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US 2003/0225112 A1Published application
Inhibitors to tubulin polymerization
AssigneeRigel Pharmaceuticals, Inc.
InventorsDane Goff, Mark K. Bennett, Susan Demo
Life of this patent
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Abstract
The invention relates to the inhibition of tubulin polymerization. The invention provides compounds and methods for inhibiting tubulin polymerization. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Claims25
A compound of the general formula (1)
- 218
- or a pharmaceutically acceptable salt thereof, wherein
- R1 and R2 are independently selected from the group consisting of —H, halo, C1-C6 alkyl, halogenated-C1-C6-alkyl, and —OR4,
- R4 is selected from the group consisting of C1-C6 alkyl, optionally substituted aryl, and optionally substituted aryl-C1-C6-alkyl,
- or wherein R1 and R2 together with the carbon to which they are attached form a heterocyclyl;
- L is selected from the group consisting of a covalent bond, C1-C6 alkyl, —C(O)—, and —(CH2)0-3C(H)(R5)—,
- R5 is selected from the group consisting of C1-C6 alkyl, aryl, aryl-C1-C6-alkyl, —R6—S—R7, —R6—C(O)OR7, and —R6—O—R7, wherein R6 and R7 are C1-C6 alkyl;
- and
- R3 is selected from the group consisting of H, C1-C6 alkyl, hydroxy C1-C6 alkyl, optionally substituted C3-C8-cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryl alkyl, —OR8, —C(O)OR9, —N(R10)R11,
- R8 is C1-C6 alkyl or hydroxy C1-C6 alkyl, and
- R9, R10, and R11 are C1-C6 alkyl.
8 more elements
Dependencies are inferred from the claim text.