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1.(R)-CHIRAL HALOGENATED SUBSTITUTED FUSED HETEROCYCLIC AMINO COMPOUNDS USEFUL FOR INHIBITING CHOLESTEROL ESTER TRANSFER PROTEIN ACTIVITY 失效
标题翻译: (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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2.(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。
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3.Piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids and their use as protease inhibitors 失效
标题翻译: 哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸及其作为蛋白酶抑制剂的用途公开(公告)号:US07119203B2
公开(公告)日:2006-10-10
申请号:US10618288
申请日:2003-04-25
申请人: Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , David L. Brown , Jeffery N. Carroll , Yiyuan Chen , Yvette M. Fobian , John N. Freskos , Alan F. Gasiecki , Margaret L. Grapperhaus , Robert M. Heintz , Susan L. Hockerman , Darren J. Kassab , Ish K. Khanna , Stephen A. Kolodziej , Mark A. Massa , Joseph J. McDonald , Brent V. Mischke , Deborah A. Mischke , Patrick B. Mullins , Mark A. Nagy , Monica B. Norton , Joseph G. Rico , Michelle A. Schmidt , Nathan W. Stehle , John J. Talley , William F. Vernier , Clara I. Villamil , Lijuan J. Wang , Thomas A. Wynn
发明人: Thomas E. Barta , Daniel P. Becker , Louis J. Bedell , Terri L. Boehm , David L. Brown , Jeffery N. Carroll , Yiyuan Chen , Yvette M. Fobian , John N. Freskos , Alan F. Gasiecki , Margaret L. Grapperhaus , Robert M. Heintz , Susan L. Hockerman , Darren J. Kassab , Ish K. Khanna , Stephen A. Kolodziej , Mark A. Massa , Joseph J. McDonald , Brent V. Mischke , Deborah A. Mischke , Patrick B. Mullins , Mark A. Nagy , Monica B. Norton , Joseph G. Rico , Michelle A. Schmidt , Nathan W. Stehle , John J. Talley , William F. Vernier , Clara I. Villamil , Lijuan J. Wang , Thomas A. Wynn
IPC分类号: C07D405/14 , C07D405/12 , A61K31/496
CPC分类号: C07D213/74 , C07D211/66 , C07D211/96 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D411/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04
摘要: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.
摘要翻译: 本发明一般涉及蛋白酶(也称为“蛋白酶”)抑制剂,尤其涉及哌啶基和哌嗪基 - 磺酰基甲基异羟肟酸,其特别是抑制基质金属蛋白酶(也称为“基质金属蛋白酶”或“MMP “)活性和/或蛋白聚糖蛋白聚糖酶活性。 这样的异羟肟酸通常在结构上对应于下式:(其中A 1,A 2,Y,E 1, 2,E 3和R x如本说明书中所定义),并且还包括这些化合物的盐。 本发明还涉及这种异羟肟酸的组合物,用于合成这种异羟肟酸的中间体,制备这种异羟肟酸的方法,以及用于治疗与MMP活性和/或蛋白聚糖蛋白聚糖酶活性相关的病症(特别是病理状态)的方法。
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公开(公告)号:US06750228B1
公开(公告)日:2004-06-15
申请号:US09570731
申请日:2000-05-12
申请人: Thomas E Barta , Daniel P Becker , Louis J Bedell , Terri L Boehm , Jeffrey N Carroll , Gary A DeCrescenzo , Yvette M Fobian , John N Freskos , Daniel P Getman , Joseph J McDonald , Madeleine H Li , Susan L Hockerman , Susan C Howard , Steve A Kolodziej , Deborah A Mischke , Joseph G Rico , Nathan W Stehle , Michael B Tollefson , William F Vernier , Clara I Villamil
发明人: Thomas E Barta , Daniel P Becker , Louis J Bedell , Terri L Boehm , Jeffrey N Carroll , Gary A DeCrescenzo , Yvette M Fobian , John N Freskos , Daniel P Getman , Joseph J McDonald , Madeleine H Li , Susan L Hockerman , Susan C Howard , Steve A Kolodziej , Deborah A Mischke , Joseph G Rico , Nathan W Stehle , Michael B Tollefson , William F Vernier , Clara I Villamil
IPC分类号: A61K31445
CPC分类号: C07D231/12 , C07D211/66 , C07D233/56 , C07D249/08 , C07D309/08 , C07D335/02 , C07D401/06 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12
摘要: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor. A contemplated compound corresponds in structure to formula B, below,
