Amorphous losartan potassium and a process for preparing amorphous losartan potassium comprising the steps of : dissolving losartan potassium in an aqueous solvent or C1-C6 alcohol to form a solution, and removing the solvent from the solution by lyophilization or by distillation at a pressure of 300 mm Hg or l...

The present invention provides processes for removing organic solvent from crystals of atorvastatin hemi-calcium containing organic solvent. In one process, the organic solvent is displaced by vapor diffusion of water in a vessel maintained at elevated humidity. In a second process, the organic solvent is removed by...

The present invention provides a novel compound of formula I:which can be used as an intermediate for preparing Valsartan. Preferably, R is an optionally substituted C1 to C7 straight, or branched alkyl group, or an optionally substituted C6 to C7 aromatic group (such as a phenyl).

Provided are candesartan cilexetil forms and methods of their preparation. Also provided are pharmaceutical com­positions prepared by combining at least one pharmaceutically-acceptable excipient with at least one candesartan cilexetil form of the invention.

disclosed is crystalline ladostigil tartrate of a specified density, impositions, including pharmaceutical compositions comprising such idostigil tartrate, and a process for the manufacture thereof.

A stable pharmaceutical formulation comprising an effective amount of high purity torsemide modification II and a pharmaceutically acceptable carrier, wherein the effective amount is an amount of torsemide modification II that would yield a dosage of about 2 to about 200 mg torsemide per day, wherein the formulation...

The present invention relates to amorphous and polymorphic forms of montelukast free acid.

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A pharmaceutical composition comprising a first therapeutic agent and a second therapeutic agent is described. A plurality of particles comprising (i) an interior comprising the second therapeutic agent and (ii) an exterior comprising a material for controlling the release of the second therapeutic agent may be disp...

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A process for making torsernide Dupont Form 2 as herein described comprising the steps of: (a) suspending torsernide in water; (b) basifying the torsernide suspension of step (a) with base to dissolve the torsernide, wherein the base is a substance that can increase the pH to greater than 7; (c) adding an or...

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A process for the preparation of alendronic acid, which comprises the steps of: a) reacting an imidobutanoyl compound of the formula I with phosphorous acid (H3PO3) at a temperature of between 25°C and 18O°C with the optional inclusion of PC13, PCl5, POCI3:(Formula Removed) wherein R is an imido g...

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A novel process for preparing a compound of formula (I) wherein R¹ denotes substituted or unsubsituted alkyl, alkoxy, aryl, aryloxy or arylalkoxy; R² denotes substituted or unsubstituted alkyl, alkoxy, aryl, aryloxy, arylalkoxy, tosyl, formyl, acetyl or amine; and R³ denotes substituted or unsubstituted alkyl, alkox...

This invention provides an isolated compound having the structure: The invention also provides for a process for preparing 4-(3- (methylsulfonyl)phenyl)- 1-propylpiperidin-4-ol, l-(3,3-bis(3-(methylsulfonyl)phenyl)propyl)-4-(3- (methylsulfonyl) phenyl)piperidone, l,4-bis((3-(l -propylpiperidin-4-yl)phenyl)sulf...

This invention provides a method of treating a patient afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the patient laquinimod as an add on therapy to or in combination with glatiramer acetate. This invention also provides a package and a pharmaceutical compo...

This invention provides a method of treating a patient afflicted with multiple sclerosis or presenting a clinically isolated syndrome comprising administering to the patient laquinimod as an add on therapy to or in combination with interferon ß. This invention also provides a package and a pharmaceutical composition...

The present invention relates to oral dosage forms comprising Memantine or a pharmaceutically acceptable salt thereof pharmaceutical formulations comprising the oral dosage forms and methods for treating mild moderate or severe Alzheimer s dementia or neuropathic pain comprising the oral dosage forms and formulation...

A method for modifying Parkinson""s disease by periodically administering a pharmaceutical composition comprising a therapeutically effective amount of rasagiline or a pharmaceutically acceptable salt of rasagiline to the patient, thereby modifying the disease. The method includes reducing the rate of progression; d...

The present invention relates to new 2-oxo-l,2-dihydro-quinoline modulators of immune function, pharmaceutical compositions thereof, and methods of use thereof.

This invention provides methods for inhibiting or reducing thalamic damage in a subject comprising administering to the subject an amount of laquinimod, wherein the subject is a human patient afflicted with a form of multiple sclerosis or presenting a clinically isolated syndrome who has been determined to have thal...

The present invention provides a method for treating a human subject afflicted with multiple sclerosis or a single clinical attack consistent with multiple sclerosis with a pharmaceutical composition comprising glatiramer acetate and a pharmaceutically acceptable carrier comprising the steps of: (i) determining a g...

The patent provides a process of preparing a pharmaceutical preparation of glatiramer acetate and mannitol in a suitable container comprising the steps of: (i) obtaining an aqueous pharmaceutical solution of glatiramer acetate and mannitol; (ii) filtering the aqueous pharmaceutical solution at a temperature of from ...

The subject invention provides a Laquinimod amine salt which is laquinimod meglumine laquinimod choline hydroxide laquinimod L lysine or laquinimod monoethanolamine.

An inhaler (10) for inhalation into the airway of a user the inhaler (10) having a housing (12) at least partially defining a flow passageway (36) extending through the inhaler (10) from an air inlet to an outlet the inhaler (10) comprising a valve (56) for selectively restricting the flow passageway. ...

This invention provides a method for treating a human subject afflicted with a progressive form of multiple sclerosis comprising periodically administering to the human subject an amount of laquinimod effective to treat the human subject. This invention also provides laquinimod for use in treating a human subject af...

A method of attenuating a biological effect of cocaine exposure in a primate. Such method includes administering to the primate an amount of a BChE-albumin fusion protein comprising the amino acid substitutions A227S  S315G  A356W  and Y360G  wherein the amount of the fusion protein is effective to cause attenuation...

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The present application provides subject-matter related to a mixture of crystalline laquinimod sodium particles, wherein (i) > 90% of the total amount by volume of the laquinimod sodium particles have a size of < 40 μιη or (ii) > 50% of the total amount by volume of the laquinimod sodium particles have a size of < 1...

Described herein are compositions and methods for treating, preventing and ameliorating diseases and conditions characterized by a lower than normal white blood cell count, such as leukopenia and neutropenia. The compositions and methods include recombinant human albumin-human granulocyte colony stimulating factor...

Disclosed are compositions and methods for treating, preventing and ameliorating conditions and diseases characterized by a lowered white blood cell count. The methods and compositions described herein include a fusion polypeptide formed from human serum albumin protein ("HSA") and human granulocyte- colony st...

Processes for coating a carrier with microparticles of a drug are described. For example, a coated canier can be ob¬tained in a one-stage process that entails evaporating a solvent from microdroplets of a solution containing an API to obtain dry microparticles, which are then coated on the carrier. ...

The present invention provides methods for treating a human patient afflicted with unresectable advanced or metastatic non small cell lung cancer comprising periodically administering to the human patient chemotherapy comprising an amount of docetaxel; and 640mg of an anti clusterin oligonucleotide having the sequen...

The subject invention provides pharmaceutical compositions Containing laquinimod or a pharmaceutically acceptable salt thereof an isolated compound of N ethyl 4 hydroxyl 1 methyl 5 (methyl (2 3 4 5 6 pentahydroxyhexyl) amino) 2 oxo N phenyl 1 2 dihydroquinoline 3 carboxamide or a salt thereof compositions containing...

A platform accessible by a user from a web browser/HMO s electronic medical record (EMR) for providing the user with information regarding a patient s drag regimen as well as generating alerts concerning potential adverse effects to a patient from taking a cluster including a plurality of pharmaceutical preparations...

This invention provides a method of treating a subject afflicted with active lupus nephritis comprising periodically administering to the subject an amount of laqumimod or pharmaceutically acceptable salt thereof effective to treat the subject This invention also provides laquinimod or pharmaceutically acceptable sa...

This invention provides a method of treating a subject afflicted with rheumatoid arthritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof and an amount of methotrexate  wherein the amounts when taken together are effective to treat the subject...

This invention provides a method of treating a subject afflicted with active lupus arthritis comprising periodically administering to the subject an amount of laqumimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laqumimod or pharmaceutically acceptable sa...

