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公开(公告)号：US6004981A
公开(公告)日：1999-12-21
申请号：US913241
申请日：1997-12-08
申请人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
发明人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
IPC分类号： C07D213/69 , A61K31/44 , C07D213/79 , C07D401/04 , C07D401/12
CPC分类号： C07D213/69
摘要： This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译： PCT No.PCT / US96 / 02641 Sec。 371 1997年12月8日第 102（e）日期1997年12月8日PCT 1996年3月8日PCT公布。 WO96 / 28427 PCT出版物 日期1996年9月19日本发明涉及可用作抗凝剂的苯甲脒衍生物。 本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。
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公开(公告)号：US5877181A
公开(公告)日：1999-03-02
申请号：US910774
申请日：1997-08-13
申请人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
发明人： Brad O. Buckman , David D. Davey , William J. Guilford , Michael M. Morrissey , Howard P. Ng , Gary B. Phillips , Shung C. Wu , Wei Xu
IPC分类号： A61P7/02 , C07C257/18 , C07C275/42 , C07D213/69 , C07D213/74 , C07D213/79 , C07D213/81 , C07D213/82 , C07D239/52 , C07D241/18 , C07D401/04 , C07D401/12 , C07D401/14 , C07D521/00 , A61K31/505 , C07D239/02 , C07D239/10
CPC分类号： C07D213/69 , C07C257/18 , C07C275/42 , C07D213/74 , C07D213/79 , C07D213/81 , C07D213/82 , C07D231/12 , C07D233/56 , C07D239/52 , C07D241/18 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14
摘要： This invention is directed to benzamidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
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公开(公告)号：US08008325B2
公开(公告)日：2011-08-30
申请号：US12332619
申请日：2008-12-11
申请人： Brad O. Buckman , Kumar Emayan , Imadul Islam , Karen May , Judi Bryant , Raju Mohan , Christopher West , Shendong Yuan
发明人： Brad O. Buckman , Kumar Emayan , Imadul Islam , Karen May , Judi Bryant , Raju Mohan , Christopher West , Shendong Yuan
IPC分类号： A61K31/445 , C07D211/00
CPC分类号： C07F9/655345 , C07C323/58 , C07C327/34 , C07D211/34 , C07F9/301 , C07F9/302 , C07F9/306 , C07F9/3211 , C07F9/3241 , C07F9/3882 , C07F9/4006 , C07F9/4056 , C07F9/4087 , C07F9/6524
摘要： Compounds of the following formula (I), for example: wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.
摘要翻译： 下列通式（I）的化合物，其中R1，R2，R3和R4如本文所述，可用作血浆羧肽酶B的抑制剂。含有这些化合物的药物组合物，使用这些化合物作为抗血栓形成剂和方法 用于合成这些化合物也在本文中描述。
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公开(公告)号：US06274091B1
公开(公告)日：2001-08-14
申请号：US09277724
申请日：1999-03-29
IPC分类号： G01N100
CPC分类号： B01J19/0046 , B01J2219/00286 , B01J2219/00308 , B01J2219/0031 , B01J2219/00335 , B01J2219/00394 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00484 , B01J2219/00495 , B01J2219/005 , B01J2219/00547 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00686 , B01J2219/0072 , C40B50/14 , C40B60/14 , C40B70/00 , Y10S436/809 , Y10T436/25 , Y10T436/25375
摘要： Multiple chemical reactions are performed in a plurality of reaction vessels mounted in inlets in a manifold valve block. The manifold valve block is connected to a channel block which is utilized in conjunction with a solvent delivery system as part of the reaction cycle. The solvent fluid is drained from the reaction vessels when valves in the manifold valve block are opened while applying a vacuum thereto. Optionally, a thermal block may be utilized in conjunction with the manifold valve block and the channel block to facilitate the reaction. Upon completion of the reactant cycle, the manifold valve block is disconnected from the channel block and connected to a cleavage block assembly which contains vials for collecting reaction products. The cleavage product is drained from the reaction vessels through the manifold valve block into the vials upon opening the valves in the manifold valve block and applying a vacuum to the channel block.
