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    • 2. 发明申请
    • 1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES
    • 作为用于治疗心脏病的甘油摄取抑制剂的1-苯甲酰基哌嗪衍生物
    • WO2005023261A1
    • 2005-03-17
    • PCT/EP2004/009699
    • 2004-08-31
    • F. HOFFMANN-LA ROCHE AGALBERATI-GIANI, DanielaJOLIDON, SyneseNARQUIZIAN, RobertNETTEKOVEN, Matthias, HeinrichNORCROSS, Roger, DavidPINARD, EmmanuelSTALDER, Henri
    • ALBERATI-GIANI, DanielaJOLIDON, SyneseNARQUIZIAN, RobertNETTEKOVEN, Matthias, HeinrichNORCROSS, Roger, DavidPINARD, EmmanuelSTALDER, Henri
    • A61K31/496
    • C07D295/16A61K31/495A61K31/496C07D213/56C07D213/69C07D213/74C07D233/64C07D239/26C07D239/42C07D241/12C07D251/42C07D251/48C07D257/04C07D263/32C07D277/30C07D295/185C07D309/04C07D309/20C07D333/24C07D409/12
    • The invention relates to compounds of formula (I) wherein Ar is substituted aryl or unsubstituted or substituted 6-membered heteroaryl, containing one, two or three nitrogen atoms, and wherein the aryl and the heteroaryl groups may be substituted by one or more substituents selected from the group consisting of hydroxy, halogen, CN, (C 1 ­C 6 )-alkyl, (C 1 -C 6 )-alkyl substituted by halogen, (C 1 -C 6 )-alkoxy, (C 1 -C 6 )-alkoxy substituted by halogen, NR 7 R 8 , C(O)R 9 or SO 2 R 10 ; R 1 is hydrogen or (C 1 -C 6 )-alkyl; R 2 is halogen, (C 1 -C 6 ) -alkyl, (C 2 -C 6 ) -alkenyl, wherein a hydrogen atom may be replaced by CN, C(O)-R 9 or (C 1 -C 6 )-alkyl, or is (C 2 -C 6 )­alkynyl, (C 1 -C 6 )-alkyl substituted by halogen, -(CH 2 ) n -(C 3 -C 7 )-cycloalkyl, -(CH 2 ) n -heterocycloalkyl, -C(O)-R 9 , -(CH 2 ) n -aryl or -(CH 2 ) n -5 or -6­membered heteroaryl containing one, two or three heteroatoms, selected from the group consisting of oxygen, sulphur or nitrogen wherein aryl, cycloalkyl, heterocycloalkyl and heteroaryl are unsubstituted or substituted by one or more substituents selected from the group consisting of hydroxy, halogen, (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkyl substituted by halogen or (C 1 -C 6 ) alkoxy; R 3 , R 4 and R 6 independently from each other are hydrogen, hydroxy, halogen, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy; R 5 is NO 2 , CN, C(O)R 9 , SO 2 R 10 or NR 11 R 12 ; R 7 and R 8 independently from each other are hydrogen or (C 1 -C 6 )-alkyl; the other substituents are defined in the claims; and to pharmaceutically acceptable acid addition salts thereof for the treatment of psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
    • 本发明涉及式(I)化合物,其中Ar是含有一个,两个或三个氮原子的取代的芳基或未取代或取代的6元杂芳基,其中芳基和杂芳基可以被一个或多个选自 由羟基,卤素,CN,(C 1 -C 6) - 烷基,被卤素取代的(C 1 -C 6) - 烷基,(C 1 -C 6) - 烷氧基,被卤素取代的(C 1 -C 6) - 烷氧基,NR 7 R 8,C(O)R 9或SO 2 R 10; R 1是氢或(C 1 -C 6) - 烷基; R 2是卤素,(C 1 -C 6) - 烷基,(C 2 -C 6) - 烯基,其中氢原子可以被CN,C(O)-R 9或(C 1 -C 6) - 烷基 或(C 2 -C 6)炔基,被卤素, - (CH 2)n - (C 3 -C 7) - 环烷基, - (CH 2)n - 杂环烷基,-C(O)-R 含有一个,两个或三个选自氧,硫或氮的杂原子的(CH 2)n - 芳基或 - (CH 2)n-5或 - (CH 2)n-5或-6元杂芳基,其中芳基,环烷基,杂环烷基和 杂芳基是未取代的或被一个或多个选自羟基,卤素,(C 1 -C 6) - 烷基,被卤素或(C 1 -C 6)烷氧基取代的(C 1 -C 6) R 3,R 4和R 6彼此独立地是氢,羟基,卤素,(C 1 -C 6) - 烷基或(C 1 -C 6) - 烷氧基; R 5是NO 2,CN,C(O)R 9,SO 2 R 10或NR 11 R 12; R 7和R 8彼此独立地是氢或(C 1 -C 6) - 烷基; 其它取代基在权利要求中限定; 以及其药学上可接受的酸加成盐,用于治疗精神病,疼痛,记忆和学习中的神经变性功能障碍,精神分裂症,痴呆和其他认知过程受损的其他疾病,如注意力缺陷障碍或阿尔茨海默病。