Compositions and methods for treating cancer

a cancer and composition technology, applied in the field of compositions and methods for treating cancer, can solve the problems of almost entirely unsuccessful attempts to directly target this enzyme with reversible inhibitors

Inactive Publication Date: 2015-03-26
RGT UNIV OF CALIFORNIA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, past attempts to directly target this enzyme with reversible inhibitors have been almost entirely unsuccessful.

Method used

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  • Compositions and methods for treating cancer
  • Compositions and methods for treating cancer
  • Compositions and methods for treating cancer

Examples

Experimental program
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embodiment 1

[0364]2. The compound of embodiment 1, wherein R1 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0365]3. The compound of embodiment 1, wherein R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.

[0366]4. The compound of embodiment 1, wherein R1 is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

[0367]5. The compound of embodiment 1, wherein R1 is substituted or unsubstituted fused ring aryl or substituted or unsubstituted fused ring heteroaryl.

[0368]6. The compound of embodiment 1, wherein R1 is R3-substituted or unsubstituted aryl or R3-substituted or unsubstituted heteroaryl; wherein, R3 is independently hydrogen, oxo, halogen,...

embodiment 10

[0374]12. The compound of embodiment 10, wherein L1 is independently substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, substituted or unsubstituted heteroarylene, or substituted or unsubstituted spirocyclic linker; or L2 is independently substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, substituted or unsubstituted heteroarylene, or substituted or unsubstituted spirocyclic linker; or L3 is independently substituted or unsubstituted cycloalkylene, substituted or unsubstituted heterocycloalkylene, substituted or unsubstituted arylene, substituted or unsubstituted heteroarylene, or substituted or unsubstituted spirocyclic linker.

[0375]13. The compound of embodiment 10, wherein L1 is independently R2C-substituted or unsubstituted cycloalkylene, R2C-substituted or unsubstituted heterocycloalkylene, R2C-substituted or unsubstit...

embodiment 19

[0382]20. The method of embodiment 19, wherein said disease is cancer.

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Abstract

K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

Description

RELATED APPLICATIONS[0001]This application claims the benefit of U.S. Provisional Patent Application Nos. 61 / 622,507, filed Apr. 10, 2012; 61 / 728,145, filed Nov. 19, 2012; and 61 / 794,956, filed Mar. 15, 2013, which are all incorporated herein by reference in their entirety and for all purposes.REFERENCE TO A “SEQUENCE LISTING,” A TABLE, OR A COMPUTER PROGRAM LISTING APPENDIX SUBMITTED AS AN ASCII TEXT FILE[0002]The Sequence Listing written in file 84850-869921_ST25.TXT, created on Apr. 9, 2013, 28,573 bytes, machine format IBM-PC, MS-Windows operating system, is hereby incorporated by reference.BACKGROUND OF THE INVENTION[0003]K-Ras is the most frequently mutated oncogene in human cancer. However, past attempts to directly target this enzyme with reversible inhibitors have been almost entirely unsuccessful.[0004]Ras proteins are small guanine nucleotide-binding proteins that act as molecular switches by cycling between active GTP-bound and inactive GDP-bound conformations. Ras signa...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): C07D487/04C07D401/12C12N9/14C07D211/62C07D409/04C07D401/06C07D211/58
CPCC07D487/04C07D401/06C07D401/12C07D211/58C07D211/62C07D409/04C12N9/14C12Y306/05002A61K38/1709C07D207/14C07D231/40C07D295/185C07D295/26C07D401/04C07D405/12C07D413/12C07D417/12C07D471/10C07D487/10C07D495/04G01N2500/04A61P35/00A61P35/02A61P43/00C07C235/20C07C317/08C12Q1/6886C12Q2600/156C12Q2600/158
Inventor OSTREM, JONATHANPETERS, ULFSHOKAT, KEVAN M.
Owner RGT UNIV OF CALIFORNIA
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