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公开(公告)号：US5401745A
公开(公告)日：1995-03-28
申请号：US33595
申请日：1993-03-19
申请人： Scott W. Bagley , Prasun K. Chakravarty , Anna Chen , Daljit S. Dhanoa , Kenneth J. Fitch , William J. Greenlee , Elizabeth M. Naylor , James R. Tata , Thomas F. Walsh , David L. Williams, Jr.
发明人： Scott W. Bagley , Prasun K. Chakravarty , Anna Chen , Daljit S. Dhanoa , Kenneth J. Fitch , William J. Greenlee , Elizabeth M. Naylor , James R. Tata , Thomas F. Walsh , David L. Williams, Jr.
IPC分类号： C07D239/91 , C07D405/12 , A61K31/505 , A61K31/54 , C07D239/86 , C07D239/95
CPC分类号： C07D405/12 , C07D239/91
摘要： Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
摘要翻译： 苯氧基苯基乙酸和一般结构式I的衍生物具有内皮素拮抗剂活性，因此可用于治疗心血管疾病，例如高血压，缺血性肾衰竭，血管痉挛，脑和心脏缺血，心肌梗死，炎性疾病，雷诺氏病， 和内毒素性休克和哮喘。
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2.发明授权Six-membered ring fused imidazoles substituted with phenoxyphenylacetic acid derivatives 失效被苯氧基苯乙酸衍生物取代的六元环稠合咪唑
公开(公告)号：US5334598A
公开(公告)日：1994-08-02
申请号：US035340
申请日：1993-03-19
申请人： Scott W. Bagley , Prasun K. Chakravarty , Anna Chen , Daljit S. Dhanoa , Kenneth J. Fitch , William J. Greenlee , Elizabeth M. Naylor , Thomas F. Walsh , David L. Williams, Jr.
发明人： Scott W. Bagley , Prasun K. Chakravarty , Anna Chen , Daljit S. Dhanoa , Kenneth J. Fitch , William J. Greenlee , Elizabeth M. Naylor , Thomas F. Walsh , David L. Williams, Jr.
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： Phenoxyphenylacetic acids and derivatives of general structural formula I have endothelin ##STR1## antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
摘要翻译： 苯氧基苯基乙酸和通式结构式I的衍生物具有内皮缩血管肽I拮抗剂活性，因此可用于治疗心血管疾病，如高血压，充血性心力衰竭，缺血性肾衰竭，血管痉挛，脑和心脏缺血，心肌梗死，炎性疾病 ，雷诺氏病，内毒素性休克和哮喘。
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3.发明授权
公开(公告)号：US5126342A
公开(公告)日：1992-06-30
申请号：US590971
申请日：1990-10-01
申请人： Prasun K. Chakravarty , William J. Greenlee , Elizabeth M. Naylor , Arthur A. Patchett , Thomas F. Walsh
发明人： Prasun K. Chakravarty , William J. Greenlee , Elizabeth M. Naylor , Arthur A. Patchett , Thomas F. Walsh
IPC分类号： A61K31/415 , A61K31/675 , A61K45/06 , A61P3/00 , A61P9/12 , A61P27/02 , A61P43/00 , C07D233/54 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/84 , C07D233/88 , C07D233/90 , C07D403/04 , C07D403/06 , C07D403/12 , C07D407/04 , C07D521/00 , C07F9/6506
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D233/68 , C07D233/88 , C07D233/90 , C07D249/08 , C07D403/04 , C07D403/06 , C07F9/65061
摘要： There are disclosed substituted imidazole derivatives of Formula I which are useful as angiotensin II antagonists. ##STR1##
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4.发明授权
公开(公告)号：US5391566A
公开(公告)日：1995-02-21
申请号：US94592
申请日：1993-07-20
IPC分类号： C07D235/26 , C07D405/12 , A61K31/415
CPC分类号： C07D405/12 , C07D235/26
摘要： Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.
摘要翻译： 苯氧基苯乙酸和一般结构式I的衍生物具有内皮素拮抗剂活性，因此可用于治疗心血管疾病，例如高血压，肺动脉高压，缺血性肾衰竭，血管痉挛，脑和心脏缺血，心肌梗塞，内毒素性休克 ，包括雷诺氏病和哮喘的炎性疾病。
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公开(公告)号：US5668279A
公开(公告)日：1997-09-16
申请号：US411655
申请日：1995-04-06
IPC分类号： A61K31/50 , A61K31/502 , A61P1/00 , A61P1/04 , A61P1/12 , A61P25/18 , A61P25/24 , A61P25/26 , A61P25/28 , C07D237/32 , C07D401/04 , C07D405/12 , C07D409/12 , C07D409/04 , C07D413/10
CPC分类号： C07D401/04 , C07D237/32 , C07D405/12 , C07D409/12
摘要： Novel substituted phthalazinones of the formula (I) ##STR1## are useful as neurotensin antagonists.