This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof, novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions cont...

Provided are novel crystal forms of atorvastatin hemi-calcium referred to herein as Form XVIII and Form XIX and processes for their preparation and use. Also provided are atorvastatin hemi-calcium acetone solvates.

The. present invention relates to a method of making it besartan including the step of reacting 2-butyI-l,3-diazaspiro[4.4]non-l-ene-4-one and 5-(4"-bromomethylbiphenyl-2-yl)-l-trityl-l#-tetrazole in the presence of a phase transfer a reaction system having first and second phases,The first phase includes a first s...

The present invention relates to solid amorphous and crystalline forms of ibandronate sodium.

The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-l-(4-fluorophenyl)-3- (3-(4-fluorophenyl)-3-oxo-propyI)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompa...

Disclosed is crystalline R( + ) -N-propargyl-1-aminoindan containing water at an amount of less than 0.5% by weight and a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is a process for the preparation of solid rasagiline base. ...

Provided are processes for the synthesis of 5 -phenyl- 1-trityl-lH-tetrazole, an intermediate useful in the synthesis of irbesartan. The tritylation of 5-phenyl-lH-tetrazole is carried out using phase transfer catalysis in a biphasic solvent system.

Provided are pharmaceutical compositions comprising at least one vitamin D-containing compound, at least one corticosteroid compound, and at least one solvent component selected from the group consisting of triglycerides, sorbitan, sorbitan fatty esters, cetearyl glucoside, PEG-n sorbitan stearate, acrylamide/sodium...

Provided are crystalline forms of clopidogrel hydrobromide and processes for their preparation.

Provided is a crystalline losuvastatin intermediate and processes for preparation thereof.

A stable composition of a 2-aza-bicyclo[3.3.0)-octane-3-carboxylic acid derivative and a method for its preparation are described. The stable composition includes an intimate admixture of the derivative and a stabilizing effective amount of a lubricant. The stable composition further includes an external excipient....

The present invention relates to the various polymorphic forms of ziprasidone HCI and processes for their preparation.

Crystalline ziprasidone HCl, characterized by data selected from the group consisting of a powder XRD pattern with peaks at 10.9, 17.4 and 19.1 ±0.2 degrees 2 tlieta and an FTIR spectrum with peaks at about 3400, 3344, 3172, 2949, 970, 940, 872 and 843 cm'1.

A method of making a bisphosphonic acid comprising: a) combining a carboxylic acid, phosphorous acid, and a halophosphorous compound selected from PC13, PC15, POC13, PBr3, POBr3, and PBr5 in the presence of a diluent, to obtain a reaction mixture of a bisphosphonic acid; wherein the diluent includes: (i) an aromatic...

The invention encompasses the synthesis of (S)-(+)-3-(aminomethyl)-5- methylhexanoic acid, (S)-Pregabalin, via the intermediate, (3R)-5-methyl-3-(2-oxo-2{|(]R)- l-phenylethyl]amino) ethyl)hexamic acid.

A process for preparing trans-4-isopropylcyclohexane acid chloride comprising the step of combining trans-4-isopropylcyclohexane carboxylic acid with thionyl chloride in the presence of a C1 to a C6 organic amide, optionally in the presence of a solvent of the kind such as herein described, with about 1 to about 5 a...

A method of making 2-butyl-3-[2"-(triphenylmethyl tetrazol-5-yl)- biphenyl-4-ylmethyl]-l,3-diazaspiro[4.4]non-l-ene-4-one comprising: a) combining 2-butyl-l ,3-diaza-spiro[4.4]non-l-ene-4-one and 5-(4"-bromomethylbiphenyl-2-yl)-l-trityl-lH-tetrazole in the presence of a phase transfer catalyst in a reaction syste...

The invention encompasses processes for the synthesis of (S)-(+)-3- (aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Provided are novel crystalline forms of gatifloxacin, denominated forms L, M, P, Q, S, and Tl, and methods for making them. Also provided are methods of transforming the novel crystalline forms of gatifloxacin of the present invention to other crystalline forms of gatifloxacin.

A process for making (3-sulfonamide-4-chloro) pyridine, (3-sulfonamide-4-fluoro) pyridine or (3-sulfonamide-4-bromo) pyridine represented by the formula

The present invention relates to new methods for the synthesis of torsemide and the torsemide synthetic intermediate, (3-sulfonylchloride-4-chloro)pyridine.

The present invention relates to a process for preparing nateglinide Form U comprising the steps of: (a) preparing a solution of nateglinide in a solvent selected from the group consisting of an ester, ketone, alcohol and mixtures thereof, at a temperature from about -15°C to about 50°C; (b) crystallizing hateglin...

"9. *', ? o The subject invention provides an improved process for obtaining a mixture of polypeptides having nonuniform amino acid sequences, where each polypeptide consists essentially of alanine, glutamic acid, tyrosine and lysine where the resulting mixture of polypeptides comprises less than 0.3% bromin...

The present invention relates to the synthesis and purification of (±)-l-Cyclopropyl-6-fluoro-l,4-dihydro-8-methoxy-7-(3-methyl-l-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin.

Provided are processes for preparing telmisartan alkyl ester and teimisartan using environmentally friendly organic solvents that are easily removed from the reaction mixture, wherein a telmisartan alkyl ester is isolated and hydrolyzed to form telmisartan or the telmisartan is prepared using a synthesis in a single...

The present invention provides novel crystalline solid anhydrous forms of famciclovir, denominated form 1, II. and III, as well as their preparations thereof.

The present invention provides tadalafil crystal forms II, III, IV, VI, VII, and VIII, and processes for preparing these forms. The present invention also provides processes for preparing tadalafil forms I and V.

Provided is a method of preparing aripiprazole anhydrous Form II from aripiprazole.

The present invention provides processes for preparing rosuvastatin calcium salt substantially free of impurities on an industrial scale (I).

This invention relates to novel amorphous losartan potassium, novel losartan potassium in a crystalline form that is a hydrate, novel crystalline losartan potassium Form IV and solvates thereof; novel crystalline losartan potassium Form V and solvates thereof, to processes for their preparation, to compositions cont...

The present invention relates to protected valacyclovir, N-tert- butoxycarbonyl-L-valine 2 [(-amino-1,6-dihydro-6-oxo-9H-purin- 9yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine sel...

The present invention relates to a process for preparing levofloxacin hemihydrate having a purity of about 99% or greater, comprising: dissolving levofloxacin in a polar solvent at an elevated temperature; and crystallizing the levofloxacin hemihydrate, wherein the polar solvent is selected from the group consisti...

The invention encompasses solid composites of the calcium receptor-active compounds, processes for preparing the solid composites, immediate and controlled-release pharmaceutical formulations comprising the solid composites, and methods of treatment therewith.

The present invention relates to a process for preparing amorphous atorvastatin comprising: a) adding atorvastatin to acetone to form a mixture; b) including the mixture for a time sufficient to convert the atorvastatin to amorphous atorvastatin; and c) recovering the amorphous atorvastatin. ...

The present invention relates to novel essentially pure venlafaxine and the process of preparation thereof. The present invention also relates to novel solvate forms of venlafaxine hydrochloride and the process of preparation thereof. Furthermore, the present invention provides a novel process for preparing venlafax...

Novel methods for the preparation of sertraline hydrochloride Forms II, III, V, VI, VII, VIII, IX and X. Novel Form II is also disclosed. According to the present invention, sertraline hydrochloride Form II may be produced directly form sertraline base or sertraline mandelate. It may also be produced from sertraline...

A method for reducing excess residual process alcohol in valacyclovir hydrochloride having excess residual process alcohol comprising the step of contacting valacyclovir hydrochloride having excess residual process alcohol with a humid gas at ambient pressure.

The invention relates to diastereomerically pure rosuvastatin and processes for preparing diastereomerically pure rosuvastatin and its intermediates. Formula (I).

This invention relates to a novel crystalline solid of carvedilol or a solvate thereof, to processes for its preparation, to compositions containing it and to its use in medicine. This invention further relates to a novel process for preparing a crystalline solid of carvedilol Form II.

