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1.发明公开ISOQUINOLINE -1,3,4-TRIONE, THE SYNTHETIC METHOD AND THE USE THEREOF 有权ISOCHINOLIN-1,3,4-TRION，合成VERFAHREN DE DESSEN VERWENDUNG
公开(公告)号：EP1640367A1
公开(公告)日：2006-03-29
申请号：EP04738186.8
申请日：2004-05-31
发明人： NAN, Fajun , LI, Jia , CHEN, Yihua , ZHANG, Yahui , GU, Min , ZHANG, Huajie
IPC分类号： C07D217/04 , A61P25/00 , A61P25/28
CPC分类号： C07D417/04 , C07D217/24
摘要： The invention relates to various substituted isoquinoline-1,3,4-trione, the synthetic method thereof and the use for treating neurodegenerative diseases, especially as the medicine for Alzhermer's disease, apoplexy and brain ischemic injuries. The compound is represented by the following structure formula:
Wherein substituents R 1 can be one, two or three groups optionally selected from the group consisting of H; alkyl; hydroxyl; alkyl substituted by the groups including halogen, alkoxyl or hydroxyl; alkoxyl or alkylamino substituted by the groups including halogen, alkoxyl or hydroxyl; C 2 -C 6 alkenyl substituted by oxygen or amine; C 3 -C 6 cycloalkyl; substituted aryl; benzyl; alkanoyl; alkanoyl substituted by the groups including halogen, alkoxyl or hydroxyl; C 2 -C 6 enoyl; C 3 -C 6 cycloalkanoyl; tert -butoxycarbonyl; benzoyl; benzoyl substituted by one, two or three groups including alkylamino; benzylacyl; benzylacyl substituted by one, two or three groups including alkylamino; thienoyl; adamantylcarbonyl; mandeloyl; alkoxyl; alkylamino; cycloalkoxyl; cycloalkylamino; amino; acylamino; alkyloxycarbonyl; cycloalkoxycarbonyl; alkanoylxy; alkanoylamino; cycloalkyanoylxy; cycloalkanoylamino; ureido; urenylene; alkanoyl; nitro; carboxyl;
R 2 is H; alkyl; alkyl or C 1 -C 4 cycloalkyl substituted by the groups including halogen, alkoxyl or hydroxyl; C 2 -C 6 alkenyl; aryl; substituted aryl;
X is H, CH 2 , NH, O, or S;
Y is CH, or N.摘要翻译： 本发明涉及各种取代的异喹啉-1,3,4-三酮，其合成方法和治疗神经变性疾病的用途，特别是作为阿尔瑟默病，中风和脑缺血损伤的药物。 该化合物由以下结构式表示：其中取代基R 1可以是任选地选自H的一个，两个或三个基团; 烷基; 羟; 由包括卤素，烷氧基或羟基的基团取代的烷基; 烷氧基或被包括卤素，烷氧基或羟基的基团取代的烷基氨基; 由氧或胺取代的C 2 -C 6烯基; C 3 -C 6环烷基; 取代芳基; 苄基; 烷; 被卤素，烷氧基或羟基取代的烷酰基; C 2 -C 6烯酰基; C 3 -C 6环烷酰基; 叔丁氧基羰基; 苯甲酰; 由一个，两个或三个基团取代的苯甲酰基，包括烷基氨基; benzylacyl; 被一个，两个或三个基团取代的苄基酰基，包括烷基氨基; 噻吩; 金刚烷基; 扁桃; 烷氧基; 烷基; 环烷; 环烷基; 氨基; 酰氨基; 烷氧羰基; 环烷; alkanoylxy; 烷酰基; cycloalkyanoylxy; cycloalkanoylamino; 脲; urenylene; 烷; 硝基; 羧基; R 2为H; 烷基; 烷基或被包括卤素，烷氧基或羟基的基团取代的C 1 -C 4环烷基; C 2 -C 6烯基; 芳基; 取代芳基; X是H，CH 2，NH，O或S; Y是CH或N.
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2.发明授权
公开(公告)号：EP1640367B1
公开(公告)日：2011-02-09
申请号：EP04738186.8
申请日：2004-05-31
发明人： NAN, Fajun , LI, Jia , CHEN, Yihua , ZHANG, Yahui , GU, Min , ZHANG, Huajie
IPC分类号： C07D217/04 , A61P25/00 , A61P25/28
CPC分类号： C07D417/04 , C07D217/24
摘要： The invention relates to all types of substituted isoquinoline -1,3,4-trione, the synthetic method thereof and the use for treatding neurodegenerative diseases , especially as the medicine for Alzhermer's disease, appplexy and brain ischernic injuries, the compound is represented by the structure, Formula (I); Dihydroisoquinoline-1,3,4-trione) wherein substituents R, can be one , two or three groups optionally selected from the group consisting of H; alkyl; hydroxyl; alkyl substituted by the groups including halogen , alkoxyl, hydroxyl; alkyl or alkylamine substituted by the groups including halogen , alkoxyl, hydroxyl; C,-,alkenyl substituted by oxygen or amine; C, 6cycloalkyl; substituted aryl; benzyl; alkanoyl; alkanoyl substituted by the groups including halogen , alkoxyl, hydroxyl; C2-6enc,yl ; C,-,cycloalkanoyl; tertbutoxycarbonyl; benzoyl; benzoyl. substituted by one, two or three groups including alkylarnine; benzylacryl; benzylacryl. substituted by one, two or three groups including alkylamine; thienylfonnyl; admantyliForrnyl; mandeloyl; alkoxyl; alkylamine; cycloalkoxyl; cycloalkoxycarbonyl; alkanoylxy; alkanoylamine; cycloalkyanoylxy; cycloalkanoylarnine; ureido; urenylene; alkanoyl; nitro; carboxyl; R2 is H; alkyl; alkyl. or Cl-C4cycloalkyl which are substituted by the groups including halogen, alkoxyl, hydroxyl; C2-C,alkenyl; acryl; substituted acryl; X is H, CH2, N-H, 0, S; is CH, N.
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