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11. 发明授权

US06677379B2 Substituted N,N-disubstituted diamino compounds useful for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译：用于抑制胆固醇酯转移蛋白活性的取代的N，N-二取代的二氨基化合物
公开(公告)号：US06677379B2
公开(公告)日：2004-01-13
申请号：US10155095
申请日：2002-05-23
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： A61K31133
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 heteroary 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 diamines. A preferred specific N,N-disubstituted diamine 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-二取代的二胺。优选的具体的N，N-二取代的二胺是化合物：

12. 发明授权

US06632921B1 Seryl-lysyl-based peptide and peptidomimetic inhibitors of N-myristoyl transferase as anti-infective agents 失效
标题翻译：作为抗感染剂的N-肉豆蔻酰基转移酶的丝氨酰赖氨酰基肽和肽模拟抑制剂
公开(公告)号：US06632921B1
公开(公告)日：2003-10-14
申请号：US09277573
申请日：1999-03-26
申请人： James A. Sikorski , Devadas Balekudru , Daniel P. Getman , David L. Brown , Srinivasan Nagarajan , Mark E. Zupec , Jeffrey I. Gordon
发明人： James A. Sikorski , Devadas Balekudru , Daniel P. Getman , David L. Brown , Srinivasan Nagarajan , Mark E. Zupec , Jeffrey I. Gordon
IPC分类号： C07K508
CPC分类号： C07K5/06191 , A61K38/00 , C07K5/0606 , C07K5/081
摘要： Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: wherein R1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C. albicans with little effect on human NMT enzyme and thus would.be useful in treating C. albicans fungal infections in humans.
摘要翻译：描述了基于丝氨酰赖氨酰的肽和拟肽化合物作为N-肉豆蔻酰转移酶酶的抑制剂，以提供对真菌生物体的真菌生物的选择性控制。特别感兴趣的拟肽化合物是下式的化合物：其中R 1选自氨基烷基，对氨基烷基苯基烷基，咪唑基烷基苯基烷基，2-烷基咪唑基烷基苯基烷基，苯并咪唑基烷基苯基烷基和2-烷基苯并咪唑基烷基苯基烷基; 其中R 1选自氢，烷基，环烷基，亚烯基，炔基，卤代烷基，苄基，烷基苯基烷基，烷氧基苯基烷基，卤代苯基烷基，苯乙基，环烷基烷基，卤代环烷基烷基，烷基环烷基烷基，其中Y选自羧酸，异羟肟酸，膦酸和四唑基; 或其药学上可接受的盐，酰胺或酯。式的化合物是 C的物种特异性抑制剂。白色念珠菌对人NMT酶几乎没有影响，因此可用于治疗 C。白色念珠菌人类真菌感染。

13. 发明授权

US06586433B2 Substituted N-heteroaryl-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译：用于抑制胆固醇酯转移蛋白活性的N-取代的N-杂芳基-N-苯基氨基醇化合物
公开(公告)号：US06586433B2
公开(公告)日：2003-07-01
申请号：US09991241
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： A61K3153
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-heteroaryl-N-phenyl aminoalcohols. A preferred specific N-heteroaryl-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-杂芳基-N-苯基氨基醇。优选的特定N-杂芳基-N-苯基氨基醇是化合物：

14. 发明授权

US06489366B1 Combinations of cholesteryl ester transfer protein inhibitors and nicotinic acid derivatives for cardiovascular indications 失效
标题翻译：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：US06489366B1
公开(公告)日：2002-12-03
申请号：US09466470
申请日：1999-12-17
申请人： James A. Sikorski , Kevin C. Glenn
发明人： James A. Sikorski , Kevin C. Glenn
IPC分类号： A61K3109
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。

15. 发明授权

US06462091B1 Combinations of cholesteryl ester transfer protein inhibitors and HMG coA reductase inhibitors for cardiovascular indications 失效
标题翻译：胆固醇酯转运蛋白抑制剂和HMG coA还原酶抑制剂用于心血管适应症的组合
公开(公告)号：US06462091B1
公开(公告)日：2002-10-08
申请号：US09466414
申请日：1999-12-17
申请人： Bradley T. Keller , James A. Sikorski , Kevin C. Glenn , Daniel T. Connolly , Mark E. Smith
发明人： Bradley T. Keller , James A. Sikorski , Kevin C. Glenn , Daniel T. Connolly , Mark E. Smith
IPC分类号： A61K31136
CPC分类号： A61K31/585 , A61K31/135 , A61K31/22 , A61K31/36 , A61K31/405 , 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 an HMG CoA reductase inhibitor 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HMG CoA还原酶抑制剂。

