Novartis Ag

Sandoz Gmbh

Johnson Matthey Inc.

Sandoz Pharm. Corp.

Johnson Matthey Public Limited Company

Astex Therapeutics Limited

Novartis Pharmaceuticals Corporation

Novartis Pharma Gmbh

Kau-Ming Chen

Prasad Koteswara Kapa

George T. Lee

Oljan Repic

Michel Crevoisier

Petr Hess

Mahavir Prashad

Eric M Loeser

George T Lee

Guang-Pei Chen

William J Houlihan

Thomas J Blacklock

Michael John Girgis

Joel Slade

Baoqing Gong

David Xu

John Vincent Calienni

Ulrich Beutler

Werner Zaugg

Russell L Underwood

Heinrich Estermann

Andrew Kucerovy

Goetz E Hardtmann

Piotr Henryk Karpinski

Liladhar Murlidhar Waykole

Sompong Wattanasin

Raeann Wu

Frederick Ray Kinder, Jr

Sushil Kumar Sharma

Lech Andrzej Ciszewski

Bin Hu

Joerg Berghausen

Hui Liu

Thalaththani Ralalage Vedananda

Jerome Linder

Joseph McKenna

Michael Lloyd Sabio

Marilyn De La Cruz

Frank Stowasser

Vishal Saxena

George Tien-San Lee

Hong-Yong Kim

John Amedio

Philip Lake

John Joseph Fitt

Pascal Michel

Xinglong Jiang

Maria Caterina Testa

Zhengming Du

James Lawrence Stanton

Orin Tempkin

Russell C Petter

Paul G Mattner

Ustun B Sunay

Frank Stowasswer

Chung-Pin Chen

Andrew Thomas Bach

Eric M Loesser

Gleb Kardash

Joseph Mckenna

Rasmus Mose

Dietmar Flubacher

This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salt(s) thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.

Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof

The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.

Manufacturing process for pyrimidine derivatives

This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.

Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-D]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof

The present technology provides novel anhydrous and hydrated crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea, amorphous and anhydrous crystalline polymorphs of its monophosphoric acid salt, and the hydrochloride salt, including its dihydrate. The present technology further provides methods for preparing the various forms, compositions containing them, and methods of treatment employing them.

Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl) -phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof

The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase inhibitors. The process makes use &#x3b1; &#x3b2;-lactarn intermediate. Certain optically pure intermediates are also claimed.

Process for preparing N-hydroxyformamido-propyl pyrrolidin compounds and intermediates

A method for preparing an alkali metal salt comprising: (a) condensing a disilyloxydiene with an aldehyde in the presence of a titanium (IV) catalyst in an inert solvent to form a 5(S)-hydroxy-3-ketoester; (b) reducing the 5(S)-hydroxy-3-ketoester to a 3(R),5(S)-dihydroxyester in the presence of a di(lower alkyl)methoxyborane; and (c) hydrolyzing the 3(R),5(S)-dihydroxyester in the presence of an aqueous base to form an alkali metal salt.

Process for the manufacture of organic compounds

Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features: (1) make use of a particular &#x3b2;-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.

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Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X. Preferred are the compounds of the invention which are dual agonists of PPAR&#x3b1; and PPAR&#x3b3; receptors.

Heterocyclic compounds and methods of use

The present invention relates to certain salts of discodermolide acid, pharmaceutical compositions containing said salts, the use of said salts in treating tumors and to a process for making said salts.

Certain salts of discodermolide acid, pharmaceutical compositions containing them and their use in treating tumors

Methods for the acylation of amine compounds

An improved process for preparing 1,4,8,11-tetraazacyclotetradecane comprising the bisacylation of an acyclic diamine to obtain a dichlorodiamide compound in a first step, the cyclization of said diamide compound to obtain dioxocyclam in a second step, and the reduction of dioxocyclam in a third step to obtain the desired 1,4,8,11-tetraazacyclotetradecane.

Process for preparing 1,4,8,11-tetraazacyclotetradecane

An improved process for preparing 1,1'-�1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane comprising the selective functionalization of an acyclic tetraamine, and subsequent dimerization and hydrolyzation/tosylation to obtain a 1,4-phenylenebis-methylene bridged hexatosyl acyclic precursor in a first step, the cyclization of said precursor to obtain a hexatosyl cyclam dimer in a second step, and the detosylation of said cyclam dimer in a third step followed by basification to obtain the desired 1,1'-�1,4-phenylenebis-(methylene)!-bis-1,4,8,11-tetraazacyclotetradecane.

Process for preparing 1,1'- (1,4- phenylenebis (methlene)-Bis

Process for preparing

An improved process for producing a water-soluble polymyxin B/dextran conjugate comprises the step of reacting polymyxin B or pharmaceutically acceptable salt thereof with dextran in an aqueous media at a pH of about 9.3 to 10.

Improved process for preparing polymyxin B/dextran conjugates

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Parsippany, NJ, United States of America

Prasad Koteswara Kapa