Schering Corporation

Tesaro, Inc.

Merck Sharp + Dohme Corp.

Opko Health, Inc.

George G Wu

Frank Xing Chen

Marc Poirier

Tiruvettipuram K Thiruvengadam

Ji Xie

Anantha R Sudhakar

Yee-Shing Wong

Tao Wang

Mingsheng Huang

Ngiap Kie Lim

Jian Cui

Daw-long Albert Kwok

Xiaojing Yang

Hoa N Nguyen

Jing Liao

Vijay Sabesan

Ilia A Zavialov

Nanfei Zou

Jeffrey Manning Eckert

Michael D Green

Hong-Chang Lee

Victoria M Sprague

Paitoon Rashatasakhon

Charles F Bernard

Alistair Stewart

Xiaoyong Fu

Shen-Chun Kuo

Robert Kevin Orr

George S K Wong

Agnes S Kim-Meade

David Jieh-Shyh Tsai

Juergen Weber

Robert Parry Williams

Jennifer R Foley

Peter C Nirchio

Feng Liang

Daw-Iong Albert Kwok

Gerald Werne

Jennifer Ann Vance

Arlene E McKeown

Anthony Joseph Toto

Nolan C Erickson

Liansheng Zeng

Louis Peter Castellanos

Yuyin Chen

John Chaber

Denise C Grogan

Michael Casey

Martin Steinman

Kartik M Keertikar

Doris P Schumacher

Alistair James Stewart

George S Wong

Ingrid Mergelsberg

Fucheng Zhang

Donald Hou

Ramani R Raghavan

Xing Chen

Yi Wang

Illia Zavialov

Ngiap-Kie Lim

Vijay Sabesen

Jianguo Yin

Daw-Long Kwok

Zou Nanfei

Ilia Zavialov

Jeffrey M Eckert

Novel salts of niraparib are provided. Also provided are pharmaceutical compositions comprising those salts, as well as methods and uses pertaining to the same.

Niraparib salts

The present invention relates to compositions comprising the compound niraparib, in particular certain solid forms of niraparib.

Niraparib compositions

Disclosed herein are methods and processes of preparing niraparib and pharmaceutically acceptable salts thereof, and intermediates and their salts useful for the synthesis of niraparib.

Methods of manufacturing of niraparib

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds

This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following: 

Exo- and diastereo-selective synthesis of himbacine analogs

This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists. The chemistry disclosed herein is exemplified in the following synthesis sequence: 

Exo-selective synthesis of himbacine analogs

Exo- and diastereo- selective synthesis of himbacine analogs

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

Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, wherein Ris a linear, branched, or cyclic alkyloxy functional group of the structure (&#x2014;R&#x2014;OH), Ris a linear, branched or cyclic alkyl group, Ris a linear, branched or cyclic alkyl group, and Ris an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1, with a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.

Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates

Exo- and diastereo-selective syntheses of himbacine analogs

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Basking Ridge, NJ, United States of America

George G Wu