专利检索 ap:("James A. Sikorski" OR "Charles Q. Meng" OR "M. David Weingarten" OR "Kimberly J. Worsencroft" OR "Liming Ni") AND inv:"James A. Sikorski" 第 8 页

71.

发明授权
(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效
标题翻译：（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：US07253211B2

公开(公告)日：2007-08-07

申请号：US11373770

申请日：2006-03-09

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： A61K31/135 , C07C211/48

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。

72.

发明授权
Heterocyclo substituted hydroxamic acid derivatives as cyclooxygenase-2 and 5-lipoxygenase inhibitors 失效
标题翻译：杂环取代的异羟肟酸衍生物作为环加氧酶-2和5-脂氧合酶抑制剂

公开(公告)号：US06875785B2

公开(公告)日：2005-04-05

申请号：US10254701

申请日：2002-09-25

申请人： John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas , Hwang-Fun Lu

发明人： John J. Talley , James A. Sikorski , Matthew J. Graneto , Jeffery S. Carter , Bryan H. Norman , Balekudru Devadas , Hwang-Fun Lu

IPC分类号： A61P29/00 , C07D231/12 , C07D263/32 , A61K31/421 , C07D413/00

CPC分类号： C07D231/12 , C07D263/32

摘要： This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

摘要翻译： 本发明涉及抗炎药物领域，具体涉及用于治疗由环氧合酶-2或5-脂氧合酶如炎症介导的病症的化合物，组合物和方法。

73.

发明授权
Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors 失效

公开(公告)号：US06730669B2

公开(公告)日：2004-05-04

申请号：US10200589

申请日：2002-07-23

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： A61K3154

CPC分类号： C07D307/79 , A61K38/00 , C07D235/30 , C07D277/62 , C07D295/15 , C07D311/58 , C07D317/62 , C07D319/18 , C07D339/06 , C07D405/12 , C07D405/14 , C07K5/06026 , C07K5/06034 , C07K5/0606 , C07K5/06069

摘要： Selected 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.

74.

发明授权
Substituted N-phenoxy-N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译：可用于抑制胆固醇酯转移蛋白活性的N-取代的N-苯氧基-N-苯基氨基醇化合物

公开(公告)号：US06696472B2

公开(公告)日：2004-02-24

申请号：US10154788

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： A61C31133

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-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-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-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：

75.

发明授权
Substituted N,N-bis-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取代的N，N-双 - 苯基氨基醇化合物

公开(公告)号：US06677382B1

公开(公告)日：2004-01-13

申请号：US10155410

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： A61K31135

CPC分类号： C07D207/335 , 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 , C07C323/25 , C07C323/31 , C07C323/32 , C07C323/37 , C07C323/44 , C07C323/65 , C07C327/30 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/18 , 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,N-bis-phenyl aminoalcohols. A preferred specific N,N-bis-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，N-双 - 苯基氨基醇。优选的具体的N，N-双 - 苯基氨基醇是化合物：

76.

发明授权
Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors 失效

公开(公告)号：US06667307B2

公开(公告)日：2003-12-23

申请号：US10082123

申请日：2002-02-26

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： A61K31343

CPC分类号： C07D263/56 , C07C317/44 , C07D215/36 , C07D217/02 , C07D217/04 , C07D235/30 , C07D235/32 , C07D249/20 , C07D277/62 , C07D277/82 , C07D307/79 , C07D307/82 , C07D311/58 , 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.

77.

发明授权
Combinations of ileal bile acid transport inhibitors and cholesteryl ester transfer protein inhibitors for cardiovascular indications 失效
标题翻译：回肠胆汁酸转运抑制剂与心血管适应症胆固醇酯转运蛋白抑制剂的组合

公开(公告)号：US06458851B1

公开(公告)日：2002-10-01

申请号：US09466415

申请日：1999-12-17

申请人： Bradley T. Keller , James A. Sikorski , Kevin C. Glenn , Daniel T. Connolly , Mark E. Smith , Joseph R. Schuh

发明人： Bradley T. Keller , James A. Sikorski , Kevin C. Glenn , Daniel T. Connolly , Mark E. Smith , Joseph R. Schuh

IPC分类号： A61K314995

CPC分类号： A61K31/585 , 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 ileal bile acid transport 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。公开的组合包括与胆固醇酯转移蛋白（CETP）抑制剂组合的回肠胆汁酸转运抑制剂。

78.

发明授权
Combinations of cholesteryl ester transfer protein inhibitors and fibric acid derivatives for cardiovascular indications 失效
标题翻译：胆固醇酯转移蛋白抑制剂和纤维酸衍生物用于心血管适应症的组合

公开(公告)号：US06458850B1

公开(公告)日：2002-10-01

申请号：US09466413

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： A61K45/06 , A61K31/216 , 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 fibric 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。公开的组合包括与胆固醇酯转移蛋白（CETP）抑制剂组合的纤维酸衍生物。