Ligand Pharmaceuticals, Inc.

Conforma Therapeutics Corporation

Chugai Seiyaku Kabushiki Kaisha

Nubridge Biosciences

Receptos, Inc.

Lin Zhang

Marcus F Boehm

David Mark Wallace

Mi Chen

Gary David Lopaschuk

Jason Roland Dyck

Alex M Nadzan

Thomas Arrhenius

Yu Ge

Alex Michael Nadzan

Yujin Huang

Junhua Fan

Srinivas Rao Kasibhatla

Jie Fei Cheng

Marco Antonio Biamonte

Kevin Hong

Richard Julius Penuliar

Luc J Farmer

Adam Richard Yeager

Junko Tamiya

Richard Alan Heyman

Lawrence C Fritz

Ranjan Mukherjee

Siead Zegar

Chan Kou Hwang

Sovouthy Tith

Marcos Steinberg

Beth Ann Badea

Jiandong Shi

Youssef L Bennani

Jean-Yves Le Brazidec

Philip Turnbull

Masayuki Haramura

Steve Joel Brown

Charles Stanford Harmon

Sean Konrad McHugh

Kevan Grant

Stacie Canan-Koch

Laura J Dardashti

Tom Fowler

Yang Tran

Deepak S Lala

Hanae Benelkebir

Raffaele Pasceri

Jie Fei Chang

Maria Ieva

Francis J Burrows

Compounds are provided having the structure of the following Formula I: where R, R, R, Rand Rare as defined herein. Pharmaceutical compositions comprising such compounds, as well as methods related to their manufacture and use, are also provided.

CXCR3 receptor agonists

A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof that is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.

Pyridine derivatives as CFTR modulators

A compound having the structure of Formula II, or a stereoisomer, tautomer, or a pharmaceutically acceptable salt thereof:  The compound is useful as CFTR modulator. Further, a method of using the compound and pharmaceutical composition comprising the compound are provided for treating diseases in lungs, pancreas, gastrointestinal system, sinuses, reproductive system, and the sweat glands.

Pyrimidine derivatives as CFTR modulators

Isothiazole derivatives as CFTR modulators

The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase. 

Malonyl-CoA decarboxylase inhibitors useful as metabolic modulators

Efficient chemical processes for preparing high yields, purities, and different polymorphic forms of 17-allyl amino geldanamycin (17-AAG) and other ansamycins are described and claimed.

Process for preparing 17-allyl amino geldanamycin (17-aag) and other ansamycins

The present invention relates to novel compounds (I), their prodrugs, and the pharmaceutically acceptable salts as well as pharmaceutical compositions containing such compounds useful in treating certain metabolic diseases and diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD). In particular, the invention relates to compounds and compositions and the methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the inhibition of malonyl-coenzyme A decarboxylase.

Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and bioavailability. Some of the derivatives described are dimers. These and others described can include one or more solubilizing groups that have expected merit in rendering the overall compounds useful as drugs and prodrugs.

Ansamycins having improved pharmacological and biological properties

The present invention relates to methods for the prophylaxis, management and treatment of certain diseases modulated by the inhibition of the enzyme malonyl-coenzyme A decarboxylase (malonyl-CoA decarboxylase, MCD) by the administration of a composition containing as an active ingredient a compound according to Formula I. In particular, the invention relates to methods for the prophylaxis, management and treatment of cardiovascular diseases, diabetes, acidosis, cancers, and obesity through the administration of a compound which inhibits malonyl-coenzyme A decarboxylase activity. The present invention also includes within its scope the novel process for the preparation of certain compounds 

Method for preparing imidazole derivatives

Novel purine compounds of Formula I. and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O); and O is selected from alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl, and heterocyclic, all optionally substituted, are described, as are pharmaceutical compositions comprising the same, complexes comprising the same, e.g., HSP90 complexes, and methods of using the same.

Purine analogs having HSP90-inhibiting activity

2-Aminopurine analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.

2-aminopurine analogs having HSP90-inhibiting activity

Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.

Dimer-selective RXR modulators and methods for their use

Novel trienoic retinoid compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

Trienoic retinoid compounds and methods

Trienoic compounds having activity as antagonists for retinoic acid receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.

Retinoic acid receptor antagonist compounds and methods

Novel trienoic compounds having activity for retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their use.

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San Diego, CA, United States of America

Lin Zhang