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公开(公告)号：US07208517B1
公开(公告)日：2007-04-24
申请号：US09653563
申请日：2000-08-31
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King , Todd J. Janus , Robert J. Padley
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King , Todd J. Janus , Robert J. Padley
IPC分类号： A61K31/40
CPC分类号： A61K31/40
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, a method of antagonizing endothelin, methods for the inhibition of bone metastases, methods for the prevention of growth of new metastases, methods for the inhibition of bone turnover, and methods for the prevention of bone loss in patients, including cancer patients, using an endothelin ET-A receptor antagonist.
摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，以及其制备方法和中间体，拮抗内皮素的方法，抑制骨转移的方法，预防生长的方法 的新转移，抑制骨转换的方法，以及使用内皮素ET-A受体拮抗剂预防患者（包括癌症患者）的骨丢失的方法。
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公开(公告)号：US06462194B1
公开(公告)日：2002-10-08
申请号：US09572493
申请日：2000-05-15
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
IPC分类号： C07D26530
CPC分类号： C07D207/27 , C07D207/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07F9/572 , C07F9/59
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，以及其制备方法和中间体，以及拮抗内皮素的方法。
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公开(公告)号：US06380241B1
公开(公告)日：2002-04-30
申请号：US09714934
申请日：2000-11-17
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
IPC分类号： C07D40502
CPC分类号： C07D207/27 , C07D207/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07F9/572 , C07F9/59
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，以及其制备方法和中间体，以及拮抗内皮素的方法。
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公开(公告)号：US07365093B2
公开(公告)日：2008-04-29
申请号：US11063476
申请日：2005-02-23
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
IPC分类号： A01N43/36 , C07D405/00
CPC分类号： C07D207/16 , C07D405/04 , C07D405/14 , C07D413/14
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，以及其制备方法和中间体，以及拮抗内皮素的方法。
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公开(公告)号：US06946481B1
公开(公告)日：2005-09-20
申请号：US10266270
申请日：2002-10-08
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
IPC分类号： A61K31/40 , C07D207/00 , C07D405/04
CPC分类号： C07D405/04
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，以及其制备方法和中间体，以及拮抗内皮素的方法。
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公开(公告)号：US6162927A
公开(公告)日：2000-12-19
申请号：US905913
申请日：1997-08-04
申请人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
发明人： Martin Winn , Steven A. Boyd , Charles W. Hutchins , Hwan-Soo Jae , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Bryan K. Sorensen , Bruce G. Szczepankiewicz , Kenneth J. Henry , Gang Liu , Steven J. Wittenberger , Steven A. King
IPC分类号： C07D207/16 , C07D207/26 , C07D207/27 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07F9/572 , C07F9/59 , C07D405/02 , C07D405/06 , A61K41/30 , A61N9/06 , A61N9/10
CPC分类号： C07D207/27 , C07D207/16 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/14 , C07D417/14 , C07F9/572 , C07F9/59
摘要： A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
摘要翻译： 公开了式（I）化合物或其药学上可接受的盐，以及其制备方法和中间体，以及拮抗内皮素的方法。
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公开(公告)号：US06204293B1
公开(公告)日：2001-03-20
申请号：US09073807
申请日：1998-05-07
