Glycomed, Inc.

Agouron Pharmaceuticals, Inc.

Pfizer Corporation

Other

Mark Brian Anderson

John H Musser

Narasinga Rao

Yufeng Hong

Haitao Li

Ved Prakash Pathak

Eileen Valenzuela Tompkins

Lance Christopher Christie

Peng Cho Tang

Jun Feng

John Joseph Naleway

Vlad Edward Gregor

Daniel E Levy

Alexander Polinsky

Ranjan Jagath Rajapakse

Eric T Sun

Ping Chen

Quyen-Quyen Thuy Do

Chun Luo

Patrick O'Connor

Binh Nguyen

David Robert Luthin

Genevieve DeGuzman Paderes

Jing Rong Cui

James Faust

Haresh Vazir

Smita Gaur

Ya-Li Deng

Chen Chen Kan

Karen Lundgren

Stephen Margosiak

James Register

Jay Sarup

Anna Tempczyk Russell

Haresh N Vazir

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Non-peptide GNRH agents, methods and intermediates for their preparation

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Non-peptide GnRH agents, pharmaceutical compositions and methods for their use

Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated.

Non-peptide GnRH agents, Pharmaceutical compositions, and methods for their use

The present invention relates to the identification, isolation and purification of the catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7&angst; crystal structure of the hChk1 kinase domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer.

Catalytic domain of the human effector cell cycle checkpoint protein kinase materials and methods for identification of inhibitors thereof

Non-peptide GnRH agents

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X,, X,, Y, and are defined variables:

Triterpenoid acid derivatives are described that exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory process as well as applications for the diagnosis of disease.

Derivatives of triterpenoid acids and uses thereof.

Compounds that possess selectin binding activity are described that have a three-dimensionally stable configuration for sialic acid and fucose, or analogs, derivatives, or mimics of these groups, such that sialic acid and fucose or their mimics are separated by a linker that permits binding between those groups and the selecting, such compounds being represented by the following general structural formula I: ##STR1##

Sialyl lewis-x mimetics containing naphthyl backbones

Sialyl Lewis.sup.x mimetics containing phenyl backbones

Derivatives of triterpenoid acids and uses thereof

Compositions of sterodial glycosides are described wherein the glycoside is linked directly, or indirectly to a desired steroidal compound via a carbon, or similar stable linkage, and methods of using the compositions to treat patients by binding to and/or blocking cellular receptors for a variety of diseases including cancer, inflammation, and autoimmune diseases.

Steroidal C-glycosides

2-Chloromethyl-3-(tri-O-benzyl-.alpha.-L-C-fucopyranoside)-1-propene and methods of making the same are described. Methods of combining this substituted fucopyranose with triterpenoid acid also are described.

Substituted fucopyranosides

Methods of treating diseases using triterpenoid acid derivatives

This invention relates generally to the field of medicinal chemistry, and more specifically to derivatives of a subclass of triterpenoid acids that have multi-medicament properties, that is derivatives of the lupane, betulinic acid, formulations containing such, and their use to prevent or treat certain diseases, and preferably to derivatives or analogues of betulinic acid, that have the following structural formula (1): ##STR1## wherein: Y is OR.sup.1, NR.sup.1.sub.2, O.sup.- M.sup.1 ;

Lupane triterpenoid derivatives

Triterpenoid acid derivatives have been found to have structures similar to natural ligands to the extent that these derivatives bind to natural selectin receptors including endothelial leukocyte adhesion molecule-1 (ELAM-1) and leukocyte/endothelial cell adhesion molecule-1 (LECAM-1). The molecules can be administered to the patients by themselves or in pharmaceutical formulations in order to alleviate inflammation and/or treat other abnormalities associated with the excessive binding of leukocytes to endothelial receptors.

Derivatives of triterpenoid acids as inhibitors of cell-adhesion

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Orinda, CA, United States of America

Mark Brian Anderson