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61.发明授权Use of substituted N,N-disubstituted non-fused heterocyclo amino compounds for inhibiting cholesteryl ester transfer protein activity 失效取代的N，N-二取代的非稠合杂环氨基化合物用于抑制胆固醇酯转移蛋白活性的用途公开(公告)号：US06451830B1
公开(公告)日：2002-09-17
申请号：US09991085
申请日：2001-11-14
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： A61K31421
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 use of 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,N-disubstituted non-fused heterocyclo amines. A preferred specific N,N-disubstituted non-fused heterocyclo amine 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-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途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，N-二取代的非稠合杂环胺。 优选的具体的N，N-二取代的非稠合杂环胺是化合物：
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62.发明授权Use of substituted N-phenoxy-N-phenyl aminoalcohol compounds for inhibiting cholesteryl ester transfer protein activity 失效使用取代的N-苯氧基-N-苯基氨基醇化合物抑制胆固醇酯转移蛋白活性公开(公告)号：US06451823B1
公开(公告)日：2002-09-17
申请号：US09990645
申请日：2001-11-14
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： C07C23300
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 use of 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-phenoxy-N-phenyl aminoalcohols. A preferred specific N-phenoxy-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-1）的抑制剂的取代多环芳基和杂芳基叔杂烷基胺化合物的用途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-苯氧基-N-苯基氨基醇。 优选的特定N-苯氧基-N-苯基氨基醇是化合物：
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63.发明授权Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors 失效磺酰基烷酰氨基羟乙氨基磺酰胺逆转录病毒蛋白酶抑制剂公开(公告)号：US06169085A
公开(公告)日：2001-01-02
申请号：US09411374
申请日：1999-10-04
申请人： Daniel P. Getman , Gary A. DeCrescenzo , John N. Freskos , Michael L. Vazquez , James A. Sikorski , Balekudru Devadas , Srinivasan Nagarajan , 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 , Joseph J. McDonald
IPC分类号： A61K3118
CPC分类号： C07D235/06 , C07C311/29 , C07C311/41 , C07C317/44 , C07D215/36 , C07D217/04 , C07D235/30 , C07D235/32 , C07D249/18 , C07D249/20 , C07D263/56 , C07D277/62 , C07D277/82 , C07D303/36 , C07D307/79 , C07D317/62 , C07D319/18
摘要： Selected sulfonylalkanoylamino hydroxyethylamine 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.
摘要翻译： 选择的磺酰基烷酰基氨基羟基胺磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人类免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及 治疗逆转录病毒感染。
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64.发明授权Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors 失效双氨基酸羟乙基氨基磺酰胺逆转录病毒蛋白酶抑制剂
公开(公告)号：US6143788A
公开(公告)日：2000-11-07
申请号：US913096
申请日：1998-01-21
申请人： Daniel P. Getman , Gary A. Decrescenzo , John N. Freskos , Michael L. Vazquez , James A. Sikorski , Belekudru Devadas , Srinivasan RAJ 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 , Belekudru Devadas , Srinivasan RAJ Nagarajan , David L. Brown , Joseph J. McDonald
IPC分类号： A61K38/00 , C07K5/06 , A61K31/18 , C07C311/17
CPC分类号： C07K5/06026 , A61K38/00
摘要： Selected bis-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.
摘要翻译： PCT No.PCT / US96 / 02685第 371日期1997年1月21日 102（e）日期1997年1月21日PCT 1996年3月7日PCT公布。 公开号WO96 / 28464 日期1996年9月19日选择的双氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及 治疗逆转录病毒感染。
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65.发明授权Unsymmetrical aminosulfinamide derivatives of N-phosphonomethylglycine triesters, herbicidal compositions and use 失效N-膦酰基甲基甘氨酸三酯，除草组合物和用途的不对称氨基亚磺酰胺衍生物
公开(公告)号：US4519832A
公开(公告)日：1985-05-28
申请号：US605003
申请日：1984-04-27
申请人： James A. Sikorski , Mary A. Hoobler
发明人： James A. Sikorski , Mary A. Hoobler
CPC分类号： C07F9/6533 , A01N57/22 , C07F9/4006 , C07F9/591
摘要： This invention relates to unsymmetrical aminosulfinamide derivatives of N-phosphonomethyl-glycine triesters which are useful as herbicides. This invention further relates to herbicidal compositions containing such derivatives and to herbicidal methods employing such compounds and compositions.
