Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Boehringer Ingelheim International Gmbh

Boehringer Ingelheim Pharmaceuticals, Inc.

Intervet Inc.

Richard John Varsolona

David Askin

Ralph P Volante

Paul J Reider

Kai Rossen

James A McCauley

Kenneth M Wells

Carl Alan Busacca

Guy R Humphrey

Ulf H Dolling

R Scott Hoerrner

Laura Marie Artino

Burkhard Jaeger

Eric Sirota

Robert M Purick

Thilo Berkenbusch

Li Feng Zhang

Chris Hugh Senanayake

Bruce D Dorsey

Zhijian Lu

Yuan Cheng

Feng Xu

Kevin Tyler Chapman

James R Tata

Philip E Sanderson

Subharekha Raghavan

John Y L Chung

Raymond Cvetovich

Terry A Lyle

Zhiguo Jake Song

Yong-Li Zhong

Zhuqing Liu

Rogelio Perez Frutos

Kevin Campos

Dhileepkumar Krishnamurthy

Xiao-Jun Wang

Joseph Leslie Duffy

Kevin Michael Belyk

Jianguo Yin

Nancy J Kevin

Zeren Wang

Jeonghan Park

Tao Wang

Thomas Nicola

Thomas A Rano

Kevin Matthew Maloney

Zhi-Hui Lu

Fengqi Zhang

Jon Charles Lorenz

Scott Trzaska

Christophe Pierre Alain Chassaing

Alexei Kalinin

Michael J Kaufman

Ji Qi

Laurence John Nummy

Thomas Wirth

Richard Desmond

Jingjun Yin

Joseph D Armstrong, Iii

Donald R Gauthier

Bangping Xiang

Jutta Kroeber

Tetsuji Itoh

David C Dubost

Yibo Xu

Rolf-Stefan Brickl

Richard J Demchak

Shirlynn Chen

Danping Li

Yingju Xu

Yong Liu

Fred Fleitz

Michael Cerreta

John Smoliga

Jana Vitous

Hong Ren

Daniel E Petrillo

Tracy Huening

Rebecca T Ruck

Chitra Telang

Brian Anthony Kirk

William J Morris

Andrew Brunskill

Jennifer L Vandrilla

Jerome P Draper

Edward Cleator

Diana Reeves

Melodie Deniz Christensen

Hongming Li

Zachary E Dance

Gregory York

Lorenzo Codan

Cynthia Marilyn Hong

Kevin M Maloney

Rositza Iordanova Petrova

Xiaoling Jin

Adrian Goodyear

Jonathan Simmons

Jihchin Chung

Mayur Suryakant Dudhedia

The present invention provides processes for the preparation of 2-fluoroadenine, as well as certain intermediates useful in the preparation of 2′-deoxy-4′-C-ethynyl-2-fluoroadenosine (EFdA): EFdA.

Process for the preparation of 2-fluoroadenine

The present application relates to crystalline forms of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide and processes for the preparation thereof. The compound is useful for the treatment of JAK-mediated diseases or conditions such as atopic dermatitis.

Crystalline forms of 1-[(3R,4S)-4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl)amino]pyrazole-4-carboxamide

The instant invention is related to a novel solid form of ceftolozane sulfate (the DMAc solvate of ceftolozane sulfate (Form 3)), compositions comprising ceftolozane sulfate DMAc solvate (Form 3), synthesis of Form 3 and an improved crystallization process using Form 3 to prepare ceftolozane sulfate Form 2. Novel compositions also include ceftolozane sulfate solid Form 3 and/or other crystalline and amorphous solid forms of ceftolozane.

Solid forms of ceftolozane and processes for preparing

The present invention provides a novel crystalline form of verubecestat (Crystalline Form II of Verubecestat) and pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A&#x3b2; pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A&#x3b2; pathologies, including Alzheimer's disease and mild cognitive impairment, are disclosed herein.

Crystalline form of a BACE inhibitor, compositions, and use

The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention. 

Process for preparing substituted tetracyclic heterocycle compounds

The present invention provides four crystalline forms of verubecestat, as well as pharmaceutically acceptable compositions thereof, each of which may be useful in treating, preventing, ameliorating, and/or delaying the onset of an A&#x3b2; pathology and/or a symptom or symptoms thereof. Non-limiting examples of such A&#x3b2; pathologies, including Alzheimer's disease, are disclosed herein.

Crystalline forms of a BACE inhibitor, compositions, and their use

The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.

Methods and intermediates for preparing macrolactams

This invention relates to novel sodium salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: 

Solid state forms of a potent HCV inhibitor

This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection: 

Crystalline forms of a potent HCV inhibitor

Disclosed is a multi-step process for preparing a compound of Formula I: wherein Rto Rare as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules to the Leukointegrins. As a result, these compounds are useful in the treatment of inflammatory and immune cell-mediated diseases.

Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides

Dihydrate and anhydrous crystalline forms of 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-dipyrido[3,2-b:2',3&#x2032;-e] [1,4]diazepin-6-one.

Crystalline forms of 5,11-dihydro-11-ethyl-5-methyl-8-{2-{(1-oxido-4-quinolinyl)oxy}ethyl}-6H-dipyrido[3,2-b:2',3&#x2032;-e] [1,4]diazepin-6-one

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

The most thermodynamically stable crystalline form of the benzoic acid salt of 4&Prime;-deoxy-4&Prime;-epi-methylamino avermectin B1a/B1b as the hemihydrate is obtained by crystallization from organic solvents containing a controlled amount of water.

Thermodynamically stable crystal form of 4&Prime;-deoxy-4&Prime;-epi-methylamino avermectin B1a/B1b benzoic acid salt and processes for its preparation

This invention relates to a sulfate salt of an HIV protease inhibitor, Compound A, of formula: ##STR1## Compound A is useful in the treatment of AIDS, ARC or HIV infection in adults and children. Processes for making the sulfate salt of Compound A are also disclosed.

HIV protease inhibitor

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Scotch Plains, NJ, United States of America

Richard John Varsolona