TAO, Zhi-Fu,WANG, Xilu,SOUERS, Andrew J.,CATRON, Nathaniel D.,SULLIVAN, Gerard
申请号：
PE0002442017
公开号：
PE04652017A1
申请日:
2011.05.25
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to a compound of formula I, where C (N: A1 or A2) A2, D1 and E1 are h, R1, R1 is OR1, among others phenyl heteroaryl, among others y1 is H, CN, NO2, among others G1 is r1b, or1b or nhr1b r1b is s (OR) 2 (OH), among others.Preferred compounds are: diacid phosphate [3 - (4 - ((4 - (4 - [2 - (4-chlorophenyl) - 4.4 - dimetilciclohex - 1 - 1 - il] methyl} piperazin-1-yl) - 2 - (1h pyrrolo [2,3-b] pyridin - 5 - iloxi sulfamoyl) benzoyl}}) amino] - 2-nitrophenyl - 2.2 - and dimetilpropilo diacid phosphate trans - [4 - (4 - ((4 - (4 - [2 - (4-chlorophenyl) - 4.4 - dimetilciclo Hex - 1 - 1 - il] methyl} piperazin-1-yl) - 2 - (1h pyrrolo [2,3 - B] pyridin-3 benzoyl) - 5 - iloxi}} - 2 - nitrofenoxi sulfamoyl Methyl cyclohexyl)]. It also relates to a Pharmaceutical composition. These compounds inhibit the activity of the anti apoptotic Proteins bcl-2, being useful in the treatment of bladder cancer, brain cancer, among othersSe refiere a un compuesto de formula Ia, donde: A1 es N o C(A2) A2, D1 y E1 son H, R1, OR1, entre otros R1 es fenilo, heteroarilo, entre otros Y1 es H, CN, NO2, entre otros G1 es R1B, OR1B o NHR1B R1B es S(O)2(OH), entre otros. Son compuestos preferidos: fosfato diacido de 3-[(4-{[4-(4-{[2-(4-clorofenil)-4,4-dimetilciclohex-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirrolo[2,3-b]piridin-5-iloxi)benzoil}sulfamoil}-2-nitrofenil)amino]-2,2-dimetilpropilo y fosfato diacido de trans-4-[(4-{[4-(4-{[2-(4-clorofenil)-4,4-dimetilciclohex-1-en-1-il]metil}piperazin-1-il)-2-(1H-pirrolo[2,3-b]piridin-5-iloxi)benzoil}sulfamoil}-2-nitrofenoxi)metil]ciclohexilo. Tambien se refiere a una composicion farmaceutica. Dichos compuestos inhiben la actividad de las proteinas anti-apoptoticas Bcl-2, siendo utiles en el tratamiento de cancer de vejiga, cancer de cerebro, entre otros
