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Macrocyclic kinase inhibitors
专利权人:
OSI Pharmaceuticals; LLC
发明人:
CREW, Andrew,DONG, Hanqing,FERRARO, Caterina,SHERMAN, Dan,SIU, Kam
申请号:
ES11794899
公开号:
ES2645508T3
申请日:
2011.11.29
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula I: in which: X is N or CH; A1 is phenylene optionally substituted with halo, - C1-3 aliphatic, or - C1-3 aliphatic, any of which is optionally substituted with one or more halo or -OCF3; A3 is a 5-membered heteroaryl ring selected from pyrazolyl, triazolyl and pyrrolyl; L2 is -O- or a link; L3 is C2-4 aliphatic optionally substituted with one or more C1-6 aliphatic or C3-6 carbocyclic; L4 is -CH2- or -CH2CH2-; 15 Q1 to Q3 are independently N or CR2; Q4 is CR3; Ra and Rb are independently H or C1-3 aliphatic; R1 is selected from H, halo, -CN, C1-3 aliphatic (optionally substituted with 1 to 3 halo), C3-6 carbocyclic, - NO2, -N (C0-3 aliphatic) 2, -SO0-2 (C1 aliphatic -3), -C (O) O (C1-3 aliphatic), -C (O) C0-3 aliphatic, or -C (O) N (C0-3 aliphatic) 2; Each R2 is independently H, halo, C1-3aliphatic, or C1-3aliphatic; wherein R2 and R3 are optionally taken together to define an optionally substituted cyclic group 5-6 condensed in Q1 and Q4 to Ring A2 and containing one or more heteroatoms; R3 is selected from halo, -OR12, R12, cyclic group 3-6, -NR10R11, -NR10SO2R13, -OSO2 (R13), -SO2 (R13), - SO2CF3, -SO2NR10R11, -C (O) NR10R11, -C (O) R12, -C (O) O (R12), -C (O) (R12) -O (R12), -C (O) CF3, -C (O) (cyclic group 3- 25 6), or -C (O) O (cyclic group 3-6); wherein any of the above is optionally substituted with one or more, halo, -OH, -CF3, -NO2, -CN, -aliphatic C1-6, -Oaliphatic C1-6, -C>; = N-OH, - C>; = N-OR12, -NR10R11, -SR13, -SOR13, - SO2R13, -CO2R12, -CONR10R11, -SO2NR10R11, -NHCOR12, -NR10CONR10R11, -NR10SO2R13, or -P (O) (OR10) 2; R4 is OH, C1-4 aliphatic, or C1-3 aliphatic; R10, R11, R12, and R13 are independently H, aliphatic C1-6, or carbocyclic C3-6, 30 or R10 and R11 attached to the same atom can be taken together with the atoms to which they are attached to form a ring containing one or more heteroatoms, or a pharmaceutically acceptable salt thereofUn compuesto de Fórmula I: en la que: X es N o CH; A1 es fenileno opcionalmente su
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