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71. 发明授权

US06207697B1 Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor Xa 有权
标题翻译：苯并咪唑啉酮，苯并恶唑啉酮，苯并二嗪酮，茚满酮及其衍生物作为因子Xa的抑制剂
公开(公告)号：US06207697B1
公开(公告)日：2001-03-27
申请号：US09149826
申请日：1998-09-08
申请人： Qi Han , Celia Dominguez , Eugene C. Amparo , Jeongsook M. Park , Mimi L. Quan , Karen A. Rossi
发明人： Qi Han , Celia Dominguez , Eugene C. Amparo , Jeongsook M. Park , Mimi L. Quan , Karen A. Rossi
IPC分类号： C07D20934
CPC分类号： C07D263/58 , C07D209/34 , C07D235/26 , C07D241/44
摘要： The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.
摘要翻译：本申请描述了式I的因子Xa或其药学上可接受的盐形式的抑制剂，其中W，W 1，W 2和W 3可以是N或C并且J，J a和J b结合形成取代的碳环或杂环。

72. 发明授权

US6043257A Amidinoindoles, amidinoazoles, and analogs thereof 有权
标题翻译：脒基吲哚，脒基吖嗪及其类似物
公开(公告)号：US6043257A
公开(公告)日：2000-03-28
申请号：US176037
申请日：1998-10-21
申请人： Celia Dominguez , Qi Han , Daniel Emmett Duffy , Jeongsook Maria Park , Mimi Lifen Quan , Karen Anita Rossi , Ruth Richmond Wexler
发明人： Celia Dominguez , Qi Han , Daniel Emmett Duffy , Jeongsook Maria Park , Mimi Lifen Quan , Karen Anita Rossi , Ruth Richmond Wexler
IPC分类号： C07D209/08 , C07D209/12 , C07D209/18 , C07D231/56 , C07D235/06 , C07D307/81 , C07D333/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/14 , C07D471/04 , A01N43/40 , A01N43/38 , C07D235/26
CPC分类号： C07D401/06 , C07D209/08 , C07D209/12 , C07D209/18 , C07D231/56 , C07D235/06 , C07D307/81 , C07D333/58 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/14 , C07D471/04
摘要： The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
摘要翻译：本申请描述了式I的脒基吲哚，脒基吖嗪及其类似物：其中W，W 1，W 2和W 3选自CH和N，条件是W 1和W 2之一为C（C（= NH）NH 2） W，W1，W2和W3中的大多数为N，并且Ja和Jb中的一个被 - （CH 2）n ZAB取代，其可用作因子Xa或凝血酶的抑制剂。

73. 发明授权

US5886191A Amidinoindoles, amidinoazoles, and analogs thereof 失效
标题翻译：脒基吲哚，脒基吖嗪及其类似物
公开(公告)号：US5886191A
公开(公告)日：1999-03-23
申请号：US916736
申请日：1997-08-18
申请人： Celia Dominguez , Qi Han , Daniel Emmett Duffy , Jeongsook Maria Park , Mimi Lifen Quan , Karen Anita Rossi , Ruth Richmond Wexler
发明人： Celia Dominguez , Qi Han , Daniel Emmett Duffy , Jeongsook Maria Park , Mimi Lifen Quan , Karen Anita Rossi , Ruth Richmond Wexler
IPC分类号： C07D209/08 , C07D209/12 , C07D209/18 , C07D231/56 , C07D235/06 , C07D307/81 , C07D333/58 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/14 , C07D471/04 , C07D209/04 , C07D209/14 , C07D209/26 , C07D333/52
CPC分类号： C07D401/06 , C07D209/08 , C07D209/12 , C07D209/18 , C07D231/56 , C07D235/06 , C07D307/81 , C07D333/58 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/14 , C07D409/14 , C07D471/04
摘要： The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.
摘要翻译：本申请描述了由式I表示的脒基吲哚，脒基吖嗪及其类似物：CH和N，条件是W1和W2之一为C（C（= NH）NH 2），W 2，W 2，W 2和 W3为N，Ja和Jb中的一个被 - （CH 2）n ZAB取代，其可用作因子Xa或凝血酶的抑制剂。

74. 发明授权

US5856318A Nitrogen-containing cyclohetero cyclo-heteroaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环芳基芳基衍生物
公开(公告)号：US5856318A
公开(公告)日：1999-01-05
申请号：US910302
申请日：1997-08-11
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： C07D207/14 , C07D211/56 , C07D223/12 , C07D409/06 , A61K31/33 , A61K31/55 , C07D295/00 , C07D405/00
CPC分类号： C07D409/06 , C07D207/14 , C07D211/56 , C07D223/12
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl;wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述某些含氮环杂环烷基氨基芳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R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 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氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

75. 发明授权

US5679679A 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：US5679679A
公开(公告)日：1997-10-21
申请号：US348654
申请日：1994-12-02
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 diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl; each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.11 is independently selected from the group consisting of hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; n is an integer of from three to four; m is an integer of two; A is selected from the group consisting of phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl and 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, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述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：R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; R 2，R 3和R 8至R 11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; n是3至4的整数; m是2的整数; A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基，其中任何前述A基团可以进一步被一个或多个独立地选自羟基，羟基，低级烷基，低级烷氧基，卤代，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基; 或其药学上可接受的盐。

