s...
The present invention relates to glucagon receptor polypeptide antagonists which inhibit the binding of the hormone glucagon to its receptor. More particularly, the present invention relates to high affinity glucagon receptor antibodies or Fab fragments thereof that inhibit binding of glucagon to its receptor and th...
CB-1 receptor inverse agonist compounds of Formula and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.
The present invention, provides isolated proteins
comprising beta-lipotropin (3LT), analogs thereof, fragments
thereof, nucleic acids encoding same, and methods for
producing and using BLT in the treatment of diabetes and
complications associated therewith.
CB-1 receptor inverse agonist compounds of Formula
and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.
This invention relates to a series of tetracyclic derivatives, to processes for their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents. In particular, the invention relates to tetracyclic derivatives which are potent and selective inhibitors of cyclic guanosine 3",5"-mono...
The present invention discloses novel compounds of Formula I: having 11β -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compos...
TITLE: A 1 H-SUBSTITUTED-INDOLE-3-GLYOXYLAMIDE COMPOUND AND PROCESS OF PREPARATION THEREOF.
A class of novel 1H-substituted-indole-3-glyoxylamides is disclosed together with the use of such indile compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
...
The present invention discloses novel compounds of Formula I: ( I ) possessing 11β -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds ...
The present invention provides a method for inhibiting
bone loss comprising administering to a human in need thereof a
first compound selected from 1) triarylethylenes; 2) 2,3-diaryl-
2H-1-benzopyrans, 3) l-aminoalkyl-2-phenylindoles; 4) 2-phenyl-
3-aroylbenzothiophenes, 5) l-substituted-2-aryl-
dihydronaphthal...
The present invention is directed to a novel,non-solvated,crystalline from of 6-hydroxy-2-(4-hydroxypheny1)-3-[4-(2-piperidinoethoxy)benzoy1]benzo[b]thiophene hydrochloride.
A Form III of (R)-7-acetyl-5-(4-aminophenyl)-8, 9-dihydro-8-methyl-7H-1, 3-dioxolo[4,5-h][2,3]benzodiazepine having an X-ray powder diffraction pattern with d spacings at 10.61, 8.83, 6.78, 5.83, 4.13 and 3.74 A. The compound is useful as an AMPA antagonist.
The present invention provides a compound of formula I
wherein
R1 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl);
R2 is -H, -OH, -0(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl) or -OSO2(C4-C6 alkyl);
n is 2 or 3; and
R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimet...
A crystalline form of (R)-7-acetyl-5-(4-aminophenyl)-8,9-dihydro-8-methyl-7H-l,3-dioxolo[4,5-h][ 2,3]benzodiazepine having an X-ray powder diffraction pattern with d spacings at 12.78, 9.48, 8.99, 8.64, 8.23, 6.39, 6.27. 5.73, 4.01 and 3.96 A'. The compound is useful as an AMPA antagonist.
The present invention discloses novel compounds of Formula: possessing I 1β-1 ISO type I antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and co...
The present invention relates to the field of diabetes. More particularly, the invention relates to a monomeric insulin analog wherein the A chain is the naturally occurring sequence of the human insulin A chain and the B chain is modified at either position B28 and B29 or both. The analog is mono-acylated at the N-...
This invention provides a process for preparing
gemcitabine hydrochloride which comprises deblocking β-1-
(2"-deoxy-2",2"-difluoro-3",5"-di-O-benzoyl-D-
ribofuranosyl)-4-aminopyrimidin-2-one with a catalytic
amount of an alkylamine in the presence of methanol or
ethanol in an environment essentially free of wat...
The invention provides GLP-1 compounds coupled to two polyethylene glycol molecule or derivative thereof, resulting in a biologically active peptide with an extended half-life and a slower clearance when compared to that of unPEGylated peptide. These PEGylated GLP-1 compounds and compositions are useful in treating ...
The present invention relates to AMPA receptor potentiators of Formula (I), formulations comprising them, methods for their use, and intermediates useful for their preparation.
A solid oral pharmaceutical formulation comprising 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno (2, 3-b)(1,5) benzodiazepine(olanzapine) as an active ingredient alongwith a bulking agent; binder, disintegrant, a dry binder to assure adequate; friability, and a lubricant; wherein such solid oral composituion is ...
The invention provides novel benzothiophenes of the
formula (I):
wherein R1 is N-pyrrolidinyl or N-piperidinyl;
R2 and R3 are independently hydrogen,-CO-(C10-C22
alkyl), -CO-(C10-C22 branched alkyl), -CO-(C10-C22
alkenyl), -CO-(C10-C22 polyalkenyl), -CO-(C10-C22
alkynyl),or -CO-(CH2)nCOR4; provided R2 and R...
This invention provides compounds of the formula:
The invention further provides the use of this compound to prepare N,N'-bridged bisindolylmaleimides. Furthermore, the invention provides pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mix...
The present invention discloses novel compounds of Formula I: ( I ) possessing 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds a...
The present invention relates to a pharmaceutical composition compnsmg a first component which is olanzapine, or pharmaceutically acceptable salt thereof in the range of 0.25 to 50 mg, once/day, and a second component which is fluoxetine, or pharmaceutically acceptable salt thereof in the range of 1 to 80 mg, once/d...
The present invention provides a compound of the formula : Formula (I) or a
pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an
effective amount of a compound of Formula (1) in combination with a suitable carrier,
diluent, or excipient; and methods for treating physiological disord...
A medicament comprising as an active ingredient the hydrochloride salt of a compound of the formula I
said medicament pharmaceutical formulation adapted for preventing breast cancer in a postmenopausal woman human by administration for a sufficient term about 60 mg of said salt is administered.
...
This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics, the improvement residing in employing pyridine.borane as 5 reducing agent.
This invention is concerned with improved processes for reductive alkylation of glycopeptide antibiotics. The improvement residing in providing a source of copper which 5 results in the initial production of a copper complex of the glycopeptide antibiotic. Reductive alkylation of this complex favors regioselectiv...
Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases
A compound of the formula (I)
wherein ;
A is phenyl or pyridyl wherein the nitrogen is at the 5-,
6-, 7- or 8-position;
one of B or D is nitrogen and the other is carbon;
Z is cyclohexenyl, phenyl, pyridyl, wherein the nitrogen
is at the 1-, 2-, or 3-position, or a 6-membered
heterocyclic ring having one het...
A method and apparatus for administering a pharmaceutical. The method employs a delivery
device including a housing, a pharmaceutical containing needled syringe movable within the
housing, an activation button disposed at one of the housing, and wherein the housing is
flared radially outward at the other end and ...
The present invention relates to novel muteins of human fibroblast growth factor 21 with reduced capacity for O-glycosylation when expressed in yeast compared to wild- type human FGF-21. Both protein and the respective encoding nucleic acid species are disclosed. The invention also embodies vectors and host cells fo...
The present invention relates to selective allosteric potentiators of the Formula (I):
or pharmaceutically acceptable salts thereof, for the treatment of disorders associated with
M4 muscarinic receptors.
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine:
I
where A is –C(H)= or –N=; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyrid...
The present invention provides compounds of formula I:
pharmaceutical compositions thereof, and methods of using the same, processes or
preparing the same, and intermediates thereof.
The present invention relates to novel, non-secosteroidal, phenyl-naphthalene compounds of Formula (I): wherein R, Rl, RP, ZP, LP1, LP2 LNP, RP3, RN, and ZNP are defined herein, their preparation, pharmaceutical compositions, and methods of use.
The invention relates to the field of pharmaceutical and organic chemistry and provides an improved process for preparing the novel heptahydrate crystalline salt of multitargeted antifolate N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid.
The present invention discloses various parenteral
pharmaceutical formulations, which comprise: a monomeric
insulin analog, zinc, protamine, and phenolic derivative.
The analog formulations provide a prolonged duration of
action. A process for preparing insulin analog-protamine
formulations is also described.
...
The present invention relates to novel substituted imidazo[l,2-b]pyridazine compounds of Formula (I): pharmaceutical compositions thereof, and the use such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric disorders and neurological diseases.
...
The present invention discloses novel compounds of Formula I: having 11 Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and com...
The present invention discloses novel compounds of Formula I: (I) having 11 -HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and com...
The present invention discloses novel compounds of Formula I: ( I ) having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and c...
Antibodies specific for mature TGF Beta 1 over mature TGF Beta 2 and mature TGF Beta 3 are provided. The antibodies are characterized by CDR3 of the heavy- chain GYRX1X2X3Y wherein X1 is W or A, X2 is F or L, X3 is A, E or Y.
discloses novel compounds of Formula 1:
5 having 11β-HSD type I antagonist activity, as well as methods for preparing such compounds, in another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula 1. as well as methods of using the compounds and compositions to ...
Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
4-[5-(2-Amino-ethanesulfonyl)-isoquinolin-7-yl]-phenol or a pharmaceutically acceptable salt thereof or a hydrate of the compound or the salt thereof as Akt inhibitors that are antineoplastic and/or antiviral agents as well as compositions comprising these compounds and methods of using these compounds.
...
The present invention provides antibodies that bind human CXCR4 and are characterized as having high affinity and strong neutralizing properties. The antibodies of the invention are useful in the treatment of tumorigenesis, including tumor growth, invasion, angiogenesis, or metastasis.
Monoclonal antibodies are provided that bind to the N-terminus of human hepcidin-25 and are characterized as having high affinity and selectivity for the polypeptide. The antibodies of the invention are useful for increasing serum iron levels, reticulocyte count, red blood cell count, hemoglobin, and/or hematocrit i...
The present invention provides AKT and p70 S6 kinase inhibitors of Formula (I). The present invention also provides pharmaceutical compositions comprising compounds of Formula (I), uses of compounds of Formula (I) and methods of using compounds of Formula (I).
