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1. 发明申请

WO2004072034A1 PIPERIDINE-BENZENESULFONAMIDE DERIVATIVES 审中-公开
标题翻译：哌嗪 - 苯甲酰胺衍生物
公开(公告)号：WO2004072034A1
公开(公告)日：2004-08-26
申请号：PCT/EP2004/001211
申请日：2004-02-10
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI-GIANI, Daniela , CECCARELLI, Simona, Maria , PINARD, Emmanuel , STALDER, Henri
发明人： ALBERATI-GIANI, Daniela , CECCARELLI, Simona, Maria , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D211/58
CPC分类号： C07D413/12 , C07D211/58 , C07D401/08 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D413/14
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is lower alkyl, -(CH 2 ) n -aryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, lower alkoxy, -OCF 3 , halogen, -NR’R” or trifluoromethyl, or heteroaryl; R 2 is lower alkyl, -(CH 2 ) n -aryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, cyano, -NR’R”, hydroxy, or by a heteroaryl group, or is heteroaryl, unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl or halogen; R 3 is heteroaryl or is aryl, unsubstituted or substituted by halogen or lower alkyl; R 4 is hydrogen or hydroxy; A is -S(O) 2 -or-C(O)-; X,Y are independently from each other -CH 2 - or -O-, with the proviso that X and Y are not simultaneously -O; R’R” are independently from each other hydrogen, lower alkyl or -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds may be used for the treatment of psychoses, pain, 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.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1为低级烷基， - （CH 2）n - 芳基，未取代或被一个或两个选自以下的取代基取代：低级烷基，低级烷氧基，-OCF 3，卤素，-NR'R“或三氟甲基或杂芳基; R 2是低级烷基， - （CH 2）n - 芳基，未取代或被一个或两个取代基取代，所述取代基选自低级烷基，低级烷氧基，卤素，三氟甲基，硝基，氰基，-NR'R“，羟基或杂芳基，或是未被取代或被一个或两个选自低级烷基或卤素的取代基取代的杂芳基; R 3是杂芳基或未被取代或被卤素或低级烷基取代的芳基; R 4是氢或羟基; A是-S（O）2 - 或-C（O） - ; X，Y彼此独立地为-CH 2 - 或-O-，条件是X和Y不同时为-O; R'R“彼此独立地为氢，低级烷基或-C（O） - 低级烷基; n为0,1或2;以及其药学上可接受的酸加成盐。该化合物可用于治疗精神病记忆障碍，学习障碍，精神分裂症，痴呆等认知过程受损的疾病，如注意力缺陷障碍或阿尔茨海默病。

2. 发明申请

WO2005023261A1 1-BENZOYL-PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES 审中-公开
标题翻译：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
公开(公告)号：WO2005023261A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009699
申请日：2004-08-31
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI-GIANI, Daniela , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： ALBERATI-GIANI, Daniela , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： A61K31/496
CPC分类号： C07D295/16 , A61K31/495 , A61K31/496 , C07D213/56 , C07D213/69 , C07D213/74 , C07D233/64 , C07D239/26 , C07D239/42 , C07D241/12 , C07D251/42 , C07D251/48 , C07D257/04 , C07D263/32 , C07D277/30 , C07D295/185 , C07D309/04 , C07D309/20 , C07D333/24 , C07D409/12
摘要： 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.
摘要翻译：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。

3. 发明申请

WO2005023260A1 1- (2-AMINO-BENZOL) -PIPERAZINE DERIVATIVES AS GLYCINE UPTAKE INHIBITORS FOR THE TREATMENT OF PSYCHOSES 审中-公开
标题翻译： 1-（2-氨基苄基） - 哌嗪衍生物作为甘油摄取抑制剂用于治疗心脏病
公开(公告)号：WO2005023260A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009665
申请日：2004-08-30
申请人： F. HOFFMANN-LA ROCHE AG , ALBERATI-GIANI, Daniela , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： ALBERATI-GIANI, Daniela , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： A61K31/496
CPC分类号： C07D295/192 , A61K31/495 , A61K31/496 , C07D207/08 , C07D207/12 , C07D207/20 , C07D211/42 , C07D231/12 , C07D233/54 , C07D237/20 , C07D249/08 , C07D257/04 , C07D307/14 , C07D309/14
摘要： A compound of formula (I) wherein the substituents are described in claim 1 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.
摘要翻译：式（I）化合物，其中取代基在权利要求1中描述，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疾病。

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