76. 发明授权

US5679673A Aralkyl bridged diazabicycloalkane derivatives for CNS disorders 失效
标题翻译：用于CNS病症的芳烷基桥连二氮杂双环烷烃衍生物
公开(公告)号：US5679673A
公开(公告)日：1997-10-21
申请号：US344304
申请日：1994-11-21
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： C07D453/02 , C07D487/08 , A61K31/55 , C07D471/08
CPC分类号： C07D487/08 , C07D453/02
摘要： Certain aralkyl diazabicycloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R, R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower-alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.9 is selected from hydrido, loweralkyl, benzyl and haloloweralkyl; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothiophenyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述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R，R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R10至R13各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中R8和R9各自选自氢，低级烷基，苄基和卤代低级烷基; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 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氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

77. 发明授权

US5346908A Nitrogen-containing cyclohetero cycloheteroaminoaryl derivatives for CNS disorders 失效
标题翻译：用于CNS疾病的含氮环杂环芳基氨基芳基衍生物
公开(公告)号：US5346908A
公开(公告)日：1994-09-13
申请号：US904354
申请日：1992-06-25
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： C07D207/14 , C07D211/56 , C07D223/12 , C07D409/06 , A61K31/55 , A61K31/40 , A61K31/445 , C07D211/08
CPC分类号： C07D409/06 , C07D207/14 , C07D211/56 , C07D223/12
摘要： Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译：描述某些含氮环杂环烷基氨基芳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R 1，R 4，R 5，R 6和R 7各自独立地选自氢，低级烷基，苄基和卤代低级烷基; 其中R2，R3和R8至R11各自独立地选自氢，羟基，低级烷基，苄基，苯氧基，苄氧基和卤代低级烷基; 其中n为4-6的整数; 其中m是2至4的整数; 其中A选自苯基，萘基，苯并噻吩基，苯并呋喃基和噻吩基; 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氢，羟基，低级烷基，低级烷氧基，卤素，卤代低级烷基，氨基，单低级烷基氨基和二低级烷基氨基的取代基取代。或其药学上可接受的盐。

78. 发明授权

US07897619B2 Heterocyclic modulators of PKB 有权
标题翻译： PKB的杂环调节剂
公开(公告)号：US07897619B2
公开(公告)日：2011-03-01
申请号：US12218754
申请日：2008-07-16
申请人： Qingping Zeng , Dawei Zhang , Guomin Yao , George E. Wohlhieter , Xianghong Wang , James Rider , Andreas Reichelt , Holger Monenschein , Fang-Tsao Hong , James R. Falsey , Celia Dominguez , Matthew P. Bourbeau , John G. Allen
发明人： Qingping Zeng , Dawei Zhang , Guomin Yao , George E. Wohlhieter , Xianghong Wang , James Rider , Andreas Reichelt , Holger Monenschein , Fang-Tsao Hong , James R. Falsey , Celia Dominguez , Matthew P. Bourbeau , John G. Allen
IPC分类号： A61K31/47 , A61K31/416 , C07D217/02 , C07D231/56
CPC分类号： C07D413/04 , C07D263/48 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/14 , C07D417/04
摘要： The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
摘要翻译：本发明涉及用于治疗由蛋白激酶B（PKB）介导的疾病的式I的杂环化合物及其组合物，其中变量具有本文提供的定义。本发明还涉及这些化合物及其组合物在治疗与异常细胞生长，癌症，炎症和代谢紊乱相关的疾病状态中的治疗用途。

79. 发明授权

US07858623B2 Substituted amide derivatives and methods of use 有权
标题翻译：取代的酰胺衍生物和使用方法
公开(公告)号：US07858623B2
公开(公告)日：2010-12-28
申请号：US11412302
申请日：2006-04-26
申请人： Tae-Seong Kim , Shon Booker , Celia Dominguez , Jean-Christophe Harmange
发明人： Tae-Seong Kim , Shon Booker , Celia Dominguez , Jean-Christophe Harmange
IPC分类号： A61K31/535 , C07D413/12
CPC分类号： C07D413/12 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D495/04
摘要： Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译：所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗疾病和其它疾病或涉及癌症等的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。

80. 发明授权

US07582761B2 Vanilloid receptor ligands and their use in treatments 失效
标题翻译：香草素受体配体及其在治疗中的应用
公开(公告)号：US07582761B2
公开(公告)日：2009-09-01
申请号：US10688246
申请日：2003-10-16
申请人： Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
发明人： Chenera Balan , Yunxin Bo , Celia Dominguez , Christopher H. Fotsch , Vijay K. Gore , Vu Van Ma , Mark H. Norman , Vassil I. Ognyanov , Yi-xin Qian , Xianghong Wang , Ning Xi , Shimin Xu
IPC分类号： C07D401/04 , C07D401/06 , C07D403/04
CPC分类号： C07D401/04 , C07D235/30 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： Therapeutic benzimidazoles having the general structure: and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
摘要翻译：具有一般结构的治疗性苯并咪唑和含有它们的组合物，用于治疗急性，炎性和神经性疼痛，牙痛，一般头痛，偏头痛，丛集性头痛，混合血管和非血管综合征，紧张性头痛，一般炎症，关节炎，风湿性疾病，骨关节炎，炎症性肠病，炎症性眼病，炎性或不稳定性膀胱疾病，牛皮癣，皮肤炎症成分炎症，慢性炎性病症，炎症性疼痛及相关的痛觉过敏和异常性疼痛，神经性疼痛和相关的痛觉过敏和异常性疼痛，糖尿病性神经病变疼痛，咳嗽，交感神经保持疼痛，交感综合征，哮喘，上皮组织损伤或功能障碍，单纯疱疹，呼吸道内脏运动紊乱，泌尿生殖道，胃肠道或血管区，伤口，烧伤，过敏性皮肤反应，瘙痒，白癜风，胃肠疾病，胃溃疡，十二指肠溃疡，腹泻，坏死因子诱导的胃损伤，毛发生长，血管舒缩或过敏性鼻炎，支气管疾病或膀胱疾病。

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