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1. 发明申请

US20080287547A1 Glycine Transport Inhibitors 失效
标题翻译：甘氨酸运输抑制剂
公开(公告)号：US20080287547A1
公开(公告)日：2008-11-20
申请号：US11718333
申请日：2005-12-21
申请人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Albert Andrzej Jaxa-Chamiec , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Albert Andrzej Jaxa-Chamiec , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/166 , A61P25/00 , C07C233/65 , A61P25/18
CPC分类号： C07C233/78 , C07C235/50 , C07C235/60 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/20 , C07D209/02 , C07D295/13 , C07D307/22
摘要： The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂化物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

2. 发明申请

US20090270510A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：US20090270510A1
公开(公告)日：2009-10-29
申请号：US11722213
申请日：2005-12-21
申请人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Martin Leonard Gilpin , Andrew Jonathan Harris , Justine Yeun Quai Lai , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simone Spada , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/166 , C07C321/10 , C07C233/78 , C07C211/27
CPC分类号： C07C235/60 , C07C211/27 , C07C233/78 , C07C235/50 , C07C323/62
摘要： The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂合物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

3. 发明申请

US20080255144A1 Acylated Piperidines as Glycine Transporter Inhibitors 审中-公开
标题翻译：酰化哌啶酮作为甘氨酸转运蛋白抑制剂
公开(公告)号：US20080255144A1
公开(公告)日：2008-10-16
申请号：US11908151
申请日：2006-03-09
申请人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Anthony William Dean , Paul Martin Doyle , Brian Evans , Martin Leonard Gilpin , Sharon Lisa Gough , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simon Edward Ward
发明人： Daniel Marcus Bradley , Clive Leslie Branch , Wai Ngor Chan , Steven Coulton , Anthony William Dean , Paul Martin Doyle , Brian Evans , Martin Leonard Gilpin , Sharon Lisa Gough , Jacqueline Anne Macritchie , Howard Robert Marshall , David John Nash , Roderick Alan Porter , Simon Edward Ward
IPC分类号： A61K31/496 , C07D241/04 , C07D405/10 , C07D401/10 , A61P25/18 , C07D401/04 , A61K31/495
CPC分类号： C07D231/12 , C07D209/08 , C07D213/56 , C07D213/74 , C07D295/192 , C07D307/54 , C07D333/24 , C07D405/12 , C07D471/04
摘要： The invention provides a compound of formula (I) or a salt or solvate thereof: wherein R1, n, X, Y and Z are as defined in the specification, and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.
摘要翻译：本发明提供式（I）化合物或其盐或溶剂合物：其中R 1，n，X，Y和Z如说明书中所定义，以及这些化合物的用途。该化合物抑制GlyT1转运蛋白并且可用于治疗某些神经和神经精神障碍，包括精神分裂症。

4. 发明申请

US20100216837A1 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸运输抑制剂
公开(公告)号：US20100216837A1
公开(公告)日：2010-08-26
申请号：US11722210
申请日：2005-12-21
申请人： Andrea Bozzoli , Daniel Marcus Bradley , Steven Coulton , Martin Leonard Gilpin , Jacqueline Anne MacRitchie , Roderick Alan Porter , Kevin Michael Thewlis
发明人： Andrea Bozzoli , Daniel Marcus Bradley , Steven Coulton , Martin Leonard Gilpin , Jacqueline Anne MacRitchie , Roderick Alan Porter , Kevin Michael Thewlis
IPC分类号： A61K31/4709 , C07C231/06 , A61K31/166 , C07D215/50 , A61K31/47 , C07D333/06 , A61K31/381 , C07D207/04 , A61K31/40 , A61P25/00
CPC分类号： C07C211/36 , C07C211/29 , C07C229/34 , C07C233/78 , C07C271/22 , C07C2601/08 , C07D215/50 , C07D295/13 , C07D333/20 , C07D409/12
摘要： The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂合物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

5. 发明申请

US20100137276A1 COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE 审中-公开
标题翻译：潜在的AMPA受体的化合物及其在医学中的应用
公开(公告)号：US20100137276A1
公开(公告)日：2010-06-03
申请号：US12447294
申请日：2007-11-01
申请人： Daniel Marcus Bradley , Wai Ngor Chan , Kevin Michael Thewlis , Simon Eward
发明人： Daniel Marcus Bradley , Wai Ngor Chan , Kevin Michael Thewlis , Simon Eward
IPC分类号： A61K31/4162 , C07D487/04 , C07D471/04 , A61K31/437 , A61K31/397 , A61P25/18
CPC分类号： C07D491/052 , C07D471/04
摘要： Compounds of formula (I), and salts and solvates thereof are provided: Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
摘要翻译：提供式（I）化合物及其盐和溶剂合物：制备方法，药物组合物及其作为药物的用途，例如治疗由谷氨酸受体功能的还原或不平衡介导的疾病或病症，如精神分裂症或认知障碍，也被披露。