Provided are processes for preparing a polymorphic form of fluvastatin sodium with PXRD peaks at 3.8, 11.1, 12.9, 8 and 21.7 {0.2 degrees two-theta..

The present invention relates to a stable compacted, compressed or hard tableted injectable composition, including a vaccine composition comprising at least one freeze dried antigenic component and a dissolution aid. A package containing the above injectable composition and method to facilitate immunizing a subject ...

The present invention relates to a process for preparing amorphous atorvastatin hemi-calcium salt comprising: a) suspending crystalline atorvastatin Form V in a mixture of 30% 1-butanol and 70% water at a temperature of about 91°C. b) cooling the suspension of step a) to room temperature and...

The present invention relates to a process of preparing benzisoxazole methane sulfonic acid-chloride (BOS-Cl) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also disloses a process of preparing zonisamide via amidation of BOS-CI. More particularly, the presen...

A zero-order release pharmaceutical dosage form for oral administration to a patient comprising a core tablet sheathed in an annular body of compressed powder or granular material is provided. A preferred embodiment of the zero-order release pharmaceutical dosage form is a solid pharmaceutical dosage form which redu...

Provided is a crystallisation method for reducing the level of impurities in ualcipotrieue in which a solution of a starling calcipotriene in a first process solvent, for example Till", is combined with second process solvent, for example methyl formate, and, after cooling, calcipotricnc is isolated. The method can ...

The present invention provides for novel polymorphs of zolpidem hemitartrate and the preparation of the polymorphs.

The compound 4-amino-l-hydroxybutylidene-l,l-bisphosphonic acid monosodium salt having water content of 1.3 % to 11.7% .

Provided are crystalline forms of cinacalcet HCI

The invention encompasses processes for the preparation of highly pure venlafaxine hydrochloride, l-[2-dimethy-lamino-(4-methoxyphenyl)ethyl]cyclohexanol hydrochloride as well as intermediates thereof.

The present invention is directed to the novel polymorphic Form F of Atorvastatin calcium, processes for the preparation thereof and pharmaceutical compositions comprising this crystalline form.

A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about (25) weight percent. A manufacturing method may include blending the ac...

The present invention relates to novel crystalline forms of the linezolid intermediate S-N-(4-morpholinyl-3-fluo-rophenyl)-2-oxo-5-oxazolidinyl-methyl amine referred to herein as Form A, Form B, and Form C.

The present invention provides an iso-lated linezolid impurity, desfluoro linezolid, the prepa-ration thereof and its use as a reference standard.

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Improved processes for preparing substituted 2-(2-pyridylmethyl) sulfinyl-1H-benzimidazoles are disclosed.

Provided is a crystalline form of nateglinide, labeled Forms and , processes tor its preparation. Also provided are its pharmaceutical formulations and methods of administration.

Provided are atorvastatin compositions which reduce the effect of food on the bioavailability of atorvastatin and methods for making such compositions. Also provided are methods of reducing low density lipoprotein by administering the compositions of the invention.

Disclosed is a process for the preparation of laquinimod sodium which removes the impurities after the salt formation step, thus resulting in crystals of higher purity as well as crystals having improved crystalline characteristics.

A process for making sertraline hydrochloride Form II comprising the steps of: (a) suspending a water or solvent adduct of sertraline hydrochloride in n- butanol, acetone, t-butyl-methyl, ether, cyclohexane, and ethyl acetate such that a slurry is formed, for a time sufficient to effect transformation to sertral...

A process for making sertraline hydrochloride Form II comprising the steps of: (a) granulating sertraline hydrochloride Form V in methanol; and (b) Stirring the mixture of sertraline hydrochloride Form V and ethanol or methanol to induce transformation to sertraline hydrochloride Form II.

A process for making sertraline hydrochloride Form VI comprising the steps of (a) dissolving sertraline base in a mixture of methanol or ethanol and water; (b) adding hydrogen chloride to the solvent; and (c) isolating sertraline hydrochloride Form VI without further drying.

A process for making sertraline hydrochloride Form V comprising the steps of: (a) dissolving or suspending sertraline base in ether (b) adding hydrogen chloride to the solvent to reduce the pH of the solution or suspension; and (c) isolating sertraline hydrochloride Form V from the solution or suspension. ...

The present invention provides substantially pure Tolterodine.

A process for making sertraline hydrochloride Form II comprising the steps of: (a) dissolving sertraline hydrochloride in acetone to obtain a solution; (b) heating  the  solution  to  effect  transformation  to  sertraline hydrochloride Form II; and (c) isolating sertraline hydrochloride Form II. ...

Provided are rosuvastatin degradation products and their use as a reference standard (including reference marker) for analysis of rosuvastatin.

The invention encompasses dry compression pharmaceutical compositions of aripiprazole, methods of making tablets from the compositions, and tablets of the dry compression pharmaceutical composition.

Provided is a process for reduction of statin ketocslers and purification of diol esters of the statins through selective crystallization.

The invention relates to a method of making optically and chemically pure levctiracelam and to the levetiracetam produced by suchlprocess.

Disclosed is a process for isolating from a reaction mixture a salt of a mono-propargylated aminoindan having the structure (I) wherein R1 is H, hydroxyl, alkoxy or (II) wherein Y is 0 or S; R2 and R3 is each independently, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl, each optionally halo substituted, or hydrogen ; where ...

Provided is a novel method of making 2-buty]-3-[[2'(l-trityl-lH-ietrazol-5-yl)biphen-4-yl]methyl]l,3-diaza-spiro[4,4]non-l-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.

Provided are amorphous and purely amorphous tegaserod maleate and processes for the preparation thereof. Also provided are pharmaceutical compositions comprising amorphous or purely amorphous tegaserod maleate and methods for the treatment of irritable bowel syndrome using the same. (I)

A process for preparing candesartan cilexetil comprising heating a solution of trityl candesartan cilexetil in a water immiscible solvent in the presence of at least one C1-C4 alcohol and a first portion of water; combining the solution with a second portion of water to obtain a two-phase system; and recovering cand...

The present invention provides a pharmaceutical composition of telmisartan comprising a) a telmisartan compound, b) a surfactant, c) a basic agent, and d) at least one diluent wherein the composition comprises less than 25% of water soluble diluents. The telmisartan compound is preferably present from about 12.5% to...

The present invention provides a pharmaceutical composition comprising oxcarbazepine and at least one pharma¬ceutical excipient, wherein the oxcarbazepine in the composition has abroad particle size distribution and an enhanced oxcarbazepine dissolutio rate. The broad particle size distribution of oxcarbazepine in t...

The invention provides orally disintegrating tablets that readily disintegrates in the mouth, releasing enteric coated drug sub-tablets.

A method of separating mixed C-24 epimers of a vitamin D analog having a hydroxyl group in the 24 position, wherein C-24 is the epimeric center, comprising the steps of: esterifying the C-24 hydroxyl group of both epimers, selectively enzyrnatically solvolyzing the C-24 ester so formed of one of the epimers, and chr...

A method of selectively enzymatically solvolyzing the esterified C-24 hydroxyl group of one epimer in a mixture of esterified C-24 epimers of a vitamin D analog having an esterified hydroxyl group at the stereogenic C-24 position thereof comprising the steps of: providing a solution of the mixed esterified C-24 epim...

In one embodiment, the present invention provides a process of preparing amorphou ziprasidone mesylate comprising the step of spray-drying a solution of ziprasidone mesylat in a solvent selected from a group consisting of: C1-C5 alcohols, C2-C8 ethers, glacial acetic acid and mixtures thereof with water, using an ou...

Alendronic acid prepared by the process which comprises the steps of: a) reacting an irnidobutanoyl compound of the formula. I with phosphorous add (H3PO3) at a temperature of between 25°C and 180°C with the optional inclusion of PCI3, PCIs, H3PO4 or POCL3: I wherein R is an imido group; and R1 is selected from ...

The subject invention provides rasagiline tannate, compositions and a process for manufacture thereof.

The present invention provides rosuvastatin and intermediates thereof having a low level of alkylether impurity and processes for the preparation thereof.

The present invention provides a process for the preparation of amorphous valsartan.

The subject invention provides crystalline R(+) -N-propargyl- 1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.

Provided is a crystal form of atorvastatin hemi-calcium and processes for its preparation.

