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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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公开(公告)号：US20050272783A1
公开(公告)日：2005-12-08
申请号：US11173073
申请日：2005-07-01
IPC分类号： A61P1/04 , A61K31/195 , A61K31/197 , A61K31/198 , A61P1/00 , A61P1/12 , A61P1/14 , A61P3/10 , A61P5/24 , A61P7/10 , A61P9/00 , A61P15/00 , A61P17/06 , A61P19/02 , A61P21/00 , A61P21/02 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/16 , A61P29/00 , C07C229/08 , C07C229/28 , C07C229/34 , A61K31/44 , C07D213/56
CPC分类号： C07C229/08 , A61K31/195 , A61K31/198 , C07C229/28 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , Y02A50/415
摘要： This invention relates to certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric pain and other disorders.
摘要翻译： 本发明涉及结合钙通道的α-2-δ（α2delta）亚基的某些β-氨基酸。 这些化合物及其药学上可接受的盐可用于治疗各种精神病性疼痛和其它疾病。
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公开(公告)号：US07064147B2
公开(公告)日：2006-06-20
申请号：US10401060
申请日：2003-03-27
IPC分类号： A61K31/195 , C07C229/00
CPC分类号： C07C229/08 , A61K31/195 , A61K31/198 , C07C229/28 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , Y02A50/415
摘要： This invention relates to certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders.
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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：US07388023B2
公开(公告)日：2008-06-17
申请号：US11567878
申请日：2006-12-07
申请人： Peter Garth Blazecka , Joseph Richard Bozelak , Norman Lloyd Colbry , Timothy Thomas Curran , Annise Paige Goodman , Kevin E. Henegar , Garrett Hoge , Paul D. Johnson , Augustine Tobi Osuma , Mark Stephen Plummer , Jacob Bradley Schwarz , Derek Clinton Vrieze , Ji Zhang
发明人： Peter Garth Blazecka , Joseph Richard Bozelak , Norman Lloyd Colbry , Timothy Thomas Curran , Annise Paige Goodman , Kevin E. Henegar , Garrett Hoge , Paul D. Johnson , Augustine Tobi Osuma , Mark Stephen Plummer , Jacob Bradley Schwarz , Derek Clinton Vrieze , Ji Zhang
IPC分类号： A61K31/44 , A61K31/195 , C07D213/38 , C07D231/46 , C07C53/134 , C07C53/126
CPC分类号： C07C229/08 , C07B2200/07 , C07C227/32 , C07C229/28 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D263/26 , Y02P20/582
摘要： Certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders. Also disclosed are methods of making the β-amino acids.
摘要翻译： 公开了结合钙通道的α-2-δ（α2delta）亚基的某些β-氨基酸。 这些化合物及其药学上可接受的盐可用于治疗各种精神病，疼痛和其它疾病。 还公开了制备β-氨基酸的方法。
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公开(公告)号：US07179934B2
公开(公告)日：2007-02-20
申请号：US10949907
申请日：2004-09-24
申请人： Peter Garth Blazecka , Joseph Richard Bozelak , Norman Lloyd Colbry , Timothy Thomas Curran , Annise Paige Goodman , Kevin E. Henegar , Garrett Hoge , Paul D. Johnson , Augustine Tobi Osuma , Mark Stephen Plummer , Jacob Bradley Schwarz , Derek Clinton Vrieze , Ji Zhang
发明人： Peter Garth Blazecka , Joseph Richard Bozelak , Norman Lloyd Colbry , Timothy Thomas Curran , Annise Paige Goodman , Kevin E. Henegar , Garrett Hoge , Paul D. Johnson , Augustine Tobi Osuma , Mark Stephen Plummer , Jacob Bradley Schwarz , Derek Clinton Vrieze , Ji Zhang
IPC分类号： C07C69/025 , C07C69/533
CPC分类号： C07C229/08 , C07B2200/07 , C07C227/32 , C07C229/28 , C07C229/34 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D263/26 , Y02P20/582
摘要： Certain β-amino acids that bind to the alpha-2-delta (α2δ) subunit of a calcium channel are disclosed. These compounds and their pharmaceutically acceptable salts are useful in the treatment of a variety of psychiatric, pain and other disorders. Also disclosed are methods of making the β-amino acids.
