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1. 发明申请

WO03080631A8 PLASMA CARBOXYPEPTIDASE B INHIBITORS 审中-公开
标题翻译：等离子体羧化酶B抑制剂
公开(公告)号：WO03080631A8
公开(公告)日：2004-06-10
申请号：PCT/US0308587
申请日：2003-03-21
申请人： SCHERING AG , BUCKMAN BRAD O , EMAYAN KUMAR , ISLAM IMADUL , MAY KAREN , BRYANT JUDI , MOHAN RAJU , WEST CHRISTOPHER , YUAN SHENDONG
发明人： BUCKMAN BRAD O , EMAYAN KUMAR , ISLAM IMADUL , MAY KAREN , BRYANT JUDI , MOHAN RAJU , WEST CHRISTOPHER , YUAN SHENDONG
IPC分类号： C07C323/58 , C07C327/34 , C07D211/34 , C07F9/30 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/6524 , C07F9/6553
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: (1), wherein R , R , R , and R 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：下文描述的下式（I）的化合物，例如：（1）其中R 1，R 2，R 3和R 4在此描述可用作血浆羧肽酶B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。

2. 发明申请

WO2003080631A3 PLASMA CARBOXYPEPTIDASE B INHIBITORS 审中-公开
公开(公告)号：WO2003080631A3
公开(公告)日：2003-10-02
申请号：PCT/US2003/008587
申请日：2003-03-21
申请人： SCHERING AKTIENGESELLSCHAFT , BUCKMAN, Brad, O. , EMAYAN, Kumar , ISLAM, Imadul , MAY, Karen , BRYANT, Judi , MOHAN, Raju , WEST, Christopher , YUAN, Shendong
发明人： BUCKMAN, Brad, O. , EMAYAN, Kumar , ISLAM, Imadul , MAY, Karen , BRYANT, Judi , MOHAN, Raju , WEST, Christopher , YUAN, Shendong
IPC分类号： C07F9/30
摘要： Compounds of the following formula (I), for example: (1), wherein R 1 , R 2 , R 3 , and R 4 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.