Provided are monoclonal antibodies, antigen-binding fragments thereof, and combinations of the foregoing, that bind to, and inhibit the activity of, c-Met, and that are effective in treating cancers and other diseases, disorders, or conditions where pathogenesis is mediated by c-Met.
ABSTRACT The present invention discloses novel compounds of Formula I: ( I ) having 11-Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the co...
Provided are lactam-cyclized peptide CXCR4 antagonists useful in the treatment of cancers, rheumatoid arthritis, pulmonary fibrosis, and HIV infection.
Compounds of formula
wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.
The present invention relates to compounds of formula I:
or a pharmaceutically acceptable acid addition salt thereof, where;
X is C(R3c= or -N=;
R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7
cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle;
R2 ...
An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also d...
A compound of the formula (I) and pharmaceutical compositions for the treatment or prevention of pain.A compound of the formula (I) and pharmaceutical compositions for the treatment or prevention of pain.
The present invention relates to a selective estrogen receptor modulator of formula I or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
A cartridge with injection needles for an injection device. The cartridge includes a plurality of injection needle assemblies each including a hub and a needle having ends that face in a first direction. The cartridge also includes a needle assembly support defining a plurality of needle assembly accommodating cavit...
The invention provides GLP-1 compounds coupled to al leasl one polyethylene glycol molecule.or derivative thereof, resulting in a biologically active peplide with an extended haif-life and a slower clearance when compared to that of unPEGylaied peplidc. These PEGyJated OLP-1 compounds and compositions are useful in ...
Disclosed are immunogenic compositions comprising a modified live bovine viral diarrhea virus type lb (BVDV lb) and methods for their use in the formulation and administration of therapeutic and prophylactic pharmaceutical agents. In particular the invention provides immunogenic compositions and methods for preventi...
Provided are analgesic compounds and salts thereof of formula: ( I ) wherein A is: ( A ) Additionally pharmaceutical formulations and methods of use employing the above compounds are provided.
This invention relates to novel heterocycles which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), also referred to as 11CBy, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in medicines. Compounds of the invention have the formula: (I)
...
The present invention relates to compounds that inhibit activity of the histone lysine methyltransferase Enhancer of Zeste Homolog 2 (EZH2) pharmaceutical compositions comprising the compounds and methods of using the compounds to treat cancer such as hematologic and solid tumors.
A guide and follower cooperate to promote a user moving the driver relative to the housing along a travel path that operates the apparatus. The cooperating elements of the nut and the driver are disengaged when the driver is disposed in a reset segment of the travel path, and the cooperating elements of the nut and ...
Bispecific antibodies are provided that bind Calcitonin Gene Related Peptide (CGRP) and Interleukin 23 (IL 23) and are characterized as having high affinity and strong simultaneous neutralizing properties to both CGRP and IL 23. The bispecific antibodies of the invention are useful for treating various autoimmune di...
The disclosure herein includes 5 (5 (2 (3 aminopropoxy) 6 methoxyphenyl) 1H pyrazol 3 ylamino)pyrazine 2 carbonitrile (S) lactate monohydrate that inhibits Chk1/2 and is useful in the treatment of cancer.
The present invention is directed to compounds represented by the following structural formula, Formula I:
wherein:
(a) X is selected from the group consisting of a single bond, O, and S;
(b) U is an aliphatic linker;
(c) Y is selected from the group consisting of O, C, and S;
(d) W is N;
(e) E is C(R3XR4)A...
The present invention relates to antibodies that bind to human CGRP compositions and kits comprising such CGRP antibodies and methods of using such CGRP antibodies for detection of human CGRP.
The present invention is directed to a novel compound, its composition and use of a compound having a structural formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomers thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor ...
"BICYCLIC SUBSTITUTED INDOLE-DERIVATIVE STEROID HORMONE NUCLEAR RECEPTOR MODULATORS"
The present invention provides a compound of the formula:
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrie...
The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
The present invention relates to an extended release once daily pharmaceutical formulation comprising venlafaxine hydrochloride and pharmaceutically acceptable excipients. More particularly, the present invention relates to an extended release composition in the form of mini-tablets which are incorporated in hard ge...
The present invention discloses compounds of formula I
wherein A, n, q, K, W, X, Y, Z, R1, R2, R3, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and its sequelae.
Compounds of Formula I wherin n,q,Y,R1,R2a,R2b,R3a,R3b,R4,R5,and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.
Compounds of Formula (I): wherein n, m, p, q, Y, R1 R2, R3a, R3b, R4, R5, and R6 are as defined herein and their pharmaceutical compositions and methods of use are disclosed.
The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising com...
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compo...
1-(lndole-6-carbonyl-D-phenylglycinyl)-4-(1-methyl-piperidin-4-yl) piperazine D-tartrate forms a stable crystalline salt and is an inhibitor of the serine protease, Factor Xa, useful in the treatment of cardiovascular disorders.
Antibodies are provided that specifically bind seven human ELR CXC chemokines. The antibodies of the invention are useful for treating various inflammatory/autoimmune diseases such as inflammatory bowel disease (IBD) plaque psoriasis and palmoplantar pustulosis; and cancer such as renal cancer or ovarian cancer.
...
The present invention relates to antibodies to proprotein convertase subtilisin/kexin type 9 (PCSK9) or antigen binding fragments thereof compositions comprising such PCSK9 antibodies or antigen binding fragments and methods of using the same for the treatment of hyperlipidemia or hypercholesterolemia.
...
The present invention provides a method for preventing and/or treating a patient with acute kidney injury caused by a variety of conditions. The method comprises administering to the patient soluble thrombomodulin variants that do not bind thrombin. In conjunction with standard of care, soluble thrombomodulin varian...
Bispecific antibodies are provided that specifically bind B cell Activating Factor of the TNF Family (BAFF) and Interleukin 17A (IL 17) and are characterized as having high affinity and strong neutralizing properties to both BAFF and IL 17. The bispecific antibodies of the invention are expected to be useful in trea...
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)= or N=, provided that at least one of A and B is -N=, n is 1-3, m is 0-3, and R14 are as defined herein.
...
A stabilized composition for reducing the risk of bone fracture and increasing toughness or stiffness of bone at a site of potential for actual trauma, said composition comprising : a) a therapeutically effective amount of a parathyroid hormone selected from the group of PTH (1-31).PTH (1-34).PTH (1-37),PTH (1-38) a...
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful in the treatment of cell proliferative diseases.
A cartridge (260) with injection needles for an injection device. The cartridge includes a plurality of injection needle assemblies (385), each including a hub and a needle. Each needle has ends that both face in a first direction. Each hub has one portion movable relative to another hub portion between a ready arra...
A dispenser (10, 10.1) for medication is disclosed which dispenser
comprises a marker (18, 24) and a set of indicia, the indicia being recognisable by
the user of the dispenser as indicating meals that are taken during each day. The
marker and indicia are displaceable with respect to one another so that the juxta...
A trigger assembly for an automatic injection device which by its operation releases a biased element of the device for movement. The trigger assembly includes a button pressable by a user and a lock member. Prior to the button being plunged a blocking element on the button is abutted by a button engaging surface of...
Methods for reducing the environmental impact of animal waste are described. In particular embodiments the methods comprise administering to an animal an enzyme such as alkaline phosphatase that is effective to reduce the amount of a detrimental compound such as ammonia or phosphorous that is present in or released ...
The present invention provides a compound of the formula:
or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising an effective amount of a compound of Formula I in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly...
The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods of using the compounds and com...
This present invention relates to pharmacologically potent and/or stable variants of human fibroblast growth factor 21 (FGF21) pharmaceutical compositions comprising FGF21 variants and methods for treating type 2 diabetes obesity dyslipidemia or metabolic syndrome or any combination thereof using such variants.
...
The present invention provides for novel compounds of formula I wherein X is S or S(O); R1 and R2 are each independently selected from the group consisting of -CH2CH3 and phenyl; or R1 and R2 combine to form morpholino; and processes to prepare arzoxifene.
The present invention provides an amino pyrazole compound which is 3 [(lR) 6 fluoro 2 3 dihydro 1H inden l yl] N (3 methyl IH pyrazol 5 yl) 3H imidazo[4 5 b]pyridin 5 amine or a pharmaceutically acceptable salt thereof that inhibits JAK1 and JAK2 and therefore may be useful in treating cancer.
A neutralizing epitope is identified within amino acids 40-64 of the mature form of human myostatin. Antibodies that bind this epitope fall within the scope of the invention and may be murine, chimeric, or humanized antibodies, immunoconjugates of the antibodies or antigen-binding fragments thereof. The antibodies o...
The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The present invention...
Provided are novel methods and formulations for topically controlling ectoparasite infestations in animals using spinetoram or a pharmaceutically acceptable salt thereof.
The present invention provides compounds of Formula I. Wherein Rl L and A are as described herein or a pharmaceutical salt thereof processes for preparing the compounds and methods of treating a condition such as hypertriglyceridemia using the compounds.
The present invention provides compounds of formula I:
pharmaceutical compositions thereof, and methods of using the same, processes or
preparing the same, and intermediates thereof.
This invention provides compositions and methods useful
for treating cancers, in particular, cancers that are not
multi drug resistant. The methods of the present invention
include the 2",2"-difluoronucleoside anti-cancer agents
described in US Patent 5,464,826 in combination with
leukotriene (LTB4) antagonists...
A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lympho...
A method to treat conditions associated with Aß peptide activity both
prophylactically and therapeutically is described. The method employs humanized
antibody fragments that specifically bind human Aß peptide between amino acid
positions 13-28, wherein the antibody fragments are covalently attached to a polyethy...