申请人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorensen , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang , Gang Liu , Indrani W. Gunawardana
发明人： Said M. Sebti , Andrew D. Hamilton , David J. Augeri , Kenneth J. Barr , Stephen A. Fakhoury , David A. Janowick , Douglas M. Kalvin , Stephen J. O'Connor , Saul H. Rosenberg , Wang Shen , Rolf E. Swenson , Bryan K. Sorensen , Gerard M. Sullivan , Andrew S. Tasker , James T. Wasicak , Lissa T. J. Nelson , Kenneth J. Henry , Le Wang , Gang Liu , Indrani W. Gunawardana
IPC分类号： C07C26302
CPC分类号： C07C237/36 , C07B2200/07 , C07C239/20 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C327/42 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2603/18 , C07C2603/24 , C07C2603/74 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/10 , C07D207/12 , C07D207/26 , C07D207/267 , C07D209/48 , C07D211/14 , C07D211/42 , C07D211/52 , C07D211/58 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/36 , C07D213/38 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/68 , C07D213/70 , C07D213/71 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D213/89 , C07D231/12 , C07D233/56 , C07D233/64 , C07D233/90 , C07D235/06 , C07D237/14 , C07D239/26 , C07D239/42 , C07D241/04 , C07D241/12 , C07D241/18 , C07D249/08 , C07D253/06 , C07D257/04 , C07D261/02 , C07D263/22 , C07D263/32 , C07D265/30 , C07D277/30 , C07D277/36 , C07D277/48 , C07D277/50 , C07D277/587 , C07D279/12 , C07D295/084 , C07D295/13 , C07D295/155 , C07D295/185 , C07D307/54 , C07D307/81 , C07D317/30 , C07D317/60 , C07D333/18 , C07D333/20 , C07D333/24 , C07D401/12 , C07D405/04 , C07D405/12 , C07D409/12 , C07D417/12 , C07D487/08 , C07F9/5333
摘要： Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is heterocyclic, aryl, substituted or unsubstituted cycloalkyl; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5—, (e) —L4—L6—S(O)m—N(R5)—L5 —, (f) —L4—N(R5)—C(W)—L7—L5 —, (g) —L4—N(R5)—S(O)p—L7—L5—, (h) optionally substituted alkylene, (i) optionally substituted alkenylene, and (j) optionally substituted alkynylene are inhibitors of protein isoprenyl transferases. Also disclosed are protein isoprenyl transferase inhibiting compositions and a method of inhibiting protein isoprenyl transferases.
摘要翻译： 具有式的化合物或其药学上可接受的盐，其中R 1是（a）氢，（b）低级烷基，（c）烯基，（d）烷氧基，（e）硫代烷氧基，（f）卤素，（g）卤代烷基，（h） 芳基-L2-和（i）杂环-L2-; R2选自（b）-C（O）NH-CH（R14）-C（O）OR15，（d）-C（O）NH-CH（R14）-C（O）NHSO2R16，（e） C（O）NH-CH（R 14） - 四唑基，（f）-C（O）NH-杂环基和（g）-C（O）NH-CH（R 14）-C（O）NR 17 R 18; R3是杂环，芳基，取代或未取代的环烷基; R4是氢，低级烷基，卤代烷基，卤素，芳基，芳基烷基，杂环或（杂环）烷基; （a）-L4-N（R5）-L5-，（b）-L4-O-L5-，（c）-L4-S（O）n-L5-（d） - L4-L6-C（W）-N（R5）-L5-，（e）-L4-L6-S（O）mN（R5）-L5 - ，（f）-L4-N（R5）-C W）-L7-L5 - ，（g）-L4-N（R5）-S（O）p-L7-L5-，（h）任选取代的亚烷基，（i）任选取代的亚烯基，和（j） 亚炔基是蛋白质异戊二烯转移酶的抑制剂。 还公开了蛋白质异戊二烯转移酶抑制组合物和抑制蛋白质异戊二烯转移酶的方法。
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8.发明授权公开(公告)号：US06878700B1
公开(公告)日：2005-04-12
申请号：US09541795
申请日：2000-03-31
申请人： James Link , Gang Liu , ZhongHua Pei , Tom von Geldern , Martin Winn , Zhili Xin , Steven A. Boyd , Gui-Dong Zhu , Jennifer C. Freeman , Indrani W. Gunawardana , Michael A. Staeger , Hwan-Soo Jae , John K. Lynch , Sheldon Wang
