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1. 发明授权

US07176207B2 Platelet adenosine diphosphate receptor antagonists 失效
标题翻译：血小板二磷酸腺苷受体拮抗剂
公开(公告)号：US07176207B2
公开(公告)日：2007-02-13
申请号：US11347768
申请日：2006-02-02
申请人： Judi A Bryant , Brad O Buckman , Imadul Islam , Raju Mohan , Michael M Morrissey , Robert Guo-Ping Wei , Wei Xu , Shendong Yuan
发明人： Judi A Bryant , Brad O Buckman , Imadul Islam , Raju Mohan , Michael M Morrissey , Robert Guo-Ping Wei , Wei Xu , Shendong Yuan
IPC分类号： A61K31/495 , A61K31/496 , C07D295/192
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, 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，a，b，R 1，R 2，R 3，R 3， 4和4本文描述的，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。

2. 发明授权

US06995156B2 Platelet adenosine diphosphate receptor antagonists 失效
标题翻译：血小板二磷酸腺苷受体拮抗剂
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

3. 发明授权

US08008325B2 Plasma carboxypeptidase B inhibitors 失效
标题翻译：血浆羧肽酶B抑制剂
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。

4. 发明授权

US06972290B2 Piperazine derivatives and their use as anti-inflammatory agents 失效
标题翻译：哌嗪衍生物及其作为抗炎剂的用途
公开(公告)号：US06972290B2
公开(公告)日：2005-12-06
申请号：US10347529
申请日：2003-01-17
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 , A61K31/497 , A61P29/00 , A61P43/00 , C07D241/04 , C07D261/14 , C07D295/185 , C07D307/52 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , A61K31/495
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。

5. 发明授权

US06686364B2 Benzamidine derivatives and their use as anti-coagulants 失效
标题翻译：苄脒衍生物及其作为抗凝剂的用途
公开(公告)号：US06686364B2
公开(公告)日：2004-02-03
申请号：US09924893
申请日：2001-08-07
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： A61K314965
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：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。

6. 发明授权

US06541476B1 Piperazine derivatives and their use as anti-inflammatory agents 失效
标题翻译：哌嗪衍生物及其作为抗炎剂的用途
公开(公告)号：US06541476B1
公开(公告)日：2003-04-01
申请号：US09713606
申请日：2000-11-14
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： A61K31496
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, for example, of the following formula (Ia): wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives are useful anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the derivatives, and methods of using the derivatives to treat inflammatory disorders in humans.
摘要翻译：本发明涉及例如下式（Ia）的酰基哌嗪衍生物：其中R1a，R2，R3，R4，R5和R6如本文所述。这些衍生物是有用的抗炎剂。本发明还涉及含有衍生物的药物组合物，以及使用该衍生物治疗人类炎性疾病的方法。

7. 发明授权

US06479485B2 Benzamidine derivatives and their use as anti-coagulants 失效
公开(公告)号：US06479485B2
公开(公告)日：2002-11-12
申请号：US09924413
申请日：2001-08-07
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： A61K31534
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.

8. 发明授权

US06350746B1 Benzamidine derivatives and their use as anti-coagulants 失效
标题翻译：苄脒衍生物及其作为抗凝剂的用途
公开(公告)号：US06350746B1
公开(公告)日：2002-02-26
申请号：US09457457
申请日：1999-12-08
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： C07D40112
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.
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。

9. 发明授权

US06306884B1 Benzamidine derivatives and their use as anti-coagulants 失效
标题翻译：苄脒衍生物及其作为抗凝剂的用途
公开(公告)号：US06306884B1
公开(公告)日：2001-10-23
申请号：US09436399
申请日：1999-11-08
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： A61K3154
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.
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。

10. 发明授权

US5753635A Purine derivatives and their use as anti-coagulants 失效
标题翻译：嘌呤衍生物及其作为抗凝剂的用途
公开(公告)号：US5753635A
公开(公告)日：1998-05-19
申请号：US689979
申请日：1996-08-16
申请人： Brad O. Buckman , Raju Mohan , Michael M. Morrissey
发明人： Brad O. Buckman , Raju Mohan , Michael M. Morrissey
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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