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US 7,977,345 B2Granted
c-MET modulators and method of use
AssigneeExelixis, Inc.
InventorsLynne Canne Bannen, Diva Sze-Ming Chan, Lisa Esther Dalrymple, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrisson B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Yong Wang, Wie Xu
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Abstract
A compound for modulating kinase activity according to Formula I, or a pharmaceutically acceptable salt thereof, Wherein J1, J2, J3, R2, J4, Z, Ar and R3 are as defined in the specification, compositions thereof, and methods of use thereof.
Claims3
A compound of formula IVc:
- wherein:
- J1 is ═CH—;
- J2 is ═C(R1)—;
- J3 is ═N—;
- J4 is ═N—;
- J5 is C—H or C—F;
- Z is O;
- R1 is independently selected from halogen, trihalomethyl, —CN, —NO2, —OR20, —N(R20)R20, —S(O)0-2R20, —SO2N(R20)R20, —CO2R20, —C(O)N(R20)R20, —N(R20)SO2R20, —N(R20)C(O)R20, —NHCO2R20, —C(O)R20, optionally substituted C1-6alkyl, optionally substituted aryl, optionally substituted aryl C1-6alkyl optionally substituted heterocyclyl, and optionally substituted heterocyclyl C1-6alkyl;
- R2 is H;
- each R3a is independently selected from —H, halogen, trihalomethyl, —CN, —NO2, —OR20, —N(R20)R20, —S(O)0-2R20, —SO2N(R20)R20, —CO2R20, —C(O)N(R20)R20, —N(R20)SO2R20, —N(R20)C(O)R20, —NHCO2R20, —C(O)R20, optionally substituted C1-6alkyl, and optionally substituted heterocyclyl;
- each R20 is independently —H, optionally substituted C1-6alkyl, optionally substituted aryl, optionally substituted aryl C1-6alkyl, optionally substituted heterocyclyl, and optionally substituted heterocyclyl C1-6alkyl;
- or two of R20, when taken together with a common nitrogen to which they are attached, can form an optionally substituted five- to seven-membered heterocyclyl, said optionally substituted five- to seven-membered heterocyclyl optionally containing at least one additional annular heteroatom selected from N, O, S, and P;
- and
- each R70 is independently selected from —H, halogen, trihalomethyl, —CN, —NO2, —OR20, —N(R20)R20, —S(O)0-2R20, —SO2N(R20)R20, —CO2R20, —C(O)N(R20)R20, —N(R20)SO2R20, —N(R20)C(O)R20, —NHCO2R20, —C(O)R20, optionally substituted C1-6alkyl, optionally substituted aryl, optionally substituted aryl C1-6alkyl, optionally substituted heterocyclyl, and optionally substituted heterocyclyl C1-6alkyl.
11 more elements
A compound selected from:
- Entry
- Name
- Structure
- 2
- N-(4-fluorophenyl)-N′-[3-fluoro-4-(7H- pyrrolo[2,3-d]pyrimidin-4- yloxy)phenyl]cyclopropane-1,1- dicarboxamide
- 12
- N-{3-fluoro-4-[(6-{[(2-morpholin-4- ylethyl)amino]carbonyl}-7H-pyrrolo[2,3- d]pyrimidin-4-yl)oxy]phenyl}-N′-(4- fluorophenyl)cyclopropane-1,1- dicarboxamide
4 more elements
Dependencies are inferred from the claim text.