3. 发明申请

WO1996028427A1 BENZAMIDINE DERIVATIVES THEIR PREPARATION AND THEIR USE AS ANTI-COAGULANTS 审中-公开
标题翻译：苯扎林衍生物他们的制备及其作为抗凝剂的使用
公开(公告)号：WO1996028427A1
公开(公告)日：1996-09-19
申请号：PCT/US1996002641
申请日：1996-03-08
申请人： BERLEX LABORATORIES, INC. , BUCKMAN, Brad, O. , DAVEY, David, D. , GUILFORD, William, J. , MORRISSEY, Michael, M. , NG, Howard, P. , PHILLIPS, Gary, B. , WU, Shung, C. , XU, Wei
发明人： BERLEX LABORATORIES, INC.
IPC分类号： C07D213/69
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. Accordingly, in one aspect, this invention provides compounds selected from the group consisting of formulae (I), (II), (III), (IV), (V), (VI), (VII), and (VIII), wherein: A is -C(R )= or -N=; Z and Z are independently -O-, -N(R )-, -S-, or -OCH2-; R and R are independently hydrogen, halo, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, -N(R )R , -C(O)OR , -C(O)N(R )CH2C(O)N(R )R , -N(R )C(O)N(R )R , -N(R )C(O)R , -N(R )S(O)2R , or -N(R )C(O)N(R )CH2C(O)N(R )R ; R is hydrogen; halo; alkyl; haloalkoxy; -OR ; -C(O)OR ; -C(O)N(R )R ; -N(R )R ; -C(O)N(R )(CH2)mC(O)OR (where m is 0 to 3); -N(R )(CH2)nC(O)OR (where n is 1 to 3); -N((CH2)nN(R )R )(CH2)nC(O)OR (where each n is 1 to 3); -O(CH2)nC(O)N(R )R (where n is 1 to 3); -O(CH2)pC(O)OR (where p is 1 to 6); -N(R )(CH2)nC(O)N(R )(CH2)nC(O)OR (where each n is independently 1 to 3); morpholin-4-yl; 3-tetrahydrofuranoxyl; etc.; R and R are independently hydrogen, halo, alkyl, nitro, -OR , -C(O)OR , -C(O)N(R )R , -N(R )R , -N(H)C(O)R , or -N(H)S(O)2R ; R is -C(NH)NH2, -C(NH)N(H)OR , -C(NH)N(H)C(O)OR , -C(NH)N(H)S(O)2R , -C(NH)N(H)C(O)N(R )R , or -C(NH)N(H)C(O)R ; R is halo, alkyl, haloalkyl, haloalkoxy, nitro, amino, ureido, guanidino, -OR , -C(NH)NH2, -C(NH)NHOH, -C(O)R , -(CH2)mC(O)N(R )R (where m is 0 to 3), -CH(OH)C(O)N(R )R , -(CH2)mN(R )R (where m is 0 to 3), -(CH2)mC(O)OR (where m is 0 to 3), -N(H)C(O)R , (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); each R and R is independently hydrogen alkyl, aryl, or aralkyl; R is hydrogen, alkyl, aryl, aralkyl, 1-pyrrolidinyl, 4-morpolinyl, 4-piperazinyl, 4-(N-methyl)piperazinyl, or piperidin-1-yl; R is hydrogen, alkyl or halo; and R is alkyl, aryl or aralkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：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。因此，一方面，本发明提供了选自式（I），（II），（III），（IV），（V），（VI），（VII）和（VIII）其中：A是-C（R 11）=或-N =; Z 1和Z 2独立地是-O - ， - N（R 8） - ， - S - 或-OCH 2 - ; R 1和R 3独立地是氢，卤素，烷基，卤代烷基，烷氧基，卤代烷氧基，硝基，-N（R 8）R 9，-C（O）OR 8，-C （O）N（R 8）CH 2 C（O）N（R 8）R 9，-N（R 8）C（O）N（R 8）R 9， -N（R 8）C（O）R 8，-N（R 8）S（O）2 R 12或-N（R 8）C（O） <8>）CH 2 C（O）N（R <8>）R <9>; R 2是氢; 光环; 烷基; 卤代烷氧基; -OR <8>; -C（O）OR <8>; -C（O）N（R <8>）R <9>; -N（R <8>）R <9>; -C（O）N（R 8）（CH 2）m C（O）OR 8（其中m为0至3）; -N（R 8）（CH 2）n C（O）OR 8（其中n为1至3）; -N（（CH 2）n N（R 8）R 9）（CH 2）n C（O）OR 8（其中n为1至3）; -O（CH 2）n C（O）N（R 8）R 9（其中n为1至3）; -O（CH 2）p C（O）OR 8（其中p为1至6）; -N（R 8）（CH 2）n C（O）N（R 8）（CH 2）n C（O）OR 8（其中每个n独立地为1至3）; 吗啉-4-基; 3- tetrahydrofuranoxyl; 等等。; R 4和R 7独立地是氢，卤素，烷基，硝基，-OR 8，-C（O）OR 8，-C（O）N（R 8）R 9 ，-N（R 8）R 9，-N（H）C（O）R 8或-N（H）S（O）2 R 12; R 5是-C（NH）NH 2，-C（NH）N（H）OR 8，-C（NH）N（H）C（O）OR 12，-C（NH）（H）S（O）2 R 12，-C（NH）N（H）C（O）N（R 8）R 9或-C（NH）N（H））R <8>; R 6是卤素，烷基，卤代烷基，卤代烷氧基，硝基，氨基，脲基，胍基，-OR 8，-C（NH）NH 2，-C（NH）NHOH，-C（O）， - （CH 2）m C（O）N（R 8）R 9（其中m为0至3），-CH（OH）C（O）N（R 8）R 9， - （CH2）mN（R8）R9（其中m为0至3）， - （CH2）mC（O）OR 8（其中m为0至3），-N（H） C（O）R 8，（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）或（1,2） - 咪唑啉基（任选被烷基）; 每个R 8和R 9独立地是烷基，芳基或芳烷基; R 10是氢，烷基，芳基，芳烷基，1-吡咯烷基，4-吗啉基，4-哌嗪基，4-（N-甲基）哌嗪基或哌啶-1-基; R 11是氢，烷基或卤素; 和R 12是烷基，芳基或芳烷基; 或其药学上可接受的盐。