Compounds of Formula (I), wherein n is 1 or 2, and R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, their preparation, pharmaceutical compositions, and methods of use are disclosed.
This invention provides a process to prepare 10,11-(optionally substituted)methanodibenzosuberne derivatives. The invention also provides an intermediate in this process.
Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts, pharmaceutical compositions, uses, and methods of use thereof are provided.
Novel selective estrogen receptor degraders (SERDs) according to the formula:, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, -CF3, or -CH3, and the other is hydrogen, and methods for their use are provided.
...
Disclosed herein are systems and methods for remote prescription of medication-dosing regimens. One embodiment takes the form of a method that includes presenting, via a healthcare- professional-(HCP)-portal user interface of an HCP system, multiple medication-dosing regimens pertaining to a patient. Each presented ...
The present invention provides the following compounds or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds useful as a Notch pathway signaling inhibitor for the treatment of named cancers sensorineural hearing loss caused by auditory hair cell loss and inducing audi...
An injection device assembly including a housing, a syringe, a drive mechanism and one or more sensing systems are described. The drive mechanism advances the syringe from a storage position to an injection position, and a plunger advances the syringe piston from an initial position to a final position. The status s...
The present invention provides a compound or a pharmaceutically acceptable salt of the Formula : X1 I V X2 S L D V P I G L L Q I L X3 E Q E K Q E K E K Q Q A K* T N A X4 I L A Q V-NH2 wherein the X1 denotes that the I residue is modified by either acetylation or methylation at the N-terminus; wherein X2 is L or T; w...
The invention provides compounds of the formula: (A) pharmaceutically acceptable salts pharmaceutical compositions thereof and methods of using these compounds salts or compositions to treat hyperphosphatemia chronic kidney disease and/or the cardiovascular diease associated with chronic kidney disease.
...
The present invention provides compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, where n and R1 are defined herein, methods of treating patients for liver disease, and processes for preparing the compounds.
The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating metabolic conditions, such as type 2 diabetes mellitus, heart failure, diabetic kidney disease, and non-alcoholic steatohepatitis.
Abstract Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl] (2-methyl-2H-tetrazol- 5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]- cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof, hydrate, and hydrate in cryst...
The present invention provides 5-[5]-[2-cycloa Ikyl ]-6-pyridazin-3-yl ]- IH-pyrimidine-2,4-dione compounds, or pharmaceutically acceptable salts thereof, that inhibit the activity of CD73 and are useful in treating cancer. (Formula (I))
The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, to pharmaceutical compositions comprising the compounds, to methods of using the compounds to treat physiological disorders such as cancer.
The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula (I) for treatment of neurodegenerative diseases and disorders, such as Alzheimer"s disease.
The present invention provides a powder formulation containing glucagon or a glucagon analog for nasal administration useful in the treatment of hypoglycemia and in particular the treatment of severe hypoglycemia. The present invention also provides a method of making this powder formulation and to devices and metho...
The present invention relates to novel aminopyridyloxypyrazole compounds that inhibit the activity of transforming growth factor beta receptor 1 (TGFpRI) pharmaceutical compositions comprising the compounds and methods of using the compounds to treat cancer preferably colon cancer melanoma hepatocellular carcinoma r...
The present invention provides an aminopyrazole compound or a pharmaceutically acceptable salt thereof that inhibits Chk1 and is useful in the treatment of cancer.
The present invention provides compounds of the Formula (I) wherein L is selected from the group consisting of -CH2NHCH2-, -CH2NH-, -NH-, -S-, -S(O)-, -S(O)2-, -O-, -OCH2-, -OCH2CH2O-, -NHSO2NH-, (II) and (III), or a pharmaceutically acceptable salt thereof; a compound of the formula: (IV), processes for preparing t...
The present invention is directed to a novelcrystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]-phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophenehydrochloride and uses for same, including inhibition ofdisease states associated with estrogen deprivationincluding cardiova...
A pharmaceutical composition for reducing mortality and morbidity comprising a compound selected from the group consisting of GLP-1, GLP1 analogs, GLP-1 derivatives, and pharmaceutically-acceptable salts thereof.
The invention provides a pharmaceutically acceptable oleaginous or cholesterol microsphere formulation of olanzapine or olanzapine pamoate or solvates thereof. The invention further provides novel olanzapine pamoate salts or solvates thereof.
This invention relates to a kit useful for preventing S. pneumoniae infection in la susceptible individual comprising NDISACC-(4-(4-chlorophenyl)-benzyl)A82846B or teicoplanin, or pharmaceutically acceptable salts, hydrates or solvates thereof, or mixtures thereof and one or more carriers, diluents or exc...
There is disclosed a parenteral pharmaceutical formulation comprising (i) anechinocandin compound such as herein described, or a pharmaceutically acceptablesalt thereof; (ii) a pharmaceutically acceptable micelle- forming surfactant,such asherein described ; (iii) a non-toxic; aqueous solve...
The present invention relates to glucagon-like-1 compounds fused to proteins that havethe effect of extending the in vivo half-life of the peptides. These fusion proteins can beused to treat non-insulin dependent diabetes mellitus as well as a variety of otherconditions. ...
The present invention is directed to a novel, non-solvated, anhydrous crystalform of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]-phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, includinginhibition of disease states associated with estrogen deprivation including<...
The invention relates to a compound of formula IWhereinR13, R14 and R17 are hydrogen;a pharmaceutically acceptable salt thereof or a pharmaceuticalcomposition comprising compound of formula I or its salt with apharmaceuticals acceptable additive.
The present invention provides the compound of formula (I), (N)-((S)-2-hydroxy-3-methyl-butyryl)-1-(L-alaninyl)-(S)-1-amino-3-methyl-2,3,4,5-tetrahydro-2H-3-benzazepin-2 one, compositions thereof, and methods for using the same.
Novel pyrrazole compounds and their use as pharmaceutical agents, in particular their use as TGF-beta signal transductioninhibitors. The disclosed invention relates to compounds of the structure (I) wherein (1) is afour, five, or six membered saturated ring and X is C, O or S. ...
N-(2-ARYLETHYL) BENZYLAMINES AS ANTAGONISTS OF THE 5-HT6RECEPTORThe present invention provides compounds of formula (I), which are antagonists of the 5-HT6 Receptor.
A N-[be nzoyl]-heteroarylsulfonamide com pounds, useful for treating susceptibleneoplasamsThe present invention provides antineoplastic compounds of the formula (I).
This invention relates to compounds of formula (I) where R1 to R12, -W-V-, -X-Y-, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals.
Human antibodies, preferably recombinant human antibodies that specifically bind tohuman Fas Ligand (hFasL) are disclosed. These antibodies have high affinity for hFasL,a slow off rate for hFasL dissociation and neutralize a Fas Ligand activity in vitro and invivo. An antibody of the invent...
The present invention provides compounds of formula (I). The present inventionfurther provides the use of a compound of formula (I) for the manufacture of amedicament for the treatment of a neurological disorder. The present inventionfurther provides the use of a compound of formula (I) for...
The compounds of formula (I) in which R represents a hydrogen atom or a fluorine atom, or a pharmaceutically acceptable salt thereof are FactorXa inhibitors useful in the treatment of thrombotic disorders.
This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof pharmaceuticalcompositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparationand intermediates therefor. (I) wherein: D is a ...
A compound of the formula (I) wherein the variables X1 to X10, R1 to R7 including R3', E, v, y, z, A and B are as described, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Dise...
The invention provides GLP-1 compounds coupled to at least one polyethylene glycolmolecule or derivative thereof, resulting in a biologically active peptide with an extendedhalf-life and a slower clearance when compared to that of unPEGylated peptide. ThesePEGylated GLP-1 compounds and comp...
A medication dispensing apparatus that provides a mechanical advantage.During dose preparing, a nut rotating element (410) and a screw element (368) are ina first axial arrangement such that a screwing motion of the nut rotating element andscrew element relative to the apparatus housing tha...
The present invention provides 6-substituted 2,3,4,5-tetrahydro-lH-benzo[d]azepines of Formula (I) as selective 5-HT2c receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety, where, R6 is -NR10R11, where RIO is substituted phenylal...
The present invention relates to a selective estrogen receptor modulator compoundcontaining phenylsulfonyl group formula I: or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosisand/or uterine leiomyoma/leiomyomata.
The present invention provides compounds of the Formula (Ia) wherein R is selected from the group consisting of CH CH (CH) CHCN CHCHF CHCF (A) (B) (C) (D) (E) (F) CHCHOCH and CHC(O)OCH(CH)R is selected from the group consisting of CF OCF and Cl; R is selected from the group consisting of H and F; or a pharmaceutica...
The present invention provides a compound of the Formula (I): wherein X R R R R R R R R R and R are as defined herein or a pharmaceutically acceptable salt thereof.
13232232323232232223343232332The present invention provides a compound of the Formula (I) below: wherein R is selected from the group consisting of H CH CN CHCN C(CH)CN F Cl and Br; R is selected from the group consisting of H O(C1 Calkylene)R4 CHCN CN OCH CF C(CH)CN C(CH) S(O)CH S(O)NH and OCF; R is select...
A cap assembly mountable to a rigid shield around a needle of a syringe. The cap assembly includes a gripper component and a base cap. The gripper component includes a support frame and a liner that is deformable when sandwiched between the support frame and the rigid shield. When the base cap is installed to the gr...
A needle covering system for a needle of a syringe. A boot of the system defines a contaminant proof pocket for the needle. A sealing ring portion of the boot forms a seal with a support portion of the syringe. A body of the boot is collapsible to allow movement of a needle pierceable end portion of the boot toward ...
The present invention provides compounds of Formula (1) or a pharmaceutically acceptable salt thereof formula (1) where R R1 and G are as described herein; methods of preparing the compounds; and use of the compounds to treat pain and/or inflammation associated with arthritis or osteoarthritis.
