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1.发明授权Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production 失效α-（N-亚磺酰氨基）乙酰胺化合物作为β-淀粉样蛋白肽生产的抑制剂公开(公告)号：US08093276B2
公开(公告)日：2012-01-10
申请号：US12407029
申请日：2009-03-19
IPC分类号： A61K31/4245 , A61P25/00
CPC分类号： C07D271/06 , A61K31/4245
摘要： The present invention provides a method for the treatment of head trauma, traumatic brain injury, and/or dementia pugilistica comprising administering a therapeutically effective amount of (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide.
摘要翻译： 本发明提供一种治疗头部创伤，创伤性脑损伤和/或痴呆症的方法，包括给予治疗有效量的（2R）-2 - [[（4-氯苯基）磺酰基] [[2-氟 - 4-（1,2,4-恶二唑-3-基）苯基]甲基]氨基] -5,5,5-三氟戊酰胺。
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2.发明授权Alpha-(N-sulfonamido)acetamide compounds incorporating deuterium as inhibitors of beta amyloid peptide production 有权结合氘作为β淀粉样蛋白肽生产抑制剂的α-（N-亚磺酰氨基）乙酰胺化合物公开(公告)号：US08044077B2
公开(公告)日：2011-10-25
申请号：US12723936
申请日：2010-03-15
IPC分类号： A61K31/4245 , C07D271/06 , A61P25/28
CPC分类号： C07D271/06 , A61K31/4245
摘要： The present disclosure provides novel deuterated alpha-(N-sulfonamido)acetamide compounds, their pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease, head trauma, traumatic brain injury, and/or dementia pugilistica and/or other conditions associated with β-amyloid peptide.
摘要翻译： 本公开提供了新的氘代α-（N-亚磺酰氨基）乙酰胺化合物，其药物组合物及其制备方法和治疗阿尔茨海默氏病，头部创伤，创伤性脑损伤和/或痴呆症和/或其他相关病症的方法 与β-淀粉样蛋白肽。
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3.发明授权Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production 有权α-（N-亚磺酰氨基）乙酰胺化合物作为β-淀粉样蛋白肽生产的抑制剂公开(公告)号：US08350084B2
公开(公告)日：2013-01-08
申请号：US13299703
申请日：2011-11-18
申请人： John E. Starrett, Jr. , Kevin W. Gillman , Richard E. Olson , Lawrence R. Marcin , Bang-Chi Chen , Huiping Zhang
发明人： John E. Starrett, Jr. , Kevin W. Gillman , Richard E. Olson , Lawrence R. Marcin , Bang-Chi Chen , Huiping Zhang
IPC分类号： C07C311/16
CPC分类号： C07C311/19 , C07C237/06 , C07C253/30 , C07D271/06 , Y02P20/582 , C07C255/50
摘要： The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide.
摘要翻译： 本发明提供了一种新的α-（N-亚磺酰氨基）乙酰胺化合物，其药物组合物，其制备方法和治疗阿尔茨海默病和与淀粉样蛋白肽相关的其它病症的方法。
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4.发明授权Alpha-(N-sulfonamido)acetamide compound as an inhibitor of beta amyloid peptide production 有权α-（N-亚磺酰氨基）乙酰胺化合物作为β-淀粉样蛋白肽生产的抑制剂公开(公告)号：US08084477B2
公开(公告)日：2011-12-27
申请号：US12249180
申请日：2008-10-10
IPC分类号： A61K31/4245 , C07D271/06 , A61P25/28
CPC分类号： C07C311/19 , C07C237/06 , C07C253/30 , C07D271/06 , Y02P20/582 , C07C255/50
摘要： The present invention provides a novel alpha-(N-sulfonamido)acetamide compound, its pharmaceutical composition, processes thereof and a method for the treatment of Alzheimer's disease and other conditions associated with β-amyloid peptide.
摘要翻译： 本发明提供了一种新的α-（N-亚磺酰氨基）乙酰胺化合物，其药物组合物，其制备方法和治疗阿尔茨海默病和与淀粉样蛋白肽相关的其它病症的方法。
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5.发明授权4-arylspirocycloalkyl-2-aminopyrimidine carboxamide KCNQ potassium channel modulators 有权4-芳基螺环烷基-2-氨基嘧啶甲酰胺KCNQ钾通道调节剂公开(公告)号：US07091202B2
公开(公告)日：2006-08-15
申请号：US11222123
申请日：2005-09-08
IPC分类号： C07D239/42 , C07D401/04 , C07D401/08 , C07D413/12 , A61K31/505
CPC分类号： C07D401/12 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/12 , C07D405/14
摘要： The invention encompasses compounds of Formula I, which are blockers of KCNQ channels. Blockers of KCNQ channels are known to enchance cognition in laboratory animals. The invention includes, salts, solvates, compositions, and methods of use
摘要翻译： 本发明包括作为KCNQ通道阻断剂的式I化合物。 已知KCNQ通道的阻断剂对实验室动物的认知具有促进作用。 本发明包括盐，溶剂合物，组合物和使用方法
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公开(公告)号：US5945561A
公开(公告)日：1999-08-31
申请号：US66206
申请日：1998-04-24
申请人： John E. Starrett, Jr. , Kenneth M. Tramposch , Xina Nair , Peter R. Reczek , Anna Ericsson , Anne Marinier , Alain Martel , Fred C. Zusi
发明人： John E. Starrett, Jr. , Kenneth M. Tramposch , Xina Nair , Peter R. Reczek , Anna Ericsson , Anne Marinier , Alain Martel , Fred C. Zusi
IPC分类号： C07C63/66 , C07C65/19 , C07C65/28 , C07C69/00 , C07C69/76 , C07C323/61 , C07D213/55 , C07D307/54 , C07C63/36
CPC分类号： C07C69/00 , C07C323/61 , C07C63/66 , C07C65/19 , C07C65/28 , C07C69/76 , C07D213/55 , C07D307/54 , C07C2103/00 , C07C2103/24
摘要： Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.