A process for preparing irbesartan comprising the steps of: a) providing a solution of 2-butyl-3-[2'-(l-trityl-lH-tetrazol-5-yl)biphenyl-4-yl methyl]-l,3-diazaspiro[4.4]non-l-ene-4-one in a water miscible solvent; b) acidifying the solution; c) neutralizing the solution, thereby precipitating trityl alcohol; d) rem...

Micronized aripiprazole Form II having a particle shape and wherein 90% or more of the particles have a particle size of about 30 µm and the micronized aripiprazole Form II does not have more than 10% by weight of aripiprazole Type C as determined by X-ray diffraction and processes for making thereof. ...

The invention encompasses processes for preparing intermediates, such as R-modafinic acid or (R)-C1-2 alkyl ester, of modafinic acid, and the conversion of the intermediates to armodafinil.

The present invention relates to an improved process for making a mixture of acetate salts of polypeptides, each of which consisting of glutamic acid, alanine, tyrosine and lysine, for use in the treatment of multiple sclerosis.

Provided are processes for preparing intermediates of rosuvastatin and their use in preparation of rosuvastatin and rosuvastatin salts thereof.

Provided are HPLC methods for analyzing BOC-L-alanine in BOC-L-valine and alanine analogues in valacyclovir hydrochloride and a use and method of selecting valacyclovir compositions.

Provided is amorphous form of ziprasidone mesylate and process for its preparation. Also provided is a process for preparing ziprasidone mesylate dihydrate needle crystals.

Provided are polymorphic forms of Icgaserod base and maleate, and processes for their preparation.

The invention provides orally disintegrating tablets that readily disintegrates in the mouth, releasing enteric coated drug sub-tablets.

The present invention relates to a process for preparing nateglinide Form U comprising the steps of: (a) preparing a solution of nateglinide in a solvent selected from the group consisting of an ester, ketone, alcohol and mixtures thereof, at a temperature from about -15°C to about 50°C; (b) crystallizing nat...

Provided are processes for the preparation of sildenafil base and the citrate salt sildenafil. Also provided are silde-nafil citrate water adduct and a method of preparing pharmaceutical compositions comprising combining the sildenafil citrate and/or sildenafil citrate water adduct with at least one pharmaceutical...

A process for preparing nateglinide comprising the steps of: (a) combining trans-4-isopropylcyclohexane carboxylic acid with thionyl chloride in the presence of a C1 to a C6organic amide, with about 1 to about 5 acid equivalents of thionyl chloride, from about 0.05% to about 10% weight of the amide to the...

The invention provides processes for making famciclovir with low levels of undesirable by-products. The present invention discloses a process comprises reacting a compound of formula I (acetic acid 2-acetbxymethyl-4-(5-amino-7-chloro-imidazo |4,5-b]pyridin-3-yl)-butyl ester) in the presence of a palladium on charcoa...

A process for preparing nateglinide comprising the step of: a) acylating a salt of D-phenylalanine with trans-4- isopropylcyclohexane acid chloride to form nateglinide; and b) recovering the nateglinide.

A process for preparing nateglinide Form Z comprising the step of: a) preparing an aqueous solution of an alkali metal or an alkaline earth metal salt of nateglinide; b) acidifying the solution to precipitate nateglinide; and c) recovering the netaglinide as Form Z.

A crystalline form of nateglinide (Form B) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 20; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 29; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2θ; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data Selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 20; and a DSC thermogram with endotherms at about 66 and 130°C.

The present invention relates to a process for preparing nateglinide Form U comprising the steps of: (a) preparing a solution of nateglinide in a solvent selected from the group consisting of an ester, ketone, alcohol and mixtures thereof, at a temperature from about -15°C to about 50°C; (b) crystallizing nategl...

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2 θ ; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5,5 13, 1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermo gram with endotherms at" about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2θ; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 20; and a DSC thermograrn with endotherms at about 66 and 130°C.

A crystalline form of\ nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

The present invention provides a controlled release dosage formulation comprising a) about 40% to about 80% of a valproic acid compound such as Divalproex Sodium and b) at least two, preferably hydrophilic, polymers each in an amount of less than about 20% of the dosage weight.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 29; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2θ ; and a DSC thermogram with endotherms at about 66 and 130°C.

Provided are novel polymorphs and pseudopolymorphs of valacyclovir hydrochloride and phamaceutical compositions containing these. Also provided are methods for making the novel polymorphs and pseudopolymorphs, which include valacyclovir hydrochloride monohydrate and valacyclovir hydrochloride dihydrate. ...

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 29; and a DSC thermogram with endotherms at about 66 and 130°C.

A process for preparing nateglinide comprising the steps of: a) combining trans-4-isopropylcyclohexane carboxylic acid with .thionyl chloride in the presence of a C1 to a C6 organic amide to obtain trans- 4-isopropylcyclohexane acid chloride substantially free of its corresponding cis isomer; and ...

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 20; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 28; and a DSC thermogram with endotherms at about 66 and 130°C.

Provided are methods of treating bone disease including, but not limited to, osteoporosis, metastatic bone disease, or Paget's disease, by administering a combination of raloxifene and alendronate in a manner that mitigates the formation of ulcerative adverse events.

(S)-N,N-Dimethyl-3-(l-naphthalenyloxy)-3-(2-thienyl)propanamine benzenesulfonate (DNT-benzenesulfonate) and polymorphs of DNT-benzenesulfonate, compositions of DNT-benzenesulfonate and its polymorphs, processes for the preparation of DNT-benzenesulfonate and its polymorphs, and processes for the preparation of dulo...

(S)-N,N-Dimethy]-3-(]-naphtha]eny]oxy)-3-(2-thienyl)propanamine succinate (DNT-succinate) and polymorphs of DNT-succinate, compositions of DNT-succinate and its polymorphs, processes for the preparation of DNT-succinate and its polymorphs, and processes for the preparation of duloxetine hydrochloride from DNT-succin...

Disclosed are pharmaceutical preparations of R (+) -N-propargyl-1-aminoindan salts having enhanced content uniformity, processes for preparation of the compositions, and their uses.

Provided is anhydrous ziprasidone mesylate polymorph and processes for its preparation

The present invention provides tadalafil of high purity and processes of making such tadalafil by cyclization of TDC1 in a solution.

The invention encompasses sable candesartan cilexetil of fine particle size, wherein desethyl-candesartan (desethyl-CNS) within the stable candesartan cilexetil does not increase to more than about 0. l% w/w by HPLC relative to the initial amount of candesartan cilexetil, when the stable candesartan cilexetil is mai...

Provided are novel crystalline forms of valacyclovir hydrochloride denominated forms VIII, IX, X, XI, and XII and methods of making them. Also provided is a novel method for making valacyclovir hydrochloride in crystalline form V.

The present invention provides particulate tadalafil having a particle size of about 200 to about 600 microns and a process for controlling the particle size of tadalafil.

The present invention provides high crystallinity montelukast sodium, crystalline forms of montelukast sodium, and processes of preparing the same.

A crystalline Conn of duloxetine hydrochloride, pharmaceutical compositions of the crystalline form of duloxetine tiydrochloride, and methods of preparing the crystalline form uf duloxetine hydrochloride are provided.

Duloxetine intermediates of formulae (I) and (II), processes for their preparation, and their conversion to pharma-ceutically acceptable salts of duloxetine are described.

Methods for preparing substantially pure O-desmethylvenlafaxine are described.

Provided are syntheses of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)- Pregabalin via a chiral intermediate of the following formula (4) wherein Ar is a C6-10 aromatic group, R is a straight or branched C1-4 alkyl, ester, or carboxylic acid, and R1 is a straight or branched C1-5 alkyl, aralkyl, or substituted...

Crystalline form of Pregabalin characterized by X-ray powder diffraction peaks at about 5.8, 18.4, 19.2, 20.7, and 23.7° 2θ ± 0.2° 2θ, methods for its preparation, its pharmaceutical compositions thereof, and methods for the preparation of crystalline form of Pregabalin characterized by X-ray powder diffraction peak...

The present invention provides crystalline Eszopiclone malate form II, crystalline Eszopiclone form V, processes from preparing the crystalline Eszopiclone malate form II or V, pharmaceutical compositions comprising the crystalline Eszopiclone malate form II or V and methods of treating insomnia comprising administe...

