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1H-PIRROLO[2,3-C] PIRIDIN-7(6H)-ONAS Y PIRAZOLO[3,4-C]PIRIDIN-7(6H)-ONAS COMO INHIBIDORES DE PROTEINAS BET
专利权人:
INCYTE CORPORATION
发明人:
COMBS, Andrew P.,MADUSKUIE, Thomas P.,FALAHATPISHEH, Nikoo
申请号:
PE0021162016
公开号:
PE01442017A1
申请日:
2015.04.22
申请国别(地区):
PE
年份:
2017
代理人:
摘要:
Refers to a compound of formula I, where X is c = o or cr8r9 and is o, s or z is CH or NR10 n R1 and R2 are independently H c1-c6 alkyl, Halo, alquenilo C2 - C6, among others, or R1 and R2 together with the carbon Atom to which they are United to form a cycloalkyl or heterocicloalquilo of C3 - C10 4 - 10 members,Each optionally substituted R3 is H or c1-c6 alkyl, optionally substituted R4 is H, c1-c4 alkyl, Halo, among others R5 is H, alkyl, Halo, C1 - C6, among others R6 h, Halo, c1-c4 alkyl, among others R7 and R10 are H or c1-c4 alkyl, R8 and R9 are H c1-c4 alkyl, Halo, or haloalquilo C1 - C 4.Preferred compounds are: 8 - (6 - methyl - 4 - oxo - 6.7 - dihydro 1h pyrrolo [2,3-c] pyridin-4-yl) - 2 - phenyl - 2 - 3 - 1.4 - benzoxazin (4H) - One 2 - isopropyl - 8 - 6 - methyl - 7 - oxo - 6.7 - dihydro 1h pyrrolo [2,3-c] pyridin-4-yl) - 2H - 1.4 - benzoxazin - 3 (2H) - One among others. It also relates to a Pharmaceutical Composition and a method of treatment.These compounds are inhibitors of Protein would be useful in the treatment of cancer, COPD, allergies, among others.Se refiere a un compuesto de la formula I, donde: X es C=O o CR8R9 Y es O, S, o NR10 Z es CH o N R1 y R2 son independientemente H, halo, alquilo C1-C6, alquenilo C2-C6, entre otros, o R1 y R2 junto con el atomo de carbono al que estan unidos forman un cicloalquilo C3-C10 o heterocicloalquilo de 4-10 miembros, cada uno opcionalmente sustituido R3 es H o alquilo C1-C6 opcionalmente sustituido R4 es H, halo, alquilo C1-C4, entre otros R5 es H, halo, alquilo C1-C6, entre otros R6 es H, halo, alquilo C1-C4, entre otros R7 y R10 son H o alquilo C1-C4 R8 y R9 son H, halo, alquilo C1-C4 o haloalquilo C1-C4. Son compuestos preferidos: 8-(6-metil-7-oxo-6,7-dihidro-1H-pirrolo[2,3-c]piridin-4-il)-2-fenil-2H-1,4-benzoxazin-3(4H)-ona 2-isopropil-8-(6-metil-7-oxo-6,7-dihidro-1H-pirrolo[2,3-c]piridin-4-il)-2H-1,4-benzoxazin-3(4H)-ona entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de tr
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