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2,4-Pyrimidinodiamine compounds and their prodrugs and their uses
专利权人:
Rigel Pharmaceuticals; Inc.
发明人:
YU, Jiaxin,CLOUGH, Jeffrey,SINGH, Rajinder
申请号:
ES11730116
公开号:
ES2562419T3
申请日:
2011.04.13
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of the formula: ** Formula ** or a pharmaceutically acceptable salt thereof, in which: Y is oxygen or sulfur; Z1, Z2 and Z3 are independently selected from CH and N; R1 is hydrogen, C1-C6 alkyl or R8; R2 and R3 are independently selected from hydrogen and methyl; R4 is hydrogen, halogen, cyano, nitro, C1-C6 alkyl or halo (C1-C6 alkyl); R5 is heterocycloalkyl optionally substituted with 1, 2, 3, 4, 5, 6, 7 or 8 R6 groups, wherein the heterocycloalkyl is morpholinyl, thiomorpholinyl, piperidinyl, pyrrolidinyl, oxazolidinyl, azetidinyl, tetrahydropyranyl, oxazepanyl or 2-oxazepanyl 5- azabicyclo [2.2.1] heptanyl, -N (R7) 2, C1-C6 alkyl, aryl optionally substituted with 1, 2, 3 or 4 R6 groups, heteroaryl optionally substituted with 1, 2, 3 or 4 R6 groups or cycloalkyl optionally substituted with 1, 2, 3, 4, 5, 6, 7 or 8 R6 groups, in which each R6 is independently selected from deuterium, halogen, cyano, nitro, hydroxy, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo (C1-C6 alkyl), C1-C6 alkoxy, halo (C1-C6 alkoxy), amino, di (C1-C6 alkyl) amino, hydroxy (C1- alkyl C6), (C1-C6 alkoxy) C1-C6 alkyl, amino (C1-C6 alkyl), ((C1-C6 alkyl) amino) (C1-C6 alkyl), (di (C1-C6 alkyl) amino) (alkyl C1-C6), -C (O) OH, -C (O) NH2, C3-C8 cycloalkyl, aryl, heteroaryl and heterocycloalkyl or two g R6 ruptures form a spiro-condensed C3-C6 cycloalkyl, a condensed spiro30 heterocycloalkyl, oxo,>; = CH2 or>; = CH (C1-C6 alkyl); and each R7 is independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo (C1-C6 alkyl), hydroxy (C1-C6 alkyl), (C1-C6 alkoxy) C1-C6 alkyl , aryl, heteroaryl, heterocycloalkyl, (aryl) C1-C6 alkyl, (heteroaryl) C1-C6 alkyl and (heterocycloalkyl) C1-C6 alkyl; and R8 is selected from - (CR11R11) kOP (O) (OR12) 2, ** Formula ** in which each R11 is independently selected from hydrogen, C1-C6 alkyl, aryl, and (aryl) C1-C6 alkyl, in that each alkyl or aryl is optionally substituted with halogen, hydroxy, C1-C6 alkoxy, aryloxy, or (C
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