The invention encompasses processes for the synthesis of (S)-Pregabalin, (S)-(+)-3-(aminomethl)-5-methlhexanoic acid.

Provided are processes for preparation of tegaserod and the maleate salt thereof.

A process for the preparation of Pregabalin comprising: a) combining an alkali hydroxide and water, b) adding CMH at a temperature of about O° C to about 40° C; c) adding bromine, in a drop-wise manner, at a temperature of about O° C to about 40° C; d) heating; e) reacting with a strong mineral acid; f) extracting w...

The present invention encompasses Pregabalin substantially free of Lactam and a process for obtaining Pregabalin substantially free of Lactam comprising extracting an acidic mixture containing a complex of Pregabalin with a strong mineral acid, with a C3-8 alcohol; and combining the organic phase with an organic ba...

Provided is a method of general applicability of epimerizing a vitamin-D analog having an asymmetric allylic carbon atom at the C-24 position, which comprises the steps of: a) esterifying the hydroxyl group on the asymmetric allylic carbon atom at the 24 position with an esterifying agent, b) contacting a solution o...

The present invention is directed to the preparation of substantially pure candesartan cilexetil by the deprotection of trityl candesartan cilexetil and crystallization and/or recrystallization of candesartan cilexetil.

A method for preparing quetiapine, 11 -[4-[2-(2-hydroxyethoxy)ethyl]-l-piperazinyl]dibenzo[6,/][l,4]thiazepine comprising the steps of: combining ll-chlorodibenzo[b,f][l,4]thiazepine (I), about 1 to about 1.5 molar equivalents with respect to (I) l-(2-hydroxyethoxy)ethyl piperazine (II), a base, and...

(R)-CMH containing less than about 0.2% area by HPLC of (S)-CMH.

The present invention provides processes for preparing montelukast.

The present invention provides an improved process for preparing modafinil, whereby it may be isolated in high purity by a single crystallization. The process produces modafinil free of sulphone products of over-oxidation and other byproducts. The invention further provides new crystalline Forms II-VI of modafinil a...

Provided are processes for the synthesis of 3-isobutylglutaric acid, an intermediate in the synthesis of (S)-Pregabalin.

Provided are stable pharmaceutical compositions comprising from about 2.5% to about 20% of a 2-aza-bj-cycIo[3.3.0]-octane-3-carboxylic acid derivative by weight of the composition and at least one pharmaceutically acceptable excipient, wherein the composition preferably has a total weight of less than 100 mg. Also p...

Isolated cinacalcet carbamate, processes for the preparation thereof, and processes for the use of cinacalcet carba-late as a reference marker and standard are provided. Also provided are cinacalcet salts substantially free of cinacalcet carbamate, and processes for the preparation thereof.

The invention encompasses stable multiparticulate pharmaceutical compositions of tolterodine having at least one pharmaceutically acceptable excipient and at least two populations of multiparticulates each population having tolterodine or a salt thereof and the ratio of the populations is from 90:10 to 10:90 by weig...

Disclosed is an isolated compound of the formula (I) along with methods of detecting it and of minimizing it in improved pharmaceutical compositions of rosiglitazone maleate.

The present invention provides methods for preparing eszopiclone Form A, substantially chemically pure eszopiclone, or eszopiclone with low level(s) of residual solvent(s). The present invention also provides eszopiclone with low level(s) of residual solvent(s). The present invention also provides a process for opti...

Processes for preparing ezetimibe-related compounds with a ketoreductase and for purifying ezetimibe are disclosed.

Provided are processes for the purification of a pure rosuvas-tatin intermediate by thin film evaporation and chemical method, and conver sion of the intermediate to rosuvastatin or salts thereof.

The present invention provides novel crystalline solid anhydrous forms of famciclovir, denominated form I, II, and III, as well as their preparations thereof.

Provided are ezetimibe compositions with improved lolubility and increased bioavailability, methods of their prepa-sation, and method of treatment using the same. An ezetimibe composition may be prepared, for example, by co-milling ezetimibe with at least one hydrophilic excipient.

Provided are processes for the synthesis of R-(+)-3-(carbamoylmethyl)-5-methylhexanoic acid and salts thereof, intermediates in the synthesis of S-pregabalin.

The invention relates to solid crystalline forms of ibandronic acid, pharmaceutical formulations thereof, and methods of treatment therewith (Formula I).

Provided is the use of enzymatic resolution for the preparation of intermediates of pregabalin, including (3S)-cyano-5-methylhexanoic acid and salts thereof and R-(-)-3-(carbamoylmethyl)-5-methylhexanoic acid and salts thereof.

A process for isolating nitrated tetracycline derivatives from a reaction mixture by precipitation using C3- C8 alcohols comprising: a. providing a reaction mixture resulting from the nitration of a tetracycline derivative; b. combining said reaction mixture with a solvent consisting of a C3-C8 alcohol to obtain a p...

The present invention relates to solid crystalline Tigecycline, and crystalline forms thereof.

This invention provides fusion proteins comprising consecutive amino acids which beginning at the amino terminus of the protein correspond to consecutive amino acids present in (i) a cytomegalovirus human MHC-restricted peptide, (ii) a first peptide linker, (iii) a human β-2 microglobulin, (iv) a second peptide link...

The invention relates to a method of making optically and chemically pure levetiracetam and to the levetiracetam produced by such process.

Provided are processes and intermediates for the synthesis of O- desmethyivenlafaxine.

Provided is a novel method of making 2-butyl-3-[[2"(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]1,3-diazaspiro[4,4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.

The present invention describes processes for the preparation of O-desmethylvenlafaxine and the intermediates cyclohexylbenzylcyanide and tridesmethylvenlafaxine, which may be used as intermediates in preparing O- desmethylvenlafaxine.

The invention encompasses novel amorphous and crystalline fonns of carvedilol phosphate, carvedilol hydrogen phosphate, and carredilot dihydrogen en phosphate as well as methods of making the novel amorphous and crystalline forms. Also disclosed are pharmaceutical compositions comprising the novel amorphous and crys...

The present invention describes processes for the preparation of O-desmethylvenlafaxine and tridesmethylvenlafaxine, which may be used as an intermediate in preparing O-desmethylvenlafaxine.

Provides are intermediates and processes for preparation of o- desmethylvenlafaxine.

The present invention provides stable pharmaceutical compositions comprising a combination of active phanna-;eutical ingredients. The pharmaceutical composition of the present invention comprises a moisture sensitive drug, in particular in angiotensin converting enzyme (ACE) inhibitor such as Cilazapril, as an acti...

The present invention provides pure paliperidone as well as purification processes to obtain thereof.

A process for preparing atorvastatin hemi-calcium comprising: a)    providing an atorvastatin ester derivative of formula: wherein R1 is a C1-C4 alkyl group, and b)    converting the  atorvastatin  ester  derivative  to  atorvastatin hemi-calcium with calcium hydroxide.

The present invention provides a process for purifying olmesartan medoxomil.

This application is a continuation-in-part and claims priority of U.S. Serial No. 09/642,913, filed August 21, 2000, which claims the benefit of U.S. Provisional Application No. 60/150,514, filed August 24, 1999. The contents of the above-identified U.S. provisional application are hereby incorporated by reference i...

The present invention is directed to (+)-cis-sertraline hydrochloride and methods of preparation. The present invention also includes processes for making sertraline having a cis/trans ratio greater than 3:1, greater than or equal to 8:1, or between about 8:1 and about 12:1, from the Schiff base of sertralone, sertr...

The present invention provides a novel crystalline form of linezolid referred to herein as Form IV as well as methods for the preparation and use of Form TV. The present invention provides pharmaceutical compositions that comprise therapeutically effective amounts of Form TV that can be used to treat patients suffer...

This invention relates to pharmaceutical compositions containing irbesartan, providing oral formulations with a high relative amount or concentration of irbesartan. In one embodiment, the present invention provides an oral formulation of irbesartan containing greater than 70% w/w irbesartan. In another embodiment, t...

A solid dosage form for oral administration to a patient comprising a core tablet sheathed in an annular body of compressed powder or granular material is provided. A preferred embodiment of the solid dosage form reduces contact of the active ingrredient in solid form with the mucosa lining the gastrointestinal trac...

