Dermira (canada), Inc.

Qlt Inc.

Valocor Therapeutics, Inc.

Kinetek Pharmaceuticals, Inc.

Phoenix Molecular Designs

Phoenix Molecular Design

Dirmira (canada), Inc.

Dermira, Inc.

Timothy Scott Daynard

Zaihui Zhang

Shisen Wang

Gregory B Chopiuk

Serguei Sviridov

Mikhail A Chafeev

Xinyao Du

Jianxin Chen

Jun Yan

Geoffrey C Winters

David W C Hunt

Subhash Annedi

Sandra Dunn

Jaipal Reddy Nagireddy

John H Van Drie

My-my Huynh

Aarthi Jayanthan

Gabriel Bela Kalmar

David W Hunt

David WC Hunt

Described herein are carboxamide derivatives of Formula (II) that are useful as inhibitors of p90 ribosomal S6 kinase (RSK), pharmaceutical compositions comprising the derivatives, and methods of using the derivatives in treating diseases or conditions associated with RSK activity: wherein R, R, R, R, R, and n are defined in the specification.

Substituted tetrahydropyrido[3',2&#x2032;:4,5]pyrrolo[1,2-&#x3b1;]pyrazine-2-carboxamides as RSK inhibitors

This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration.

TOFA analogs useful in treating dermatological disorders or conditions

Substituted tetrahydropyrido[3',2&#x2032;:4,5]pyrrolo[1,2-a]pyrazine-2-carboxamides as RSK inhibitors

Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R, R, Rand Rare described herein.

Pyrazolylbenzothiazole derivatives and their use as therapeutic agents

This invention is directed to analogs of 5-(tetradecyloxy)-2-furancarboxylic acid (TOFA) and their use in the treatment of dermatological disorders or conditions characterized by sebaceous gland hyperactivity, such as acne and oily skin, and other dermatological disorders and conditions. This invention is also directed to pharmaceutical compositions comprising analogs of TOFA and a pharmaceutically acceptable excipient for dermatological or oral administration. Formula (I) 

Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.

Hydrazonopyrazole derivatives and their use as therapeutics

Pharmaceutical compositions and compounds are provided. The compounds of the invention have use as therapeutic agents, e.g., they demonstrate anti-proliferative, anti-inflammatory, anti-angiogenic, anti-migration activities. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of, e.g., anti-inflammatory, renal, and hyperproliferative disorders. The compounds of the invention are pyrazolylbenzothiazole derivatives of the following formula (1) wherein X, R, R, Rand Rare described herein.

Pharmaceutical pyrazolybenzothiazole compositions of formula (1) are provided. The compositions may be pharmaceutically acceptable salts. R, Rand Rat each occurrence are independently selected from amino, aminosulfinyl, aminosulfonyl, aryl, azido, halogen, heteroalkyl, heteroaryl, hydrazinyl, hydrocarbyl, hydrogen, hydroxyl, nitro, nitroso, phosphate, phosphinate, phosphonate, phosphonium, phosphorothioate, phosphoryl, sulfamoyl, sulfate, sulfinic acid, sulfonamido, sulfonate, sulfonic acid, sulfonyl, sulfoxido, thiol, thioureido, and ureido, and Ris selected from hydrogen, heteroalkyl, heteroaryl, and hydrocarbyl. 

Methods of using thiazolidine derivatives of formula (I) to treat cancer, inflammation, or other disorders related to the activities of protein phosphatases PTPN12 or PTPN2 in a mammal are disclosed. Pharmaceutical compositions containing such derivatives are disclosed 

Methods of using thiazolidine derivatives to treat cancer or inflammation

This invention is directed to methods of using compounds having the structure: and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R, R, Rand Ris independently selected from hydrogen, R, R, and R; Ris selected from alkyl, heteroalkyl, aryl and heteroaryl; Ris selected from (R)-alkylene, (R)-heteroalkylene, (R)-arylene and (R)-heteroarylene; Ris selected from (R)-alkylene, (R)-heteroalkylene, (R)-arylene, and (R)-heteroarylene; and n is selected from 0, 1, 2, 3, 4 and 5, where Rand Rmay together form a heterocyclic structure including the nitrogen to which they are both attached, and Rand Rmay together form a heterocyclic structure including the nitrogen to which they are both attached; and each of Land Lis independently selected from -A1-A2-A3- where each of A1, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene. These compounds are useful in treating hyperproliferative disorders and inducing apoptosis.

Antiproliferative 1,2,3-thiadiazole compounds

Pyrazole compounds

Pharmaceutical compositions and compounds are provided. The compounds of the invention have anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, formulations of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical formulations are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are 1,2,3-thiadiazoles having the structure:and including stereoisomers, solvates, and pharmaceutically acceptable salts thereof, wherein each of R, R2 , Rand Ris independently selected from hydrogen, RR, and R, Ris selected from alkyl, heteroalkyl, aryl and heteroaryl; Ris selected from (R)-alkylene, (R)-heteroalkylene, (R)-arylene and (R)-heteroarylene; Ris selected from (R)-alkylene, (R)-heteroalkylene, (R)-arylene, and (R)-heteroarylene; and n is selected from 0, 1, 2, 3, 4 and 5, where Rand Rmay together form a heterocyclic structure including the nitrogen to which they are both attached, and Rand Rmay together form a heterocyclic structure including the nitrogen to which they are both attached; and each of Land Lis independently selected from -A1-A2-A3- where each of Al, A2, and A3 is independently selected from a direct bond, alkylene, heteroalkylene, arylene and heteroarylene.

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Vancouver, Canada

Timothy Scott Daynard