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US 2011/0301192 A1Published application
Inhibitors of Cyclin Kinase Inhibitor p21
AssigneeThe Regents of the University of California
InventorsRobert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
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Abstract
The present invention provides compounds that inhibit cyclin kinase inhibitor p21, such as compounds of formula I. The present invention also provides compositions including compounds of Formula I and a pharmaceutically acceptable excipient. In addition, the present invention provides methods of inhibiting cyclin kinase inhibitor p21 and of treating cancer.
Claims18
A compound of formula I:
- wherein
- R1 is selected from the group consisting of C1-6 alkyl, C0-6 alkyl-NR8R9, C0-6 alkyl-cycloalkyl, C0-6 alkyl-heterocycloalkyl, C0-6 alkyl-aryl and C0-6 alkyl-heteroaryl, each optionally substituted with from 1-4 R1a groups;
- each R1a is independently selected from the group consisting of H, halogen, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 haloalkoxy, C1-6 hydroxyalkyl, —OH, —C0-6 alkyl-NR8R9, —SR8, —C(O)R8, —C0-6 alkyl-C(O)OR8, —C(O)NR8R9, —N(R8)C(O)R9, —N(R8)C(O)OR9, —N(R8)C(O)NR8R9, —OP(O)(OR8)2, —S(O)2OR8, —S(O)2NR8R9, —CN, C0-6 alkyl-cycloalkyl, heterocycloalkyl, C0-6 alkyl-aryl and heteroaryl, alternatively, two R1a groups are joined to form ═O;
- R2 is selected from the group consisting of C0-6 alkyl-aryl, C2-6 alkenyl-aryl, C0-6 alkyl-heteroaryl, and —N(R8)-aryl, each optionally substituted with 1-4 members each independently selected from the group consisting of R1a, —OR10, —SR10 and —NR8R10;
- R3 is selected from the group consisting of —C(O)—C1-6 alkyl, —C(O)—C1-6 hydroxyalkyl, —C(O)—C1-6 alkylamine, —C(O)—heterocycloalkyl, —C(O)—NR3aR3b, —C(O)OR3a, —S(O)2R3a and an amino acid;
- each of R3a and R3b are independently selected from the group consisting of H, C1-6 alkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl each optionally substituted with from 1-4 R8 groups;
- R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H and C1-6 alkyl;
- R10 is selected from the group consisting of cycloalkyl, heterocycloalkyl, aryl and heteroaryl, each optionally substituted with from 1-4 R1a groups;
- subscript m is an integer from 0-2;
- and
- salts, hydrates, prodrugs, and isomers thereof.
8 more elements
Dependencies are inferred from the claim text.