Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Dupont Pharmaceuticals Company

Taisho Pharmaceutical Co., Ltd.

Lushi Tan

Cheng Yi Chen

Qinghao Chen

Michael J Zacuto

Nobuyoshi Yasuda

Feng Xu

Richard D Tillyer

Jeremy Peter Scott

Frederick W Hartner

Jacob M Janey

John Y L Chung

Robert F Dunn

Dalian Zhao

Zhiguo Jake Song

Aaron S Cote

Lilian Alicia Radesca

Wenjie Li

Yonggang Chen

Faye Sheen

Aaron J Moment

David R Lieberman

Yang Cao

Anusuya Choudhury

Jeffrey T Kuethe

Amude Kassim

Nadine Bremeyer

Benjamin Cohen

Robert S Meissner

James J Perkins

Edward J Grabowski

Robert D Larsen

Paul J Reider

Joseph F Payack

Peter Emmanuel Maligres

Yi Xiao

Kevin Michael Belyk

John Limanto

Michael Ernest Pierce

Feng Peng

Mark McLaughlin

Mathew Thomas Maust

Cheng-yi Chen

Naoki Yoshikawa

Paul O'Shea

Weirong Chen

Daniel J Kumke

Shane W Krska

Yuan-Hon Kiang

Gavin William Stewart

Carl A Baxter

Michael Palucki

Joyce Stellabott

Enrique Vazquez

Andrew Gibb

James Christopher McWilliams

Wenji Li

Benjamin T Dorner

Philippe Dagneau

Benjamin Dorner

This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.

Process for making M1 receptor positive allosteric modulators

A process for preparing a compound of structural Formula Ia:   

Process for preparing chiral dipeptidyl peptidase-IV inhibitors

A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of: 

A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.

The present invention relates to a process for the production of crystalline particles of a glucagon receptor antagonist compound. The process includes the steps of generating microseeds and subjecting the microseeds to a crystallization process. The resulting crystalline particles have a mean particle size of less than about 100 mm. The present invention also provides for a pharmaceutical composition which includes the crystalline particles produced by the method described herein and a pharmaceutically acceptable carrier.

Process for the production of a crystalline glucagon receptor antagonist compound

Processes for the preparation of certain [3.1.0]hexane derivatives which are useful as mGluR agonists, and intermediates prepared during such processes.

Processes for preparing bicyclo [3.1.0] hexane derivatives, and intermediates thereto

The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.

Process for synthesizing a substituted pyrazole

Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. These compounds are useful in the enhancement of weakened muscle tone and the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, benign prostatic hyperplasia (BPH), abdominal adiposity, metabolic syndrome, type II diabetes, cancer cachexia, Alzheimer's disease, muscular dystrophies, cognitive decline, sexual dysfunction, sleep apnea, depression, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

Polymorphs of an androgen receptor modulator

The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivity, such as osteoporosis, periodontal disease, bone fracture, frailty, erectile dysfunction, loss of libido, androgen-dependent cancers and sarcopenia. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.

Process for making fluorinated 4-azasteroid derivatives

A novel process is provided for the preparation of optionally protected 2,5-di-(3&prime;-aminopropyl)-pyridines which are useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

Process for preparing integrin antagonist intermediates

Synthesis of ketosulfone esters

Described is a process of preparing 3-aryl, 4-aryloxy furan-5-ones which are useful as inhibitors of cyclooxygenase-2 (COX-2). Such compounds are useful as anti-inflammatory agents. The process is directed to an asymmetric synthesis which involves: a trisubstituted styrene derivative preparation via Horner-Wadsworth-Emmons reaction and subsequent one pot trifluoromethylation of the allylic alcohol; preparation of the .alpha.-hydroxyl ketone using Sharpless asymmetric dihydroxylation and Swern oxidation; the esterification of the .alpha.-hydroxyl ketone with the phenoxy acetic acid; and the Dieckman condensation of the resulting ester.

Process of making 3-aryloxy, 4-aryl furan-2-ones useful as inhibitors of

The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Asymmetric synthesis of benzoxazinones

An efficient method for the preparation of key intermediate, in the synthesis of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, a reverse transcriptase inhibitor is achieved using a chiral addition reaction to the 4-chloro-2-trifluoromethylketoaniline with an organozinc complex to give the desired alcohol. This instant method has broad applicability in the chiral addition to any prochiral ketone.

Efficient enantioselective addition reaction using an organozinc reagent

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Edison, NJ, United States of America

Lushi Tan