Schering Corporation

Incara Research Laboratories

Pharmacopeia Inc.

Advanced Medicine, Inc.

Tin Yau Chan

Michael J Sofia

Ramesh Kakarla

Rakesh K Jain

Dashan Liu

Nicole T Hatzenbuhler

Nigel Mark Allanson

Rui Liang

Domingos J Silva

Viyyoor Moopil Girijavallabhan

Ronald J Doll

Anandan Palani

Lawrence Wayne Dillard

Timothy J Guzi

John W Clader

Michael P Dwyer

Hubert B Josien

Kamil Paruch

Vincent Stewart Madison

Thierry Olivier Fischmann

Carmen S Alvarez

Vinh D Tran

Ray Anthony James

Haengsoon Park

Zhen Min He

Alan K Mallams

Vidyadhar Madhav Paradkar

Douglas Walsh Hobbs

Kartik M Keertikar

Chad E Knutson

Jocelyn Rivera

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

Trisubstituted 4-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors

The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

MCH antagonists and their use in the treatment of obesity

A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula

Combinatorial library of moenomycin analogs and methods of producing same

A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula ##STR1## wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.

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Edison, NJ, United States of America

Tin Yau Chan