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公开(公告)号:US06194416B1
公开(公告)日:2001-02-27
申请号:US08844307
申请日:1997-04-10
申请人: Leander Merritt , Jon K. Reel , John S. Ward , Celia A. Whitesitt
发明人: Leander Merritt , Jon K. Reel , John S. Ward , Celia A. Whitesitt
IPC分类号: A61K31496
CPC分类号: C07D451/06 , C07D209/52 , C07D241/18 , C07D271/08 , C07D403/12 , C07D413/12 , C07D453/02 , C07D471/08 , C07D487/08
摘要: The present invention relates to therapeutically active compounds of the formula: wherein G is an azacyclic or azabicyclic ring system, W is oxygen or sulfur, r is 0, 1, or 2, and R is defined in the specification; and to methods of treatment using, and pharmaceutical compositions comprising, these compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
摘要翻译: 本发明涉及下式的治疗活性化合物:其中G是氮杂环或氮杂双环系,W是氧或硫,r是0,1或2,R在说明书中定义; 以及使用这些化合物的治疗方法和药物组合物。 新型化合物可用于治疗由毒蕈碱胆碱能系统功能障碍引起的中枢神经系统疾病。
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公开(公告)号:US5556981A
公开(公告)日:1996-09-17
申请号:US453532
申请日:1995-05-30
申请人: Donald B. Boyd , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , K. Jeff Thrasher , Venkatraghaven Vasudevan , Celia A. Whitesitt
发明人: Donald B. Boyd , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , K. Jeff Thrasher , Venkatraghaven Vasudevan , Celia A. Whitesitt
IPC分类号: A61K31/40 , A61K31/401 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K38/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D471/04 , C07D491/10 , C07F9/6524 , C07K5/06 , C07K5/078 , C07K14/81 , C07D413/10
CPC分类号: C07D403/14 , C07D209/08 , C07D401/14 , C07D403/10 , C07D403/12 , C07D471/04 , C07D491/10 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
摘要翻译: 本发明提供新的杂环衍生物,其药物制剂及其在哺乳动物中拮抗血管紧张素II受体的用途。
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3.N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds 失效
标题翻译: N-(芳基/杂芳基)氨基酸酯,包含其的药物组合物,以及通过使用这些化合物抑制α-淀粉样肽释放和/或其合成的方法公开(公告)号:US06399628B1
公开(公告)日:2002-06-04
申请号:US09266908
申请日:1999-03-12
申请人: James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Jon K. Reel , Eugene D. Thorsett , Celia A. Whitesitt
发明人: James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Jon K. Reel , Eugene D. Thorsett , Celia A. Whitesitt
IPC分类号: C07D21538
CPC分类号: C07C259/10 , A61K31/216 , C07C229/18 , C07C257/14 , C07C257/16 , C07C2601/02 , C07C2601/08 , C07C2601/14
摘要: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译: 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物,因此具有治疗阿尔茨海默病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及用这种药物组合物预防性和治疗性地治疗阿尔茨海默病的方法。
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公开(公告)号:US5484780A
公开(公告)日:1996-01-16
申请号:US355778
申请日:1994-12-14
申请人: Donald B. Boyd , Kenneth L. Hauser , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Kumiko Takeuchi , K. Jeff Thrasher , Celia A. Whitesitt
发明人: Donald B. Boyd , Kenneth L. Hauser , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Kumiko Takeuchi , K. Jeff Thrasher , Celia A. Whitesitt
IPC分类号: C07D233/64 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/675 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P43/00 , C07D233/58 , C07D233/70 , C07D233/88 , C07D233/90 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/6506 , C07F9/6524 , C07F9/02 , C07D231/10
CPC分类号: C07D401/12 , C07D233/88 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.
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公开(公告)号:US5401851A
公开(公告)日:1995-03-28
申请号:US049917
申请日:1993-04-20
申请人: Donald B. Boyd , Kenneth L. Hauser , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Kumiko Takeuchi , K. Jeff Thrasher , Celia A. Whitesitt
发明人: Donald B. Boyd , Kenneth L. Hauser , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Kumiko Takeuchi , K. Jeff Thrasher , Celia A. Whitesitt
IPC分类号: C07D233/64 , A61K31/41 , A61K31/415 , A61K31/4164 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/675 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P43/00 , C07D233/58 , C07D233/70 , C07D233/88 , C07D233/90 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07F9/6506 , C07F9/6524 , A61K31/505 , C07D213/06 , C07D239/26
CPC分类号: C07D401/12 , C07D233/88 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their methods of use for antagonizing angiotensin II receptors in mammals.
