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JAK2 inhibitors and their use for the treatment of myeloproliferative diseases and cancer
专利权人:
BRISTOL-MYERS SQUIBB COMPANY
发明人:
PURANDARE, ASHOK V.,GREBINSKI, JAMES W.,HART, AMY,INGHRIM, JENNIFER,SCHROEDER, GRETCHEN,WAN, HONGHE
申请号:
ES10757878
公开号:
ES2505270T3
申请日:
2010.09.02
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of the formula or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein X is C1-4 alkyl; Y is C1-4 alkyl; R is any of which is optionally condensed with a 5 or 6 membered carbocycle or heterocycle, said heterocycle having a heteroatom selected from NR3 or S, said condensed carbocycle or heterocycle optionally substituted with 0-3 R1, R1 is H, halo , CN, C1-6 alkyl substituted with 0-3 Rc, CF3, CONRaRa, NRaRa, COORb, SO2-C1-4 alkyl, C (O) Rd, cycloalkyl substituted with 0-3 Re, furanyl, tetrahydropyranyl or pyridinyl; R2 is H, C1-6 alkyl substituted with 0-3 Rc, C (O) O-C1-4 alkyl, SO2-C1-4 alkyl, cycloalkyl substituted with 0-3 Re, tetrahydropyranyl or R2 is absent; R3 is H, C (O) O-C1-4alkyl, or R3 is absent; Ra is H, C1-6 alkyl substituted with 0-3 Re, C3-6 cycloalkyl substituted with 0-3 Re, tetrahydropyranyl or dioxotetrahydrothiophenyl; Rb is H or C1-6 alkyl; Rc is H, halo, CN, OH, O-C1-4 alkyl, O-C1-4 alkyl-O-C1-4 alkyl, NH2, N (C1-4 alkyl) 2, C (O) N (C1 alkyl -4) 2, SO2-C1-4 alkyl, or morpholinyl or piperazinyl any of which is optionally substituted with 0-1 C1-4 alkyl; Rd is C1-6 alkyl or azeridinyl, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, dioxidothiomorpholinyl or tetrahydropyranyl, any of which is substituted with 0-2 Re; and Re is H, halo, CN, C1-4 alkyl, OH, O-C1-4 alkyl, SO2-C1-4 alkyl, NHC (O) -C1-4 alkyl, morpholinyl, OC (O) -C1 alkyl 4, C (O) N (C1-4 alkyl) 2 or O-C1-4 alkyl-O-C1-4 alkyl.Un compuesto de fórmula o un estereoisómero, tautómero o sal farmacéuticamente aceptable del mismo, en la que X es alquilo C1-4; Y es alquilo C1-4; R es cualquiera de los cuales está opcionalmente condensado con un carbociclo o heterociclo de 5 o 6 miembros, teniendo dicho heterociclo un heteroátomo seleccionado entre NR3 o S, estando dicho carbociclo o heterociclo condensado opcionalmente sustituido con 0-3 R1, R1 es H, halo, CN, alquilo C1-6 sustituido con 0-3 Rc, CF3, CONRaRa, NRaRa, COORb, SO2-alquilo C
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