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1.Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method 失效
标题翻译: 构象限制的微粒体甘油三酯转运蛋白的芳香族抑制剂和方法公开(公告)号:US5760246A
公开(公告)日:1998-06-02
申请号:US767923
申请日:1996-12-17
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Jeffrey A. Robl , William A. Slusarchyk , Richard B. Sulsky , Joseph A. Tino
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Jeffrey A. Robl , William A. Slusarchyk , Richard B. Sulsky , Joseph A. Tino
IPC分类号: C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C233/78 , C07C235/40 , C07C237/12 , C07C237/24 , C07C255/41 , C07C259/08 , C07C271/22 , C07C271/24 , C07C291/04 , C07C307/06 , C07C311/21 , C07C311/46 , C07C317/12 , C07C317/44 , C07C321/22 , C07C323/60 , C07D207/32 , C07D207/335 , C07D213/40 , C07D213/64 , C07D213/75 , C07D221/16 , C07D233/88 , C07D233/90 , C07D233/92 , C07D295/185 , C07D307/52 , C07D311/82 , C07D333/20 , C07D405/12 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/40 , C07F9/576 , C07F9/58 , C07F9/6506 , C07F9/655 , C07F9/6571 , C07D235/16
CPC分类号: C07D207/335 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C233/78 , C07C235/40 , C07C237/12 , C07C237/24 , C07C255/41 , C07C259/08 , C07C271/22 , C07C271/24 , C07C291/04 , C07C307/06 , C07C311/21 , C07C311/46 , C07C317/12 , C07C317/44 , C07C321/22 , C07C323/60 , C07D213/40 , C07D213/64 , C07D213/75 , C07D221/16 , C07D233/88 , C07D233/90 , C07D233/92 , C07D295/185 , C07D307/52 , C07D311/82 , C07D333/20 , C07D405/12 , C07D407/12 , C07D409/12 , C07F7/1856 , C07F9/4006 , C07F9/4018 , C07F9/5765 , C07F9/582 , C07F9/588 , C07F9/65061 , C07F9/65062 , C07F9/65067 , C07F9/65068 , C07F9/65515 , C07F9/6552 , C07F9/65522 , C07F9/657181 , C07C2101/02 , C07C2101/14 , C07C2103/18 , C07C2103/32 , C07C2103/76
摘要: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure ##STR1## including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; R.sup.x is H, alkyl, aryl or halogen; A is (1) a bond; (2) --O--; or (3) ##STR2## B is: ##STR3## and wherein L.sup.2, L.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.3', R.sup.3a, R.sup.3b, R.sup.4, R.sup.4', R.sup.5, X, ##STR4## are as defined herein.
摘要翻译: 提供了新的化合物,其是MTP的抑制剂,因此可用于降低血清脂质和治疗动脉粥样硬化和相关疾病,并且具有包含其药学上可接受的盐或前药酯的结构(图) 其中q为0,1或2; Rx是H,烷基,芳基或卤素; A是(1)债券; (2)-O- 或(3)
B是: 或 或 或 或 或 或 ,其中L2,L1,R1,R2,R3,R3 ',R3a,R3b,R4,R4',R5,X, 如本文所定义。 -
2.
公开(公告)号:US5712279A
公开(公告)日:1998-01-27
申请号:US548811
申请日:1996-01-11
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Jeffrey A. Robl , Richard B. Sulsky , Joseph A. Tino
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Jeffrey A. Robl , Richard B. Sulsky , Joseph A. Tino
IPC分类号: A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/52 , A61K31/535 , A61P3/06 , A61P9/10 , A61P43/00 , C07D211/00 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/98 , C07D215/38 , C07D217/00 , C07D217/22 , C07D221/16 , C07D241/04 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12
CPC分类号: C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
摘要: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein Z, X.sup.1, X.sup.2, x and R.sup.5 are as defined herein.