摘要翻译： 公开了结合钙通道的α-2-δ（α2delta）亚基的某些β-氨基酸。 这些化合物及其药学上可接受的盐可用于治疗各种精神病，疼痛和其它疾病。 还公开了制备β-氨基酸的方法。
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公开(公告)号：US07030267B2
公开(公告)日：2006-04-18
申请号：US10760032
申请日：2004-01-16
IPC分类号： C07C229/46 , C07C229/00
CPC分类号： C07C229/46 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2602/50
摘要： This invention relates to novel cyclopropyl β-amino acids derivatives of the formula 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环丙基β-氨基酸衍生物：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。 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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公开(公告)号：US08278457B2
公开(公告)日：2012-10-02
申请号：US12823224
申请日：2010-06-25
申请人： Anton F. J. Fliri , Randall James Gallaschun , Christopher John O'Donnell , Jacob Bradley Schwarz , Barbara E. Segelstein
发明人： Anton F. J. Fliri , Randall James Gallaschun , Christopher John O'Donnell , Jacob Bradley Schwarz , Barbara E. Segelstein
IPC分类号： C07D291/00 , A61K31/335
CPC分类号： C07D409/14 , C07C307/02 , C07C311/07 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D213/65 , C07D295/096 , C07D307/22 , C07D307/42 , C07D333/38 , C07D405/12 , C07D407/12 , C07D409/04 , C07D409/12
摘要： The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.
摘要翻译： 本发明涉及一类化合物，包括具有式I结构的化合物的药学上可接受的盐：如说明书中所定义的。 本发明还涉及包含和使用式I化合物的组合物。
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9.发明申请Oxopiperdinyl And Pyranyl Sulfonamides and Pharmaceutical Compositions Thereof 审中-公开氧哌啶基和吡喃磺酰胺及其药物组合物公开(公告)号：US20110172297A1
公开(公告)日：2011-07-14
申请号：US13061684
申请日：2009-09-18
申请人： Kimberly Gail Estep , Antone F.J. Fliri , Randall James Gallaschun , Christopher John O'Donnell , Nandini Chaturbhai Patel , Jacob Bradley Schwarz , Longfei Xie
发明人： Kimberly Gail Estep , Antone F.J. Fliri , Randall James Gallaschun , Christopher John O'Donnell , Nandini Chaturbhai Patel , Jacob Bradley Schwarz , Longfei Xie
IPC分类号： A61K31/351 , C07D309/14 , C07D409/10 , C07D405/10 , C07D211/56 , A61K31/381 , A61P25/00 , A61P25/28 , A61P9/10 , A61P27/02 , A61P25/16 , A61P25/08 , A61P25/06 , A61P25/18 , A61P25/22
CPC分类号： C07D211/76 , C07D309/14 , C07D405/10 , C07D409/10
摘要： The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of Formula (I): as defined in the specification. The invention is also directed to compositions containing the compounds of Formula (I) as AMPA modulators.
摘要翻译： 本发明涉及一类化合物，包括具有式（I）结构的化合物的药学上可接受的盐：如说明书中所定义的。 本发明还涉及含有式（I）化合物作为AMPA调节剂的组合物。
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公开(公告)号：US20090197859A1
公开(公告)日：2009-08-06
申请号：US12365305
申请日：2009-02-04
IPC分类号： A61K31/496 , C07D401/14 , A61K31/551 , A61P25/18 , A61K31/397 , C07D243/08
CPC分类号： C07D401/06 , C07D213/81 , C07D401/12 , C07D401/14 , G11C5/025 , G11C5/063 , G11C13/0004 , G11C13/0023 , G11C13/003 , G11C2213/72 , G11C2213/74 , G11C2213/78 , G11C2213/79 , H01L27/1021
摘要： The present invention relates to novel pyridinyl derivatives of Formula wherein Y, Z, L, R1 through R11, n, m, p, q, t are as defined herein, that are 5-HT receptor ligands, particularly the 5-HT6 subtype, and as such are useful for treating diseases wherein modulation of 5-HT activity is desired. The present invention relates to novel pyridinyl derivatives including their pharmaceutically acceptable salts. The invention also relates to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing and the uses of such compounds in treating diseases of the central nervous system such as schizophrenia.
摘要翻译： 本发明涉及新的式I的吡啶基衍生物，其中Y，Z，L，R 1至R 11，n，m，p，q，t如本文所定义，其为5-HT受体配体，特别是5-HT6亚型， 并且因此可用于治疗其中期望5-HT活性的调节的疾病。 本发明涉及包括其药学上可接受的盐的新的吡啶基衍生物。 本发明还涉及制备用于制备含有此类化合物的药物组合物的中间体的方法，以及用于治疗中枢神经系统疾病如精神分裂症的用途。
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