Irm LLC

Dermira (canada), Inc.

Qlt Inc.

Valocor Therapeutics, Inc.

Novartis Ag

Dirmira (canada), Inc.

Dermira, Inc.

Gregory B Chopiuk

Zaihui Zhang

Timothy Scott Daynard

Shisen Wang

Serguei Sviridov

Xinyao Du

Jianxin Chen

Jun Yan

Pamela Ann Albaugh

Mikhail A Chafeev

Yi Fan

Pingda Ren

Chengzhi Zhang

Paul A Renhowe

Daniel J Poon

Valentina Molteni

Martin Sendzik

Shifeng Pan

Qiong Zhang

Shenlin Huang

Xing Wang

Qiang Ding

Guobao Zhang

Yongping Xie

Brenton Todd Flatt

Jon Christopher Loren

Zuosheng Liu

Paul Vincent Rucker

Jeffrey M Smith

Ha-Soon Choi

Xia Wang

Zhicheng Wang

Serguei V Sviridov

Timothy S Daynard

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

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TRK kinase activity.

Compounds and compositions as TRK inhibitors

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.

Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors

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.

The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases.

Compounds and compositions as protein kinase inhibitors

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. 

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

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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San Diego, CA, United States of America

Gregory B Chopiuk