摘要翻译: 提供抑制微粒体甘油三酯转运蛋白的化合物,因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。 化合物具有结构
,其中Z,X1,X2,X和R5如本文所定义。 -
3.Conformationally restricted aromatic inhibitors of microsomal triglyceride transfer protein and method 有权
标题翻译: 构象限制的微粒体甘油三酯转运蛋白的芳香族抑制剂和方法公开(公告)号:US06472414B1
公开(公告)日:2002-10-29
申请号:US09313883
申请日:1999-05-18
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Jeffrey A. Robl , William A. Slusarchyk , Richard B. Sulsky , Joseph A. Tino
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Jeffrey A. Robl , William A. Slusarchyk , Richard B. Sulsky , Joseph A. Tino
IPC分类号: C07D23516
CPC分类号: C07D207/335 , C07C233/58 , C07C233/59 , C07C233/60 , C07C233/62 , C07C233/63 , C07C233/78 , C07C235/40 , C07C237/12 , C07C237/24 , C07C255/41 , C07C259/08 , C07C271/22 , C07C271/24 , C07C291/04 , C07C307/06 , C07C311/21 , C07C311/46 , C07C317/12 , C07C317/44 , C07C321/22 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07C2603/18 , C07C2603/32 , C07C2603/76 , C07D213/40 , C07D213/64 , C07D213/75 , C07D221/16 , C07D233/88 , C07D233/90 , C07D233/92 , C07D295/185 , C07D307/52 , C07D311/82 , C07D333/20 , C07D405/12 , C07D407/12 , C07D409/12 , C07F7/1804 , C07F9/4006 , C07F9/4018 , C07F9/5765 , C07F9/58 , C07F9/6506 , C07F9/65068 , C07F9/65515 , C07F9/6552 , C07F9/65522 , C07F9/657181
摘要: Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0, 1 or 2; Rx is H, alkyl, aryl or halogen; A is (1) a bond; (2) —O—; or (3) B is: and wherein L2, L1, R1, R2, R3, R3′, R3a, R3b, R4, R4′, R5, X, are as defined herein.
摘要翻译: 提供了作为MTP抑制剂的新型化合物,因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病,并且其结构包括其药学上可接受的盐或其前药酯,其中q为0,1或2; Rx为H, 烷基,芳基或卤素; A是(1)键;(2)-O-; 或(3)B是:并且其中L2,L1,R1,R2,R3,R3',R3a,R3b,R4,R4',R5,X如本文所定义。
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4.
公开(公告)号:US6066650A
公开(公告)日:2000-05-23
申请号:US898303
申请日:1997-07-21
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino , John E. Lawson , Henry M. Holava , Richard A. Partyka
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino , John E. Lawson , Henry M. Holava , Richard A. Partyka
IPC分类号: A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/52 , A61K31/535 , A61P3/06 , A61P9/10 , A61P43/00 , C07D211/00 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/98 , C07D215/38 , C07D217/00 , C07D217/22 , C07D221/16 , C07D241/04 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12
CPC分类号: C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
摘要: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
摘要翻译: 提供抑制微粒体甘油三酯转运蛋白的化合物,因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。 化合物具有其中R 1至R 7,Q,X和Y如本文所定义的结构。
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公开(公告)号:US6034098A
公开(公告)日:2000-03-07
申请号:US898304
申请日:1997-07-21
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino , John E. Lawson , Henry M. Holava , Richard A. Partyka
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino , John E. Lawson , Henry M. Holava , Richard A. Partyka
IPC分类号: A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/52 , A61K31/535 , A61P3/06 , A61P9/10 , A61P43/00 , C07D211/00 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/98 , C07D215/38 , C07D217/00 , C07D217/22 , C07D221/16 , C07D241/04 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12
CPC分类号: C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
摘要: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
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6.
公开(公告)号:US5883099A
公开(公告)日:1999-03-16
申请号:US896872
申请日:1997-07-21
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino , John E. Lawson , Henry M. Holava , Richard A. Partyka
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino , John E. Lawson , Henry M. Holava , Richard A. Partyka
IPC分类号: A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/52 , A61K31/535 , A61P3/06 , A61P9/10 , A61P43/00 , C07D211/00 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/98 , C07D215/38 , C07D217/00 , C07D217/22 , C07D221/16 , C07D241/04 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12
CPC分类号: C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
摘要: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
摘要翻译: 提供抑制微粒体甘油三酯转运蛋白的化合物,因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。 化合物具有结构
ein。 -
7.
