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91. 发明授权

US06849639B2 Integrin inhibitors and their methods of use 失效
标题翻译：整合素抑制剂及其使用方法
公开(公告)号：US06849639B2
公开(公告)日：2005-02-01
申请号：US09732546
申请日：2000-12-08
申请人： Celia Dominguez , Guoqing Chen , Ning Xi , Shimin Xu , Nianhe Han , Qingyian Liu , Qi Huang , Aaron Siegmund , Michael Handley , Longbin Liu , Alexander Kiselyov
发明人： Celia Dominguez , Guoqing Chen , Ning Xi , Shimin Xu , Nianhe Han , Qingyian Liu , Qi Huang , Aaron Siegmund , Michael Handley , Longbin Liu , Alexander Kiselyov
IPC分类号： C07D401/06 , A61K31/402 , A61K31/4025 , A61K31/4178 , A61K31/4355 , A61K31/438 , A61K31/4406 , A61K31/4709 , A61K31/496 , A61K31/506 , A61P3/10 , A61P9/00 , A61P9/10 , A61P17/02 , A61P19/00 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/04 , C07D207/26 , C07D207/277 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10
CPC分类号： C07D207/277 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D417/14
摘要： The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as a αvβ3, αvβ5, αvβ6, α5β1 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：本发明包括有效预防和治疗诸如整联蛋白受体介导的疾病，特别是整联蛋白受体介导的疾病或病症的新型化合物，例如阿尔法派3，阿尔法派5，阿尔法博特6，α5β1等。本发明包括新型化合物，其药学上可接受的盐，用于预防和治疗这些疾病和病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

92. 发明授权

US06514964B1 Fused cycloheptane and fused azacycloheptane compounds and their methods of use 失效
标题翻译：熔融环庚烷和稠合氮杂环庚烷化合物及其使用方法
公开(公告)号：US06514964B1
公开(公告)日：2003-02-04
申请号：US09671025
申请日：2000-09-26
申请人： Zhidong Chen , Celia Dominguez , Ellen Grenzer-Laber , Nianhe Han , Longbing Liu , Ofir A. Moreno , Melvin C. Rutledge , Andrew S. Tasker
发明人： Zhidong Chen , Celia Dominguez , Ellen Grenzer-Laber , Nianhe Han , Longbing Liu , Ofir A. Moreno , Melvin C. Rutledge , Andrew S. Tasker
IPC分类号： C07D22316
CPC分类号： C07D213/74 , C07D223/16 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/14 , C07D417/12 , C07D471/04 , C07D487/04
摘要： The invention comprises novel compounds that are effective in the prophylaxis and treatment of diseases, such as integrin receptors mediated diseases, in particular, diseases or conditions mediated by integrin receptors, such as &agr;v&bgr;3, &agr;v&bgr;5, &agr;v&bgr;6 and the like. The invention encompasses novel compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of such diseases and disorders. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：本发明包括有效预防和治疗疾病的新型化合物，例如整联蛋白受体介导的疾病，特别是由整合素受体介导的疾病或病症，例如α-角蛋白3，阿尔法派5，阿尔韦博特等。本发明包括新型化合物，其药学上可接受的盐，用于预防和治疗这些疾病和病症的药物组合物和方法。本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

93. 发明授权

US06310064B1 Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US06310064B1
公开(公告)日：2001-10-30
申请号：US09347659
申请日：1999-07-06
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： C07D47104
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis, and convulsions. For example, compounds of interest are of the formula:
摘要翻译：公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，例如脑缺血，精神病和抽搐。例如，感兴趣的化合物具有下式：

94. 发明授权

US5998424A Inhibitors of factor Xa with a neutral P1 specificity group 失效
公开(公告)号：US5998424A
公开(公告)日：1999-12-07
申请号：US99752
申请日：1998-06-18
申请人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
发明人： Robert A. Galemmo, Jr. , Celia Dominguez , John M. Fevig , Qi Han , Patrick Y. Lam , Donald J. P. Pinto , James R. Pruitt , Mimi L. Quan
IPC分类号： C07D231/14 , C07D257/04 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , A01N43/54 , C07D211/32 , C07D277/64
CPC分类号： C07D257/04 , C07D231/14 , C07D277/56 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12
摘要： The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.