...
The invention relates to engineered humanized antibodies that have high binding affinity for and neutralize human IL 21 methods of using the antibodies to treat conditions in which antagonism or neutralization of the effects of IL 21 is warranted such as autoimmune conditions compositions and methods for recombi...
The present invention relates to antibodies that bind human angiopoietin 2 (Ang2) and may be useful for treating cancer alone and in combination with VEGF pathway inhibitors especially cancer driven by VEGFR2 and Ang2 including gastric hepatocellular carcinoma ovarian colorectal and breast cancers.
...
The present invention relates to compounds that bind to human vascular endothelial growth factor receptor 2 (VEGFR2) and human angiopoietin 2 (Ang2) and may be useful for treating cancer especially solid tumors driven by VEGFR2 and Ang2 including gastric hepatocellular carcinoma ovarian colorectal non small cell lun...
The present invention relates to novel 5 substituted nucleoside compounds pharmaceutical compositions comprising the compounds and methods of using the compounds to treat cancer more particularly for the treatment of cancer in particular glioblastomas melanoma sarcomas gastric cancer pancreatic cancer cholangiocarci...
The present invention relates to fusion proteins comprising an insulin receptor agonist fused to a human IgG Fc region through the use of a peptide linker and the use of such fusion proteins in the treatment of diabetes. The fusion protein of the present invention has an extended time action profile and is useful fo...
The present disclosure relates to antibodies that bind human T-cell immunoglobulin- and mucin-domain-containing protein-3 (Tim-3) and may be useful for treating solid and hematological tumors alone and in combination with chemotherapy and ionizing radiation.
The present invention provides N-[3-[2-Amino-5-(11-difluoroethyl) -44a57-tetrahydrofuro[34-d][13]oxazin-7a-yl]-4-fluoro-phenyl]-5- (trifluoromethyl)pyridine-2-carboxamide i.e. the compound of Formula I: [Formula should be inserted here] or a pharmaceutically acceptable salt thereof and in particular its (4aR5S7aS) i...
A medical delivery device for advancing a piston in a medicament container to expel a medicament. A support structure supports the container and a drive assembly that advances the piston. The drive assembly includes a drive ribbon that can be retracted and extended. The retracted ribbon defines a spiral and the exte...
The present invention relates to certain novel 23-dihydro-1H-indole compounds pharmaceutical compositions comprising the compounds and methods of using the compounds to treat cancer more particularly for the treatment of cancer selected from the group consisting of melanoma acute myeloid leukemia chronic lymphocytic...
Antibodies and methods of using these antibodies are provided which bind human and mouse receptor activator of nuclear factor kappa-B ligand, said antibodies are useful as agents for treating conditions associated with bone-related disorders or skeletal abnormalities caused by cancer.
The present invention relates to antibodies that bind human T-cell immunoglobulin- and mucin-domain-containing protein-3 (Tim-3), and may be useful for treating solid and hematological tumors in combination with anti-human PD-1 antibodies, chemotherapy, and ionizing radiation.
Antibodies which bind and neutralize human IL-33 and methods of using same are provided said antibodies are useful as agents for treating conditions associated with allergic disease including treating atopic dermatitis.
A compound, as defined herein, or pharmaceutical composition containing the compound, for use in treating IDH1 or IDH2 mutant cancer and having the structure: (I).
Antibodies to human N3pGlu Aß compositions comprising such N3pGlu Aß antibodies and methods of using such N3pGlu Aß antibodies for the treatment of a disease characterized by deposition of Aß including clinical or pre-clinical Alzheimers disease Downs syndrome and clinical or pre-clinical cerebral amyloid angiopathy...
Antibodies which bind BTLA and methods of using same are provided said antibodies are useful as agents for treating conditions associated with autoimmune disease including treating lupus.
The present disclosure relates to a dose detection system for use in combination with a medication delivery device. In one aspect, the system includes a module keyed to the device and including a sensor operable to detect the relative angular position of a sensed element attached to the medication delivery device. T...
Medication delivery devices are provided having a dose delivery sensing capability. A sensed element is attached to a dose setting member of the device. The sensed element includes surface features radially-spaced from one another. A rotational sensor is attached to an actuator of the device. The rotational sensor i...
Incretin analogs are provided that have activity at each of the GIP, GLP-1 and glucagon receptors. The incretin analogs have structural features resulting in balanced activity and extended duration of action at each of these receptors. Methods also are provided for treating diseases such as diabetes mellitus, dyslip...
ABSTRACT The present invention provides novel CDK7 inhibitors and pharmaceutical compositions thereof: (I), or a pharmaceutically acceptable salt thereof.
A medication delivery device including a drive mechanism, a retraction mechanism and a sensing system. A medication container is movable relative to the medication delivery device between storage and delivery positions. The drive mechanism drives a plunger in a translational movement to move the medication container...
A medication delivery device usable with a medication container wherein advancement of a piston within the container expels medication. The device includes a housing and a drive assembly. The drive assembly includes a drive ribbon having distal and proximal edge sections. The drive ribbon has a retracted configurati...
Antibodies to human pituitary adenylate cyclase-activating peptide, compositions comprising such antibodies, and methods of using such antibodies for the treatment of pain including headache and / or migraine.
The present invention relates to novel variants of human BMP7 protein. The invention embodies vectors and host cells for the propagation of nucleic acid sequences encoding said proteins and the production thereof. Also disclosed are methods for the treatment of cancer, cartilage damage and degeneration, pain associa...
The invention provides certain (phenyl)-(pyrazol)-3,4-dihydroisoquinolin-2(1H)- yl)ethan-1-one compounds of formula I as D1 positive allosteric modulators (PAMs), and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I, or a pharmaceutically acceptable salt th...
A gripping attachment (10) is disclosed which facilitates the handling of a medication bottle (12). The medication bottle includes a container (14) having a cylindrical wall (16) extending parallel to a longitudinal axis. The container is closed at one end by a base wall (18) and has an opposed open end. The contain...
Dose detection systems for medication delivery devices are described. One is a module for removable attachment to a dose button of a medication delivery device. A device with a dose detection system is also disclosed. The module includes a processor and a plurality of magnetic sensors, such as, for example, five or ...
A medication delivery device including a device body and a dose setting component coupled to the device body. Component is rotatable relative to the device body in relation to an amount of a set or delivered dose. An annular sensed element, such as a metal or magnetic ring, is positioned on a proximal surface of the...
Incretin analogs are provided that have activity at each of the GIP, GLP-1 and glucagon receptors. The incretin analogs have structural features resulting in balanced activity and extended duration of action at each of these receptors. Methods also are provided for treating diseases such as diabetes mellitus, dyslip...
The present invention relates to compounds having activity at both the human glucose-dependent insulinotropic polypeptide (GIF) and glucagon-like peptide-1 (GLP-1) receptors. The present invention also relates to compounds having an extended duration of action at each of these receptors. Furthermore, the present inv...
The present disclosure relates to a medication delivery system (10) including a medication administration device (12), a medication within the medication administration device (12), a container (14) defining a cavity (32) receiving the medication administration device (12), and a cap (16) attached to the container (...
Angiopoietin-like protein (ANGPTL)3/8 complexes and antibodies are disclosed, where the antibodes bind to and thereby neutralize ANGPTL3/8 complexes. Pharmaceutical compositions also are disclosed that include one or more anti-ANGPTL3/8 complex antibodies herein in a pharmaceutically acceptable carrier. Methods of m...
PYY analogs are disclosed that include modifications that increase half-life when compared to native, human PYY, as well as additional modifications that increase potency and selectivity to the NPY2 receptor. Pharmaceutical compositions also are disclosed that include one or more of the PYY analogs described herein ...
Angiopoietin-like protein (ANGPTL)3/8 complexes and antibodies are disclosed, where the antibodes bind to and thereby neutralize ANGPTL3/8 complexes. Pharmaceutical compositions also are disclosed that include one or more anti-ANGPTL3/8 complex antibodies herein in a pharmaceutically acceptable carrier. Methods of m...
The present invention provides compounds of the Formula (I), or a pharmaceutically acceptable salt thereof, where n and R1 are defined herein, methods of treating patients for liver disease, and processes for preparing the compounds.
The present invention relates to sodium-hydrogen exchanger 3 (NHE3) inhibitor compounds of the Formula: to pharmaceutical compositions comprising the compound and to the use of the compound for the treatment of certain diseases associated with elevated sodium and/or phosphate levels.
Small molecule potentiatiors to potassium channels (such as Kv7 potentiators - which are also called KCNQ potentiators), compositions including such compounds, and methods of using such compounds for the treatment of Amyotrophic Lateral Sclerosis and other neurological diseases caused by changes in motor neuron exci...
The invention provides certain difluorocyclohexyl-imidazopyridazinyl-imidazolidinone compounds of formula II as IL-17A inhibitors, pharmaceutical compositions thereof, and methods of using a compound of formula II to treat certain symptoms of psoriasis, rheumatoid arthritis or multiple sclerosis.
...
The present invention generally relates to the treatment of Crohns Disease with an anti-IL-23p19 antibody, particularly dosage regimens for the treatment of the disease.
The present invention relates to antibodies that are heterodimeric and bind human PD-L1 and human TIM-3, and may be useful for treating cancer alone and in combination with chemotherapy and other cancer therapeutics.
The present invention provides a novel compound of the formula: methods of making this compound, methods of using this compound for pretargeted imaging, and preparations of such formulations.
Mammalian cell lines with reduced expression and/or activity of lipases/esterases, and methods of producing the same are provided. Also provided are compositions comprising polysorbate and recombinant proteins produced in said mammalian cells which have improved polysorbate stability.