A method of formulating a pharmaceutical composition comprising Form IV sustancially free of linezolid Form II and methods of treating a condition responsive to linezolid in a patient comprising administering to the patient a solid pharmaceutical composition comprising linezolid form IV sustantially free of linezoli...

One of the objects of the invention relates to a pharmaceutical composition in the form of a granulate, wherein the granulates comprises an active pharmaceutical ingredient (API) having a poor water solubility intimately associated with at least one pharmaceutically acceptable sugar, and optionally or preferably at ...

The invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable salt of N-ethyl-N- phenyl -1,2, -dihydro- 4 -hydroxy- 5 - chloro- 1 -methyl -2 - oxoquinoline-3-carboxamide, N-methylglucamine, and a pharmaceutically acceptable carrier.

Provided are compositions of imatinib, methods for their preparation, and methods for treatment using the same.

Provided is rosuvastatin calcium with a low salt by product content and processes for preparing such rosuvastatin calcium.

NThe present invention relates to a process for preparing amorphous atorvastatin comprising: a) adding atorvastatin to acetone to form a mixture; b) including the mixture for a time sufficient to convert the atorvastatin to amorphous atorvastatin; and c) recovering the amorphous atorvastatin. ...

Provided are processes for preparing intermediates of rosuvastatin and their use in preparation of rosuvastatin and rosuvastatin salts thereof.

The invention encompasses processes for the preparation of darifenacin hydrobromide.

Provided are darifenacin hydrobromide free of oxidized darifenacin, and processes for the preparation thereof.

Provided is a crystallization method for reducing the level of impurities in calcipotriene in which a solution of a starting calcipotriene in a first process solvent, for example THF, is combined with second process solvent, for example methyl formate, and, after cooling, calcipotriene is isolated. The method can in...

The invention relates to processes for preparing cefdinir via its potassium and cesium salts.a) reacting a protected thioester of Formula, 7-amino-3-vinyl-3-cephem-4-carboxylic acid and at least one organic base in the presence of water and a water-miscible organic solvent to form protected cefdinir;(b) converting...

The present invention provides a process for the preparation of the rosu-vastatin intermediate FPP-CHO and its conversion to rosuvastatin and pharmaceutically acceptable salts thereof.

A process for preparing amorphous form of valsartan comprising the steps of: a) precipitating amorphous valsartan from a solution of valsartan in a solvent selected from the group consisting of methyl t-butyl ether and acetone; and b) recovering valsartan amorphous form.

The present invention provides a pharmaceutical dosage form for oral administration to a patient comprising an enterically coated core tablet sheathed in an annular body of compressed powder or granular material. The present invention also provides a pharmaceutical dosage form for co-administration of two or more ac...

The present invention encompasses processes for the preparation of optically pure clopidogrel camphorsulfonic acid salt without the need to isolate or recover (+) clopidogrel.

Novel processes for the preparation of amorphous atorvastatin hemi-calcium salt are provided, which involve dissolving atorvaslatin hemi-calcium salt in certain organic solvents, and removing the solvent such as by spray drying, rapid vacuum evaporation, and/or thin film evaporation. Preferred embodiments of these p...

A method of preparing crystalline lansoprazole form A, comprising the steps of: a). preparing a solution of lansoprazole in a solvent selected from the group consisting of methanol, n-butanol, acetone, methylethylketone, ethyl acetate, dimethyl sulfoxide, dimethylformamide and their mixtures optionally with water; a...

Provided is a process for the purification of tegaserod maelate. Also provided is an isolated compound and the preparation thereof. This compound may be used as a reference marker and a reference standard, in the analysis of the purity of the tegaserod maleate.

The invention encompasses processes for the synthesis of eilexetil trityl candesartan from the reaction of trilyl can-desartan with eilexetil halide in the presence of a base and a low boiling organic solvent. Optionally, the reaction may be conducted in (he presence of a phase transfer catalyst. ...

The present invention provides a pharmaceutical composition comprising benazepril and amlodipine wherein the benazepril and the amlodipine are in physical contact with one another, and methods for making the same.

Provided are two novel crystalline forms of gatifloxacin, denominated form O and form V, methods for their preparation and pharmaceutical compositions thereof.

A method of epimerizing a C-24 epimer of a vitamin D analog having a hydroxyl substituent on an asymmetric allylic carbon at the 24 position comprising the steps of: a) esterifying the hydroxyl group on the asymetric allylic carbon atom at the 24 position with an esterifying agent, b) contacting a solution of the ...

A crystalline fexofenadine hydrochloride in the solid state characterized by a PXRD pattern with peaks at 10.1, 15.2, 18.6, 19.2, 20.1 + 0.2 degrees two theta.

Provided are processes for preparing ziprasidone from CEI and BIPT.

Provided are alkyl ammonium crystalline salts of rosuvaslatin Ihat provide for purification of rosuvastatin and its pharnaceutically acceptable sails.

Provided is an improved of quetiapine and pharmaceutically acceptable salts.

Provided is a crystalline form of ziprasidone base and process for its preparation.

The invention encompasses synthesizing 7-(4-bromobutoxy)-3,4-dihydrocarbostyril by mixing 7-hydroxy-tetrahy-droquinolinone, dibromobutane, and at least one base to form a reaction mixture; heating the reaction mixture; cooling the reaction mixture; and isolating the 7-(4-bromobutoxy)-3,4-dihydrocarbostyril from the ...

Provided aiv process for the preparation of valsartan and the precursors thereof and processes for preparing Valsartan containing less than uboui 5(X)0 ppm residual solvent.

The present invention provides a stable pharmaceutical composition of an acid labile drug such as a pharmaceutically active substituted benzimidazole compiond comprising: a) an inner core coated with the acid labile drug; b) a first intermediate coating devoid of an alkaline stabilizing agent and the benzimidazole c...

The present invention provides a process comprising admixing a thioether with about 1.05 to about 1,6 molar equivalents of an active chlorine-containing oxidant, preferably sodium hypochlorile, and about 2.5 to about 5.0 molar equivalents of an alkali metal base; and recovering a sulfoxide thai is preferably pantopr...

The present invention provides improved methods of converting R-N-(4-morpholiyl- 3-fluorophenyl)-2-oxo-5-ox-azolidinyl-methyl azide (III) to the intermediate S-N-(4- morpholinyl-3-fluorophenyl)-2-oxo-5-oxazolidinyl-methyl amine (II) that involve the production of fewer by-products than previous methods. The amine (I...

The present invention provides an isolated linezolid (1) impurity, bis-linezolid (4), preparation thereof and its use as a reference standard.

The invention encompasses a process for preparing cefdinir cesium of claim 1 comprising combining water (or a mixture of water and a water-posscible organic solvent) cefdinir, a base and a source of cesium ions to obtain cefdinir cesiuna.

The invention encompasses amorphous montelukast sodium having less than about 50 ppm heptane or less than about 100 ppm hexane, less than about 150 ppm toluene, and less than about 2500 ppm C1-C5 alcohols, as well as processes for its preparation.

The present invention relates to protected valacyclovir, N-tert-butoxycarbonyl-L-valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy] ethyl ester, and a method of making it. The present invention further relates to a method of making valacyclovir including the steps of coupling an amine protected valine selec...

Provided are processes for preparing crystalline forms of ezetimibe, such as ezetimibe Form A or Form B, for example, by precipitating ezetimibe from selected solvents. Alternatively, some forms may be transformed into different forms at elevated temperatures or under various humidity conditions, or by micronization...

This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharma...

One of the objects of the present invention is directed to a process of preparing a pharmaceutical formulation of a drug of low aqueous solubility, comprising (A) fixing the drug in a strong matrix comprising at least one at least partially amorphous sugar to obtain a sugar-drug matrix; and (B) milling the sugar-dr...

The present invention relates to novel essentially pure venlafaxine and the process of preparation thereof. The present invention also relates to novel solvate forms of venlafaxine hydrochloride and the process of preparation thereof. Furthermore, the present invention provides a novel process for preparing venlafax...

