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1. 发明申请

US20070072912A1 Alicyclic-amine-substituted 4-carboxamido-benzimidazoles as parp-inhibitors and antioxidants 审中-公开
标题翻译：脂环胺 - 胺取代的4-甲酰氨基 - 苯并咪唑作为对位抑制剂和抗氧化剂
公开(公告)号：US20070072912A1
公开(公告)日：2007-03-29
申请号：US10553937
申请日：2004-04-27
申请人： Kalman Hideg , Tamas Kalai , Balazs Sumegi
发明人： Kalman Hideg , Tamas Kalai , Balazs Sumegi
IPC分类号： A61K31/4439 , A61K31/4184 , C07D403/02
CPC分类号： C07D401/04 , C07D403/04 , C07D403/10 , C07D405/14 , C07D495/04
摘要： Compounds of the formula (I) and their pharmaceutically acceptable or technically applicable acid salts—where in the formula R1 represents hydrogen, C(1-4)alkyl or C(1-4)alkoxy R2 represents hydrogen, C(1-4)alkyl, carboxyl, C(1-4)alkoxycarbonyl, carboxamido, aryl or hetero-aryl R3 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—(CH2)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.
摘要翻译：式（I）化合物及其药学上可接受的或技术上可应用的酸盐 - 其中在式R 1表示氢，C 1-4（1-4） - 烷基或C （1-4）烷氧基R 2表示氢，C 1-4（1-4）烷基，羧基，C 1-4（1-4）烷氧基羰基，甲酰胺基，芳基或杂芳基R 3表示氢，C 1-4（1-4）烷基，芳基 - 亚甲基或芳基，Y是直链或支链C 1-4（1-4）烯烃，羰基 - 氨基-C 1-4（1-4） - 烯烃或-S-（CH 其中所有上述烯烃基团可以被亚芳基间隔开，n表示0或整数1m表示整数1,2或3个Q 表示氢，羟基或氧自由基（0）或与相邻环的N原子一起形成a + N = O（有机基元素）基团Z表示单键或双键及其药学上可接受或技术上有用的盐，准备 n及其生物用作PARP抑制剂和抗氧化剂。

2. 发明申请

US20070042935A1 Quinazolinone-derivatives and their use for preparation of pharmaceutical compositions having parp enzyme inhibitory effect 有权
标题翻译：喹唑啉酮衍生物及其制备具有酶抑制作用的药物组合物的用途
公开(公告)号：US20070042935A1
公开(公告)日：2007-02-22
申请号：US10554749
申请日：2004-04-30
申请人： Balazs Sumegi , Kalman Hideg , Tamas Kalai
发明人： Balazs Sumegi , Kalman Hideg , Tamas Kalai
IPC分类号： A61K31/00
CPC分类号： C07D401/04 , C07D239/95 , C07D401/06 , C07D401/12
摘要： The subject of the present invention are quinazoline derivatives and their pharmaceutically acceptable salts of general formula (I), that inhibit a DNA-repairing enzyme, poly(ADP-ribose) polymerase (PARP), enabling them to be used for the preparation of pharmaceutical compositions for preventing or treating illnesses where PARP-inhibition yields a beneficial effect. In general formula (I) R1 stands for either hydrogen or a group of general formula (a); R2 stands for a) hydrogen or C1-6 alkyl group, if R1 is other than hydrogen, and b) if R1 is hydrogen, then R2 may be a group of general formula (b), (c) or (d). The subject of the present invention also embraces the preparation processes of the compounds described above.
摘要翻译：本发明的主题是抑制DNA修复酶，聚（ADP-核糖）聚合酶（PARP））的喹唑啉衍生物及其药学上可接受的通式（I）的盐，使其能够用于制备药物用于预防或治疗PARP抑制产生有益效果的疾病的组合物。在通式（I）中，R 1表示氢或通式（a）的基团; R 2代表a）氢或C 1-6烷基，如果R 1不是氢，和b）如果R' SUP> 1是氢，则R 2可以是通式（b），（c）或（d）的基团。本发明的主题还包括上述化合物的制备方法。

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