Incretin analogs are provided that have activity at each of the glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide- 1 (GLP-1) and glucagon (GCG) receptors. The incretin analogs have structural features resulting in balanced activity and extended duration of action at each of these receptors. M...
The present invention provides compounds of the formula: where R1, R2, R3, R4, R5, A, B, and Y are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and salts for treating patients for cancer.
The invention provides methods of using environmentally compatible detergents in the field of recombinant protein manufacturing for inactivating viruses in a product feedstream in the manufacturing process of proteins intended for administration to a patient, such as therapeutic or diagnostic proteins. The invention...
Medication delivery devices are provided having a housing comprising a reservoir sized sufficiently to hold medication, a dose button being rotatable relative to the housing to select a dose size of the medication for an injection, a printed circuit board, a switch mounted to the printed circuit board, and a control...
The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating metabolic conditions, such as type 2 diabetes mellitus, heart failure, diabetic kidney disease, and non-alcoholic steatohepatitis.
The present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type 2 diabetes mellitus.
Disclosed herein are compounds of Formula I: wherein R1 is CH3 or CH2CH3; and pharmaceutically acceptable salts thereof, which are useful for treating cancer.
In an embodiment, the present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type II diabetes mellitus.
The present invention relates to methods for treating, preventing or delaying disorders relating to cognition, such as cognitive decline, cognitive impairment or dementia. The present invention also relates to method for treating, preventing or delaying heart failure, such as heart failure with preserved ejection fr...
Provided herein are methods and uses of antibodies that bind all seven human ELR+ CXC chemokines with high affinity for preventing and/or treating respiratory diseases, e.g., acute respiratory distress syndrome (ARDS). The present invention also relates to doses and dosing regimens for the methods and uses of antibo...
The techniques described herein relate to computerized methods and apparatus of at least one of for determining whether a dose sensing module is attached to a medication delivery device, such as, for example, with dose detection sensors, for detecting a color of a portion of a medication delivery device to determine...
Relaxin (RLN) analogs are disclosed including modifications that increase half-life when compared to native, human RLN, that maintain selectivity to the RXFP1 receptor and that provide in vitro and in vivo stability for improved druggability properties and less immunogenicity. Pharmaceutical compositions also are di...
Intermediate compounds are disclosed for making incretin analogs, or pharmaceutically acceptable salts thereof. In addition, methods are disclosed for making incretin analogs by coupling from two to four of the intermediate compounds herein via hybrid liquid solid phase synthesis or native chemical ligation.
...
The present invention relates to compounds having activity at the human glucose- dependent insulinotropic polypeptide (GIP) receptor. The present invention also relates to compounds having an extended duration of action at the GIP receptor. Such compounds may be useful in the treatment of diabetes, including type 2 ...
The present invention relates to crystalline forms of 5-[5-[2-isopropylcyclopropyl] -6-methyl-pyridazin-3-yl]-1H-pyrimidine-2,4-dione, and pharmaceutical compositions comprising them, which inhibit the activity of CD73 and are useful for treating cancer.
The present disclosure relates to antibodies that bind human CD19 (anti-human CD19 antibodies or anti-human CD19 antibodies), compositions comprising such anti-human CD19 antibodies, and methods of using such anti-human CD19 antibodies.
The present invention relates to IL-34 antibodies, compositions comprising the same, and methods of using the antibodies and or compositions thereof for treating immune-mediated diseases such as neurodegenerative diseases, for example Alzheimer's Disease or a tauopathy disease.
Provided herein are RET kinase inhibitors according to the formula (I): pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods for their use in the treatment of diseases that can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders. A, R1, n, X1...
The presently described compounds relate to the treatment of Type I and /or Type II diabetes and/or hyperglycemia. More particularly, the described compounds relate to extended time action acylated insulin compounds that lower blood glucose, pharmaceutical compositions containing such compounds, therapeutic uses of ...
A compound of the formula (I), useful as modulators of metabotropic glutamate receptor in which R1 and R2 are as defined in the specification, non-toxic metabolically labile esterand amides or a pharmaceutical acceptable salt thereof and a process for preparing thesame. ...
This invention relates to a process for preparing a stable pharmaceutically elegantsolid oral formulation containing olanzapine as an active ingredient and having apolymer coating selected from the group consisting of hydroxypropyl methylcellulose, hydroxyethyl cellulose, methylhydroxyethyl...
Disclosed are glucagon-like peptide-1 (GLP-1) compoundswith modifications at one or more of the followingpositions: 7, 8, 12, 16, 18, 19, 20, 22, 25, 27, 30, 33,and 37. Methods of treating a subject in need of GLP-1receptor stimulation using these GLP-1 compounds are alsodisclos...
The present invention relates to a compound of a compound of Formula I. X and Y together represent -CH2-CH2, -CH2-O-, or -O-CH2-: represents a double bond;R4-R7 each independently represent hydrogen, hydroxyl, halo, (C1-C6)alkyl. or(C1-C)alkoxy; andR8 represents hy...
The invention provides specific GLP-1 analogs fused to specific IgG4-Fc derivatives. These fusion proteins have an increased half-life, decreased immunogenicity, and reduce effector activity. The fusion proteins are useful in treating diabetes, obesity, irritable bowel syndrome and other conditions that woul...
The invention provides active therapeutic peptides fused to specific IgG4-Fc derivatives.These fusion proteins have an increased half-life, reduced half antibody formation, andreduced effector activity, while not being immunogenic. The fusion proteins are useful intreating human diseases as...
The present invention provides a compound of the Formula (I) below: Wherein R is selected from the group consisting of H CH CN CHCN C(CH)CN and F; R is selected from the group consisting of H O(C Calkyl)R CHCN and CN; R is selected from the group consisting of H OCH CN C(CH)CN and CHCN; R is selected from the group ...
1234 The present invention provides a compound of the Formula I: wherein A is: and W Y X R R R and Rare as defined herein or a pharmaceutically acceptable salt thereof for use as an inhibitor of the EP4 receptor.
The present disclosure provides a water dispersible granule formulation comprising from about 5% to about 80% (w/w) of monensin; from about 1% to about 20% (w/w) of one or more surfactants; from about 1% to about 30% (w/w) of one or more binders; from about 1% to about 90% (w/w) of one or more fillers; and water up ...
The present invention provides a compound of Formula I: which is crystalline. The compound of Formula (I) is useful in the treatment of Akzheimer s disease (BACE imnhibitor).
Antibodies to human N3pGlu Aß compositions comprising such N3pGlu Aß antibodies and methods of using such N3pGlu Aß antibodies for the treatment of a disease characterized by deposition of Aß including clinical or pre-clinical Alzheimers disease Down"s syndrome and clinical or pre-clinical cerebral amyloid angiopath...
The present invention provides compounds of the formula below (I"): where R, and R1-R3 are as described herein, methods of treating patients for certain types of autoimmune diseases and cancer, and processes for preparing the compounds.
The presently described compounds relate to the treatment of diabetes and/or hyperglycemia. More particularly, the described compounds relate to acylated insulin compounds that lower blood glucose, pharmaceutical compositions containing such compounds, therapeutic uses of such compounds, and an intermediate compound...
The present invention provides compounds of the formula below pharmaceutically acceptable salts of the compounds methods of treating patients for liver disease and processes for preparing the compounds.
The present invention relates to solid oral fixed dose compositions of metformin, atorvastatin, and valsartan, or their pharmaceutically acceptable salts, processes for the preparation thereof, and the use of the composition to treat certain diseases.
The present invention relates to antibodies that are heterodimeric and bind human PD-L1 and human PD-1, and may be useful for treating cancer alone and in combination with chemotherapy and other cancer therapeutics.
The present invention relates to antibodies that bind to human CD137 and display agonist activity, and may be useful for treating solid and hematological tumors alone and in combination with chemotherapy and ionizing radiation.
The invention provides BTK Inhibitor compounds, pharmaceutically acceptable salts, pharmaceutical compositions thereof, and methods of using these compounds, salts, or compositions to treat autoimmune diseases such as Rheumatoid Arthritis.
The present invention relates to anti-human PD-1 agonist antibodies, and uses thereof for treating autoimmune disorders such as rheumatoid arthritis or for decreasing rejection of transplanted cells and/or tissues.
Compounds are provided herein that induce weight loss and that treat diabetes, dyslipidemia, NASH and/or obesity. Also provided are pharmaceutical compositions containing such compounds and therapeutic uses of such compounds and compositions, where such compounds act as GDF15 agonists with extended time of action an...
The present invention provides an improved method for preparing a powder formulation containing a peptide. The present invention further provides an improved method for preparing a powder formulation containing glucagon or a glucagon analog, wherein said powder formulation is suitable for nasal administration.
...
The present invention relates to anti-human CD200R agonist antibodies, and uses thereof for treating diseases such as atopic dermatitis, chronic spontaneous urticaria, allergy, asthma, scleroderma, IBD, SLE, MS, RA, GvHD, or psoriasis.
The present invention relates to chronic nightly use of lasmiditan for the prevention of migraine, particularly therapy resistant migraine which is defined herein as migraine refractory to two or more prior monotherapy and/or dual therapy treatment or prevention regimens.
Medication delivery devices are provided having a dose delivery sensing capability. A dose button includes a support and a cover that at least partially encloses an electronics assembly including a sensor for detecting rotation of a component during dose delivery to determine a dosage of delivered medication. The el...
The present invention provides novel intermediates and processes useful in the manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.
The present invention relates to polypeptide molecules that bind to human TIGIT, and to polypeptide molecules that bind to human PD-1 and human TIGIT, and are useful for treating solid tumors, alone and in combination with chemotherapy and/or ionizing radiation.