摘要翻译： PCT No.PCT / US93 / 10386 Sec。 371日期：1995年4月6日 102（e）日期1995年4月6日PCT提交1993年10月28日PCT公布。 公开号WO94 / 10151 日期1994年5月11日新颖的式（I）取代的2,3-二氮杂萘酮酮可用作神经降压素拮抗剂。
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公开(公告)号：US07947714B2
公开(公告)日：2011-05-24
申请号：US12084027
申请日：2006-10-27
申请人： David Hallett , Craig W. Lindsley , Elizabeth M. Naylor , Zhijian Zhao , Cory R. Theberge , Scott E. Wolkenberg , M. Brad Nolt
发明人： David Hallett , Craig W. Lindsley , Elizabeth M. Naylor , Zhijian Zhao , Cory R. Theberge , Scott E. Wolkenberg , M. Brad Nolt
IPC分类号： A61K31/445 , C07D211/32
CPC分类号： C07D211/96 , C07D401/04 , C07D405/06
摘要： The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
摘要翻译： 本发明涉及抑制甘氨酸转运蛋白GlyT1的哌啶化合物，其可用于治疗与甘氨酸能或谷氨酸能神经传递功能障碍相关的神经和精神疾病以及其中涉及甘氨酸转运蛋白GlyT1的疾病。
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公开(公告)号：US06291491B1
公开(公告)日：2001-09-18
申请号：US09689169
申请日：2000-10-12
IPC分类号： C07D21356
CPC分类号： C07D213/73 , C07D213/38 , C07D213/56 , C07D213/84 , C07D277/40 , C07D417/12
摘要： Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
摘要翻译： 酰胺衍生物是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。
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8.发明授权Substituted sulfonamides as selective .beta..sub.3 agonists for the treatment of diabetes and obesity 失效取代磺酰胺作为治疗糖尿病和肥胖症的选择性β3激动剂
公开(公告)号：US5561142A
公开(公告)日：1996-10-01
申请号：US445630
申请日：1995-05-22
申请人： Michael H. Fisher , Elizabeth M. Naylor , Dong Ok , Ann E. Weber , Thomas Shih , Hyun Ok
发明人： Michael H. Fisher , Elizabeth M. Naylor , Dong Ok , Ann E. Weber , Thomas Shih , Hyun Ok
IPC分类号： C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/44 , A61K31/47 , C07D213/30
CPC分类号： C07D213/73 , C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
摘要翻译： 取代磺酰胺是具有非常少的β1和β2肾上腺素能受体活性的选择性β3肾上腺素能受体激动剂，因此这些化合物能够增加细胞中的脂肪分解和能量消耗。 因此，这些化合物在治疗II型糖尿病和肥胖中具有有效的活性。 该化合物也可用于降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或降低肠道运动性。 此外，该化合物可用于减少神经源性炎症或作为抗抑郁剂。 通过将氨基烷基苯基磺酰胺与适当取代的环氧化物偶合来制备化合物。 还公开了用于治疗糖尿病和肥胖以及降低甘油三酯水平和胆固醇水平或提高高密度脂蛋白水平或增加肠蠕动的组合物和方法。
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公开(公告)号：US20090270451A1
公开(公告)日：2009-10-29
申请号：US12084027
申请日：2006-10-27
申请人： David Hallett , Craig W. Lindsley , Elizabeth M. Naylor , Zhijian Zhao , Cory R. Theberge , Scott E. Wolkenberg , M. Brad Nolt
发明人： David Hallett , Craig W. Lindsley , Elizabeth M. Naylor , Zhijian Zhao , Cory R. Theberge , Scott E. Wolkenberg , M. Brad Nolt
IPC分类号： A61K31/4545 , C07D211/30 , A61P25/18 , C07D401/04 , C07D211/96 , A61K31/5355 , A61K31/497 , A61K31/445
CPC分类号： C07D211/96 , C07D401/04 , C07D405/06
摘要： The present invention is directed to piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
摘要翻译： 本发明涉及抑制甘氨酸转运蛋白GlyT1的哌啶化合物，其可用于治疗与甘氨酸能或谷氨酸能神经传递功能障碍相关的神经和精神疾病以及其中涉及甘氨酸转运蛋白GlyT1的疾病。
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10.发明授权
公开(公告)号：US5541197A
公开(公告)日：1996-07-30
申请号：US404566
申请日：1995-03-21
IPC分类号： C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D213/73 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D215/04 , A61K31/47
CPC分类号： C07D213/73 , C07C311/21 , C07C311/47 , C07D209/08 , C07D213/38 , C07D215/36 , C07D233/32 , C07D271/06 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Substituted sulfonamides are selective .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.
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