Schering Corporation

Celgene Corporation

Signal Pharmaceuticals, Inc.

Merck Sharp + Dohme Corp.

Lexicon Pharmaceuticals, Inc.

Jeffrey Manning Eckert

Nanfei Zou

Alexander L Ruchelman

George G Wu

Frank Xing Chen

Terrence Joseph Connolly

Anthony Frank

Chinnapillai Rajendiran

Jasti Venkateswaralu

Nallamaddi Ravikumar Reddy

Hong-Chang Lee

George S K Wong

David Jieh-Shyh Tsai

Juergen Weber

Peter C Nirchio

Paitoon Rashatasakhon

Jennifer Ann Vance

Nolan C Erickson

Wenxue Wu

William W Leong

Tiruvettipuram K Thiruvengadam

Shen-Chun Kuo

Marc Poirier

Dinesh Gala

Doris P Schumacher

Yee-Shing Wong

Matthew Mangzhu Zhao

Ilia A Zavialov

Ngiap-Kie Lim

Agnes S Kim-Meade

Yonggang Chen

Mark S Bednarz

Feng Liang

Vilas H Dahanukar

Brian Lucas

Kuangchu Dai

Gabriel C Kuklis

Lauren Sirois

Methods of preparing, and solid forms of N-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide, and salts, solvates and cocrystals thereof, are disclosed.

Crystalline solid forms of N-(1-((2-(dimethylamino)ethyl)amino)-2-methyl-1-oxopropan-2-yl)-4-(4-(2-methyl-5-((2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(methylthio)tetrahydro-2H-pyran-2-yl)benzyl)phenyl)butanamide and methods of their synthesis

Provided herein are formulations, processes, solid forms and methods of use relating to the compound of formula (I): 

Solid forms of 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-YL)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1H)-one as tor kinase inhibitors

Provided herein are new processes for the preparation of aminosulfone intermediates for the synthesis of 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, which is useful for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-&#x3b1;. Further provided herein are processes for the commercial production of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine.

Processes for the preparation of (S)-1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethylamine

Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.

Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer

Provided herein are formulations, processes, solid forms and methods of use relating to the Compound for formula 1: 

Solid forms of 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, as TOR kinase inhibitors

A process for preparing 7-[2-[4-(6-fluoro-3-methyl-1,2-benzisoxazol-5-yl)-1-piperazinyl]ethyl]-2-(1-propynyl)-7H-pyrazolo-[4,3-e]-[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, intermediates useful in that process, and processes for preparing said intermediates are disclosed.

Process for preparing a 2-alkynyl substituted 5-amino-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine

The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid ('D-DTTA') salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt ('L-DTTA') in a high enantiomeric excess. This invention also provides for a process for preparing a (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (&#x201c;D-DBTA&#x201d;) salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (&#x201c;L-DBTA&#x201d;) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.

Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.3.0]-hexane compounds and enantiomeric salts thereof

The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid ('D-DTTA') salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt ('L-DTTA') in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (&#x201c;D-DBTA&#x201d;) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (&#x201c;L-DBTA&#x201d;) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.

Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.1.0]-hexane compounds and enantiomeric salts thereof

An enantioselective process for preparing intermediates useful in the preparation of the chiral tricyclic compound of formula I is disclosed.

Enantioselective process

In one embodiment, the present invention describes the synthesis of a compound of formulaand intermediates therefor.

Process for synthesis of D1 receptor antagonists

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Hazlet, NJ, United States of America

Jeffrey Manning Eckert