A process for making sertraline hydrochloride Form VIII comprising the steps of: (a) suspending or dissolving sertraline hydrochloride ethanolate Form VI or sertraline hydrochloride Form II in a mixture of water and isopropyl alcohol; and (b) isolating sertraline hydrochloride Form VIII.

A process for making sertraline hydrochloride Form V comprising the steps of: (a) dissolving sertraline hydrochloride in trichloroethane or suspending sertraline hydrochloride in a suitable solvent; (b) removing the solvent; or (a) dissolving or suspending sertraline base in water, optionally in a mixture wit...

The present invention provides a drying process for preparing crystalline solid famciclovir form I comprising the steps of: (i) preparing a wet crystalline form of famciclovir, (ii) drying the wet crystalline form of famciclovir at a temperature of below 50"C until the crystalline form contains less than 15% (wt/wt)...

The present invention encompasses a method of preparing a ready-to-dissolve or ready-to-disperse composition of difficult to dissolve in water compounds and suspensions or aqueous solutions of difficult to dissolve in water compounds.

The invention encompasses wet granulation pharmaceutical compositions of aripiprazole, methods of making tablets from the compositions, and tablets of the wet granulation pharmaceutical composition.

The invention provides pharmaceutical metaxalone compositions having improved bioavailability, food effect, and/or relative food effect, as well as methods of making such metaxalone compositions.

Provided are stable pharmaceutical formulations of benzimidazole compounds, particularly esomeprazole magnesium, and processes for their preparation.

Provided is valacyclovir hydrochlonde stable against formation of N'-formylvalacyclovir upon storage at elevated humidity and pharmaceutical compositions including such valacyclovir hydrochlonde.

1. Solid crystalline atorvastatin hemi-calcium Form IXa and solvates thereof characterized by a powder X-ray diffraction pattern having peaks at 9.3, 9.5, 15.7, 20.5, 21.1, 22.8, 23.8, 24.0, 25.3, 26.4, 26.8, 27.2, 29.2 and 31.6±0.2 degrees two theta.

A process of making a 3-(haloaryl)-l,3-diazaspiro[4.4]non-l-ene-4-one compound comprising the step of : combining a l,3-diazaspiro[4.4]non-l-ene-4-one acid addition salt with a haloaryl compound in a two-phase solvent system comprising first and second solvents, in the presence of a phase transfer catalyst. ...

Novel crystalline forms of Linezolid, designated as Form Tiii Form V, Form VI, Form IX, Form X, Form XII, Form XIV, Form XVII, and Form XVIII, are disclosed. The novel crystalline forms are characterized by powder X-ray diffraction, FTIR and FTRaman spectroscopy, and differential scanning calorimetry. Methods of pr...

The present invention provides a process for preparing olmesartan medoxomil at pH higher than 2.5.

Provided are new intermediates of solifenacin and methods for their preparation, as well as methods of preparing solifenacin and solifenacin succinate.

The present invention provides the preparation of olmesartan medoxomil containing less than about 0.1% of one or more of the impurities O1.M Me, OLM -Cl, and OLM-eliminate.

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The subject invention provides compounds having the structure (I): wherein R1 is present or absent, and when present is H, C1-C6alkyl, C1-C6 alkynyl, - (CH2)yS (CH2 )xCH3, C1-C6 aminoalkyl, C1-C6 hydroxyalkyl or -(CH2)nC(=0) (C6H4) (CH2)R2; R2 is H or C1-C4 alkyl; R3 is H or C1-C4 alkyl; R4 is present or absent, and...

A process for making risedronate sodium, comprising: refluxing a combination comprising risedronic acid, a sodium base, and an iron-reducing amount of EDTA in a liquid; and isolating risedronate sodium from the combination.

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"PROCESSES FOR PREPARING (3-SULFONAMIDE-4-CHLORO) PYRIDINE, (3-SULFONAMIDE-4-FLUORO) PYRIDINE OR (3-SULFONAMIDE-4-BROMO) PYRIDINE"

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Novel, stable pharmaceutical formulations for the oral administration of high purity torsemide modification II are disclosed. These formulations release high purity torsemide modification II in water at a constant and high purity rate, and the high purity torsemide modification II therein does not rearrange to torse...

Provided are processes and intermediates for preparation of rosuvastatin.

The present invention is directed to new crystalline forms of Atorvastatin calcium (2:1), referred to hereinafter as polymorphic Forms X, A, B1, B2, C. D and E. Furthermore, the present invention is directed to processes for the preparation of these crystalline forms and pharmaceutical compositions comprising the cr...

Provided are a method of making irbesartan via a Suzuki coupling reaction and a novel intermediate, 2-butyl-3-(4'-bromobenzyl)-l,3-diazaspiro[4.4]non-l-ene-4-one, for such process. The novel process includes the step of reacting such intermediate with a protected imidazolephenylboronic acid.

The present invention provides an isolated N-formal Val acyclovir, its preparation and its use as a reference market and/or reference standard. (A)

The preparation of atorvastatin calcium epoxide dihydroxy (AED) is described. AED can be used as a standard or marker in determining the amount of AED in a sample. AED can therefore be used as a tool in preparing atorvastatin calcium substantially free of AED.

Optically pure 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is prepared. The 1(S)-phenyl-1,2,3,4-tetrahydroisoquinoline tartrate is particularly useful for preparing solifenacin succinate.

Provided are hydrogenation processes of sertraline imine intermediates with catalysis in various reactors.

The invention encompasses processes for making tolterodine tartrate.

A process for making sertraline hydrochloride Form V comprising the steps of: (a) dissolving or suspending sertraline hydrochloride in water, optionally in a mixture with an alcohol; (b) removing the solvent; and (c) spray drying to form sertraline hydrochloride Form V.

Provided are pharmaceutical compositions of fenofibrate, and dosage forms containing them, that include fenofi-brate, a polyethylene glycol, and a polethylene-polypropylene glycol; wherein the compositions are made by subliming a sublimable carrier from a combination of fenofibrate, the polyethylene glycol, and the ...

Provided is clopidogrel base suitable for pharmaceutical formulation, and processes for its preparation.

One of the embodiments of the present invention is directed toward a process for preparing a stable zonisamide pharmaceutical composition, comprising subjecting zonisamide to wet granulation with a granulation liquid to form a granulated mixture as the stable zonisamide pharmaceutical composition, wherein the granul...

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 26; and a DSC thermo gram with endotherms at about 66 and 130°C.

The present invention relates to a process for preparing nateglinide Form U comprising the steps of: (a) preparing a solution of nateglinide in a solvent selected from the group consisting of an ester, ketone, alcohol and mixtures thereof, at a temperature from about -15°C to about 50°C; (b) crystallizing nat...

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21,1+0.2 degrees 26; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form P) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2; and a DSC thomgram. with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2θ; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 2θ; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 29; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data selected from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 20; and a DSC thermogram with endotherms at about 66 and 130°C.

A crystalline form of nateglinide (Form D) characterized by data seleoted from the group consisting of: an XRPD pattern with peaks at 6.6, 7.5, 13.1, 16.5, 17.4 and 21.1+0.2 degrees 20; and a DSC thermogram with endotherms at about 66 and 130°C.

The present invention relates to a process for preparing nateglinide Form U comprising the steps of: (a) preparing a solution of nateglinide in a solvent selected from the group consisting of an ester, ketone, alcohol and mixtures thereof, at a temperature from about -15°C to about 50°C; (b) crystallizing nategl...

The present invention relates to a process for preparing nateglinide Form U comprising the steps of: (a) preparing a solution of nateglinide in a solvent selected from the group consisting of an ester, ketone, alcohol and mixtures thereof, at a temperature from about -15°C to about 50°C; (b) crystallizing nategl...

Substantiaily glidant free levetiracetam compositions, pharmaceutical compositions incorporating substantially gli¬dant free levetiracetam compositions, and methods of preparing such compositions are provided.

A novel, non-hygroscopic form of azithromycin is disclosed, as well as a method for preparing it by the gradual crystallization of azithromycin from ethanol by the addition of a minimal amount of water to effect crystal formation. Pharmaceutical compositions containing this novel form of azithromycin are also disclo...

Provided are polymorphic forms of ziprasidone mesylate and processes for their preparation

The invention encompasses stable pharmaceutica] compositions comprising monleiukasi or salts thereof and meth ods of preparing the same.

