Rottlerin for the treatment of pulmonary hypertension and related diseases and disorders
申请人:ATB Innovation Ltd.
公开号:EP2578210A1
公开(公告)日:2013-04-10
The inventions discloses a pharmaceutical composition comprising rottlerin or a pharmaceutically acceptable salt thereof or one or more of its derivatives or a pharmaceutically acceptable salt thereof said derivative having the formula
wherein X is selected from the group consisting of CH2, O, N, P, and S; R1 and R3 are selected from the group consisting of H, OH, NH2, SH, SO, S-NH-R, NH-R (R selected from the group consisting of alkyl, alkenyl, alkinyl, aryl, phenyl, benzyl, ester, ether, carbonyl, carboxyl, F, Cl, Br, I, H), alkyl, alkenyl, alkinyl, aryl, phenyl, benzyl, ester, ether, carbonyl, carboxyl, F, Cl, Br, I and H; R2 is selected from the group consisting of ethanone, acetyl, alkyl, alkenyl alkinyl, aryl, phenyl, benzyl, ester ether, carbonyl, carboxyl, F, Cl, Br, I and H; R4 is CO-[(E)CHCH]n-Ph, CN-[(E)CHCH]n-Ph, or COOZ, wherein Z is selected from the group consisting of alkenyl, aryl, and alkyl, alkyl, alkenyl, alkinyl, aryl, phenyl, benzyl, ester, ether, carbonyl, carboxyl, F, Cl, Br, I and H; R5, R6, R7 and R8 are selected from the group consisting of methyl, H, P, OH, NH2, SH, SO, S-NH-R, NH-R (R selected from the group consisting of alkyl, alkenyl, alkinyl, aryl, phenyl, benzyl, ester, ether, carbonyl, carboxyl, F, Cl, Br, I, H), alkyl, alkenyl, alkinyl, aryl, phenyl, benzyl, ester, ether, carbonyl, carboxyl, F, Cl, Br, I and H, for use in a method of preventing or treating pulmonary hypertension.
本发明公开了一种药物组合物,该组合物包含腐霉利或其药学上可接受的盐或其一种或多种衍生物或其药学上可接受的盐,所述衍生物的化学式为
其中 X 选自 CH2、O、N、P 和 S 组成的组;R1 和 R3 选自 H、OH、NH2、SH、SO、S-NH-R、NH-R(R 选自烷基、烯基、烷基、芳基、苯基、苄基、酯、醚、羰基、羧基、F、Cl、Br、I、H 所组成的组)、烷基、烯基、烷基、芳基、苯基、苄基、酯、醚、羰基、羧基、F、Cl、Br、I 和 H;R2 选自乙酮、乙酰基、烷基、烯基烷基、芳基、苯基、苄基、酯、醚、羰基、羧基、 F、Cl、Br、I 和 H 所组成的组;R4 是 CO-[(E)CHCH]n-Ph、CN-[(E)CHCH]n-Ph 或 COOZ,其中 Z 选自由烯基、芳基和烷基、烷基、烯基、烷基、芳基、苯基、苄基、酯、醚、羰基、羧基、F、Cl、Br、I 和 H 组成的组;R5、R6、R7 和 R8 选自由甲基、H、P、OH、NH2、SH、SO、S-NH-R、NH-R (R 选自由烷基、烯基、烷基、芳基、苯基、苄基、酯、醚、羰基、羧基、F、Cl、Br、I 和 H 组成的组)、羰基、羧基、F、Cl、Br、I、H)、烷基、烯基、烷基、芳基、苯基、苄基、酯、醚、羰基、羧基、F、Cl、Br、I 和 H,用于预防或治疗肺动脉高压的方法。