Qlt Inc.

Dermira (canada), Inc.

Kinetek Pharmaceuticals, Inc.

Valocor Therapeutics, Inc.

Dirmira (canada), Inc.

Dermira, Inc.

Shisen Wang

Zaihui Zhang

Timothy Scott Daynard

Gregory B Chopiuk

Serguei Sviridov

Jun Yan

Mikhail A Chafeev

Xinyao Du

Jianxin Chen

Jasbinder Sanghera

Danny Leung

Penelope C Costello

Serguei V Sviridov

Timothy S Daynard

Greg B Chopiuk

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

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. 

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.

An assay system is provided for detecting the enzymatic activity of a phosphorylation enzyme. The enzyme may be a phosphatase or protein kinase. The substrate for the enzyme is immobilized on a solid support via covalent or non-covalent binding through a signal enhancing polymer. The immobilized substrate provides an enhanced signal to background ratio when compared to a substrate in solution. The methods are easily adapted to high throughput screening systems.

Assay for detecting the enzymatic activity of a phosphorylation enzyme using enhanced signal generation

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 substituted pyrazoles and pyrazolines.

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Coquitlam, Canada

Shisen Wang