Alicyclic-amine-substituted 4-carboxamido-benzimidazoles as parp-inhibitors and antioxidants
申请人:Hideg Kalman
公开号:US20070072912A1
公开(公告)日:2007-03-29
Compounds of the formula (I) and their pharmaceutically acceptable or technically applicable acid salts—where in the formula R
1
represents hydrogen, C
(1-4)
alkyl or C
(1-4)
alkoxy R
2
represents hydrogen, C
(1-4)
alkyl, carboxyl, C
(1-4)
alkoxycarbonyl, carboxamido, aryl or hetero-aryl R
3
represents hydrogen, C
(1-4)
alkyl, aryl-methylene, or aryl, Y is a valency bond, a straight or branched chain C
(1-4)
alkene, a carbonyl-amino-C
(1-4)
alkene, or a —S—(CH
2
)
m
— group, where all alkene groups above may be spaced by an arylene group, n represents zero or the integer 1 m represents the integer 1, 2 or 3 Q represents hydrogen, hydroxyl or the oxygen radical (0) or together with the N atom of the adjacent ring forms a +N=O (oxoimmonium) group Z represents a single or double bond and their pharmaceutically acceptable or technically useful salts, processes for their preparation and their biological use as PARP inhibitors and antioxidants.
公式(I)的化合物及其药学上可接受或技术上适用的酸盐——其中在公式中,R1代表氢,C(1-4)烷基或C(1-4)烷氧基;R2代表氢,C(1-4)烷基,羧基,C(1-4)烷氧羰基,羧酰胺基,芳基或杂环芳基;R3代表氢,C(1-4)烷基,芳基-亚甲基或芳基;Y是一个价键,一条直链或支链C(1-4)烯烃,一个羰基-氨基-C(1-4)烯烃,或一个—S—(CH2)m—基团,其中上述所有烯烃基团可以由一个芳基基团间隔;n代表零或整数1;m代表整数1、2或3;Q代表氢,羟基或氧基(0)或与相邻环的N原子一起形成+ N = O(氧代亚氨基)基团;Z代表单键或双键及其药学上可接受或技术上有用的盐,制备它们的过程以及它们作为PARP抑制剂和抗氧化剂的生物学用途。