The present invention relates to dosing regimens for antibodies that bind human T-cell immunoglobulin- and mucin-domain-containing protein-3 (TIM-3), and may be useful for treating tumors in combination with anti-human PD-L1 antibodies, anti-human PD-1 antibodies, chemotherapy, and ionizing radiation as well as the ...
The present invention provides compounds and methods targeting human tau, particularly human tau phosphorylated at threonine (217) and isoforms of tau expressed only in the CNS, including therapeutic antibodies, pharmaceutical compositions and diagnostic applications useful in the field of neurodegenerative diseases...
The embodiments of present invention provide processes and an intermediate for the large-scale preparation of 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and formulations and product forms made by these processes. The embodiments of the present invention further provide fo...
CDK7 inhibitors according to the formula (I): wherein X is -CH(OH)CH3, -CHFCH3, -CF2CH3, or -CF3; Y is -CH=CH2 or C2H=C2H2; and Z is CH(CH3)2 or C2H(CH3)(CH22H), pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods for their use are provided.
The present disclosure relates to IL-34 antibodies, compositions comprising the same, and methods of using the antibodies and or compositions thereof for treating immune-mediated diseases such as neurodegenerative diseases, for example Alzheimer's Disease or a tauopathy disease.
The present disclosure relates to antibodies that specifically bind soluble and membrane forms of human TNFa, compositions comprising such TNFa antibodies, and methods of using such TNFa antibodies and compositions.
ABSTRACT
“MEDICAL DELIVERY DEVICE WITH AXIALLY EXPANDABLE DRIVE MEMBER”
A medical delivery device (20, 20B, 20C) for advancing a piston (26) in a medicament container (22) to expel a medicament. A support structure (30, 30B) supports the container (24) and a drive assembly (32, 32B) that advances the piston (26). ...
The present disclosure relates to antibodies that specifically bind human IL-4Ra, compositions comprising such IL-4Ra antibodies, and methods of using such IL-4Ra antibodies.
A therapeutic agent delivery device includes a disposable portion and a reusable portion that detachably carries the disposable portion. The reusable portion includes a drive mechanism having a guide, a rotary actuator, and a follower drivably coupled to the rotary actuator and movably coupled to the guide. The rota...
The present invention relates to specific salts of (1S,5R)-(1a,5a,6a)-N-[1,1-dimethyl-2-[(3-methyl-2-pyridyl)oxy]ethyl]-3-azabicyclo[3.1.0]hexane-6-carboxamide, to pharmaceutical compositions comprising said salts, to methods of using said salts to treat physiological disorders, and to intermediates useful in the sy...
The present disclosure comprises hydrophilic linker compounds of Formula 1: and describes methods for their use in liquid phase synthesis. In Formula 1, "m" is 0 to 20, "n" is 1 to 50, and "Z" is a linker compound as described herein.
ABSTRACT
The presently described compounds relate to the treatment of diabetes and/or hyperglycemia. More particularly, the described compounds relate to acylated insulin compounds that lower blood glucose, pharmaceutical compositions containing such compounds, therapeutic uses of such compounds, and an inter...
ABSTRACT
The presently described compounds relate to the treatment of diabetes and/or 5 hyperglycemia. More particularly, the described compounds relate to acylated insulin compounds that lower blood glucose, pharmaceutical compositions containing such compounds, therapeutic uses of such compounds, and an interme...
The present invention relates to certain substituted AHR agonist compounds, to pharmaceutical compositions comprising the compounds and to methods of using the compounds to treat immune-mediated diseases.
The present invention relates to certain substituted AHR agonist compounds, to pharmaceutical compositions comprising the compounds and to methods of using the compounds to treat immune-mediated diseases.
The present invention relates to compounds having activity at both the human glucose-dependent insuli notropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. The present invention also relates to compounds having an extended duration of action at each of these receptors. Furthermore, the present in...
The present invention relates to methods for treating, preventing or delaying disorders relating to cognition, such as cognitive decline, cognitive impairment or dementia in a patient. Specifically, the method comprising administering dulaglutide in a therapeutically effective amount to the patient once weekly. Furt...
Dose detection systems for medication delivery devices are described. One is a module for
removable attachment to a dose button of a medication delivery device. A device with a dose
detection system is also disclosed. The module includes a processor and a plurality of magnetic
sensors, such as, for example, five ...
The present invention provides a compound of Formula (I) wherein R is (II), (III), (IV) or a pharmaceutically acceptable salt thereof, useful for treating psoriasis, systemic lupus erythematosus, or type 1 diabetes.
ABSTRACT
“PROCESSES AND INTERMEDIATE FOR THE LARGE-SCALE PREPARATION OF
2,4,6-TRIFLUORON-[6-(1-METHYL-PIPERIDINE-4-CARBONYL)-PYRIDIN-2-YL]-
BENZAMIDE HEMISUCCINATE, AND PREPARATION OF 2,4,6-TRIFLUORO-N-[6-
(1-METHYL-PIPERIDINE-4-CARBONYL)-PYRIDIN-2-YL]-BENZAMIDE ACETATE”
The embodiments of present invention pro...
The present invention provides a compound of Formula (I): wherein R1 is hydrogen or methyl; and R2 is: or a pharmaceutically acceptable salt thereof, useful for treating pain, including chronic pain, chronic lower back pain, diabetic peripheral neuropathic pain, and osteoarthritis pain.
In an embodiment, the present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type II diabetes mellitus.
Stable pharmaceutical formulations for therapeutic dual GLP-1 receptor/glucagon receptor agonists and methods of using such stable pharmaceutical formulations.
A Solid Phase Peptide Synthesis (SPPS) device and method of using the same for manufacturing peptides is taught herein. The system comprises at least two reactors, each reactor including a quantity of SPPS resin. The reactors are positioned in series. A de-protecting agent is added to the first reactor and then tran...
The present disclosure relates to compounds that bind to human GITR, pharmaceutical compositions comprising such compounds, and methods of using such compounds.
A method and device for building an oligonucleotide on a solid phase resin within a filter reactor, wherein the method and device as used as a solid phase synthesis system. As part of the solid phase synthesis process, a protecting group will be removed from the 5'position of an oligonucleotide that is attached to t...
Described herein are variant adeno-associated virus (AAV) capsid polypeptides and gene therapeutics thereof for use in the treatment or prevention of hearing loss.
Disclosed herein are compounds of formula I: or a pharmaceutically acceptable salt thereof, where the variables are as defined herein. These compounds are useful in treating RET associated cancers. Formulations containing the compounds of formula I and methods of making the compounds of formula I are also disclosed....
The invention is directed to treatment or prevention of a disease characterized by deposition of Aß in the brain using anti-N3pGlu Aß antibodies. The diseases that can be treated or prevented include, e.g., Alzheimer's disease, Down's syndrome, and cerebral amyloid angiopathy. The invention, in some aspects, is rela...
The disclosure relates generally to biology and medicine, and more particularly it relates to compounds acting as half-life (t½)-extending moieties for use with therapeutics, especially for improving t½ of biological-based therapeutics (i.e., biotherapeutics or biologics). The disclosure further relates to fusions a...
A composition is provided that includes an incretin analog having activity at each the glucose-dependent insulinotropic polypeptide (GIP), glucagon-like peptide-1 (GLP-1) and glucagon (GCG) receptors (i.e., tri-receptor agonist) and one or more additional agents such as a tonicity agent and a preservative. Methods a...
The present invention provides novel compounds: (I), and (II) methods of making such compounds, methods of using such compounds for pretargeted imaging, and preparations of formulations for such use.
The present invention relates to methods of treating and dosing regimens using Mevidalen, also described as 2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(3- hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanone, and/or pharmaceutical compositions thereof, for treatment of hallucinations a...
The present invention relates to methods of treating and dosing regimens using Mevidalen, also described as 2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(3- hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanone, and/or pharmaceutical compositions thereof, for slowing Parkinson's disease p...
The present disclosure relates to the field of medicine. More particularly, the disclosure is in the field of treatment of diabetes, obesity and/or chronic weight management, dyslipidemia and/or NASH. The disclosure relates to compounds that agonize the amylin receptor and can lower food intake, body weight, glucose...
The present invention provides a compound of Formula I: wherein R is H or R1 is H, halogen, C1-C3 alkyl, C3-C6 cycloalkyl, C1-C3 alkoxy, C2-C3 alkenyl, OCF3, R2 is H, halogen, C1-C3 alkyl, C1-C3 alkoxy, or C2-C4 alkenyl; R3 is NH2, or CH2NH2; and X is O, OCH2, OCH2CH2, OCH(CH3), CH2O, SCH2, CH2S, CH2, NHCH2, CH2NH, ...
A needle assembly configured to be part of a drug delivery device comprises a plurality of extendable and retractable needles. The needles are fluidly coupled by a flexible connector, which is configured to maintain fluid connection between the needles throughout their movement. When the needles are extended, a firs...
Novel selective estrogen receptor degraders (SERDs) according to the formula: and pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof, wherein R is selected from or.
The present invention provides compounds of the formula:, for use in the treatment of systemic sclerosis, fibrosis (e.g. pulmonary fibrosis), achondroplasia, thanatophoric dysplasia (e.g. type I), severe achondroplasia with developmental delay and acanthosis nigricans (SADDAN), muenke syndrome or cancer.
...
The present invention provides a compound of Formula I: wherein R is hydrogen, -P(=O)(OH)2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoimmune and inflammatory diseases, such as atopic dermatitis, rheumatoid ...
The present invention provides a compound of Formula I: (I) wherein R1 is H, halogen, C1-C3 alkyl, or C1-C3 alkoxy; R2 is H or halogen; and X is O, OCH2, or CH2, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is useful for treating autoim...
