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公开(公告)号：US06642398B2
公开(公告)日：2003-11-04
申请号：US10324929
申请日：2002-12-20
申请人： Thomas Richard Belliotti , Justin Stephen Bryans , Ihoezo Victor Ekhato , Augustine Tobi Osuma , Robert Michael Schelkun , Jacob Bradley Schwarz , Andrew John Thorpe , Lawrence David Wise , David Juergen Wustrow , Po-Wai Yuen
发明人： Thomas Richard Belliotti , Justin Stephen Bryans , Ihoezo Victor Ekhato , Augustine Tobi Osuma , Robert Michael Schelkun , Jacob Bradley Schwarz , Andrew John Thorpe , Lawrence David Wise , David Juergen Wustrow , Po-Wai Yuen
IPC分类号： C07D1000
CPC分类号： C07C229/32 , C07B2200/07 , C07C229/08 , C07C229/20 , C07C229/22 , C07C229/30 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14
摘要： The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
摘要翻译： 本发明是一系列新型的单取代和二取代的3-丙基γ-氨基丁酸，其化合物可用作治疗癫痫，微弱发作，运动功能减退，颅内疾病，神经变性障碍，抑郁症，焦虑症，恐慌症， 疼痛，神经病理学障碍，关节炎，睡眠障碍，IBS和胃损伤。 制备化合物和有用的中间体的方法也是本发明的一部分。
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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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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：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：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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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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公开(公告)号：US06436974B1
公开(公告)日：2002-08-20
申请号：US09980187
申请日：2001-11-30
IPC分类号： A61K314245
CPC分类号： C07D403/04 , C07D413/04
摘要： The instant invention is a novel series of amino heterocycles useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, and sleep disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.
摘要翻译： 本发明是用于治疗癫痫，微弱发作，运动功能减退，颅内障碍，神经变性障碍，抑郁，焦虑，恐慌，疼痛，神经病理学障碍和睡眠障碍的新型氨基杂环。 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：US5945421A
公开(公告)日：1999-08-31
申请号：US909171
申请日：1997-08-11
申请人： Thomas Richard Belliotti , Clifton John Blankley , Suzanne Ross Kesten , Lawrence David Wise , David Juergen Wustrow
发明人： Thomas Richard Belliotti , Clifton John Blankley , Suzanne Ross Kesten , Lawrence David Wise , David Juergen Wustrow
IPC分类号： C07D215/12 , A61K31/495 , A61K31/47 , C07D401/06 , C07D403/06
CPC分类号： C07D215/12
摘要： This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.
摘要翻译： 本发明涉及作为多巴胺D4受体的拮抗剂的化合物，使用作为多巴胺D4受体的拮抗剂的化合物治疗精神病和精神分裂症的方法以及含有多巴胺D4受体拮抗剂的药学上可接受的组合物。
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公开(公告)号：US07250433B2
公开(公告)日：2007-07-31
申请号：US10795760
申请日：2004-03-08
申请人： Nancy Sue Barta , Norman Lloyd Colbry , Raymond Hudack, Jr. , Kristin Knapp Lin , Jacob Bradley Schwarz , Andrew John Thorpe , David Juergen Wustrow , Zhijian Zhu
发明人： Nancy Sue Barta , Norman Lloyd Colbry , Raymond Hudack, Jr. , Kristin Knapp Lin , Jacob Bradley Schwarz , Andrew John Thorpe , David Juergen Wustrow , Zhijian Zhu
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07D257/04 , C07D271/07
摘要： This invention relates to novel tetrazole and oxadiazalone β-amino acids derivatives of the formula wherein G is wherein R1 through R4 are defined as in the specification, pharmaceutical compositions containing them and their use for the treatment of various central nervous system and other disorders. The cyclopropyl β-amino acids derivatives of this invention exhibit activity as alpha2delta ligands (α2δ ligands). Such compounds have affinity for the α2δ subunit of a calcium channel.
摘要翻译： 本发明涉及下式的新型四唑和恶二唑类β-氨基酸衍生物，其中G是其中R 1至R 4定义如说明书中所定义，含有它们的药物组合物 及其用于治疗各种中枢神经系统等疾病的用途。 本发明的环丙基β-氨基酸衍生物表现出作为α2delta配体（α2delta配体）的活性。 这些化合物对钙离子通道的α2delta亚基具有亲和力。
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