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41.发明授权
公开(公告)号：US4395374A
公开(公告)日：1983-07-26
申请号：US222213
申请日：1981-01-02
申请人： Gerard A. Dutra , James A. Sikorski
发明人： Gerard A. Dutra , James A. Sikorski
CPC分类号： C07F9/4006 , A01N57/22
摘要： This disclosure relates to arylsulfenyl derivatives of benzyl and aryl esters of N-phosphonomethylglycines. This disclosure further relates to herbicidal compositions containing arylsulfenyl derivatives of benzyl and aryl esters of N-phosphonomethylglycines, to the use thereof, and to herbicidal methods employing such compounds and compositions.
摘要翻译： 本公开涉及N-膦酰基甲基甘氨酸的苄基和芳基酯的芳硫基衍生物。 本公开还涉及含有N-膦酰基甲基甘氨酸的苄基和芳基酯的芳基亚硫酰基衍生物及其用途的除草组合物，以及使用这种化合物和组合物的除草方法。
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公开(公告)号：US4300943A
公开(公告)日：1981-11-17
申请号：US222219
申请日：1981-01-02
申请人： Gerard A. Dutra , James A. Sikorski
发明人： Gerard A. Dutra , James A. Sikorski
CPC分类号： A01N57/22 , C07F9/4006
摘要： This disclosure relates to novel ester derivatives of N-arylthio-N-phosphonomethylglycinonitrile which are useful as herbicides. This disclosure further relates to herbicidal compositions containing such N-phosphonomethylglycinonitriles and to herbicidal methods employing such compounds and compositions.
摘要翻译： 本公开涉及可用作除草剂的N-芳基硫代-N-膦酰基甲基甘氨腈的新型酯衍生物。 本公开进一步涉及含有N-膦酰基甲基甘氨腈的除草组合物和使用这种化合物和组合物的除草方法。
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43.发明授权1,3-bis-(substituted-phenyl)-2-propyn-1-ones and their use to treat disorders 失效1,3-二 - （取代苯基）-2-丙炔-1-酮及其用于治疗疾病的用途公开(公告)号：US07202247B2
公开(公告)日：2007-04-10
申请号：US10325087
申请日：2002-12-19
IPC分类号： C07C49/213 , C07D213/06 , C07D231/02 , A61K31/12
CPC分类号： C07D333/38 , C07D333/22
摘要： The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
摘要翻译： 本发明涉及使用通式化合物的化合物，药物组合物和方法
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44.发明授权Compounds and methods to increase plasma HDL cholesterol levels and improve HDL functionality 失效提高血浆HDL胆固醇水平和提高HDL功能的化合物和方法公开(公告)号：US07183317B2
公开(公告)日：2007-02-27
申请号：US10886927
申请日：2004-07-08
IPC分类号： A61K31/255 , C07C323/00 , C07C229/00
CPC分类号： G01N33/92 , C07C323/20 , G01N2500/00 , G01N2500/10 , G01N2800/044
摘要： It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.
摘要翻译： 已经发现，普罗布考的某些选择的醚及其药学上可接受的盐或前药可用于增加循环HDL胆固醇。 这些化合物还可以通过（a）增加胆固醇酯的清除率，（b）增加对肝细胞表面受体的HDL-粒子亲和力或（c）增加apoAI-HDL的半衰期来改善HDL功能。
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45.发明授权公开(公告)号：US07141594B2
公开(公告)日：2006-11-28
申请号：US10715852
申请日：2003-11-19
申请人： Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Michael L. Vazquez , James A. Sikorski , Balekudru Devadas , Srinivasan Nagarajan , David L. Brown , Joseph J. McDonald
发明人： Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Michael L. Vazquez , James A. Sikorski , Balekudru Devadas , Srinivasan Nagarajan , David L. Brown , Joseph J. McDonald
IPC分类号： A61K31/428 , C07D417/12
CPC分类号： C07K5/021 , A61K38/00 , C07K5/06139 , C07K5/06165
摘要： Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
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46.发明授权(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效（R） - 用于抑制胆固醇酯转移蛋白活性的卤代取代稠合杂环氨基化合物公开(公告)号：US07122536B2
公开(公告)日：2006-10-17
申请号：US10929013
申请日：2004-08-27
申请人： James A. Sikorski , Richard C. Durley , Margaret L. Grapperhaus , Mark A. Massa , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Brian S. Hickory , Monica B. Norton , William F. Vernier , Deborah A. Mischke , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Margaret L. Grapperhaus , Mark A. Massa , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Brian S. Hickory , Monica B. Norton , William F. Vernier , Deborah A. Mischke , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K31/33 , A61K31/557 , A61K31/535
CPC分类号： C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要： The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-1）的抑制剂的取代的芳基和杂芳基（R） - 手性卤代1-取代氨基 - （n + 1） - 阿尔卡醇化合物，化合物，组合物和方法 用于治疗动脉粥样硬化和其他冠状动脉疾病。 描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。
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47.发明授权Substituted tertiary-heteroalkylamines useful for inhibiting cholesteryl ester transfer protein activity 失效用于抑制胆固醇酯转移蛋白活性的取代的叔杂烷基胺公开(公告)号：US06924313B1
公开(公告)日：2005-08-02
申请号：US10326035
申请日：2002-12-23
申请人： James A. Sikorski , Richard C. Durley , Melvin L. Rueppel , Deborah A. Mischke , Barry L. Parnas
发明人： James A. Sikorski , Richard C. Durley , Melvin L. Rueppel , Deborah A. Mischke , Barry L. Parnas
IPC分类号： A61K31/135 , A61K31/136 , A61K31/137
CPC分类号： A61K31/135 , A61K31/136 , A61K31/137
摘要： The invention relates to substituted tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid trans: protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease.