摘要翻译: 本发明提供新颖的苯基和杂环衍生物,其药物制剂及其用于拮抗哺乳动物血管紧张素II受体的方法。
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6.
公开(公告)号:US5073566A
公开(公告)日:1991-12-17
申请号:US444456
申请日:1989-11-30
申请人: Sherryl L. Lifer , Winston S. Marshall , Fariborz Mohamadi , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Celia A. Whitesitt
发明人: Sherryl L. Lifer , Winston S. Marshall , Fariborz Mohamadi , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Celia A. Whitesitt
IPC分类号: A61K31/075 , A61K31/00 , A61K31/085 , A61K31/13 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/41 , A61K31/415 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07C63/331 , C07C65/24 , C07C65/34 , C07C69/76 , C07C205/56 , C07C229/42 , C07C235/24 , C07C255/41 , C07D207/34 , C07D231/12 , C07D231/14 , C07D231/20 , C07D231/38 , C07D233/88 , C07D233/90 , C07D249/04 , C07D249/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D257/04 , C07D257/06 , C07D311/82 , C07D311/84 , C07D311/86 , C07D311/88 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12
CPC分类号: C07D257/04 , C07C229/42 , C07C255/41 , C07C65/24 , C07C65/34 , C07C69/76 , C07D207/34 , C07D231/14 , C07D233/88 , C07D233/90 , C07D249/10 , C07D257/06 , C07D403/04 , C07D403/12 , C07D405/12
摘要: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
摘要翻译: 本发明提供新颖的苯基和杂环衍生物,它们的药物制剂及其在哺乳动物中拮抗血管紧张素II受体的用途。
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公开(公告)号:US5814646A
公开(公告)日:1998-09-29
申请号:US398188
申请日:1995-03-02
申请人: Lawrence J. Heinz , Jill A. Panetta , Michael L. Phillips , Jon K. Reel , John K. Shadle , Richard L. Simon , Celia A. Whitesitt
发明人: Lawrence J. Heinz , Jill A. Panetta , Michael L. Phillips , Jon K. Reel , John K. Shadle , Richard L. Simon , Celia A. Whitesitt
IPC分类号: A61K31/433 , A61K31/415 , A61K31/425 , C07D285/135
CPC分类号: A61K31/433
摘要: A method of protecting a warm-blooded mammal from the progression of Alzheimer's disease, which comprises administering an effective amount of a compound of general formula. ##STR1## in which: R.sup.1 represents an optionally substituted aromatic or heteroaromatic group; L.sup.1 and L.sup.2 each independently represents a bond or an unbranched (1-4C) alkylene group, which alkylene group may optionally bear a (1-4C) alkyl, phenyl or phenyl (1-2C) alkyl substituent; one of Y.sup.1 and Y.sup.2 represents NR.sup.3 and the other represents O, S or NR.sup.3, in which R.sup.3 represent hydrogen, hydroxyl, (1-4C) alkoxy, (1-4C) alkyl or di (1-4C) alkylamino; Z represents O or S; and R.sup.2 represents (3-8C) cycloalkyl, heterocyclyl, and optionally substituted aromatic or heteroaromatic group, or together with L.sup.2, (1-10C) alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译: 一种保护温血哺乳动物免受阿尔茨海默病进展的方法,其包括施用有效量的通式化合物。 其中:R1表示任选取代的芳族或杂芳族基团; L1和L2各自独立地表示键或非支链(1-4C)亚烷基,该亚烷基可以任选地具有(1-4C)烷基,苯基或苯基(1-2C)烷基取代基; Y 1和Y 2中的一个表示NR 3,另一个表示O,S或NR 3,其中R 3表示氢,羟基,(1-4C)烷氧基,(1-4C)烷基或二(1-4C)烷基氨基; Z表示O或S; 并且R 2表示(3-8C)环烷基,杂环基和任选取代的芳族或杂芳族基团,或与L2,(1-10C)烷基一起; 或其药学上可接受的盐。
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公开(公告)号:US5612360A
公开(公告)日:1997-03-18
申请号:US49916
申请日:1993-04-20
申请人: Donald B. Boyd , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , K. Jeff Thrasher , Venkatraghavan Vasudevan , Celia A. Whitesitt
发明人: Donald B. Boyd , Sherryl L. Lifer , Winston S. Marshall , Alan D. Palkowitz , William Pfeifer , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , K. Jeff Thrasher , Venkatraghavan Vasudevan , Celia A. Whitesitt
IPC分类号: A61K31/40 , A61K31/401 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/4184 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K38/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P13/02 , A61P15/00 , A61P27/02 , A61P27/06 , A61P43/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D231/56 , C07D235/06 , C07D235/08 , C07D235/12 , C07D235/14 , C07D235/16 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D471/04 , C07D491/10 , C07F9/6524 , C07K5/06 , C07K5/078 , C07K14/81 , A61K31/41 , C07D471/00
CPC分类号: C07D403/14 , C07D209/08 , C07D401/14 , C07D403/10 , C07D403/12 , C07D471/04 , C07D491/10 , C07K5/06139 , C07K5/06191 , A61K38/00
摘要: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.
