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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：US06995156B2
公开(公告)日：2006-02-07
申请号：US10947635
申请日：2004-09-22
申请人： Judi A. Bryant , Brad O. Buckman , Imadul Islam , Raju Mohan , Michael M. Morrissey , Guo Ping Wei , Wei Xu , Shendong Yuan
发明人： Judi A. Bryant , Brad O. Buckman , Imadul Islam , Raju Mohan , Michael M. Morrissey , Guo Ping Wei , Wei Xu , Shendong Yuan
IPC分类号： A61K31/496 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D295/205 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. 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： 下式（I）的化合物：化学式id =“CHEM-US-00001”num =“000
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公开(公告)号：US06861424B2
公开(公告)日：2005-03-01
申请号：US10163742
申请日：2002-06-05
申请人： Judi A. Bryant , Brad O. Buckman , Imadul Islam , Raju Mohan , Michael M. Morrissey , Guo Ping Wei , Wei Xu , Shendong Yuan
发明人： Judi A. Bryant , Brad O. Buckman , Imadul Islam , Raju Mohan , Michael M. Morrissey , Guo Ping Wei , Wei Xu , Shendong Yuan
IPC分类号： C07D295/20 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P7/02 , A61P43/00 , C07D215/48 , C07D215/54 , C07D215/56 , C07D295/205 , C07D307/33 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
CPC分类号： C07D295/205 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. 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： 下式（I）的化合物：其中a，b，R 1，R 2，R 3，R 4和R 6如本文所述，可用作血小板二磷酸腺苷的抑制剂 。 本文还描述了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的方法和合成这些化合物的方法。
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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：US07026323B2
公开(公告)日：2006-04-11
申请号：US10947579
申请日：2004-09-22
申请人： Judi A. Bryant , Brad O. Buckman , Imadul Islam , Raju Mohan , Michael M. Morrissey , Guo Ping Wei , Wei Xu , Shendong Yuan
发明人： Judi A. Bryant , Brad O. Buckman , Imadul Islam , Raju Mohan , Michael M. Morrissey , Guo Ping Wei , Wei Xu , Shendong Yuan
IPC分类号： A61K31/497
CPC分类号： C07D295/205 , C07D215/48 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. 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： 下式（I）的化合物：其中a，b，R 1，R 2，R 3，R 4， / SUP>和R 6 6在本文中描述，可用作血小板二磷酸腺苷的抑制剂。 本文还描述了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的方法和合成这些化合物的方法。
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公开(公告)号：US07268140B2
公开(公告)日：2007-09-11
申请号：US11248618
申请日：2005-10-13
申请人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
发明人： John G. Bauman , Brad O. Buckman , Ameen F. Ghannam , Joseph E. Hesselgesser , Richard Horuk , Imadul Islam , Meina Liang , Karen B. May , Sean D. Monahan , Michael M. Morrissey , Howard P. Ng , Kenneth J. Shaw , Guo Ping Wei , Wei Xu , Zuchun Zhao , Wei Zheng
IPC分类号： A61K31/4965 , C07D241/04
CPC分类号： C07D295/185 , C07D215/18 , C07D241/04 , C07D241/38 , C07D261/14 , C07D295/192 , C07D307/52 , C07D403/06 , C07D403/12 , C07D405/12 , C07D413/12
摘要： This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.
摘要翻译： 本发明涉及可用作抗炎剂的酰基哌嗪衍生物。 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人类炎性疾病的方法。
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