发明人： James Link , Gang Liu , ZhongHua Pei , Tom von Geldern , Martin Winn , Zhili Xin , Steven A. Boyd , Gui-Dong Zhu , Jennifer C. Freeman , Indrani W. Gunawardana , Michael A. Staeger , Hwan-Soo Jae , John K. Lynch , Sheldon Wang
IPC分类号： A61K31/454 , A61K31/495 , A61K31/496 , A61K31/537 , A61K31/54 , C07C323/62 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/26 , C07D207/27 , C07D209/08 , C07D211/20 , C07D211/46 , C07D211/60 , C07D213/40 , C07D213/81 , C07D217/06 , C07D241/04 , C07D295/185 , C07D295/26 , C07D401/04 , C07D521/00 , A61K31/33 , A61K31/415 , C07D221/02 , C07D265/30 , C07D319/00
CPC分类号： C07D207/27 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/537 , A61K31/54 , C07C323/62 , C07C2601/02 , C07D205/04 , C07D207/09 , C07D207/14 , C07D209/08 , C07D211/20 , C07D211/46 , C07D211/60 , C07D213/40 , C07D213/81 , C07D217/06 , C07D231/12 , C07D233/56 , C07D241/04 , C07D249/08 , C07D295/185 , C07D295/26 , C07D401/04
摘要： The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immunune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
摘要翻译： 本发明涉及可用于治疗炎性和免疫疾病的新型肉桂酰胺化合物，含有这些化合物的药物组合物，以及抑制哺乳动物炎症或抑制免疫应答的方法。
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9.发明申请公开(公告)号：US20050250768A1
公开(公告)日：2005-11-10
申请号：US10921965
申请日：2004-08-20
申请人： James Link , Gang Liu , ZhongHua Pei , Tom Geldern , Martin Winn , Zhili Xin , Steven Boyd , Gui-Dong Zhu , Jennifer Freeman , Indrani Gunawardana , Michael Staeger , Hwan-Soo Jae , John Lynch , Sheldon Wang
发明人： James Link , Gang Liu , ZhongHua Pei , Tom Geldern , Martin Winn , Zhili Xin , Steven Boyd , Gui-Dong Zhu , Jennifer Freeman , Indrani Gunawardana , Michael Staeger , Hwan-Soo Jae , John Lynch , Sheldon Wang
IPC分类号： A61K31/454 , A61K31/495 , A61K31/496 , A61K31/537 , A61K31/54 , C07C323/62 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/26 , C07D207/27 , C07D209/08 , C07D211/20 , C07D211/46 , C07D211/60 , C07D213/40 , C07D213/81 , C07D217/06 , C07D241/04 , C07D295/185 , C07D295/26 , C07D401/04 , C07D521/00
CPC分类号： C07D207/27 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/537 , A61K31/54 , C07C323/62 , C07C2601/02 , C07D205/04 , C07D207/09 , C07D207/14 , C07D209/08 , C07D211/20 , C07D211/46 , C07D211/60 , C07D213/40 , C07D213/81 , C07D217/06 , C07D231/12 , C07D233/56 , C07D241/04 , C07D249/08 , C07D295/185 , C07D295/26 , C07D401/04
摘要： The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.
摘要翻译： 本发明涉及可用于治疗炎症和免疫疾病的新颖的肉桂酰胺化合物，含有这些化合物的药物组合物，以及抑制哺乳动物炎症或抑制免疫反应的方法。
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公开(公告)号：US20060229280A1
公开(公告)日：2006-10-12
申请号：US11063476
申请日：2005-02-23
申请人： Martin Winn , Steven Boyd , Charles Hutchins , Hwan-Soo Jae , Andrew Tasker , Thomas von Geldern , Jeffrey Kester , Bryan Sorensen , Bruce Szczepankiewicz , Kenneth Henry , Gang Liu , Steven Wittenberger , Steven King
发明人： Martin Winn , Steven Boyd , Charles Hutchins , Hwan-Soo Jae , Andrew Tasker , Thomas von Geldern , Jeffrey Kester , Bryan Sorensen , Bruce Szczepankiewicz , Kenneth Henry , Gang Liu , Steven Wittenberger , Steven King
IPC分类号： A61K31/675 , A61K31/454 , C07D413/02 , C07D43/02
CPC分类号： C07D207/16 , C07D405/04 , C07D405/14 , C07D413/14
摘要： A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, and a method of antagonizing endothelin.
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