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公开(公告)号：US06245801B1
公开(公告)日：2001-06-12
申请号：US09673277
申请日：2000-10-13
申请人： Justin Stephen Bryans , Ihoezo Victor Ekhato , David Christopher Horwell , Rong Ling , Jean-Marie Receveur , David Juergen Wustrow
发明人： Justin Stephen Bryans , Ihoezo Victor Ekhato , David Christopher Horwell , Rong Ling , Jean-Marie Receveur , David Juergen Wustrow
IPC分类号： A61K3140
CPC分类号： C07D207/16
摘要： Branched alkyl pyrrolidines of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropatnological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公开了式（I）的支链烷基吡咯烷，并且可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，惊恐，疼痛和神经病学疾病的药物。 还公开了用于制备的方法和可用于制备的中间体。
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公开(公告)号：US06489352B2
公开(公告)日：2002-12-03
申请号：US09924803
申请日：2001-08-08
IPC分类号： C07D20954
CPC分类号： C07D209/96 , C07D205/12 , C07D209/44 , C07D209/46 , C07D209/54
摘要： Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公开的新型取代的氨基酸被公开并且可用作治疗癫痫，微弱发作，运动功能减退，颅内障碍，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛和神经病理学障碍的药物。 还公开了用于制备的方法和可用于制备的中间体。
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3.发明授权Conformationally constrained amino acid compounds having affinity for the alpha2delta subunit of a calcium channel 失效具有对钙通道的α2delta亚基具有亲和性的构象约束的氨基酸化合物公开(公告)号：US06316638B1
公开(公告)日：2001-11-13
申请号：US09622429
申请日：2000-08-16
IPC分类号： C07D20512
CPC分类号： C07D209/96 , C07D205/12 , C07D209/44 , C07D209/46 , C07D209/54
摘要： Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公开的新型取代的氨基酸被公开并且可用作治疗癫痫，微弱发作，运动功能减退，颅内障碍，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛和神经病理学障碍的药物。 还公开了用于制备的方法和可用于制备的中间体。
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公开(公告)号：US06921835B2
公开(公告)日：2005-07-26
申请号：US10448834
申请日：2003-05-30
申请人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
发明人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： A61P1/04 , A61K20060101 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/215 , A61P25/04 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P29/00 , C07C20060101 , C07C61/04 , C07C61/06 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/00 , C07C229/28 , C07C229/32 , C07C229/34 , C07D209/96 , C07D221/20 , C07D307/94 , C07D311/96
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
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5.发明授权4(3)substituted-4(3)-aminomethyl-(thio)pyran or piperidine derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders 失效4（3）取代-4（3） - 氨基甲基 - （硫代）吡喃或哌啶衍生物（=加巴喷丁类似物），其制备及其在治疗神经系统疾病中的应用公开(公告)号：US06545022B1
公开(公告)日：2003-04-08
申请号：US09529055
申请日：2000-04-07
申请人： Justin Stephen Bryans , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
发明人： Justin Stephen Bryans , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
IPC分类号： A61K31445
CPC分类号： C07F9/655363 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D257/04 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/59 , C07F9/6552
摘要： Novel amines of formulas 1D and 1E are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 式1D和1E的新型胺公开并且可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理学障碍，炎性疾病和胃肠道疾病，特别是IBS 。 还公开了用于制备的方法和可用于制备的中间体。
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公开(公告)号：US07122678B2
公开(公告)日：2006-10-17
申请号：US11078961
申请日：2005-03-11
申请人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
发明人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： C07D209/54 , C07C69/74 , C07C61/06
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
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公开(公告)号：US06635673B1
公开(公告)日：2003-10-21
申请号：US09485382
申请日：2000-02-08
申请人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
发明人： Justin Stephen Bryans , David Christopher Horwell , Andrew John Thorpe , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： A61K3119
CPC分类号： C07D221/20 , C07C49/417 , C07C69/608 , C07C69/612 , C07C205/51 , C07C205/53 , C07C229/28 , C07C229/34 , C07C2601/04 , C07C2601/08 , C07C2602/50 , C07D209/96 , C07D307/94 , C07D311/96
摘要： The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
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公开(公告)号：US06521650B1
公开(公告)日：2003-02-18
申请号：US09509917
申请日：2000-04-04
申请人： Thomas Richard Belliotti , Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
发明人： Thomas Richard Belliotti , Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
IPC分类号： C07D25704
CPC分类号： C07C311/32 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D257/04 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D407/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/59 , C07F9/6552 , C07F9/655363
摘要： Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 公开了式（I）的新型γ-氨基丁酸，并且可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经退行性疾病，抑郁症，焦虑，恐慌，疼痛，神经病理学障碍，炎症和胃肠损伤的药剂。 还公开了用于制备的方法和可用于制备的中间体。
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9.发明授权1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders 失效1-取代-1-氨基甲基 - 环烷烃衍生物（=加巴喷丁类似物），其制备及其在治疗神经障碍中的应用公开(公告)号：US06518289B1
公开(公告)日：2003-02-11
申请号：US09509905
申请日：2000-04-03
申请人： Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
发明人： Justin Stephen Bryans , Thomas Capiris , David Christopher Horwell , Clare Octavia Kneen , David Juergen Wustrow
IPC分类号： C07D25704
CPC分类号： C07D257/04 , C07C233/36 , C07C239/14 , C07C259/06 , C07C309/25 , C07C311/05 , C07C311/09 , C07C311/33 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/46 , C07C2603/74 , C07D211/26 , C07D271/07 , C07D285/18 , C07D309/04 , C07D335/02 , C07D401/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06 , C07D419/06 , C07F9/3808 , C07F9/383 , C07F9/59 , C07F9/6552 , C07F9/655363
摘要： Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A′ is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, especially irritable bowel syndrome.
摘要翻译： 式（1），（1C），（1F），（1G）和（1H）的新型胺或其药学上可接受的盐，其中n为0-2的整数; m为0〜3的整数; R是磺酰胺，酰胺，膦酸，杂环，磺酸或异羟肟酸; A'是选自（1），（2），（3），（4），（5）中的桥环，其中是连接点; Z 1至Z 4各自独立地选自氢和甲基; o是1至4的整数; 并且p为0至2的整数。在式（1）中，当m为2时，R不能为磺酸，n为1，并且可用作治疗癫痫，微弱发作，运动不良，颅内疾病的药剂 ，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，特别是肠易激综合征。
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公开(公告)号：US6153650A
公开(公告)日：2000-11-28
申请号：US254093
申请日：1999-03-01
申请人： Justin Stephen Bryans , David Christopher Horwell , Clare Octavia Kneen , Andrew John Thorpe , David Juergen Wustrow
发明人： Justin Stephen Bryans , David Christopher Horwell , Clare Octavia Kneen , Andrew John Thorpe , David Juergen Wustrow
IPC分类号： A61P1/00 , A61K31/197 , A61P1/04 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , C07C229/22 , C07C229/28 , C07C229/34 , C07C323/58 , A01N37/44 , C07C321/16 , C07C321/28
CPC分类号： C07C323/58 , C07C229/22 , C07C2101/14
摘要： Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： PCT No.PCT / US97 / 17997 Sec。 371日期1999年3月1日 102（e）1999年3月1日PCT PCT 1997年10月7日PCT公布。 公开号WO98 / 17627 日期：1998年4月30日公开了新的式（I）的γ-氨基丁酸，可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，炎症 ，和胃肠道损伤。 还公开了用于制备的方法和可用于制备的中间体。
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