摘要翻译： 在安装在歧管阀块中的入口中的多个反应容器中进行多次化学反应。 歧管阀块连接到通道块，其与作为反应循环的一部分的溶剂输送系统结合使用。 当在歧管阀块中的阀打开同时向其施加真空时，将溶剂流体从反应容器中排出。 可选地，热块可以与歧管阀块和通道块一起使用以促进反应。 在完成反应物循环后，歧管阀块与通道块断开连接并连接到包含用于收集反应产物的小瓶的裂解块组件。 在打开歧管阀块中的阀并且向通道块施加真空时，裂解产物从反应容器通过歧管阀块排出到小瓶中。
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公开(公告)号：US5888830A
公开(公告)日：1999-03-30
申请号：US717797
申请日：1996-09-23
CPC分类号： B01J19/0046 , B01J2219/00286 , B01J2219/00308 , B01J2219/0031 , B01J2219/00335 , B01J2219/00394 , B01J2219/00416 , B01J2219/00423 , B01J2219/00454 , B01J2219/00484 , B01J2219/00495 , B01J2219/005 , B01J2219/00547 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00686 , B01J2219/0072 , C40B50/14 , C40B60/14 , C40B70/00 , Y10S436/809 , Y10T436/25 , Y10T436/25375
摘要： Multiple chemical reactions are performed in a plurality of reaction vessels mounted in inlets in a manifold valve block. The manifold valve block is connected to a channel block which is utilized in conjunction with a solvent delivery system as part of the reaction cycle. The solvent fluid is drained from the reaction vessels when valves in the manifold valve block are opened while applying a vacuum thereto. Optionally, a thermal block may be utilized in conjunction with the manifold valve block and the channel block to facilitate the reaction. Upon completion of the reactant cycle, the manifold valve block is disconnected from the channel block and connected to a cleavage block assembly which contains vials for collecting reaction products. The cleavage product is drained from the reaction vessels through the manifold valve block into the vials upon opening the valves in the manifold valve block and applying a vacuum to the channel block.
摘要翻译： 在安装在歧管阀块中的入口中的多个反应容器中进行多次化学反应。 歧管阀块连接到通道块，其与作为反应循环的一部分的溶剂输送系统结合使用。 当在歧管阀块中的阀打开同时向其施加真空时，将溶剂流体从反应容器中排出。 可选地，热块可以与歧管阀块和通道块一起使用以促进反应。 在完成反应物循环后，歧管阀块与通道块断开连接并连接到包含用于收集反应产物的小瓶的裂解块组件。 在打开歧管阀块中的阀并且向通道块施加真空时，裂解产物从反应容器通过歧管阀块排出到小瓶中。
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公开(公告)号：US5846972A
公开(公告)日：1998-12-08
申请号：US877231
申请日：1997-06-17
IPC分类号： A61K31/519 , A61K31/535 , A61K31/5383 , A61K31/542 , A61P7/02 , A61P43/00 , C07D475/02 , C07D475/04 , C07D475/06 , C07D475/08 , C07D498/04 , C07D513/04 , C07D265/36 , C07D498/02
CPC分类号： C07D475/02
摘要： This invention is directed to bicyclic pyrimidine derivatives of the following formulae: ##STR1## where A is --O--and Z.sup.1,Z.sup.2,R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.7 are defined herein. These compounds are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing these compounds and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译： 本发明涉及下式的双环嘧啶衍生物：其中A是-O - 和Z 1，Z 2，R 1，R 2，R 3，R 4，R 5，R 6，R 7 在本文中定义。 这些化合物可用作抗凝剂。 本发明还涉及含有这些化合物的药物组合物和使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。
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公开(公告)号：US5846970A
公开(公告)日：1998-12-08
申请号：US877318
申请日：1997-06-17
IPC分类号： A61K31/519 , A61K31/535 , A61K31/5383 , A61K31/542 , A61P7/02 , A61P43/00 , C07D475/02 , C07D475/04 , C07D475/06 , C07D475/08 , C07D498/04 , C07D513/04 , A61K31/54 , C07D513/00
CPC分类号： C07D475/02
摘要： This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译： 本发明涉及可用作抗凝剂的双环嘧啶衍生物。 本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。