The present disclosure relates to methods for reducing host cell protein content in antibody preparation recombinantly produced in a host cell in the manufacturing process of antibodies intended for administration to a patient. The disclosed methods may be performed in order to prepare therapeutic antibody preparati...
The present disclosure relates to methods for reducing host cell protein content in a protein preparation recombinantly produced in a host cell in the manufacturing process of proteins intended for administration to a patient.
The present invention relates to novel compounds comprising novel delivery moieties for delivery of oligonucleotides, which are useful in the treatment of disease, suitably diseases of the liver.
The present disclosure provides a novel palatable pharmaceutical composition in the form of taste-masked 2,4,6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl]benzamide hemisuccinate, and orally disintegrating tablets comprising the same. The taste-masked orally disintegrating tablets of this invention will...
ABSTRACT
The present invention relates to solid oral fixed dose compositions of metformin, atorvastatin, and valsartan, or their pharmaceutically acceptable salts, processes for the preparation thereof, and the use of the composition to treat certain diseases.
The present disclosure related to the field of medicine. More particularly, the disclosure is in the field of treatment of diabetes, obesity, and/or dyslipidemia. The disclosure relates to compounds that agonize both the calcitonin and amylin receptors and can lower food intake, body weight, glucose and/or triglycer...
The present invention provides compounds and methods targeting insulin-like peptide-5 (INSL5), including antibodies, cells and vectors comprising DNA encoding the same, and methods for producing the antibodies. In addition, the present invention provides for use of INSL5 antibodies in diagnostic assays.
...
ABSTRACT The present invention provides a compound of Formula I:, or a pharmaceutically acceptable salt thereof, wherein the compound of Formula I, or pharmaceutically acceptable salt thereof is administered orally with a total dose of the compound of 0.1 mg/day to 5 mg/day, useful for treating a neurodegenerative d...
The present invention provides compounds and methods targeting human interleukin-19, including therapeutic antibodies, pharmaceutical compositions and methods of use thereof, useful in the field of immune-mediated diseases including psoriasis, atopic dermatitis, asthma, psoriatic arthritis, rheumatoid arthritis, axi...
Disclosed herein is a tablet composition comprising 3-[(1S,2S)-1-[5-[(4S)-2,2-dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one, or a ...
Tangential flow filtration systems and, more specifically, continuous tangential flow filtration ("cTFF") systems comprised of single-pass modules are disclosed herein. Each single-pass module is configured to transition from a first process configuration to a second process configuration and/or operate under both t...
The present invention relates to an oral capsule composition comprising 3-[(1S,2S)-1-[5-[(4S)-2,2-dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-ox...
The present invention provides compounds of the formula (I):, or a pharmaceutically acceptable salt thereof, wherein A, X1, X2, X3, Y, Z, Z1, Z2, R2 and R6 are as defined herein, for use in the treatment of cancer and a method of treating cancer.
The present invention provides novel intermediates and processes useful in the
manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.
The present invention provides novel intermediates and processes useful in the manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.
ABSTRACT
PROCESS FOR PREPARING A GIP/GLP1 DUAL AGONIST
The present invention provides novel intermediates and processes useful in the
manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.
Disclosed herein are intermediate preparations for the manufacture of glucagon and GLP-1 dual agonist compounds or pharmaceutically acceptable salts thereof. Also disclosed herein are processes for the manufacture of glucagon and GLP-1 dual agonist compounds by coupling two to four intermediate preparations via hybr...
A method is disclosed for washing an amino acid that has been added to a solid phase resin during solid phase peptide synthesis (SPPS), comprising: adding a first quantity of wash solvent, wherein once the wash with the first quantity of wash solvent is complete, sending the first quantity of wash solvent to waste; ...
Disclosed are methods of making selective estrogen receptor degraders (SERDs) of Formula (A), as well as intermediates thereof, salts thereof including a pharmaceutically acceptable salt, and pharmaceutical compositions thereof: wherein either R1 or R2 is independently Cl, F, -CF3, or -CH3, and the other is H; and R...
A composition and methods of dosing such tirzepatide composition, comprising a tirzepatide, or a salt thereof at a concentration selected from the group consisting of 2.5 mg/mL, 40 mg/mL, and 50 mg/mL; NaCl; and dibasic sodium phosphate is provided.
The techniques described herein relate to computerized methods and apparatus of at
least one of for detecting a color of a portion of a medication delivery device to
determine a medication contained in the medication delivery device, such as, for
example, with a set of LEDs and light sensor for different temperat...
The present disclosure provides human tumor necrosis factor alpha antibody glucocorticoid receptor agonist conjugates and methods of using the conjugates for the treatment of autoimmune and inflammatory diseases.
A fluid delivery cassette includes a cartridge assembly and a needle assembly. The cartridge assembly includes a cartridge configured to contain a fluid, a septum positioned at a distal opening of the cartridge, a piston sealing a proximal opening of the cartridge and movable in an axial direction, and a drive assem...
Provided herein are SARM1 RNAi agents and compositions comprising a SARM1 RNAi agent. Also provided herein are methods of using the SARM1 RNAi agents or compositions comprising a SARM1 RNAi agent for reducing SARM1 expression, reducing axon degeneration, and/or treating SARM1-mediated neurological disease in a subje...
The present invention provides compounds of the formula: wherein A, B, D1, X, Y, Z, G, R1, R2, and R3a are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and pharmaceutically acceptable salts thereof for treating patients for cancer.
The present disclosure relates to pharmaceutical solutions of certain anti-N3pGlu Aß antibodies. Uses of such pharmaceutical solutions, including use in the treatment of Alzheimer's disease, are also disclosed.
The present disclosure provides human CD33 antibodies and antibody glucocorticoid receptor agonist conjugates and methods of using the conjugates for the treatment of myeloid cell associated diseases.
The present disclosure provides human interleukin 4 receptor alpha antibody glucocorticoid receptor agonist conjugates and methods of using the conjugates for the treatment of inflammatory diseases, such as type 2 inflammatory diseases.
The present invention provides processes and compounds for the preparation of glucagon and GLP-1 co-agonist compounds that are useful in the treatment of type 2 diabetes, obesity, nonalcoholic fatty liver disease (NAFLD) and/or nonalcoholic steatohepatitis (NASH).
Provided herein are polymorphs of (2E)-3-fluoro-2-({[2-( 4-methoxypiperidin- 1 - yl)pyrimidin-5-yl]oxy}methyl)prop-2-en-1-aminium 4-methylbenzenesulfonate, compositions thereof, methods of preparation thereof, and methods of use thereof.
The present invention relates to an erodible tablet comprising a therapeutic peptide which is suitable for oral administration and, in addition, to a non-granulation process for making the erodible tablet.
The present invention relates to epiregulin antibodies, compositions comprising the same, and methods of making and/or using the antibodies and/or compositions thereof for chronic pain disorders such as chronic osteoarthritis pain, or chronic diabetic peripheral neuropathy pain, or chronic low back pain.
...
The present invention relates to methods for treating, preventing or delaying disorders relating to obstructive sleep apnea. The present invention relates to methods for treating, preventing or delaying obstructive sleep apnea. Provides a method of treatment for obstructive sleep apnea.
Described herein are preserved formulations of insulin-Fc fusions. The formulations include insulin-Fc fusions having prolonged pharmacokinetic and pharmacodynamic profiles sufficient for once weekly administration in the treatment of diabetes and are sufficiently stable to allow for storage and use without unaccept...
Dose detection systems for medication delivery devices are described. One is a module for
removable attachment to a dose button of a medication delivery device. A device with a dose
detection system is also disclosed. The module includes a processor and a plurality of magnetic
sensors, such as, for example, fiv...
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof, useful for treating pain, including chronic pain, chronic lower back pain, diabetic peripheral neuropathic pain, and osteoarthritis pain.
The present disclosure relates to IL-34 antibodies, compositions comprising the same, and methods of using the antibodies and or compositions thereof for treating immune-mediated diseases such as neurodegenerative diseases, for example Alzheimer's Disease or a tauopathy disease.
The present disclosure relates to IL-34 antibodies, compositions comprising the same, and methods of using the antibodies and or compositions thereof for treating immune-mediated diseases such as neurodegenerative diseases, for example Alzheimer's Disease or a tauopathy disease.
Provided herein are MAPT RNAi agents and compositions comprising a MAPT RNAi agent. Also provided herein are methods of using the MAPT RNAi agents or compositions comprising a MAPT RNAi agent for reducing MAPT expression and/or treating tauopathy in a subject.
The present disclosure provides compounds of the formula (III) and their pharmaceutically acceptable salts, and compounds of the formula (IV) and their pharmaceutically acceptable salts, and pharmaceutical compositions comprising these compounds, as well as intermediates for preparing the compounds.
...
The present invention relates to a dosage form suitable for oral administration comprising a therapeutic peptide or protein in a sealed capsule having a co-polymer coating.
The present invention relates to cocrystalline forms of 4-[4-[3- chloro-4-[l-(5-fluoro-2-pyridyl)-2-hydroxy-ethoxy]pyrazolo[l,5- a]pyridin-6-yl]-5-methyl-triazol-l-yl]piperidine-l-carbonitrile, R- enantiomer ("Isomer 2"), with gallic acid (I), and to cocrystalline forms of 4-[4-[3-chloro-4-[l-(2-pyridyl)-2- hydroxy-...
This invention provides certain piperidine compounds as AT2R antagonists, e.g., compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and X are as defined herein, pharmaceutical compositions thereof, and methods of using the same to treat pain associated with AT2R activity.
...
The present invention relates to compounds having activity at both the human glucosedependent
insulinotropic polypeptide (GIF) and glucagon-like peptide-1 (GLP-1)
receptors. The present invention also relates to compounds having an extended duration
of action at each of these receptors. Furthermore, the present...
