专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 发明申请

WO2005014563A1 PIPERAZINE WITH OR-SUBSTITUTED PHENYL GROUP AND THEIR USE AS GLYT1 INHIBITORS 审中-公开
标题翻译：具有或取代的苯基的哌嗪及其作为GLYT1抑制剂的用途
公开(公告)号：WO2005014563A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008633
申请日：2004-08-02
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D295/192
CPC分类号： C07D239/42 , C07D213/85 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
摘要： The invention relates to compounds of formula (I) wherein the substituents are described in claim 1. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as 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，其中取代基描述于权利要求1中。该化合物可用于治疗基于甘氨酸摄取抑制剂的疾病，例如精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆症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。

4. 发明申请

WO2006072436A1 [4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译：作为用于治疗神经病学和神经病学疾病的甘氨酸运输1（GLYT-1）抑制剂的[4-（异丁基）哌嗪-1-基] - （2,5-取代的苯基）甲酮衍生物
公开(公告)号：WO2006072436A1
公开(公告)日：2006-07-13
申请号：PCT/EP2005/014082
申请日：2005-12-28
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
IPC分类号： A61K31/427 , A61K31/433 , A61P25/28 , C07D277/42 , C07D277/56 , C07D417/12 , C07D285/12 , C07D285/08
CPC分类号： C07D285/08 , C07D277/42 , C07D277/56 , C07D285/135 , C07D417/12
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is-OR 1’ ,-SR 1’ or is a heterocycloalkyl group; R 1’ is lower alkyl, lower alkyl substituted by halogen or is -(CH 2 ) n -cycloalkyl; R 2 is-S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; X 1 is CR 3 or N; X 2 is CR 3’ or N; R 3 /R 3’ are independently from each other hydrogen, halogen, lower alkyl, CN, NO 2 ,-S(O) 2 -phenyl, -S(O) 2 -lower alkyl, -S(O) 2 -pyridin-2, 3 or 4-yl, phenyl, optionnally substituted by one or two substituents selected from the group consisting of NO 2 or halogen, or is lower alkyl substituted by halogen or is -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1). They may be used in the treatment of schizophrenia.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是 - 或 - 1'， - SR 1'或其是杂环烷基 R 1是低级烷基，被卤素取代的低级烷基或是 - （CH 2 CH 2）n - 环烷基; R 2是-S（O）2 - 低级烷基，-S（O）2 NH-低级烷基，NO 2 或CN; X 1是CR 3或N; X 2是CR 3或N; R 3和R 3彼此独立地为氢，卤素，低级烷基，CN，NO 2，-S（O） -S（O）2 - 低级烷基，-S（O）2 - 吡啶基-2,3或4-基 - ，苯基，其选自一个或两个选自NO 2或卤素的取代基，或被卤素取代的低级烷基或-C（O） - 低级烷基; n为0,1或2; 及其药学上可接受的酸加成盐。已经发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂。它们可用于治疗精神分裂症。

5. 发明申请

WO2006061135A1 PHENYL-PIPERAZIN METHANONE DERIVATIVES 审中-公开
标题翻译：苯基哌嗪甲酮衍生物
公开(公告)号：WO2006061135A1
公开(公告)日：2006-06-15
申请号：PCT/EP2005/012833
申请日：2005-12-01
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
IPC分类号： C07D277/82 , C07D277/64 , C07D275/04 , C07D263/58 , C07D215/38 , C07D241/44 , A61K31/428 , A61K31/423 , A61K31/47 , A61K31/498 , A61P25/00
CPC分类号： C07D215/38 , C07D241/44 , C07D263/58 , C07D275/04 , C07D277/64 , C07D277/82
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is the group (A) or (B) or (C) or (D); R 2 is a non aromatic heterocycle, or is OR' or N(R") 2 ; R' is lower alkyl, lower alkyl substituted by halogen or -(CH 2 ) n -cycloalkyl; R" is lower alkyl; R 3 is NO 2 , CN or SO 2 R'; R 4 is hydrogen, hydroxy, halogen, NO 2 , lower alkyl, lower alkyl, substituted by halogen, lower alkoxy, SO 2 R' or C(O)OR"; R 5 /R 6 /R 7 are hydrogen, halogen, lower alkyl or lower alkyl, substituted by halogen; X 1 /X 1’ are CH or N, with the proviso that X 1 /X 1’ are not simultaneously CH; X 2 is O, S, NH or N(lower alkyl); n is 0, l or 2; and to pharmaceutically active acid addition salts and to their use in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是基团（A）或（B）或（C）或（D）; R 2是非芳族杂环，或是OR'或N（R“）2; R'是低级烷基，被卤素取代的低级烷基或 - （CH 3） N 2 - 环烷基; R“是低级烷基; R 3是NO 2，CN或SO 2 R'; R 4是氢，羟基，卤素，NO 2，低级烷基，被卤素取代的低级烷基，低级烷氧基，SO 2 R' 或C（O）OR“; R 5，R 6，R 6和R 7是氢，卤素，低级烷基或低级烷基，被卤素; X 1 / X 1'是CH或N，条件是X 1 / X 1' >不同时为CH; X 2为O，S，NH或N（低级烷基）; n为0,1或2;以及药学活性的酸加成盐及其在治疗中的用途的神经和神经精神障碍。