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5.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:
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6.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:
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7.Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds 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-苯基-N-杂芳烷基氨基醇化合物公开(公告)号:US06458803B1
公开(公告)日:2002-10-01
申请号:US09991084
申请日:2001-11-23
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: A61K31426
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-phenyl-N-heteroaralkyl aminoalcohols. A preferred specific N-phenyl-N-heteroaralkyl 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-苯基-N-杂芳烷基氨基醇。 优选的特定N-苯基-N-杂芳烷基氨基醇是化合物:
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8.Use of substituted N, N-disubstituted fused-heterocyclo amino compounds for inhibiting cholesteryl ester transfer protein activity 失效
标题翻译: 使用取代的N,N-二取代的稠合 - 杂环氨基化合物来抑制胆固醇酯转移蛋白活性公开(公告)号:US06455519B1
公开(公告)日:2002-09-24
申请号:US09991116
申请日:2001-11-15
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: A61K31536
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 fused-heterocyclo amines. A preferred specific N,N-disubstituted 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-二取代稠合 - 杂环胺。 优选的具体的N,N-二取代稠合 - 杂环胺是化合物:
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9.
公开(公告)号:US5281571A
公开(公告)日:1994-01-25
申请号:US763762
申请日:1991-09-25
申请人: Scott S. Woodard , Bruce C. Hamper , Kurt Moedritzer , Michael D. Rogers , Deborah A. Mischke , Gerard A. Dutra
发明人: Scott S. Woodard , Bruce C. Hamper , Kurt Moedritzer , Michael D. Rogers , Deborah A. Mischke , Gerard A. Dutra
IPC分类号: A01N43/56 , A01N43/78 , A01P7/04 , C07C45/29 , C07C45/45 , C07C49/80 , C07C49/835 , C07D231/12 , C07D231/16 , C07D231/18 , C07D231/22 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/10 , C07D409/12 , C07D411/04 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D498/04 , C07D521/00 , A01N43/84 , C07D413/02 , C07D417/02
CPC分类号: C07D231/12 , C07C45/292 , C07C45/455 , C07C49/80 , C07C49/835 , C07D231/16 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/12 , C07D409/04 , C07D409/12 , C07D411/04 , C07D413/10 , C07D413/12 , C07D417/04
摘要: The invention herein relates to titled compounds having the structure ##STR1## wherein the R.sub.1 -(R.sub.4).sub.n members are as defined in the claims. Characteristic features of these compounds are the haloalkyl R.sub.2 radical and cyclization of two R.sub.4 members at the meta and para positions of the phenyl ring to form a substituted benzoxazinone ring fused to the phenyl or benzthiazinone ring. Such compounds are useful as active ingredients in herbicidal compositions to control undesirable weeds in various crops.
摘要翻译: 本发明涉及具有结构“IMAGE”的标题化合物,其中R1-(R4)n构件如权利要求中所定义。 这些化合物的特征是卤代烷基R2基和两个R 4成员在苯环的间位和对位环化,形成与苯基或苯并噻嗪酮环稠合的取代的苯并恶嗪酮环。 这些化合物可用作除草组合物中的活性成分,以控制各种作物中的不期望的杂草。
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10.Use of substituted N, N-disubstituted reverse 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-二取代的反向氨基醇化合物的用途公开(公告)号:US06765023B2
公开(公告)日:2004-07-20
申请号:US10155921
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 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 reverse aminoalcohols. A preferred specific N,N-disubstituted reverse aminoalcohols 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-二取代的反向氨基醇。 优选的具体的N,N-二取代的反向氨基醇是化合物:
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