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INHIBIDORES DE BTK
专利权人:
MERCK SHARP AND DOHME B.V.
发明人:
BARF, TJEERD A.,JANS, CHRISTIAAN GERARDUS JOHANNES MARIA,MAN, DE ADRIANUS PETRUS ANTONIUS,OUBRIE, ARTHUR A.,RAAIJMAKERS, HANS C.A.,REWINKEL, JOHANNES BERNARDUS MARIA,STERRENBURG, JAN-GERARD,WIJKMANS,
申请号:
PE0000962014
公开号:
PE16812014A1
申请日:
2012.07.11
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Refers to a compound of formula I, where X is CH, N, o, s and N, o, S Z is n or CH, Link a is CH or N B1, B2, B3, B4 are n or C (R7), C (R8), C (R9), C (R10) respectively r1 is r11c r12s (OR), (OR), r13so2 R2 is H, alkyl, cycloalkyl (1C, 3C - 3c) - 7c) R3 is H, alkyl (1c - 6C), cicloalquil Or (3C 7c) is H or alkyl R4 and R5 (3C - 3c) is H, halogeno, cyano,Among others, R6 is H or alkyl (1c - 3c) R7 is H, halogen or alkyl or alkoxy R8 is H (3C - 3c) R9 and R10 are independently H or alkoxy, halogen (3C - 3c) R11 is alkyl (1c - 6C), alquenilo (2C - 6C) and alquinilo (2C - 6C), among others, R12 and R13 are independently alquenilo (2C, 2C - alquinilo (6c) 6c) R14 is halogeno, cyano, alquenilo (2C - 6C), among others.Preferred compounds are: (S) - 4 - (3 - (1 - acriloilpirrolidin - il - 2) - 8 - aminoimidazol [1,5-a] pirazin - 1 - il) - N - (pyridin-2-yl) benzamide (S, e) - 4 - (3 - amino - 4 - (1 - (4 - (pyrrolidin-1-yl) but - 2 - enoil) pyrrolidin-2-one il) imidazole [1,5-a] pirazin - 1 - il) - N - (pyridin-2-yl) benzamide among others. This Compound is an inhibitor of Btk (Brutons tyrosine kinase).It also relates to a Pharmaceutical composition that is useful in the treatment of non Hodgkins lymphoma and Leukaemia.SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE: X ES CH, N, O, S Y ES N, O , S Z ES CH, N O ENLACE A ES CH O N B1, B2, B3, B4 SON N O C(R7), C(R8), C(R9), C(R10) RESPECTIVAMENTE R1 ES R11C(O), R12S(O), R13SO2 R2 ES H, ALQUILO (1C-3C), CICLOALQUILO (3C-7C) R3 ES H, ALQUILO (1C-6C), CICLOALQUILO (3C-7C) R4 ES H O ALQUILO (1C-3C) R5 ES H, HALOGENO, CIANO, ENTRE OTROS R6 ES H O ALQUILO (1C-3C) R7 ES H, HALOGENO O ALCOXI R8 ES H O ALQUILO (1C-3C) R9 Y R10 SON INDEPENDIENTEMENTE H, HALOGENO O ALCOXI (1C-3C) R11 ES ALQUILO (1C-6C), ALQUENILO (2C-6C) Y ALQUINILO (2C-6C), ENTRE OTROS R12 Y R13 SON INDEPENDIENTEMENTE ALQUENILO (2C-6C), ALQUINILO (2C-6C) R14 ES HALOGENO, CIANO, ALQUENILO (2C-6C), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: (S)-4-(3-(1-ACRILOILPIRROLIDIN-2-
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