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公开(公告)号:US06914158B2
公开(公告)日:2005-07-05
申请号:US10815375
申请日:2004-04-01
申请人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
发明人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
IPC分类号: A61P1/00 , A61K31/198 , A61K31/4166 , A61K31/4245 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/00 , A61P3/08 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/06 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/10 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P39/02 , A61P43/00 , C07C317/48 , C07C317/50 , C07C323/58 , C07C323/59 , C07D233/76 , C07D271/06 , C07D271/07 , C07D277/56 , C07C323/00
CPC分类号: C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
摘要翻译: 本发明涉及脒基化合物及其盐和前药。 在另一个实施方案中,本发明还提供本发明化合物在治疗中的用途,特别是作为一氧化氮合酶抑制剂。 在另一个实施方案中,本发明提供了制备脒基化合物的方法。
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公开(公告)号:US06403830B2
公开(公告)日:2002-06-11
申请号:US09816577
申请日:2001-03-23
申请人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey S. Snyder , Mahima Trivedi , Sofya Tsymbalov
发明人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey S. Snyder , Mahima Trivedi , Sofya Tsymbalov
IPC分类号: C07C32358
CPC分类号: C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要: The present invention relates to S-[2-[(1-Iminoethyl)amino]ethyl]-2-methyl-L-cysteine, or a pharmaceutically acceptable salt thereof.
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3.Methods of making amidino compounds useful as nitric oxide synthase inhibitors 有权
标题翻译: 制备脒基化合物可用作一氧化氮合酶抑制剂的方法公开(公告)号:US07102013B2
公开(公告)日:2006-09-05
申请号:US10321969
申请日:2002-12-17
申请人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
发明人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
IPC分类号: C07D233/40 , C07C271/00 , C07C323/00
CPC分类号: C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要: Method of making an alpha-amino acid compound having the structure of Formula 32: comprising treating under hydrolyzing conditions a hydantoin compound having the structure of Formula 33: where the substituents are described herein.
摘要翻译: 制备具有式32结构的α-氨基酸化合物的方法:包括在水解条件下处理具有结构式33的乙内酰脲化合物:其中取代基在本文中描述。
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公开(公告)号:US07196118B2
公开(公告)日:2007-03-27
申请号:US11032650
申请日:2005-01-10
申请人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
发明人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
IPC分类号: A61K31/195
CPC分类号: C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
摘要翻译: 本发明涉及脒基化合物及其盐和前药。 在另一个实施方案中,本发明还提供本发明化合物在治疗中的用途,特别是作为一氧化氮合酶抑制剂。 在另一个实施方案中,本发明提供了制备脒基化合物的方法。
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公开(公告)号:US06586474B2
公开(公告)日:2003-07-01
申请号:US09816575
申请日:2001-03-23
申请人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
发明人: Ronald Keith Webber , Richard C. Durley , Alok K. Awasthi , Arija A. Bergmanis , Kam F. Fok , Scott S. Ganser , Timothy J. Hagen , E. Ann Hallinan , Donald W. Hansen, Jr. , Brian S. Hickory , Pamela T. Manning , Michael Mao , Alan E. Moormann , Barnett S. Pitzele , Michelle A. Promo , Richard R. Schartman , Jeffrey A. Scholten , Jeffrey S. Snyder , Mihaly V. Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Siong Tjoeng
IPC分类号: A61K31195
CPC分类号: C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要: The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
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6.2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译: 可用作一氧化氮合酶抑制剂的2-氨基-2-烷基-4-己烯酸和己炔酸衍生物公开(公告)号:US07005450B2
公开(公告)日:2006-02-28
申请号:US10819853
申请日:2004-04-07
申请人: Richard C. Durley , James Sikorski , Donald W. Hansen, Jr. , Michelle A. Promo , Ronald Keith Webber , Barnett S. Pitzele , Alok K. Awasthi , Alan Moormann
发明人: Richard C. Durley , James Sikorski , Donald W. Hansen, Jr. , Michelle A. Promo , Ronald Keith Webber , Barnett S. Pitzele , Alok K. Awasthi , Alan Moormann
IPC分类号: A61K31/195
CPC分类号: C07D209/48 , A61K31/198 , C07C229/30 , C07C251/08 , C07C251/16 , C07C255/30 , C07C257/14 , C07C271/22 , C07D271/07 , C07D413/06
摘要: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
摘要翻译: 本发明涉及2-氨基-2-烷基-4-己烯酸和己酸衍生物及其在治疗中的用途,特别是其用作一氧化氮合酶抑制剂。
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7.2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives useful as nitric oxide synthase inhibitors 失效
标题翻译: 可用作一氧化氮合酶抑制剂的2-氨基-2-烷基-4-己烯酸和己炔酸衍生物公开(公告)号:US06756406B2
公开(公告)日:2004-06-29
申请号:US09952906
申请日:2001-09-15
申请人: Richard C. Durley , James Sikorski , Donald W. Hansen, Jr. , Michelle A. Promo , Ronald Keith Webber , Barnett S. Pitzele , Alok K. Awasthi , Alan Moorman
发明人: Richard C. Durley , James Sikorski , Donald W. Hansen, Jr. , Michelle A. Promo , Ronald Keith Webber , Barnett S. Pitzele , Alok K. Awasthi , Alan Moorman
IPC分类号: C07D27106
CPC分类号: C07D209/48 , A61K31/198 , C07C229/30 , C07C251/08 , C07C251/16 , C07C255/30 , C07C257/14 , C07C271/22 , C07D271/07 , C07D413/06
摘要: The present invention relates to 2-amino-2-alkyl-4 hexenoic and hexynoic acid derivatives and their use in therapy, in particular their use as nitric oxide synthase inhibitors.
摘要翻译: 本发明涉及2-氨基-2-烷基-4-己烯酸和己酸衍生物及其在治疗中的用途,特别是其用作一氧化氮合酶抑制剂。
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8.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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9.Substituted N,N-disubstituted cycloalkyl 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取代的N,N-二取代的环烷基氨基醇化合物公开(公告)号:US06683099B2
公开(公告)日:2004-01-27
申请号:US10155451
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 cycloalkyl aminoalcohols. A preferred specific N,N-disubstituted cycloalkyl 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-二取代的环烷基氨基醇。 优选的具体的N,N-二取代的环烷基氨基醇是化合物:
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10.Substituted N, N-disubstituted mercapto amino 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-二取代的巯基氨基化合物公开(公告)号:US06677380B2
公开(公告)日:2004-01-13
申请号:US10155346
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: A61K31145
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 mercapto amines. A preferred specific N,N-disubstituted mercapto 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-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-二取代的巯基胺。 优选的具体的N,N-二取代巯基胺是化合物:
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