摘要翻译： 某些具有通式的新的取代的（5,6） - 二氢蒽基化合物其中A，n，p，R1，R2，R3，R4，R5，R6，R7和R8如本说明书中所定义，表示类视黄醇样物质， 特别适用于预防手术后粘连。
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公开(公告)号：US6162817A
公开(公告)日：2000-12-19
申请号：US488227
申请日：2000-01-20
IPC分类号： C07D271/10 , A61K31/4245 , A61P1/00 , A61P9/08 , A61P9/10 , A61P11/06 , A61P15/10 , A61P25/00 , A61P25/06 , A61P43/00 , C07D271/113 , C07O271/113
CPC分类号： C07D271/113
摘要： The present invention provides novel carbamate oxadiazolone derivatives having the general formula ##STR1## wherein R.sup.1 and R.sup.2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of the large conductance calcium-activated potassium channels.
摘要翻译： 本发明提供新的具有通式的氨基甲酸酯恶二唑酮衍生物，其中R1和R2如本文所定义，或其无毒的药学上可接受的盐或溶剂合物，并且可用于治疗对大电导钙 - 活化钾通道。
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公开(公告)号：US5869509A
公开(公告)日：1999-02-09
申请号：US902684
申请日：1997-07-30
申请人： Jeffrey L. Romine , Scott W. Martin , Piyasena Hewawasam , Nicholas A. Meanwell , Valentin K. Gribkoff , John E. Starrett, Jr.
发明人： Jeffrey L. Romine , Scott W. Martin , Piyasena Hewawasam , Nicholas A. Meanwell , Valentin K. Gribkoff , John E. Starrett, Jr.
IPC分类号： C07D271/02 , A61K31/4164 , A61K31/4166 , A61K31/4196 , A61K31/4245 , A61P9/10 , A61P25/00 , A61P25/08 , A61P43/00 , C07D233/32 , C07D233/54 , C07D233/64 , C07D233/70 , C07D233/74 , C07D233/76 , C07D235/12 , C07D249/08 , C07D249/12 , C07D249/14 , C07D263/58 , C07D271/10 , C07D271/113 , C07D413/10 , A61K31/42 , A61K31/425 , C07D271/06
CPC分类号： C07D263/58 , C07D233/64 , C07D233/70 , C07D233/76 , C07D235/12 , C07D249/12 , C07D249/14 , C07D271/113 , C07D413/10
摘要： Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R.sup.a, R.sup.b and R.sup.c each are independently selected from hydrogen, halogen, OH, CF.sub.3, ##STR2## provided R.sup.c is not hydrogen; and when R.sup.a and R.sup.b are hydrogen, R.sup.c may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol- 2-yl, and pyridinyl; R.sup.d and R.sup.e each are independently selected from hydrogen, halogen, CF.sub.3, NO.sub.2 or imidazol-1-yl; m, n and p each are independently selected from an integer of O or 1; and R.sup.f and R.sup.g each are independently hydrogen; C.sub.1-4 alkyl; or R.sup.f and R.sup.g, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine, N-benzylpiperazine and imidazolinone.
摘要翻译： 式1的新型化合物可用于治疗对大电导钙激活钾通道的开放剂起反应的病症：其中“Het”是选择性杂环部分组之一; Z独立地选自O或S; Ra，Rb和Rc各自独立地选自氢，卤素，OH，CF 3，提供的R c不是氢; 当R a和R b为氢时，R c可以是选自咪唑-1-基，吗啉代甲基，N-甲基咪唑-2-基和吡啶基的杂环部分。 Rd和Re各自独立地选自氢，卤素，CF 3，NO 2或咪唑-1-基; m，n和p各自独立地选自O或1的整数; Rf和Rg各自独立地为氢; C 1-4烷基; 或R f和R g与它们所连接的氮原子一起是选自N-甲基哌嗪，吗啉，硫代吗啉，N-苄基哌嗪和咪唑啉酮的杂环部分。
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公开(公告)号：US4904770A
公开(公告)日：1990-02-27
申请号：US173473
申请日：1988-03-24
申请人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
发明人： John E. Starrett, Jr. , Muzammil M. Mansuri , John C. Martin , Carl E. Fuller , Henry G. Howell
IPC分类号： C07D405/04 , C07H19/04 , C07H19/073
CPC分类号： C07D405/04 , C07H19/04
摘要： There are disclosed novel processes for producing 2',3'-dideoxy-2'3'-didehydronucleosides, for example, 2',3'-dideoxy-2',3'-didehydrothymidine in high yields and on a large scale. The compounds so-produced are useful as antiviral agents, especially as agents effective against the human immunodeficiency viruses (HIV).
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公开(公告)号：US07169803B2
公开(公告)日：2007-01-30
申请号：US11074288
申请日：2005-03-07
IPC分类号： A61K31/405 , C07D209/34
CPC分类号： C07D209/34 , C07D403/12
摘要： The present invention provides novel N-substituted fluorooxindoles having the general Formula I wherein the wavy bond represents the racemate, the (R)-enantiomer or the (S)-enantiomer and m, n, p, q, A, B, D, Q, X, and Z are as defined below, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.
摘要翻译： 本发明提供具有通式I的新型N-取代的氟代吲哚，其中波状键表示外消旋物，（R） - 对映体或（S） - 对映体，m，n，p，q，A，B，D， Q，X和Z如下所定义，或其无毒的药学上可接受的盐或溶剂化物，并且可用于治疗对钾通道开放有响应的病症。
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