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质反式：蛋白I）的抑制剂的取代的叔杂烷基胺化合物以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。
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48.发明授权Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications 失效胆固醇酯转运蛋白抑制剂和烟酸衍生物用于心血管适应症的组合公开(公告)号：US06890958B2
公开(公告)日：2005-05-10
申请号：US10245506
申请日：2002-09-18
申请人： James A. Sikorski , Kevin C. Glenn
发明人： James A. Sikorski , Kevin C. Glenn
IPC分类号： A01N25/00 , A61K31/075 , A61K31/09 , A61K31/133 , A61K31/135 , A61K31/136 , A61K31/343 , A61K31/4196 , A61K31/44 , A61K31/4422 , A61K31/455 , A61K31/47 , A61K31/495 , A61K31/4965 , A61K31/55 , A61K31/575 , A61K31/585 , A61K31/785 , A61K45/06 , A61P3/06 , A61P9/00 , A61P9/10
CPC分类号： A61K31/585 , A61K31/19 , A61K31/195 , A61K31/215 , A61K31/455 , A61K31/55 , A61K31/575 , A61K31/785 , A61K45/06 , Y10S514/824 , A61K2300/00
摘要： The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.
摘要翻译： 本发明提供用于预防或治疗包括高胆固醇血症，动脉粥样硬化或高脂血症的心血管疾病的心血管治疗化合物的组合。 所公开的组合包括与胆固醇酯转移蛋白（CETP）抑制剂组合的烟酸衍生物。
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49.发明授权Substituted N-cycloalkyl-N-benzyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity 失效可用于抑制胆固醇酯转移蛋白活性的取代的N-环烷基-N-苄基氨基醇化合物公开(公告)号：US06787570B2
公开(公告)日：2004-09-07
申请号：US10320858
申请日：2002-12-16
申请人： James A. Sikorski , Richard C. Durley , Margaret L. Grapperhaus , Deborah A. Mischke , Emily J. Reinhard , Barry L. Parnas , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Margaret L. Grapperhaus , Deborah A. Mischke , Emily J. Reinhard , Barry L. Parnas , Melvin L. Rueppel
IPC分类号： A61K31137
CPC分类号： C07D493/08 , C07C215/08 , C07C215/12 , C07C217/08 , C07C217/20 , C07C217/52 , C07C217/58 , C07C217/84 , C07C217/86 , C07C217/90 , C07C229/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/38 , C07D307/14 , C07D309/04
摘要： The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols. A specific N-cycloalkyl N-benzyl aminoalcohol is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-I）抑制剂的取代的N-烷基/烯基/环烷基/杂环N-芳基/杂芳基叔杂烷基胺化合物及其治疗动脉粥样硬化的化合物，组合物和方法 和其他冠状动脉疾病。 优选的叔杂烷基胺化合物是取代的N-环烷基N-苄基氨基醇。 特定的N-环烷基N-苄基氨基醇是化合物：
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50.发明授权Substituted n-benzyl-n-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity 失效用于抑制胆固醇酯转移蛋白活性的取代的正苄基 - 正 - 苯基氨基醇化合物公开(公告)号：US06723753B2
公开(公告)日：2004-04-20
申请号：US10071518
申请日：2002-02-07
申请人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
发明人： James A. Sikorski , Richard C. Durley , Deborah A. Mischke , Emily J. Reinhard , Yvette M. Fobian , Michael B. Tollefson , Lijuan Wang , Margaret L. Grapperhaus , Brian S. Hickory , Mark A. Massa , Monica B. Norton , William F. Vernier , Barry L. Parnas , Michele A. Promo , Ashton T. Hamme , Dale P. Spangler , Melvin L. Rueppel
IPC分类号： A61K3137
CPC分类号： C07C323/25 , B01D2201/345 , C07B2200/07 , C07C215/08 , C07C215/16 , C07C217/58 , C07C217/84 , C07C217/88 , C07C217/90 , C07C217/92 , C07C219/06 , C07C219/28 , C07C219/34 , C07C225/22 , C07C229/38 , C07C229/52 , C07C229/60 , C07C233/25 , C07C233/43 , C07C233/69 , C07C233/80 , C07C235/20 , C07C235/24 , C07C235/56 , C07C237/30 , C07C237/38 , C07C255/13 , C07C255/21 , C07C255/24 , C07C255/54 , C07C255/58 , C07C271/28 , C07C275/34 , C07C275/40 , C07C311/21 , C07C311/58 , C07C317/32 , C07C317/36 , C07C323/19 , C07C323/20 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , C07D207/335 , C07D209/82 , C07D213/38 , C07D213/62 , C07D225/08 , C07D239/26 , C07D239/34 , C07D251/46 , C07D257/04 , C07D263/04 , C07D265/14 , C07D295/088 , C07D295/108 , C07D295/135 , C07D295/192 , C07D307/04 , C07D307/38 , C07D333/20 , C07D333/28 , C07D491/10
摘要： The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols. A preferred specific N-benzyl-N-phenyl aminoalcohol is the compound:
摘要翻译： 本发明涉及可用作胆固醇酯转移蛋白（CETP;血浆脂质转移蛋白-I）抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物以及用于治疗动脉粥样硬化和其它冠状动脉疾病的化合物，组合物和方法。 优选的叔杂烷基胺化合物是取代的N-苄基-N-苯基氨基醇。 优选的特定N-苄基-N-苯基氨基醇是化合物：
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