Merck Sharp + Dohme Corp.

Merck + Co., Inc.

The Scripps Research Institute

Scripps Clinic and Research Foundation

Idenix Pharmaceuticals, Inc.

Merck Sharpe & Dohme Corp.

Peter Emmanuel Maligres

Kyriacos Costa Nicolaou

David Askin

Artis Klapars

Chan-Kou Hwang

Wilhelm Stahl

Adrian Leonard Smith

Erwin Paul Schreiner

Wei-Min Dai

Toshio Suzuki

Ralph P Volante

Nobuyoshi Yasuda

Guy R Humphrey

Steven A Weissman

Bryon Ladd Simmons

Marjorie See Waters

Alan Michael Hyde

Wolfgang A Wrasidlo

J Christopher McWilliams

Michael Shevlin

Timothy James Wright

Sebastian V Wendeborn

Jennifer A Cowen

Adel M Moussa

John S Wai

Peter D Williams

Kai Rossen

Paul J Reider

Shankar Venkatraman

Wayne J Thompson

Hongmei Li

Dai-Shi Su

John Y L Chung

Shen-Chun Kuo

James Francis Dropinski

Michel M Chartrain

Mark W Embrey

Zhiguo Jake Song

Yong-Li Zhong

Benjamin Alexander Mayes

Kevin Campos

Ross A Miller

Lushi Tan

Edward Cleator

Jianguo Yin

Kevin Michael Belyk

Ilia A Zavialov

John Limanto

Alistair James Stewart

Jeremy Peter Scott

Thorsten E Fisher

Tao Pei

Edward C Sherer

Hoa N Nguyen

Cheol Keun Chung

Jingjun Yin

Yonggang Chen

Ian Mangion

Aaron J Moment

Bangping Xiang

Ingyu Jeon

Qinghao Chen

Kan K Eng

David C Dubost

Jaemoon Lee

Carl A Baxter

Richard C A Isaacs

Neil A Strotman

Gavin William Stewart

Shane W Krska

Amude Kassim

Steven Mark Silverman

Daniel A DiRocco

Susan L Zultanski

Ralph Calabria

Veena Upadhyay

Cheng-yi Chen

Matthew L Maddess

Dietrich P Steinhuebel

Richard G Ball

Eric J Choi

Mikhail Reibarkh

Kenneth Baker

Sarah L Trice

Neil Campbell

Louis Charles Campeau

Tyler A Davis

Sebastian V Wenderborn

Yi Ning Ji Chen

Rose Mathew

Andrew Gibb

Kara Van Valkenburg

Kevin M Belyk

Matthew Maddess

Steven Weissman

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

The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I). 

Process for making nucleoside phosphoramidate compounds

The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

Process for making chloro-substituted nucleoside phosphoramidate compounds

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

The invention encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, which are CGRP receptor antagonists useful for the treatment of migraine, utilizing a highly effective spiroacid synthesis.

Process for making CGRP receptor antagonists

An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis: 

Process for synthesizing a CETP inhibitor

Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed. 

Process for preparing N-substituted hydroxypyrimidinone carboxamides

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X, X, Y, R, R, Rand Rare defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Processes for making compounds of Formula I and intermediates thereof are also described.

HIV integrase inhibitors

An improved and efficient synthesis for the preparation of 2-amino-6-&lsqb;(4-aminopiperidin-1-yl&rsqb;methyl&rsqb;pyridine, an intermediate compound in the preparation of muscarinic M3 receptor antagonists, includes as a final step the removal of trimethylacetyl and an amino protecting group from 2-trimethylacetyl-amino-6-&lsqb;(4-protected aminopiperidin-1-yl)methyl&rsqb;pyridine.

Process for the preparation of chemical compounds

The present invention is directed to a process for synthesizing 1,5 disubstituted imidazoles with biaryl components of the formula (I):

Process for synthesizing biaryl inhibitors of farnesyl-protein transferase

The present invention is directed to a process for synthesizing 1,5-disubstituted imidazoles, which are useful in the preparation of farnesyl-protein transferase inhibitors.

Process for making 1,5-disubstituted imidazoles

The present invention is concerned with a novel process for the preparation of a compound of the formula: ##STR1## This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.

Process for the preparation of (S)-3-carbethoxy-3-benzylpiperidine

A process for synthesizing the epoxide of the formula ##STR1## consists of, at a minimum, formation of a halohydrin from the allyl acetonide reactat, followed by base-induced cyclization, the epoxide product I being useful as an intermediate for the synthesis of inhibitors of renin or HIV protease or other proteases.

Process for making an epoxide

Chemotherapeutic agents that exhibit cytotoxicity similar to that of daunomycin against cancer cells, but exhibit lessened cytotoxicity against normal, non-transformed cells are disclosed, as are compositions, processes for making and using the same. A contemplated chemotherapeutic agent is a daunomycin derivative whose structure corresponds to structural Formula I, wherein Ar is phenyl, 1-naphthyl or 2-naphthyl ##STR1##

Daunomycin derivative with reduced cytotoxicity toward normal cells

A fused ring system compound is disclosed that contains an epoxide group on one side of the fused rings and an enediyne macrocyclic ring on the other side of the fused rings. The compounds have DNA-cleaving, antimicrobial and tumor growth-inhibiting properties. Chimeric compounds having the fused ring system compound as an aglycone bonded to (i) a sugar moiety as the oligosaccharide portion or (ii) a monoclonal antibody or antibody combining site portion thereof that immunoreacts with target tumor cells are also disclosed. Compositions containing a compound or a chimer are disclosed, as are methods of preparing a compound.

Dynemicin analogs: syntheses, methods of preparation and use

Growing community of inventors

Fanwood, NJ, United States of America

Peter Emmanuel Maligres