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公开(公告)号：US5668162A
公开(公告)日：1997-09-16
申请号：US646188
申请日：1996-05-07
申请人： John Michael Domagala , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
发明人： John Michael Domagala , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
IPC分类号： A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/14 , C07D275/04 , C07D417/04 , C07D513/04 , C07D513/14 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Plasma levels of Lp(a) are lowered by administering an isothiazolone having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het.
摘要翻译： 通过施用具有一般结构
的异噻唑酮来降低Lp（a）的血浆水平，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。 -
公开(公告)号：US5786335A
公开(公告)日：1998-07-28
申请号：US744698
申请日：1996-10-31
申请人： Wayne Livingston Cody , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
发明人： Wayne Livingston Cody , Helen Tsenwhei Lee , Randy Ranjee Ramharack , Bruce David Roth , Tomi Sawyer , Drago Robert Sliskovic
CPC分类号： C07K7/06 , C07K5/06026 , C07K5/081 , C07K5/1008 , C07K5/1013 , A61K38/00
摘要： Sulfhydryl containing peptides having the formula X--A.sub.1 --A.sub.2 --A.sub.3 --A.sub.4 --A.sub.5 --Y inhibit the formation of Lp(a) and thus are useful for treating vascular diseases such as coronary heart disease, myocardial infarction, ischemic stroke, cervical atherosclerosis, cerebral infarction, and restenosis.
摘要翻译： 具有式X-A1-A2-A3-A4-A5-Y的含巯基的肽抑制Lp（a）的形成，因此可用于治疗血管疾病如冠心病，心肌梗塞，缺血性中风，颈动脉粥样硬化， 脑梗死和再狭窄。
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公开(公告)号：US06780883B2
公开(公告)日：2004-08-24
申请号：US10021633
申请日：2001-12-12
申请人： Richard John Booth , Helen Tsenwhei Lee , Jason Keith Pontrello , Randy Ranjee Ramharack , Bruce David Roth
发明人： Richard John Booth , Helen Tsenwhei Lee , Jason Keith Pontrello , Randy Ranjee Ramharack , Bruce David Roth
IPC分类号： A61K3144
CPC分类号： C07D213/40 , C07D213/75 , C07D215/38 , C07D333/38 , C07D405/12 , C07D409/12
摘要： The present invention provides compounds having the Formula I The present invention also provides pharmaceutical compositions comprising a compound of Formula I and methods of treatment of atherosclerosis, obesity, restenosis, coronary heart disease, hyperlipoproteinemia, hypercholesterolemia, and hypertriglyceridemia.
摘要翻译： 本发明提供了具有式I的化合物本发明还提供包含式I化合物和治疗动脉粥样硬化，肥胖症，再狭窄，冠心病，高脂蛋白血症，高胆固醇血症和高甘油三酯血症的药物组合物。
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4.发明授权Sulfonamide compounds and methods of treating atherosclerosis and restenosis 失效磺酰胺化合物和治疗动脉粥样硬化和再狭窄的方法公开(公告)号：US06458815B2
公开(公告)日：2002-10-01
申请号：US09835239
申请日：2001-04-13
IPC分类号： A61K314436
CPC分类号： C07D213/76 , C07C311/13 , C07C2601/14 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
摘要翻译： 本发明提供具有式I的化合物本发明还提供使用式I化合物治疗或预防动脉粥样硬化，冠心病和再狭窄的方法，以及包含式I化合物的药物组合物。
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5.发明授权Sulfonamide compounds and methods of treating atherosclerosis and restenosis 失效磺酰胺化合物和治疗动脉粥样硬化和再狭窄的方法公开(公告)号：US06284795B1
公开(公告)日：2001-09-04
申请号：US09376268
申请日：1999-08-18
IPC分类号： A61K3118
CPC分类号： C07D213/76 , C07C311/13 , C07C2601/14 , C07D409/12 , C07D409/14
摘要： The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
摘要翻译： 本发明提供具有式I的化合物本发明还提供使用式I化合物治疗或预防动脉粥样硬化，冠心病和再狭窄的方法，以及包含式I化合物的药物组合物。
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公开(公告)号：US5929091A
公开(公告)日：1999-07-27
申请号：US166678
申请日：1998-10-05
IPC分类号： A61K31/454 , A61K31/445
CPC分类号： A61K31/454
摘要： The present invention comprises a method of lowering plasma levels of Lp(a) in animals by administering an effective Lp(a)-reducing amount of a microsomal triglyceride transfer protein inhibitor of the structural formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is alkyl, alkenyl alkynyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, cycloalkyl, or cycloalkylalkyl, each of which is independently optionally substituted through available carbon atoms with 1, 2, or 3 groups selected from halo, alkyl, alkenyl, alkoxy, aryloxy, aryl, arylalkyl, alkylmercapto, arylmercapto, cycloalkyl, cycloalkylalkyl, heteroaryl, and heteroarylalkyl. By lowering Lp(a) levels, the animals are protected against developing premature atherosclerosis and consequent cardiovascular and cerebrovascular diseases.
摘要翻译： 本发明包括通过施用有效的Lp（a）减少量的结构式的微粒体甘油三酯转运蛋白抑制剂或其药学上可接受的盐来降低动物中的血浆Lp（a）水平的方法，其中R1是 烷基，烯基炔基，芳基，杂芳基，芳基烷基，杂芳基烷基，环烷基或环烷基烷基，其各自独立地通过可用的碳原子任选被1,2或3个选自卤素，烷基，烯基，烷氧基，芳氧基，芳基 ，芳基烷基，烷基巯基，芳基巯基，环烷基，环烷基烷基，杂芳基和杂芳基烷基。 通过降低Lp（a）水平，动物被保护免于发展过早的动脉粥样硬化和随之而来的心血管和脑血管疾病。
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公开(公告)号：US06607893B2
公开(公告)日：2003-08-19
申请号：US10027938
申请日：2001-12-19
IPC分类号： C12Q148
CPC分类号： C12Q1/48 , G01N2500/00 , G01N2500/02
摘要： The present invention provides a method for measuring diacylglycerol acetyltransferase (DGAT) activity which utilizes a novel solvent system to reduce and/or eliminate the activities of related compounds. The present invention also discloses a method for determining whether a compound is useful for modulating DGAT biological activity. The method is capable of being utilized for mass screening of compounds as modulators of the biological activity of DGAT.
摘要翻译： 本发明提供了一种测量二酰基甘油乙酰转移酶（DGAT）活性的方法，其利用新的溶剂体系来减少和/或消除相关化合物的活性。本发明还公开了一种用于测定化合物是否可用于调节DGAT生物 活动。 该方法能够用于大规模筛选化合物作为DGAT生物活性的调节剂。
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