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公开(公告)号：US5693641A
公开(公告)日：1997-12-02
申请号：US699372
申请日：1996-08-16
IPC分类号： A61K31/519 , A61K31/535 , A61K31/5383 , A61K31/542 , A61P7/02 , A61P43/00 , C07D475/02 , C07D475/04 , C07D475/06 , C07D475/08 , C07D498/04 , C07D513/04 , A61K31/505
CPC分类号： C07D475/02
摘要： This invention is directed to bicyclic pyrimidine derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译： 本发明涉及可用作抗凝剂的双环嘧啶衍生物。 本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。
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公开(公告)号：US5753635A
公开(公告)日：1998-05-19
申请号：US689979
申请日：1996-08-16
IPC分类号： C07D487/04 , A61K31/52 , A61P7/02 , A61P43/00 , C07D473/00 , C07D473/02 , C07D473/04 , C07D473/16 , C07D473/18 , C07D473/30 , C07D473/22
CPC分类号： C07D473/00 , C07D473/04
摘要： This invention is directed to purine derivatives of the following formulae: ##STR1## wherein Z.sup.1 is --O--, --N(R.sup.10)-- or --CH.sub.2 O--; Z.sup.2 is --O--, --N(R.sup.10)-- or --OCH.sub.2 --; R.sup.1 and R.sup.4 are each independently hydrogen, halo, alkyl, --OR.sup.10, --C(O)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --N(R.sup.10)C(O)R.sup.10, or --N(H)S(O).sub.2 R.sup.13 ; R.sup.2 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(NH)N(H)C(O)OR.sup.13, --C(NH)N(H)C(O)R.sup.10, --C(NH)N(H)S(O).sub.2 R.sup.13, or --C(NH)N(H)C(O)N(H)R.sup.10 ; R.sup.3 is halo, alkyl, haloalkyl, haloalkoxy, ureido, cyano, guanidino, --OR.sup.10, --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --R.sup.12 --C(O)N(R.sup.10)R.sup.11, --CH(OH)C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --R.sup.12 --N(R.sup.10)R.sup.11, --C(O)OR.sup.10, --R.sup.12 --C(O)OR.sup.10, --N(R.sup.10)C(O)R.sup.10, (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); R.sup.5 is hydrogen, halo, alkyl, cycloalkyl, haloakyl, aryl, aralkyl, alkylthio, hydroxy, mercapto, alkoxy, or --N(R.sup.10)R.sup.11 ; and R.sup.6 is defined herein. These compounds are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译： 本发明涉及以下分子式的嘌呤衍生物：其中Z 1为-O - ， - N（R 10） - 或（III）的化合物 -CH 2 O- Z2是-O - ， - N（R10） - 或-OCH2-; R 1和R 4各自独立地为氢，卤素，烷基，-OR 10，-C（O）OR 10，-C（O）N（R 10）R 11，-N（R 10）R 11，-N（R 10） ，或-N（H）S（O）2 R 13; R 2是-C（NH）NH 2，-C（NH）N（H）OR 10，-C（NH）N（H）C（O）OR 13，-C（NH）N（H）C（O） -C（NH）N（H）S（O）2 R 13或-C（NH）N（H）C（O）N（H） R 3是卤素，烷基，卤代烷基，卤代烷氧基，脲基，氰基，胍基，-OR 10，-C（NH）NH 2，-C（NH）N（H）OR 10，-C（O）N（R 10）R 11，-R 12 -C（O）N（R10）R11，-CH（OH）C（O）N（R10）R11，-N（R10）R11，-R12-N（R10）R11，-C（O）OR10， R 12 -C（O）OR 10，-N（R 10）C（O）R 10，（1,2） - 四氢嘧啶基（任选被烷基取代），（1,2） - 咪唑基（任选被烷基取代） ，2） - 咪唑啉基（任选被烷基取代）; R5是氢，卤素，烷基，环烷基，卤代烷基，芳基，芳烷基，烷硫基，羟基，巯基，烷氧基或-N（R10）R11; 并且R6在本文中定义。 这些化合物可用作抗凝剂。 本发明还涉及含有本发明化合物的药物组合物，以及使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。
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公开(公告)号：US20090257979A1
公开(公告)日：2009-10-15
申请号：US12423720
申请日：2009-04-14
IPC分类号： A61K31/5415 , C07D285/22 , C12N9/99 , A61K38/21 , A61P31/18 , A61P31/20
CPC分类号： C07D471/04 , C07D285/30 , C07D417/04 , C07D487/04
摘要： The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
摘要翻译： 实施方案提供了通式I的化合物，以及包含主题化合物的组合物，包括药物组合物。 实施方案还提供治疗方法，包括治疗丙型肝炎病毒感染的方法和治疗肝纤维化的方法，所述方法通常涉及向有需要的个体施用有效量的主题化合物或组合物。
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