公开(公告)号:US5739135A
公开(公告)日:1998-04-14
申请号:US472067
申请日:1995-06-06
申请人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino
发明人: Scott A. Biller , John K. Dickson , R. Michael Lawrence , David R. Magnin , Michael A. Poss , Richard B. Sulsky , Joseph A. Tino
IPC分类号: A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/52 , A61K31/535 , A61P3/06 , A61P9/10 , A61P43/00 , C07D211/00 , C07D211/56 , C07D211/58 , C07D211/60 , C07D211/94 , C07D211/98 , C07D215/38 , C07D217/00 , C07D217/22 , C07D221/16 , C07D241/04 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12
CPC分类号: C07D401/04 , C07D211/58 , C07D211/60 , C07D211/94 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D419/12 , G01N2800/044
摘要: Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure ##STR1## wherein R.sup.1 to R.sup.7, Q, X and Y are as defined herein.
摘要翻译: 提供抑制微粒体甘油三酯转运蛋白的化合物,因此可用于降低血清脂质和治疗动脉粥样硬化及相关疾病。 化合物具有本文定义的结构
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8.Method for preparing compounds employing solid phase synthesis and novel linker-resin 失效
标题翻译: 使用固相合成制备化合物的方法和新的接头 - 树脂公开(公告)号:USH1729H
公开(公告)日:1998-05-05
申请号:US837560
申请日:1997-04-21
CPC分类号: C08F8/00 , C08F8/30 , C08F212/08 , C08F8/32 , C08F8/18 , C08F8/34 , C08F8/02 , C08F8/10 , C08F8/24
摘要: A method is provided for preparing various intermediates and final products including MTP inhibitors employing solid phase syntheses. A new dialkoxyaryl aldehyde linker-resin of the structure ##STR1## which serves as a starting material and method for preparing same, are also provided.
摘要翻译: 提供了一种用于制备各种中间体和最终产物的方法,包括使用固相合成的MTP抑制剂。 还提供了用作起始原料的结构“IMAGE”的新的二烷氧基芳基醛连接体 - 树脂及其制备方法。
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9.Amino-benzazoles as P2Y1 receptor inhibitors with pyridine ring and heterocyclic components 有权
标题翻译: 氨基 - 苯并唑类作为P2Y1受体抑制剂与吡啶环和杂环组分公开(公告)号:US08053450B2
公开(公告)日:2011-11-08
申请号:US12104732
申请日:2008-04-17
申请人: Timothy F. Herpin , George C. Morton , Robert P. Rehfuss , R. Michael Lawrence , Michael A. Poss , Jacques Y. Roberge , Timur Gungor
发明人: Timothy F. Herpin , George C. Morton , Robert P. Rehfuss , R. Michael Lawrence , Michael A. Poss , Jacques Y. Roberge , Timur Gungor
IPC分类号: A61K31/4436 , C07D417/12
CPC分类号: C07D401/12 , C07D235/30 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D513/04
摘要: The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译: 本发明提供了新的氨基 - 苯并唑类似物,它们是人P2Y1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y1受体活性调节作用的疾病的方法。
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公开(公告)号:US07470712B2
公开(公告)日:2008-12-30
申请号:US11038862
申请日:2005-01-19
申请人: Timothy F. Herpin , George C. Morton , Robert P. Rehfuss , R. Michael Lawrence , Michael A. Poss , Jacques Y. Roberge , Timur Gungor
发明人: Timothy F. Herpin , George C. Morton , Robert P. Rehfuss , R. Michael Lawrence , Michael A. Poss , Jacques Y. Roberge , Timur Gungor
IPC分类号: A61K31/4439 , C07D401/12
CPC分类号: C07D401/12 , C07D235/30 , C07D401/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D513/04
摘要: The present invention provides novel amino-benzazoles and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.
摘要翻译: 本发明提供了新的氨基 - 苯并唑类似物,它们是人P2Y1受体的选择性抑制剂。 本发明还提供了相同的各种药物组合物以及治疗对P2Y1受体活性调节作用的疾病的方法。
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