Merck Sharp + Dohme Corp.

Schering Corporation

Ligand Pharmaceuticals, Inc.

Pharmacopeia Drug Discovery, Inc.

Pharmacopeia Inc.

Guizhen Dong

Zhiqiang Yang

Brian F McGuinness

Subharekha Raghavan

Alexander J Kim

Neng-Yang Shih

Joseph A Kozlowski

Koc-Kan Ho

Stuart B Rosenblum

Douglas Walsh Hobbs

Milana M Maletic

Lin Chu

XiaoXia Qian

Seong Heon Kim

James Francis Dropinski

Kurt William Saionz

Petr Vachal

James M Apgar

Gopinadhan N Anilkumar

Hong Li

Fengqi Zhang

Yuefei Shao

Vincent Colandrea

Debra L Ondeyka

Raphaelle Berger

Lisa Guise Zawacki

John J Baldwin

Tesfaye Biftu

Roland Ellwood Dolle

John A McCauley

Tao Guo

Wensheng Yu

Peter J Sinclair

Jinlong Jiang

Robert R Wilkening

Zhicai Wu

Sherman Tim Waddell

Zhijian Lu

Bandarpalle B Shankar

Danqing D Feng

Iyassu Sebhat

Suresh D Babu

Izzat Tiedje Raheem

Bing Li

Ping Chen

Christopher Francis Thompson

Michael K C Wong

Edward McDonald

Wanying Sun

Rajan Anand

Cameron James Smith

Tao Yu

Qingbei Zeng

Ramzi Farah Sweis

Yi-Heng Chen

Brian T Campbell

Sandra Lee Knowles

John J Acton, Iii

Thuy X H Le

Jacqueline D Hicks

Lan Wei

Paul J Zavodny

Kenneth J Leavitt

Dann LeRoy Parker, Jr

Deyou Sha

Feng Ye

Libo Xu

Yi Zang

Steven G Kultgen

Julianne A Hunt

Kake Zhao

Alan Whitehead

Joie Garfunkle

Ruiyan Liu

Chung-Her Jenh

Jingqi Duo

Anton Egbert Peter Adang

Peng Geng

Olga Ornoski

Yueheng Jiang

Florida Kallashi

Nicole Corine Renee Van Straten

Carolyn Dilanni Carroll

Cangmeng Yang

Xiaoxia Qian

Samantha E Adamson

Zhiquang Yang

Vincent J Colandrea

Michael KC Wong

John J Iii Acton

Changmeng Yang

Provided are methods for treating or preventing a fibrotic disease selected from systemic sclerosis, cystic fibrosis, non-alcoholic steatohepatitis, Peyronie's disease, or interstitial lung disease; the method comprising administering a therapeutically effective amount of a compound of Formula (I) (wherein R, R, R, R, and Rare as herein described) or a pharmaceutically acceptable salt thereof, to a patient in need of such therapy. 

Methods for using triazolo-pyrazinyl soluble guanylate cyclase activators in fibrotic disorders

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1 is as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject. 

Substituted quinolizine derivatives useful as HIV integrase inhibitors

The present invention relates to bicyclic himbacine derivatives of the formula   and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.

Preparation and use of 7a-heterocycle substituted-6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists

A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ('cGMP') and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.

Triazolo-pyrazinyl derivatives useful as soluble guanylate cyclase activators

A compound of Formula II or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate ('cGMP') and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula II, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of Formula II or a pharmaceutically acceptable salt thereof. 

Imidazo-pyrazine derivatives useful as soluble guanylate cyclase activators

The present invention relates to bicyclic himbacine derivatives of the formula  and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.

Preparation and use of 7a-amide substituted- 6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. 

Cyclic amine substituted heterocyclic CETP inhibitors

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, Ais a substituted phenyl group or indanyl group. Formula (I). 

Cyclic amine substituted oxazolidinone CETP inhibitor

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 

Biaryl oxyacetic acid compounds

Novel compounds of structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension. 

Cyclic azabenzimidazole derivatives useful as anti-diabetic agents

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates and esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Pyrazinyl substituted piperazine-piperidines with CXCR3 antagonist activity

Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity

The invention relates to bisaryl derivatives of the formula I,wherein (R,R) is selected from (H,H), O, (H,CH), (H,OH) and (H,CN); Ar is substituted phenyland A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.

Bisaryl derivatives having FSH modulatory activity

Growing community of inventors

Dayton, NJ, United States of America

Guizhen Dong