16. 发明授权

US06407134B1 Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors 失效
标题翻译：杂环羰基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：US06407134B1
公开(公告)日：2002-06-18
申请号：US09775682
申请日：2001-02-05
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： A61K314025
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.
摘要翻译：选择的杂环羰基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。

17. 发明授权

US6143747A Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors 失效
标题翻译：双磺酰胺羟乙基氨基酸逆转录病毒蛋白酶抑制剂
公开(公告)号：US6143747A
公开(公告)日：2000-11-07
申请号：US875025
申请日：1998-02-26
申请人： John N. Freskos , Daniel P. Getman , John J. Talley , James A. Sikorski
发明人： John N. Freskos , Daniel P. Getman , John J. Talley , James A. Sikorski
IPC分类号： C07D295/08 , A61K31/18 , A61K31/185 , A61K31/195 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/443 , A61K31/445 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/5355 , A61K31/5375 , A61K31/5377 , A61P31/12 , A61P43/00 , C07C311/29 , C07C311/38 , C07D213/38 , C07D233/54 , C07D233/61 , C07D235/06 , C07D235/26 , C07D235/30 , C07D235/32 , C07D263/54 , C07D277/66 , C07D277/82 , C07D295/12 , C07D295/22 , C07D295/26 , C07D303/36 , C07D307/14 , C07D307/79 , C07D317/62 , C07D319/18 , C07D333/34 , C07D405/12 , C07D417/12 , 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: ##STR1## or a pharmaceutically acceptable salt, prodrug or ester thereof, wherein the variables are as defined herein.
摘要翻译： PCT No.PCT / US96 / 00607 Sec。 371日期1998年2月26日 102（e）1998年2月26日PCT PCT 1996年1月18日PCT公布。第WO96 / 22287号公报日期1996年7月25日双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。

18. 发明授权

US6063795A Heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors 失效
公开(公告)号：US6063795A
公开(公告)日：2000-05-16
申请号：US307711
申请日：1999-05-10
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： A61K38/55 , A61K31/18 , A61K38/00 , A61P3/00 , A61P31/12 , A61P31/18 , C07D215/48 , C07K5/062 , C07K5/078 , A61K31/445 , C07D405/12
CPC分类号： C07K5/06165 , C07K5/06139 , A61K38/00
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.

19. 发明授权

US4428765A Thiosulfenamide derivatives of N-phosphonomethylglycine triesters as herbicides 失效
标题翻译： N-膦酰基甲基甘氨酸三酯的亚硫酰胺衍生物作为除草剂
公开(公告)号：US4428765A
公开(公告)日：1984-01-31
申请号：US309322
申请日：1981-10-05
申请人： James A. Sikorski , Tommie G. Curtis
发明人： James A. Sikorski , Tommie G. Curtis
IPC分类号： A01N57/22 , A01N57/30 , C07F9/40
CPC分类号： A01N57/22
摘要： This invention relates to thiosulfenamide derivatives of N-phosphonomethylglycine which are useful as herbicides. This invention further relates to herbicidal compositions containing such derivatives and to herbicidal methods employing such compounds and compositions, and a process for preparing such compounds.
摘要翻译：本发明涉及可用作除草剂的N-膦酰基甲基甘氨酸的硫代亚磺酰胺衍生物。本发明还涉及含有这种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，以及制备这种化合物的方法。

20. 发明授权

US4405356A Ester derivatives of N-arylsulfinyl-N-phosphonomethylglycinates as herbicides 失效
标题翻译： N-芳基亚磺酰基-N-膦酰基甲基甘氨酸酯的酯衍生物作为除草剂
公开(公告)号：US4405356A
公开(公告)日：1983-09-20
申请号：US298057
申请日：1981-08-31
申请人： James A. Sikorski , Mary A. Hoobler
发明人： James A. Sikorski , Mary A. Hoobler
IPC分类号： A01N57/20 , A01N57/22 , C07F9/40
CPC分类号： A01N57/20
摘要： Ester derivatives of N-arylsulfinyl-N-phosphonomethylglycinates useful as herbicides. Also disclosed is a process for preparing the same, herbicidal compositions containing the same and herbicidal methods employing such glycinates as herbicidal compositions.
摘要翻译：用作除草剂的N-芳基亚磺酰基-N-膦酰基甲基甘氨酸酯的酯衍生物。还公开了一种制备相同的除草组合物的方法，该组合物含有相同的除草方法，使用这种甘氨酸盐作为除草组合物。

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