4. 发明申请

WO2002098856A3 PIPERAZINE OXYQUINOLINE (NAPHTHALINE) PLATELET ADENOSINE DIPHOSPHATE RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2002098856A3
公开(公告)日：2002-12-12
申请号：PCT/US2002/017821
申请日：2002-06-06
申请人： SCHERING AKTIENGESELLSCHAFT , BRYANT, Judi, A. , BUCKMAN, Brad, O. , ISLAM, Imadul , MOHAN, Raju , MORRISSEY, Michael, M. , WEI, Guo, Ping , XU, Wei , YUAN, Shendong
发明人： BRYANT, Judi, A. , BUCKMAN, Brad, O. , ISLAM, Imadul , MOHAN, Raju , MORRISSEY, Michael, M. , WEI, Guo, Ping , XU, Wei , YUAN, Shendong
IPC分类号： C07D403/12
摘要： Compounds of the following formula (I): where a, b, R 1 , R 2 , R 3 , R 4 and R 6 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.

5. 发明申请

WO1997010896A1 APPARATUS AND PROCESS FOR MULTIPLE CHEMICAL REACTIONS 审中-公开
标题翻译：多种化学反应的装置和方法
公开(公告)号：WO1997010896A1
公开(公告)日：1997-03-27
申请号：PCT/US1996015124
申请日：1996-09-23
申请人： BERLEX LABORATORIES, INC. , MOHAN, Raju , BUCKMAN, Brad, O. , MORRISSEY, Michael, M. , CHITTY, Andrew, I. , MARTIN, John, T.
发明人： BERLEX LABORATORIES, INC.
IPC分类号： B01J19/00
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 (12) mounted in inlets in a manifold valve block (30). The manifold valve block (30) is connected to a channel block (34) which is utilized in conjunction with a solvent delivery system (21) as part of the reaction cycle. The solvent fluid is drained from the reaction vessels (12) when valves in the manifold valve block (30) are opened while applying a vacuum thereto. Optionally, a thermal block (40) may be utilized in conjunction with the manifold valve block (30) and the channel block (34) to facilitate the reaction. Upon completion of the reactant cycle, the manifold valve block (30) is disconnected from the channel block (34) and connected to a cleavage block assembly (120, 121) which contains vials (128) for collecting reaction products. The cleavage product is drained from the reaction vessels (12) through the manifold valve block (30) into the vials (128) upon opening the valves in the manifold valve block (30) and applying a vacuum to the channel block (34).
摘要翻译：在安装在歧管阀块（30）中的入口中的多个反应容器（12）中进行多个化学反应。歧管阀块（30）连接到与溶剂输送系统（21）结合使用的通道块（34），作为反应循环的一部分。当在歧管阀块（30）中的阀打开同时向其施加真空时，将溶剂流体从反应容器（12）排出。可选地，热块（40）可以与歧管阀块（30）和通道块（34）结合使用以促进反应。在反应物循环完成时，歧管阀块（30）与通道块（34）断开并连接到裂解块组件（120,121），裂解块组件包含用于收集反应产物的小瓶（128）。在打开歧管阀块（30）中的阀并且向通道块（34）施加真空时，将裂解产物从反应容器（12）通过歧管阀块（30）排出到小瓶（128）中。

6. 发明申请

WO2009134616A3 NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译： HEPATITIS C VIRUS REPLICATION的新型抑制剂
公开(公告)号：WO2009134616A3
公开(公告)日：2010-03-18
申请号：PCT/US2009040567
申请日：2009-04-14
申请人： INTERMUNE INC , BEIGELMAN LEONID , WANG GUANGYI , BUCKMAN BRAD O , STOYCHEVA ANTITSA DIMITROVA
发明人： BEIGELMAN LEONID , WANG GUANGYI , BUCKMAN BRAD O , STOYCHEVA ANTITSA DIMITROVA
IPC分类号： C07D285/30 , A61K31/5415 , A61P31/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/12
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。

7. 发明申请

WO2002098856A2 PLATELET ADENOSINE DIPHOSPHATE RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2002098856A2
公开(公告)日：2002-12-12
申请号：PCT/US2002/017821
申请日：2002-06-06
申请人： SCHERING AKTIENGESELLSCHAFT , BRYANT, Judi, A. , BUCKMAN, Brad, O. , ISLAM, Imadul , MOHAN, Raju , MORRISSEY, Michael, M. , WEI, Guo, Pin , XU, Wei , YUANG, Shendong
发明人： BRYANT, Judi, A. , BUCKMAN, Brad, O. , ISLAM, Imadul , MOHAN, Raju , MORRISSEY, Michael, M. , WEI, Guo, Pin , XU, Wei , YUANG, Shendong
IPC分类号： C07D
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, R 1 , R 2 , R 3 , R 4 and R 6 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。