Provided herein are ATXN2 RNAi agents and compositions comprising an ATXN2 RNAi agent. Also provided herein are methods of using the ATXN2 RNAi agents or compositions comprising an ATXN2 RNAi agent for reducing ATXN2 expression, and/or treating ATXN2-associated neurological disease in a subject.
...
The present invention provides compounds of the formula as fibroblast growth factor receptor 3 (FGFR3) inhibitors for the treatment of e.g. cancer systemic sclerosis fibrosis pulmonary fibrosis achondroplasia thanatophoric dysplasia severe achondroplasia with developmental delay and acanthosis nigricans (SADDA...
The present disclosure relates to novel PD 1 agonist antibodies and methods and uses of anti human PD 1 agonist antibodies for the treatment of autoinflammatory and/or autoimmune diseases. Also provided are doses and dosing regimens for the methods and uses of anti human PD 1 agonist antibodies for the treatment of...
The present invention relates to the synthesis of 3-[(1S,2S)-1-[5-[(4S)-2,2-dimethyloxan-4-yl]-2-[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methylindazol-5-yl)-2-oxoimidazol-1-yl]-4-methyl-6,7-dihydro-4H-pyrazolo[4,3-c]pyridine-5-carbonyl]indol-1-yl]-2-methylcyclopropyl]-4H-1,2,4-oxadiazol-5-one, or a sa...
Provided herein are novel compounds and RNAi agents comprising modified nucleotides, compositions comprising such compounds or RNAi agents, and methods of using such compounds or RNAi agents.
The present invention provides novel intermediates and processes useful in the manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.
Synthetic nucleic acids are described that can be used for astrocyte-directed expression of heterologous nucleotide sequences. Also described are methods of using the same for astrocyte-directed expression of such nucleotide sequences for the treatment of neurodegenerative diseases.
Methods are disclosed for making a targeting ligand-conjugated nucleotide phosphoramidite known as adem-A-GalNAc phosphoramidite, which can be used in the synthesis of oligonucleotides such as therapeutic oligonucleotides.
Methods are disclosed for making a 4'-phosphate analog phosphoramidite known as MeMOP, which can be used in the synthesis of oligonucleotides such as therapeutic oligonucleotides.
In an embodiment, the present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type II diabetes mellitus.
In an embodiment, the present invention provides a compound of the formula: or a pharmaceutically acceptable salt thereof, and methods of using this compound for treating type II diabetes mellitus.
The present disclosure relates to certain AHR agonist compounds their method of making and to pharmaceutical compositions comprising the compounds and to methods of using the compounds to treat immune mediated diseases such as psoriasis and atopic dermatitis.
Provided are crystalline forms of peptide fragments, method of preparation thereof, and use thereof for preparing peptides. The present crystalline compounds may be employed as intermediates with improved purity and physical properties for peptide syntheses.
An apparatus is described for concentrating biomolecules in solution such as oligonucleotide containing solutions via tangential flow filtration (TFF) where the apparatus can concentrate the oligonucleotides to a concentration > 100 mg/mL. Also described are methods of concentrating a biomolecule containing solut...
The present disclosure relates to certain AHR agonist compounds, for example, having a general formula (I) to pharmaceutical compositions comprising the compounds, and to methods of using the compounds to treat immune-mediated diseases, such as psoriasis and atopic dermatitis.
The present disclosure relates to antibodies that bind human LAIR1 ("anti human LAIR1 antibodies" or "anti human LAIR1 antibodies") compositions comprising such anti human LAIR1 antibodies and methods of using such anti human LAIR1 antibodies.
Provided herein are improved methods of cleaning a protein A chromatography matrix that has previously been used to purify an Fc-containing protein. The methods generally involve washing the protein A chromatography matrix with a series of three solutions, the first containing an acid, the second containing Tris, an...
The present disclosure relates to novel therapeutic compounds, known as RNAi agents, that decrease expression of the HMGCR receptor (expressed by the HMGCR gene), thereby decreasing expression of mRNA and protein expression. Such RNAi agents are useful in the treatment of diseases and disorders involving the regulat...
Pharmaceutical compositions are disclosed that include a double-stranded RNAi agent that modulates LPA expression or its pharmaceutically acceptable salt thereof in water. Doses and dosing regimens for such RNAi agents also are disclosed that include administering doses from about 4 mg to about 608 mg at a frequency...
Intermediate compounds (i.e., oligonucleotide fragments) are disclosed for making RNAi agents, or pharmaceutically acceptable salts thereof. In addition, methods are disclosed for making single-stranded oligonucleotides by ligating two or more of the intermediate compounds herein via a hybrid chemical-enzymatic rout...
The present invention relates to novel therapeutic compounds, known as RNAi agents, that decrease expression of the FAS receptor (expressed by the FAS gene), thereby decreasing expression of FAS mRNA and protein expression. Such RNAi agents are useful in the treatment of diseases involving the regulation of FAS expr...
Provided herein are improved methods of purifying an Fc-containing protein from a mixture comprising the Fc-containing protein and one or more host cell protein (HCP). The methods generally involve applying the mixture to a chromatography column comprising a protein A chromatography matrix, and washing the chromatog...
The treatment or prevention of a disease characterized by deposition of amyloid beta (A??) plaques in the brain of a human subject in particular intravenous and subcutaneous doses and dosing regimens of anti N3pG antibodies.
The present invention relates to novel therapeutic compounds, known as RNAi agents, that decrease expression of the ANGPTL8 receptor (expressed by the ANGPTL8 gene), thereby decreasing expression of mRNA and protein expression. Such RNAi agents are useful in the treatment of diseases involving the regulation of ANGP...
Linkers for the connection of a therapeutic to another moiety, such as an Fc region of an antibody. Linkers with two or more maleimide functional groups which can undergo nucleophilic conjugate addition reactions. Methods of increasing the duration of action of a therapeutic by attaching to a novel linker and an Fc ...
The present invention provides new intermediates and processes useful in the manufacture of tirzepatide, or a pharmaceutically acceptable salt thereof.
The disclosure provides methods for measuring polysorbate levels in a sample. The method comprises applying an aliquot of the sample onto a high-performance liquid chromatography system with a mixed-mode column, eluting the sample with a gradient from a first mobile phase to a second mobile phase, and applying evapo...
The present invention relates to novel cGAS inhibitor compounds, having a formula of (IIa) to pharmaceutical compositions comprising the compounds, and to methods of using the compounds and compositions to treat certain pathological conditions such as immune-mediated diseases.
Provided herein are improved methods for purifying an Fc-containing protein from a mixture comprising the Fc-containing protein and a contaminant (e.g., an undesired host cell protein). The methods generally comprise heating the mixture to produce a heat-treated mixture, and applying the heat-treated mixture to a de...
Antibodies that bind UNC5C and fragments thereof are described. Compositions comprising these antibodies, as well as methods, including therapeutic methods and therapeutic uses of the antibodies are also described.
The present disclosure provides novel compounds of the formula: (I) wherein R1, R2, R3, R4, and R5 are as described herein, methods of preparing the same, pharmaceutical compositions the same, tau imaging formuations, and methods of using the compounds for tau imaging.
Polypeptides are provided that have activity at each of the GIP, GLP-1 and glucagon receptors. The polypeptides have structural features resulting in activity and extended duration of action at each of these receptors. Methods also are provided for treating diseases and/or conditions such as obesity, chronic weight ...
The present disclosure is directed to methods of purifying a dulaglutide composition. For example, the methods comprise loading the dulaglutide composition in-line with a buffer B solution onto a hydrophobic interaction chromatography (HIC) column in a downflow direction, washing the HIC column with a buffer mixture...
Method for preparing SSTR4 agonist compounds. Method for preparing SSTR4 agonist compounds through a diasteromerically selective cyclization reaction without the need for a separate epimerization step. Novel intermediates for preparing SSTR4 agonist compounds. Novel salts of certain SSTR4 agonists, such as (1R,5S,6r...
The present invention provides compounds of the formula I wherein A, Z, G, R1, R2, and R4 are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and pharmaceutically acceptable salts thereof for treating patients for cancer.
The present disclosure generally relates to methods, and diagnostic applications, for the treatment of ulcerative colitis. More particularly the methods and diagnostic applications of the present invention relate to expression profiles of certain gene transcripts in ulcerative colitis patients and the usefulness of ...
Provided herein are improved methods for producing an Fc-containing protein. The methods generally involve culturing mammalian cells that produce the Fc-containing protein at a first pH setpoint for a first period of time followed by culturing the cell at a second pH setpoint that is higher than the first pH set poi...
The present invention provides compounds of the formula (I) wherein A, Z, G, R1, R2, and R4 are as described herein, pharmaceutically acceptable salts thereof, and methods of using these compounds and pharmaceutically acceptable salts thereof for treating patients for cancer.
Methods are described for concentrating a biomolecule-containing solution, such as an oligonucleotide-containing solution, to a concentration = about 200 mg/mL from an initial concentration of about = 20 mg/mL, via thin film evaporation (TFE), for high dose/low volume applications. Apparatuses also are described for...
One or more needle assemblies for a fluid delivery device includes a needle support that includes a connector coupler having various manufacturing methods to form a leak-tight seal around the needle. A flexible connector has a connector bore forming a fluid path in fluid communication with a bore of the needle. A dr...
The present invention relates to therapeutic compounds, novel RNA interference (RNAi) agents, that decrease expression of the Voltage-Gated Sodium Channel Alpha Subunit 10 (SCN10A) gene, which encodes a subunit of the Nav 1.8 or Nav 1.8 sodium channel. Such RNAi agents decrease levels of intact Nav 1.8 sodium channe...
The present disclosure provides nectin-4 antibody drug conjugates and pharmaceutical compositions thereof, and methods of using for the treatment of cancer.