摘要翻译： 本发明涉及可用作除草剂的N-膦酰基甲基 - 甘氨酸三酯的不对称氨基亚磺酰胺衍生物。 本发明还涉及含有这些衍生物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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66.发明授权Process for preparing thiosulfenamide derivatives of N-phosphonomethylglycinonitriles 失效制备N-膦酰基甲基甘氨腈的硫代亚磺酰胺衍生物的方法
公开(公告)号：US4508663A
公开(公告)日：1985-04-02
申请号：US514403
申请日：1983-07-18
申请人： James A. Sikorski , Mary A. Hoobler
发明人： James A. Sikorski , Mary A. Hoobler
CPC分类号： A01N57/22 , C07F9/4006
摘要： This invention relates to a process for preparing sulfenyl chloride derivatives of N-phosphonomethylglycinonitriles which are useful as herbicides or as intermediates for the production of thiosulfenamide derivatives of N-phosphonomethylglycinonitriles which are useful as herbicides.
摘要翻译： 本发明涉及一种制备N-膦酰基甲基甘氨腈的亚磺酰氯衍生物的方法，其可用作除草剂或用作生产用作除草剂的N-膦酰基甲基甘氨腈的硫代亚磺酰胺衍生物的中间体。
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67.发明授权N-Nitroso-N-phosphonomethylglycinonitrile esters and the herbicidal use thereof 失效N-亚硝基-N-膦酰基甲基甘氨酸酯及其除草用途
公开(公告)号：US4322238A
公开(公告)日：1982-03-30
申请号：US177653
申请日：1980-08-13
申请人： Gerard A. Dutra , James A. Sikorski
发明人： Gerard A. Dutra , James A. Sikorski
CPC分类号： C07F9/3808 , A01N57/20 , A01N57/22 , C07F9/4006
摘要： This disclosure relates to N-nitroso-N-phosphonomethylglycinonitrile compounds, the preparation thereof and their use as herbicides and in herbicidal compositions.
摘要翻译： 本公开涉及N-亚硝基-N-膦酰基甲基甘氨腈化合物，其制备方法及其作为除草剂和除草组合物的用途。
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公开(公告)号：US09944597B2
公开(公告)日：2018-04-17
申请号：US15021972
申请日：2014-09-16
申请人： Glen E. Kellogg , Chenxiao Da , Ashutosh Tripathi , John T. Gupton , Nakul Telang , James A. Sikorski , Susan L. Mooberry , Cristina Rohena
发明人： Glen E. Kellogg , Chenxiao Da , Ashutosh Tripathi , John T. Gupton , Nakul Telang , James A. Sikorski , Susan L. Mooberry , Cristina Rohena
IPC分类号： C07D207/34 , C07D207/36 , C07D207/46 , C07D403/04 , C07D403/06 , C07D403/12
CPC分类号： C07D207/34 , C07D207/36 , C07D207/46 , C07D403/04 , C07D403/06 , C07D403/12
摘要： The present invention provides polysubstituted pyrrole compounds, pharmaceutically effective salts, prodrugs, solvates and hydrates thereof, having antimitotic, antiproliferative and cytotoxic activity, activity against cells expressing the drug efflux protein, P-glycoprotein, or cells expressing the β-III isotype of tubulin and antitumor activity. Also provided are methods of utilizing these compounds for inhibiting the proliferation of cancer cells as well as their medical use, in particular for treating cancer, including drug resistant cancer.
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69.发明申请(R)-CHIRAL HALOGENATED SUBSTITUTED FUSED HETEROCYCLIC AMINO COMPOUNDS USEFUL FOR INHIBITING CHOLESTEROL ESTER TRANSFER PROTEIN ACTIVITY 失效（R）-CHIRAL HALOGENATED取代的FUSED杂环氨基化合物用于抑制胆固醇转运蛋白活性公开(公告)号：US20090156685A1
公开(公告)日：2009-06-18
申请号：US12021813
申请日：2008-01-29
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： A61K31/137 , A61P9/00
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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公开(公告)号：US07297793B2
公开(公告)日：2007-11-20
申请号：US11349352
申请日：2006-02-08
IPC分类号： C07D295/26 , C07D413/12 , C07D401/14 , C07D401/12
CPC分类号： C07C311/29 , C07D235/26 , C07D235/32 , C07D277/82 , C07D295/26 , C07D307/79 , C07D317/62 , C07D319/18 , C07D405/12
摘要： Bis-sulfonamido hydroxyethylamino compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to retroviral protease inhibiting compounds of the formula: or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
摘要翻译： 双亚磺酰氨基羟乙基氨基化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及下式的逆转录病毒蛋白酶抑制化合物：或其药学上可接受的盐，前药或酯，其中变量如本文所定义。
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