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US 2006/0189671 A1Published application
Compounds, compositions, and methods
AssigneesCytokinetics, Inc., SmithKline Beecham Corporation
InventorsXianping Qian, Gustave Bergnes, David Morgans, Steven Knight, Dashyant Dhanak
Life of this patent
Estimating the term…
Abstract
1,2,4-Tiazole-5-ones useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
Claims21
A compound selected from the group represented by Formula I:
- wherein:
- T and T′ are independently a covalent bond or optionally substituted lower alkylene;
- R1 is chosen from hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl;
- R2 and R2′ are independently chosen from hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl;
- or R2 and R2′ taken together form an optionally substituted 3-to 7-membered ring;
- R3 is chosen from hydrogen, optionally substituted alkyl-, optionally substituted aryl-, optionally substituted aralkyl-, optionally substituted heteroaryl-, optionally substituted heteroaralkyl-, —C(O)—R6, and —S(O)2—R6a;
- R4 is independently chosen from hydrogen, optionally substituted alkyl, carboxyalkyl, aminocarbonyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, optionally substituted heterocyclyl and optionally substituted heteroaryl;
- R5 is chosen from hydrogen, optionally substituted alkyl-, optionally substituted aryl-, optionally substituted aralkyl-, optionally substituted heteroaralkyl-, and optionally substituted heterocyclyl-;
- or R5 taken together with R3, and the nitrogen to which they are bound, form an optionally substituted 5- to 12-membered nitrogen-containing heterocycle, which optionally incorporates from one to two additional heteroatoms, selected from N, O, and S in the heterocycle ring;
- or R5 taken together with R2 form an optionally substituted 5- to 1 2-membered nitrogen-containing heterocycle, which optionally incorporates from one to two additional heteroatoms, selected from N, O, and S in the heterocycle ring;
- R6 is chosen from hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroaralkyl, R7O— and R11—NH—;
- R6a is chosen from hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroaralkyl, and R11—NH—;
- R7 is chosen from optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl;
- R11 is chosen from hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl;
- a pharmaceutically acceptable salt of a compound of Formula I;
- a pharmaceutically acceptable solvate of a compound of Formula I;
- or
- a pharmaceutically acceptable solvate of a pharmaceutically acceptable salt of a compound of Formula I,
- provided that R1 is not optionally substituted phenyl when R4 is optionally substituted phenyl.
16 more elements
Dependencies are inferred from the claim text.