6. 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。

7. 发明申请

WO2008022938A1 DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1 审中-公开
标题翻译：作为GLYT1抑制剂的DI-AROMATIC取代的氨基酸
公开(公告)号：WO2008022938A1
公开(公告)日：2008-02-28
申请号：PCT/EP2007/058350
申请日：2007-08-13
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , PINARD, Emmanuel
IPC分类号： C07C237/22 , C07C255/57 , C07C271/22 , C07C275/24 , C07D213/40 , C07D213/81 , C07D261/18 , C07D275/02 , C07D279/02 , C07D307/79 , C07D333/20 , C07D333/38 , C07D333/44 , C07D335/18 , A61K31/16
CPC分类号： C07C237/22 , C07C255/57 , C07C271/22 , C07C275/24 , C07C2601/14 , C07D213/40 , C07D213/81 , C07D261/18 , C07D275/02 , C07D279/02 , C07D307/79 , C07D333/20 , C07D333/38 , C07D333/44 , C07D335/18
摘要： The present invention relates to compounds of the general Formula (I) wherein (A) is a 5 or 6-membered aromatic or heteroaromatic ring; R 1 is cycloalkyl or is aryl or heteroaryl, wherein at least one ring is aromatic in nature, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -C(O) -lower alkyl, -S(O) 2 -lower alkyl, nitro or cyano; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or nitro; R 5 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -(CH 2 ) m -, -CH 2 O- or -CH 2 NH-; The dotted line denotes a bond or not; n is 1 or 2; m is 1, 2 or 3; and pharmaceutically acceptable acid addition salts thereof and their use in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中（A）是5或6元芳族或杂芳族环; R 1是环烷基或芳基或杂芳基，其中至少一个环在本质上是芳族的，未被取代或被1至3个选自以下的取代基取代：卤素，低级烷基，被卤素，低级烷氧基，被卤素取代的低级烷氧基，-C（O） - 低级烷基，-S（O）2 - 低级烷基，硝基或氰基; R 2是氢或低级烷基; R 3是氢或低级烷基; R 4是卤素，低级烷基，被卤素取代的低级烷基，低级烷氧基，被卤素或硝基取代的低级烷氧基; R 5是氢，卤素，被卤素取代的低级烷基或低级烷基; X是一个键， - （CH 2）2 - ， - CH 2 O-或-CH 2 - NH-; 虚线表示不是键; n为1或2; m为1,2或3; 及其药学上可接受的酸加成盐及其在治疗神经和神经精神障碍中的用途。

8. 发明申请

WO2007147770A3 SUBSTITUTED PHENYL METHANONE DERIVATIVES 审中-公开
公开(公告)号：WO2007147770A3
公开(公告)日：2007-12-27
申请号：PCT/EP2007/055871
申请日：2007-06-14
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger , PINARD, Emmanuel
IPC分类号： C07D205/04 , C07D207/06 , C07D211/16 , C07D407/10 , A61K31/445 , A61P25/18
摘要： The present invention relates to compounds of the general formula (i), wherein R 1 is -OR 1 ' , heterocycloalkyl, aryl or heteroaryl, which are unsubstituted or substituted by lower alkyl or halogen; R1' is lower alkyl, lower alkyl substituted by halogen, or is -(CH 2 ) o -cycloalkyl; R 2 is -S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; R 3 is aryl or heteroaryl, which are unsubstituted or substituted by one to three substituents, selected from the group consisting of lower alkyl, lower alkoxy, CN, NO 2 , halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, aryl or sulfonamide; X is a bond, -CH 2 -, -NH-, -CH 2 O- or -OCH 2 -; n is 1 or 2; m is 1 or 2; o is 0 or 1; to pharmaceutically acceptable acid addition salts thereof, to pharmaceutical compositions containing them and their use in the treatment of neurological and neuropsychiatric disorders. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1).

