Schering Corporation

Merck Sharp + Dohme Corp.

Merck Sharp & Dohme LLC

Frank Xing Chen

Mingsheng Huang

Tao Wang

Marc Poirier

Daw-Long Kwok

Ngiap Kie Lim

Jian Cui

Vijay Sabesan

Xiaojing Yang

Ji Xie

Jing Liao

Anantha Sudhakar

Hoa N Nguyen

Ilia A Zavialov

Anantha R Sudhakar

Tiruvettipuram K Thiruvengadam

George G Wu

Cecilia A Orr

Daw-long Albert Kwok

Vilas Hareshwar Dahanukar

Ingyu Jeon

Fucheng Zhang

Vilas A Dahanukar

Ilia Zavialov

Nobuyoshi Yasuda

Wenxue Wu

Craig D Boyle

William W Leong

Hongmei Li

Peter Emmanuel Maligres

Minzhang Chen

Kevin Joseph Klopfer

Artis Klapars

Jeonghan Park

George S Wong

Michael D Green

Hong-Chang Lee

Yonggang Chen

Loc Thanh Tran

Juergen Weber

Ian Mangion

Daw-Iong Albert Kwok

Feng Liang

Bosco D'Sa

Man Zhu

Cheng-yi Chen

Xiongwei Shi

Tetsuo Iwama

Vilas H Dahanukar

Shannon Zhao

Yi Liu

Illia Zavialov

Albert W Buchholz, Jr

Jeffrey M Skell

Funcheng Zhang

Cecelia Proietti

Xiongwei Shih

Cecilia Proietti

The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I). 

Process for preparing tetracyclic heterocycle 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

Exo- and diastereo- selective synthesis of himbacine analogs

Exo- and diastereo-selective syntheses of himbacine analogs

A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9.   

Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof

The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.

Synthesis of CCR5 receptor antagonists

Exo- and diastereo- selective syntheses of himbacine analogs

In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.

Process and intermediates for the preparation of (1R,2S,5S)-3-azabicyclo[3,1,0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[1,1-dimethylethyl]amino]carbonylamino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl

Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS.and, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS.and, respectively, and are represented by the formula:  Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.

Xanthine phosphodiesterase V inhibitor polymorphs

A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9 

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Dayton, NJ, United States of America

Hoa N Nguyen