The invention is directed to a dipyridaraole fonnulation comprising an extended release formulation of dipyridamole and a pharmaceutically acceptable carboxylic acid, wherein the formulation is in a tablet solid form having a diameter of about 1.5 mm to about 3 mm. Optionally, the fonnulation may further comprise a...

The invention is directed to a method of purifying tadalafil by crystallization of tadalafil from a solution of crude tadalafil in a suitable crystallization solvent.

Chemically and/or enanliomericaily pure duloxetine HCI and process for preparing chemicai/y and/or enanliomerically pure duloxetine HCI are provided. (Formul I)

A crystalline solid form of lansoprazole, wherein data selected from the group consisting of an X-ray diffraction pattern having peaks at 20.7, 23.8, 24.8, 25.2, 25.6 and 29.9+0.2 degrees two theta; an X-ray diffraction pattern substantially as depicted in Figure 1; a FTIR spectrum having absorption bands at 1168, 1...

Diasteromerically enriched salts Of (S)-DNTH+ EPA" and (R)-DNTH+ EPA", methods of preparing such diasteromerically enriched salts Of (S)-DNTH+ EPA" and (R)-DNTH+ EPA, and methods of preparing enantiomerically enriched (S)-DNT and enantiomerically enriched (R)-DNT are provided.

Processes for the purification of duloxetine HCI are provided (formula (I)).

A crystalline polymorph F of [R- (R*, R*)]-2- (4-fluorophenyl)-beta, delta-dihydroxy-5- (1- methylethyl)-3-phenyl-4-[(phenylamino) carbonyl]-l H-pyrrole-1-heptanoic acid calcium salt (2: 1) which exhibits a characteristic X-ray powder diffraction pattern with characteristic peaks expressed in d-values (A) at 24.3 (s...

A chiral resolution process for the preparation of (S)-AT-OL, and a process for the racemization of AT-OL are provided. A one pot continuous process for preparing (S)-AT-OL or (S)-AT-OL mandelate comprising: a) converting (R) -AT-OL to (R/S) -AT-OL in a mixture of a Cl-8 alcohols and a C2-8 ether in presence of an a...

The invention provides at least a composition for the treatment of elevated levels of triglycerides, comprising a therapeutically effective amount of a fibrate drug, preferably fenofibrate, intimately associated with a surfactant mixture, preferably a mixture comprising PGE 6000 and poloxamer 407. The invention also...

Provided are a novel solid states of fluvastatin sodium and processes for preparation thereof.

A process for manufacturing (R)-propynylaminoindans, and alternatively, a process for manufacturing (S)- propynylaminoindans. The chiral propynylaminoindans include alkoxy or alkylcarbamates derivatives. The process comprises transfer or pressure hydrogenation in the presence of an optically active catalyst to reduc...

The present invention provides pharmaceutical compositions comprising aliphatic amine polymers such as for example Sevelamer HQ as the active phannaceatical ingredient, wherein the aliphatica amine polymiers are spray granulated. The present invention fiirther provides methods of preparing stable pharmaceutical com...

The invention encompasses crystalline forms of armodatinil , processes for preparing the crystalline forms, aid pharmacculical formulation.

Provided is a process for preparing a dnloxetine intennediate(S)-(+)-N,N-Dimethyl-3-(l- naphthalenyloxy)-3-(2-thienyl)propanamine (DNT), and its conversion to dnloxetine or a pharmaceutically acceptable salt thereof.

Non-caking azithmmycin powder for oral suspension compositions and methods of making such compositions are disclosed. The compositions comprise a hydrated buffer, preferably a hydrate of sodium phosphate such as tribasic sodium phosphate dodecahydrate.

Various fluvastatin compositions and methods for preparing them are described. One example is a controlled release pharmaceutical composition comprising fluvastatin and at least one non-ionic hydrophilic polymer, wherein the composition is sub-stantially free of hydroxypropyl methylcellulose. Another example is a st...

The present invention relates to atorvastatin hemi-calcium Form VI and solvates thereof having a powder X-ray diffraction pattern substantially as depicted in figure 1.

The invention provides at least a composition for the treatment of elevated levels of triglycerides, comprising a therapeutically effective amount of fenofibrate or another fibrate drug intimately associated with menthol or a surfactant mixture, wherein the menthol can be menthol or menthol surfactant mixture, and w...

The invention provides at least a composition for the treatment of elevated levels of triglycerides, comprising a therapeutically effective amount of fenofibrate or another fibrate drug intimately associated with menthol, optionally in the presence of at least one surfactant mixture. The invention also provides a me...

A process of making risedronate sodium in crystalline in form B in admixture with crystalline form B1 comprising the steps of: refluxing a combination of risedronic acid and a sodium base in a liquid comprising between about 5% and about 25%, v!v, ethanol, the remainder consisting essentially of water, cooling t...

A process of making risedronate sodium having at least one characteristic pf form B comprising the step of treating risedronate sodium form A with 1:1, v/v, mixture of a lower alkanol and water at a temperature between about room temperature and about reflux temperature.

Provided are novel polymorphs and pseudopolymorphs of risefronate sodium and risedronate disodium, methods for making them, and pharmaceutical compositions containing them.

Pharmaceutical compositions are described containing carrier particles bearing microparticles of a drug. The drug microparticles may be deposited on the carrier particles, for example, by sublimation. Preferred embodiments of these pharmaceuti¬cal compositions are suitable for administration by inhalation or injecti...

Provided are new crystalline Forms III, IV, V and VI of clopidogrel hydrogensulfate and the amorphous form of clopidogrel hydrogensulfate, as well as their pharmaceutical compositions, and method of treatments with such compositions. Also provided are novel processes for preparation of clopidogrel hydrogensulfate Fo...

Provided is a process for preparing Cinacalcet, (R)-α-methyl-N-[3-[3- (trifluoromethyl)phenyl]propyl]-l-naphthalenemethane amine and intermediates thereof.

Delayed release formulations of duloxetine hydrochloride and methods for its manufacture are described. A preferred formulation includes an inert core, a drug layer comprising duloxetine hydrochloride, a separating layer and an enteric layer comprising at least one of methacrylic acid copolymer and hydroxypropy] met...

A crystalline form of duloxetine hydrochloride, pharmaceutical compositions of the crystalline form of duloxetine hydrochloride, and methods of preparing the crystalline form of duloxetine hydrochloride are provided.

The present invention provides methods of purifying montelukast, a new isolated impurity of montelukast of formula I, method for its isolation, and method of using montelukast impurity as a reference marker and a reference standard.

Provided is a solid particulate tadalafil having a bimodal particle size distribution.

The present invention provides stable pharmaceutical compositions comprising moisture sensitive drugs, in particular an angiotensin converting enzyme (ACE) inhibitor such as Cilazapril, as the active ingredient, and at least one pharmaceutical excipient, wherein the active pharmaceutical ingredient is wet granulated...

Provided is a novel method of making 2-butyl-3-[[2"(1-trityl-1H-tetrazol-5-yl)biphen-4-yl]methyl]1,3-diazaspiro[4,4]non-1-ene-4-one, which can be converted to irbesartan. Also provided are methods of making irbesartan.

(54) Title: COMPOSITIONS WITH CONTROLLED PHARMACOKINETICS (57) The invention encompasses methods for reducing food effect in a drug which exhibits such food effect by preparing a fonnuiation comprising a drag which exhibits food effect and at least one biodegradable binder or lipophilic binder. The invention also ...

This invention relates to oral pharmaceutical compositions suitable for making pharmaceutical formulations for oral administration that provide for the rapid dissolution of the phosphodiesterase 5 inhibitor tadalafil. In particular, the pharmaceutical compositions comprise solid composites of tadalafil exhibiting hi...

Novel forms of atorvastatin hemi-calcium have been prepared and characterized These novel forms are particularly useful in pharmaceutical compositions.

Provided are processes for the preparation of clopidogrel bisulphate Form 1.

The present invention relates to a process for preparing atorvastatin comprising: a) adding atorvastatin to acetone to form a mixture; b) including the mixture for a time sufficient to convert the atorvastatin to amorphous atorvastatin; and c) recovering the amorphous atorvastatin. ...