Invention Grant
- Patent Title: Pyrimidine derivatives as kinase modulators and method of use
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Application No.: US11722719Application Date: 2005-12-28
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Publication No.: US08211929B2Publication Date: 2012-07-03
- Inventor: Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
- Applicant: Jeff Chen , Lisa Esther Dalrymple Meyr , Sergey Epshteyn , Timothy Patrick Forsyth , Tai Phat Huynh , Mohamed Abdulkader Ibrahim , James W. Leahy , Gary Lee Lewis , Grace Mann , Larry W. Mann , Robin Tammie Noguchi , Brian Hugh Ridgway , Joan Cruz Sangalang , Kevin Luke Schnepp , Xian Shi , Craig Stacy Takeuchi , Matthew Alan Williams , John Nuss , Atwood K. Cheung
- Applicant Address: US CA South San Francisco
- Assignee: Exelixis, Inc.
- Current Assignee: Exelixis, Inc.
- Current Assignee Address: US CA South San Francisco
- Agency: McDonnell Boehnen Hulbert & Berghoff LLP
- International Application: PCT/US2005/047402 WO 20051228
- International Announcement: WO2006/074057 WO 20060713
- Main IPC: A01N43/56
- IPC: A01N43/56 ; A61K31/415 ; C07D239/02 ; C07D231/00

Abstract:
The invention provides compounds and methods for inhibition of kinases, more specifically IGF 1 R kinases. The invention also provides compounds and methods for inhibition of wildtype Abl. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, or prodrug thereof, wherein, V is NR1R1a, or O—R1, wherein X is H, halo, C1-C6 alkyl, NO2, mono-, di-, or tri-halo substituted methyl, NR13R,14. C(O)O—C1-C6 alkyl, or N(R13)—C(O)—C1-C6 alkyl; Y is H, halo, OH, C1-C6 alkyl, C0-C6alkyl-NR,15R16, NR15R,6, C1-C6 alkoxy, —N(R13)—(CH2)n-NR15R16, —C(O)O—C1-C6 alkyl, —O—(CH2)n—NR15R16, —C(O)—C1-C6 alkyl, —C0-C6-alkyl-R21, —O—R21, —C(O)—R21, —O—(CH2)n—R21, —C(O)—NR13R14, —C(O)—N(R13)-aryl, —C(O)—N(R13)(CH2)n—NR15R16, —C(O)—N(R13)—(CH2)n-aryl —C(O)—N(R13)—(CH2)n-heterocyclyl; or X and Y together with the atoms to which they are attached form a 4-7 membered heterocyclyl or heteroaryl group containing one or two heteroatoms independently selected from O, N, and S. Z is H, NR2R3, —S—R2a, or —O—R2a
Public/Granted literature
- US20080249079A1 Pyrimidine Derivatives As Kinase Modulators and Method of Use Public/Granted day:2008-10-09
Information query
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