Schering Corporation

Pharmacopeia Drug Discovery, Inc.

Merck Sharp + Dohme Corp.

Pharmacopeia Inc.

Pharacopeia Drug Discovery, Inc.

Douglas Walsh Hobbs

Stuart B Rosenblum

Brian F McGuinness

Joseph A Kozlowski

Tao Guo

Andrew William Stamford

Neng-Yang Shih

Jared N Cumming

Ying Huang

Corey Strickland

Ulrich Iserloh

Suresh D Babu

Yusheng Wu

Seong Heon Kim

Viyyoor Moopil Girijavallabhan

Ronald J Doll

Samuel Chackalamannil

Timothy J Guzi

Lawrence Wayne Dillard

Alan K Mallams

Michael P Dwyer

Kamil Paruch

Vincent Stewart Madison

Yan Xia

Thierry Olivier Fischmann

Michael K C Wong

Wensheng Yu

Vidyadhar Madhav Paradkar

Tin-Yau Chan

Johannes H Voigt

John W Clader

Hubert B Josien

Elizabeth M Smith

Bandarpalle B Shankar

Theodros Asberom

John J Baldwin

Guoqing Li

Dmitri A Pissarnitski

De-Yi Yang

Gopinadhan N Anilkumar

Yuefei Shao

Qingbei Zeng

Thuy X H Le

Carmen S Alvarez

Kartik M Keertikar

Kurt William Saionz

Vinh D Tran

Ray Anthony James

Haengsoon Park

Jocelyn Rivera

Zhen Min He

Huizhong Gu

Jeffrey F Lowrie

Guizhen Dong

Rachael Catherine Hunter

Johannes H Voight

Lisa Guise Zawacki

Jeffrey H Lowrie

Jianping Pan

Paul J Zavodny

Youheng Shu

Tin Yau Chan

Chung-Her Jenh

Yueheng Jiang

Zhenmin He

Paul Kirschmeier

Rajat Bannerji

Cangmeng Yang

Carolyn Dilanni Carroll

Dimitri A Pissarntiski

Vidyadhar M Hobbs

Michael KC Wong

Rachael C Hunter

Jocelyn D Rivera

Brian F Mc Guinness

Brian F Mcguiness

Changmeng Yang

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein  and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &#x3b2;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Cyclic amide BACE-1 inhibitors having a benzamide substituent

In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An example pyrazolo[1,5-a]pyrimidine compound useful in the present invention is shown below: 

Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors

Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein Ris  R is &#x2014;C(O)&#x2014;N(R)(R) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a &#x3b2;-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.

Cyclic amine BACE-1 inhibitors having a benzamide substituent

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: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. 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.

Heterocyclic substituted piperazines with CXCR3 antagonist activity

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: or a pharmaceutically acceptable salt, solvate or ester 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.

Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity

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: or a pharmaceutically acceptable salt, solvate or ester 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, zenograft 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.

Heterocyclic substituted piperazine compounds with CXCR3 antagonist activity

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

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors

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: or a pharmaceutically acceptable salt, solvate or ester 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, zenograft 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.

Heterocyclic substituted pyridine or phenyl compounds with CXCR3 antagonist activity

Pyridyl and phenyl substituted piperazine-piperidines with CXCR3 antagonist activity

Piperazine-piperidines with CXCR3 antagonist activity

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Yardley, PA, United States of America

Douglas Walsh Hobbs