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1.发明授权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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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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5.发明授权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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公开(公告)号：US5571925A
公开(公告)日：1996-11-05
申请号：US183685
申请日：1994-01-19
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 , C07D407/12
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.
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7.发明授权Disubstituted tetrazole leukotriene antagonists and methods for their use thereas 失效二取代四唑白三烯拮抗剂及其使用方法
公开(公告)号：US4820723A
公开(公告)日：1989-04-11
申请号：US085588
申请日：1987-08-14
IPC分类号： A61K31/41 , A61P11/00 , A61P37/08 , C07D257/04 , C07D403/06
CPC分类号： C07D257/04
摘要： The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive release or production of leukotrienes C.sub.4, D.sub.4 or E.sub.4 or any combination thereof. Such conditions include an immediate hypersensitivity reaction of the type represented by asthma, or by shock or other adverse cardiovascular effects.
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公开(公告)号：US4777299A
公开(公告)日：1988-10-11
申请号：US142112
申请日：1988-01-11
IPC分类号： C07C45/46 , C07C49/825 , C07C49/83 , C07C49/835 , C07C45/00
CPC分类号： C07C45/46 , C07C49/825 , C07C49/83 , C07C49/835
摘要： 1,3-Dialkylbenzenes are acylated and deprotected in a mixture of acetic or propionic acid and hydrobromic acid. The dihydroxyphenones thus produced are intermediates in the synthesis of leukotriene antagonists.
摘要翻译： 将1,3-二烷基苯酰化并在乙酸或丙酸和氢溴酸的混合物中脱保护。 由此产生的二羟基苯并噻吩是合成白三烯拮抗剂的中间体。
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公开(公告)号：US4195021A
公开(公告)日：1980-03-25
申请号：US845766
申请日：1977-10-26
IPC分类号： C07D205/08 , A61K31/395 , A61K31/397 , A61K31/44 , A61K31/4427 , A61P31/04 , C07D205/085 , C07D401/06
CPC分类号： C07D205/085
摘要： Novel 3-acylaminoazetidin-4-one antibiotic compounds, prepared by reduction of known 2-chloroazetidin-4-one compounds with tri(butyl)tin hydride, are antinicrobial agents.
摘要翻译： 通过用三（丁基）锡氢化物还原已知的2-氯氮杂环丁烷-4-酮化合物制备的新型3-酰氨基氮杂环丁烷-4-酮抗生素化合物是抗微生物剂。
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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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