9. 发明申请

WO2008025694A1 INHIBITORS FOR GLYT-1 审中-公开
标题翻译： GLYT-1的抑制剂
公开(公告)号：WO2008025694A1
公开(公告)日：2008-03-06
申请号：PCT/EP2007/058610
申请日：2007-08-20
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , PINARD, Emmanuel
IPC分类号： C07C233/51 , C07C235/52 , C07C235/56 , C07C237/40 , C07C255/57 , C07D213/56 , C07D213/61 , C07D213/74 , C07D261/18 , C07D333/70 , A61K31/166 , A61K31/167 , A61K31/44 , A61K31/381 , A61K31/415
CPC分类号： C07C237/12 , C07C255/57 , C07D213/81 , C07D213/82 , C07D317/52 , C07D333/20 , C07D333/70
摘要： The present invention relates to compounds of the general formula I wherein R 1 is lower alkyl, aryl or heteroaryl, wherein aryl and heteroaryl are optionally substituted by halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, cyano, amino, di-lower alkyl amino or morpholinyl; R 2 is lower alkyl, -(CH 2 )n-aryl, -(CH 2 )n-heteroaryl or -(CH 2 )n-cycloalkyl, wherein the aryl or heteroaryl groups are optionally substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl, cyano, or lower alkoxy; R 3 is hydrogen or lower alkyl; R 4 is aryl or heteroaryl, wherein at least one ring is aromatic in nature, wherein aryl and heteroaryl are optionally substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl substituted by halogen, lower alkoxy substituted by halogen, lower alkyl; X is a bond or -OCH 2 -; n is 0, 1 or 2; or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2, 4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]- benzeneacetamide. and to their use in the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式I的化合物，其中R 1是低级烷基，芳基或杂芳基，其中芳基和杂芳基任选被卤素，低级烷基，低级烷氧基，被卤素取代的低级烷基由卤素，氰基，氨基，二低级烷基氨基或吗啉基取代的低级烷氧基; R 2是低级烷基， - （CH 2）2 - 芳基， - （CH 2 CH 2）n - 杂芳基或 - （CH

10. 发明申请

WO2007101802A1 4-AMINO-1,5-SUBSTITUTED 1,5-DIHYDRO-IMIDAZOL-2-ONES 审中-公开
标题翻译： 4-氨基-1,5-取代的1,5-二氢-1H-咪唑-2-酮
公开(公告)号：WO2007101802A1
公开(公告)日：2007-09-13
申请号：PCT/EP2007/051824
申请日：2007-02-27
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger , PINARD, Emmanuel
IPC分类号： C07D233/92 , A61K31/4025 , A61P25/18
CPC分类号： C07D233/92
摘要： The present invention relates to compounds of the general formula wherein R 1 is -(CH 2 ) n -aryl or -(CH 2 ) n -heteroaryl, wherein such groups are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkyl substituted by halogen, lower alkoxy, lower alkyl, cyano, nitro, -O-lower alkyl substituted by halogen or morpholinyl; R 2 is -(CH 2 ) n -aryl or -(CH 2 ) n -heteroaryl, wherein such groups are unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, halogen or -N(lower alkyl) 2 ; R 3 is hydrogen or lower alkyl; R 4 is -(CH 2 ) n -aryl or -(CH 2 ) n -heteroaryl, wherein such groups are unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen or lower alkoxy, or is lower alkyl, -(CH 2 ) n -cycloalkyl; or R 3 and R 4 form together with the N-atom a heterocyclic ring; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula I or their tautomeric forms are good inhibitors of the glycine transporter 1 (GIyT-1), and that they have a good selectivity to glycine transporter 2 (GIyT-2) inhibitors, useful for the treatment of schizophrenia.
摘要翻译：本发明涉及以下通式的化合物：其中R 1是 - （CH 2）n - 芳基或 - （CH 2）其中这些基团是未取代的或被一个或多个选自以下的取代基取代：卤素，被卤素取代的低级烷基，低级烷氧基，低级烷基，低级烷氧基，氰基，硝基，被卤素或吗啉基取代的-O-低级烷基; R 2是 - （CH 2）n - 芳基或 - （CH 2 2）n - 其中这些基团是未取代的或被一个或多个选自低级烷基，低级烷氧基，卤素或-N（低级烷基）2个取代基取代的取代基取代。 R 3是氢或低级烷基; R 4是 - （CH 2）n - 芳基或 - （CH 2）n - 其中这些基团是未取代的或被一个或多个选自卤素或低级烷氧基的取代基取代，或者是低级烷基， - （CH 2 CH 2） ñ - 环烷基; 或R 3和R 4形成与N-原子一起形成杂环; n为0,1或2; 及其药学上可接受的酸加成盐。已经发现，通式I或其互变异构形式的化合物是甘氨酸转运蛋白1（GlyY-1）的良好抑制剂，并且它们对甘氨酸转运蛋白2（GlyT-2）抑制剂具有良好的选择性，可用于治疗精神分裂症。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式