摘要翻译: 本发明提供新的杂环衍生物,其药物制剂及其在哺乳动物中拮抗血管紧张素II受体的用途。
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公开(公告)号:US5563278A
公开(公告)日:1996-10-08
申请号:US453537
申请日:1995-05-30
申请人: Sherryl L. Lifer , Winston S. Marshall , Fariborz Mohamadi , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Celia A. Whitesitt
发明人: Sherryl L. Lifer , Winston S. Marshall , Fariborz Mohamadi , Jon K. Reel , Richard L. Simon , Mitchell I. Steinberg , Celia A. Whitesitt
IPC分类号: A61K31/075 , A61K31/00 , A61K31/085 , A61K31/13 , A61K31/16 , A61K31/18 , A61K31/19 , A61K31/35 , A61K31/352 , A61K31/40 , A61K31/41 , A61K31/415 , A61P5/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P43/00 , C07C63/331 , C07C65/24 , C07C65/34 , C07C69/76 , C07C205/56 , C07C229/42 , C07C235/24 , C07C255/41 , C07D207/34 , C07D231/12 , C07D231/14 , C07D231/20 , C07D231/38 , C07D233/88 , C07D233/90 , C07D249/04 , C07D249/06 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/14 , C07D257/04 , C07D257/06 , C07D311/82 , C07D311/84 , C07D311/86 , C07D311/88 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , A61K31/215 , A61K31/275 , C07C69/66
CPC分类号: C07D257/04 , C07C229/42 , C07C255/41 , C07C65/24 , C07C65/34 , C07C69/76 , C07D207/34 , C07D231/14 , C07D233/88 , C07D233/90 , C07D249/10 , C07D257/06 , C07D403/04 , C07D403/12 , C07D405/12
摘要: This invention provides novel phenyl and heterocyclic derivatives, their pharmaceutical formulations and their use for antagonizing angiotensin II receptors in mammals.
摘要翻译: 本发明提供新颖的苯基和杂环衍生物,它们的药物制剂及其在哺乳动物中拮抗血管紧张素II受体的用途。
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10.N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting .beta.-amyloid peptide release and/or its synthesis by use of such compounds 失效
标题翻译: N-(芳基/杂芳基)氨基酸酯,包含其的药物组合物,以及通过使用这些化合物抑制β-淀粉样蛋白肽释放和/或其合成的方法公开(公告)号:US5965614A
公开(公告)日:1999-10-12
申请号:US975977
申请日:1997-11-21
申请人: James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Jon K. Reel , Eugene D. Thorsett , Celia A. Whitesitt
发明人: James E. Audia , Beverly K. Folmer , Varghese John , Lee H. Latimer , Jeffrey S. Nissen , Jon K. Reel , Eugene D. Thorsett , Celia A. Whitesitt
IPC分类号: A61K31/216 , C07C229/18 , C07C257/14 , C07C257/16 , C07C259/10 , A01N37/12 , A01N37/52 , C07C229/28
CPC分类号: C07C259/10 , A61K31/216 , C07C229/18 , C07C257/14 , C07C257/16 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要翻译: 公开了抑制β-淀粉样蛋白肽释放和/或其合成的化合物,因此具有治疗阿尔茨海默氏病的效用。 还公开了包含抑制β-淀粉样蛋白肽释放和/或其合成的化合物的药物组合物以及预防和治疗这些药物组合物的阿尔茨海默氏病的方法。
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