8. 发明申请

WO2009134616A8 NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION 审中-公开
标题翻译：新型丙型肝炎病毒复制抑制剂
公开(公告)号：WO2009134616A8
公开(公告)日：2010-05-14
申请号：PCT/US2009040567
申请日：2009-04-14
申请人： INTERMUNE INC , BEIGELMAN LEONID , WANG GUANGYI , BUCKMAN BRAD O , STOYCHEVA ANTITSA DIMITROVA
发明人： BEIGELMAN LEONID , WANG GUANGYI , BUCKMAN BRAD O , STOYCHEVA ANTITSA DIMITROVA
IPC分类号： C07D285/30 , A61K31/5415 , A61P31/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/12
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。该实施方案进一步提供了治疗方法，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，所述方法通常包括向有需要的个体施用有效量的主题化合物或组合物。

9. 发明申请

WO03080631A2 PLASMA CARBOXYPEPTIDASE B INHIBITORS 审中-公开
标题翻译：等离子体羧化酶B抑制剂
公开(公告)号：WO03080631A2
公开(公告)日：2003-10-02
申请号：PCT/US0308587
申请日：2003-03-21
申请人： SCHERING AG , BUCKMAN BRAD O , EMAYAN KUMAR , ISLAM IMADUL , MAY KAREN , BRYANT JUDI , MOHAN RAJU , WEST CHRISTOPHER , YUAN SHENDONG
发明人： BUCKMAN BRAD O , EMAYAN KUMAR , ISLAM IMADUL , MAY KAREN , BRYANT JUDI , MOHAN RAJU , WEST CHRISTOPHER , YUAN SHENDONG
IPC分类号： C07C323/58 , C07C327/34 , C07D211/34 , C07F9/30 , C07F9/32 , C07F9/38 , C07F9/40 , C07F9/6524 , C07F9/6553
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: (1), wherein R , R , R , and R 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：下文描述的下式（I）的化合物，例如：（1）其中R 1，R 2，R 3和R 4在此描述可用作血浆羧肽酶B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。

10. 发明申请

WO2003080564A1 MENTHOL SUBSTITUTED ANTITHROMBOTIC PAI-1 INHIBITORS 审中-公开
标题翻译： MENTHOL替代抗生素PAI-1抑制剂
公开(公告)号：WO2003080564A1
公开(公告)日：2003-10-02
申请号：PCT/US2003/007506
申请日：2003-03-12
申请人： SCHERING AKTIENGESELLSCHAFT , BAUER, Shawn , MOHAN, Raju , SHAW, Kenneth, J. , WU, Qingyu , YE, Bin , BUCKMAN, Brad, O. , GHANNAM, Ameen , GRIEDEL, Brian, D. , KHIM, Seock-kyu , ZHAO, Zuchun
发明人： BAUER, Shawn , MOHAN, Raju , SHAW, Kenneth, J. , WU, Qingyu , YE, Bin , BUCKMAN, Brad, O. , GHANNAM, Ameen , GRIEDEL, Brian, D. , KHIM, Seock-kyu , ZHAO, Zuchun
IPC分类号： C07C235/06
CPC分类号： C07D213/74 , C07C235/10 , C07C235/16 , C07C2601/14 , C07D207/16 , C07D211/60 , C07D211/62 , C07D213/79 , C07D213/80 , C07D235/26 , C07D241/04 , C07D257/04 , C07D319/08 , C07D401/04
摘要： This invention is directed to menthol-substituted compounds and their pharmaceutically acceptable salts which are useful as antithrombotic agents by inhibiting plasminogen activator inhibitor-1 (PAI-1). In addition, the present invention relates to pharmaceutical compositions and their pharmaceutically acceptable salts, containing the menthol substituted compounds, derivatives of the menthol substituted compounds, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
摘要翻译：本发明涉及通过抑制纤溶酶原激活物抑制剂-1（PAI-1）可用作抗血栓形成剂的薄荷醇取代的化合物及其药学上可接受的盐。此外，本发明涉及含有薄荷醇取代的化合物，薄荷醇取代的化合物的衍生物的药物组合物及其药学上可接受的盐，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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