6. 发明授权

US07572819B2 Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
标题翻译：增强谷氨酸受体的药物及其在药物中的应用
公开(公告)号：US07572819B2
公开(公告)日：2009-08-11
申请号：US11673044
申请日：2007-02-09
申请人： Daniel Marcus Bradley , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/445 , C07D213/56
CPC分类号： C07D213/64 , C07D213/42 , C07D213/50 , C07D213/61 , C07D213/84 , C07D213/85 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D333/20
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.
摘要翻译：公开了式（I）化合物或其药学上可接受的盐，溶剂合物或前体药物：其中R 1是C 1-6烷基，卤代C 1-6烷基，C 2-6烯基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; R 2和R 3可以相同或不同，为氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; 每个R 4可以相同或不同，为C 1-6烷基，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，硝基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; p为0,1或2; n为1或2; R 5和R 6可以相同或不同，为氢，卤素，C 1-6烷基，卤代C 1-6烷基，C 1-4烷氧基，卤代C 1-4烷氧基，氰基，氨基，单C 1-4烷基氨基或二C 1-4烷基氨基; 并且Het是噻吩基，吡啶基，嘧啶基，哒嗪基，嘧啶基，吡嗪基，咪唑基，吡唑基，吡咯基，喹啉基，噻唑基或呋喃基，其各自可以被一个或多个独立地选自C 1-6烷基， 1-6烷氧基，乙酰基，卤素，卤代C 1-6烷基，氰基，硝基，氨基，单C 1-4烷基氨基和二C 1-4烷基氨基。还公开了化合物的制备方法及其在药物中的用途，例如精神分裂症的治疗。

7. 发明授权

US07618969B2 Compounds which potentiate glutamate receptor and uses thereof in medicine 失效
公开(公告)号：US07618969B2
公开(公告)日：2009-11-17
申请号：US11573370
申请日：2005-08-05
申请人： Daniel Marcus Bradley , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D213/64 , C07D213/42 , C07D213/50 , C07D213/61 , C07D213/84 , C07D213/85 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D333/20
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

8. 发明申请

US20080194648A1 COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE 失效
公开(公告)号：US20080194648A1
公开(公告)日：2008-08-14
申请号：US11673044
申请日：2007-02-09
申请人： Daniel Marcus Bradley , Kevin Michael Thewlis , Simon Edward Ward
发明人： Daniel Marcus Bradley , Kevin Michael Thewlis , Simon Edward Ward
IPC分类号： A61K31/44 , A61P25/18 , C07D211/84
CPC分类号： C07D213/64 , C07D213/42 , C07D213/50 , C07D213/61 , C07D213/84 , C07D213/85 , C07D231/12 , C07D233/64 , C07D237/08 , C07D239/26 , C07D333/20
摘要： Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R1 is C1-6alkyl, haloC1-6alkyl, C2-6alkenyl, amino, monoC1-4alkylamino or diC1-4alkylamino; R2 and R3, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; each R4, which may be the same or different, is C1-6alkyl, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, nitro, amino, monoC1-4alkylamino or diC1-4alkylamino; p is 0, 1 or 2; n is 1 or 2; R5 and R6, which may be the same or different, are hydrogen, halogen, C1-6alkyl, haloC1-6alkyl, C1-4alkoxy, haloC1-4alkoxy, cyano, amino, monoC1-4alkylamino or diC1-4alkylamino; and Het is thienyl, pyridyl, pyrimidinyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl, pyrazolyl, pyrrolyl, quinolyl, thiazolyl or furyl, each of which may be substituted by one or more groups independently selected from the list consisting of C1-6alkyl, C1-6alkoxy, acetyl, halogen, haloC1-6alkyl, cyano, nitro, amino, monoC1-4alkylamino and diC1-4alkylamino. Methods of preparation of the compounds, and uses thereof in medicine, for example treatment of schizophrenia, are also disclosed.

9. 发明授权

US07745642B2 Glycine transport inhibitors 失效
标题翻译：甘氨酸转运抑制剂
公开(公告)号：US07745642B2
公开(公告)日：2010-06-29
申请号：US11718333
申请日：2005-12-21
申请人： Daniel Marcus Bradley , Roderick Alan Porter
发明人： Daniel Marcus Bradley , Roderick Alan Porter
IPC分类号： C07C233/78 , C07C211/36
CPC分类号： C07C233/78 , C07C235/50 , C07C235/60 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D205/04 , C07D207/20 , C07D209/02 , C07D295/13 , C07D307/22
摘要： The present invention relates to compounds of formula (I), or to salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
摘要翻译：本发明涉及式（I）化合物或其盐或溶剂化物，其用于制备用于治疗神经和神经精神障碍，特别是精神病，痴呆或注意力缺陷障碍的药物。本发明还包括制备这些化合物及其药物制剂的方法。

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