95. 发明授权

US5958920A Aralkyl diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基二氮杂双环烷烃衍生物
公开(公告)号：US5958920A
公开(公告)日：1999-09-28
申请号：US954284
申请日：1997-10-20
申请人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人： Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号： A61K31/495 , C07D471/04 , C07D487/04 , C07D31/495 , C07D31/55
CPC分类号： C07D471/04 , A61K31/495 , C07D487/04
摘要： Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein m is three or four; wherein z is selected from the group consisting of ##STR2## wherein when Z is ##STR3## n and p are integers of from one to four, with a sum of four or five, and when Z is ##STR4## n and p are integers of from one to three, with a sum of three or four; wherein A is selected from the group consisting of aryl, heteroaryl, aryloxy, heteroaryloxy, aralkoxy, heteroaralkoxy, arylamino, heteroarylamino, aralkylamino, heteroaralkylamino, arylthio, heteroarylthio, aralkylthio, and heteroaralkylthio; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, aryl, alkoxy, aryloxy, aralkoxy, alkoxyalkyl, halo, haloalkyl, hydroxyalkyl, cyano, amino, monoalkylamino, dialkylamino, carboxy, carboxyalkyl, alkanoyl, alkenyl and alkynyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病，如脑缺血，精神病和抽搐。特别感兴趣的化合物具有下式：其中m为三或四; 其中z选自其中当Z为n且p为1至4的整数时，其总数为4或5，当Z为n且p为1至3的整数时，其总和为三或四; 其中A选自芳基，杂芳基，芳氧基，杂芳氧基，芳烷氧基，杂芳烷氧基，芳基氨基，杂芳基氨基，芳烷基氨基，杂芳烷基氨基，芳硫基，杂芳硫基，芳烷硫基和杂芳烷硫基。其中前述A基团中的任一个可以进一步被一个或多个独立地选自羟基，羟基，烷基，环烷基，环烷基烷基，芳烷基，芳基，烷氧基，芳氧基，芳烷氧基，烷氧基烷基，卤素，卤代烷基，，氰基，氨基，单烷基氨基，二烷基氨基，羧基，羧基烷基，烷酰基，烯基和炔基; 或其药学上可接受的盐。

96. 发明授权

US5925635A N-(amidinophenyl) cyclourea analogs as factor XA inhibitors 失效
标题翻译： N-（脒基苯基）环脲类似物作为因子XA抑制剂
公开(公告)号：US5925635A
公开(公告)日：1999-07-20
申请号：US838246
申请日：1997-04-16
申请人： Thomas Peter Maduskuie, Jr. , Robert Anthony Galemmo, Jr. , Celia Dominguez , Mimi Lifen Quan , Karen Anita Rossi , Petrus Fredericus Wilhelmus Stouten , Jung-Hui Sun , Brian Lloyd Wells
发明人： Thomas Peter Maduskuie, Jr. , Robert Anthony Galemmo, Jr. , Celia Dominguez , Mimi Lifen Quan , Karen Anita Rossi , Petrus Fredericus Wilhelmus Stouten , Jung-Hui Sun , Brian Lloyd Wells
IPC分类号： A61P7/02 , C07D243/04 , C07D401/04 , C07D401/14 , C07D409/14 , C07D413/04 , C07D417/14 , A61K31/55 , C07D243/10 , C07D487/04
CPC分类号： C07D401/04 , C07D243/04 , C07D401/14 , C07D409/14 , C07D413/04 , C07D417/14
摘要： The present application describes N-(amidinophenyl)cyclourea analogs of formula I: ##STR1## which are useful as inhibitors of factor Xa.
摘要翻译：本申请描述了式I的N-（脒基苯基）环脲类似物：其可用作因子Xa的抑制剂。

97. 发明授权

US5639739A Imidazole containing aminoboronic acids 失效
标题翻译：咪唑含氨基硼酸
公开(公告)号：US5639739A
公开(公告)日：1997-06-17
申请号：US409573
申请日：1995-03-24
申请人： Celia Dominguez , Joseph Cacciola , John Matthew Fevig
发明人： Celia Dominguez , Joseph Cacciola , John Matthew Fevig
IPC分类号： A61K38/00 , C07F5/02 , C07K5/06 , A61K31/69 , C07F5/04 , C07K5/065
CPC分类号： C07F5/025 , C07K5/06191 , A61K38/00
摘要： The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs of the formula (I): ##STR1## in which the .alpha.-carbon is substituted with an optionally functionalized imidazole containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes, especially thrombin, Factor X and Factor VII.
摘要翻译：本发明一般涉及式（I）的α-氨基硼酸和相应的肽类似物：其中α-碳被含有烷基的任选官能化的咪唑取代。这些化合物可用作胰蛋白酶样丝氨酸蛋白酶的抑制剂，特别是凝血酶因子X和因子VII。

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