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11. 发明申请

US20070043049A1 Substituted heterocyclic diarylamine analogues 审中-公开
标题翻译：取代的杂环二芳基胺类似物
公开(公告)号：US20070043049A1
公开(公告)日：2007-02-22
申请号：US10564431
申请日：2004-07-09
申请人： Rajagopal Bakthavatchalam , Kevin Hodgetts , Alan Hutchison , Robert Ohliger , Taeyoung Yoon , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Kevin Hodgetts , Alan Hutchison , Robert Ohliger , Taeyoung Yoon , Xiaozhang Zheng
IPC分类号： A61K31/53
CPC分类号： C07D401/12 , A61K31/506 , A61K31/53 , C07D251/52 , C07D251/54 , C07D401/14 , G01N33/566
摘要： Substituted heterocyclic diarylamine analogues of Formula I are provided: wherein X, Y and Z are independently N or optionally substituted C, and other variables are as described in the specification. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供式I的取代的杂环二芳基胺类似物：其中X，Y和Z独立地为N或任选被取代的C，并且其它变量如说明书中所述。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

12. 发明申请

US20060194805A1 Capsaicin receptor agonists 审中-公开
标题翻译：辣椒素受体激动剂
公开(公告)号：US20060194805A1
公开(公告)日：2006-08-31
申请号：US11412526
申请日：2006-04-26
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Daniel Cortright , Kevin Hodgetts , John Peterson , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Daniel Cortright , Kevin Hodgetts , John Peterson , Xiaozhang Zheng
IPC分类号： A61K31/525 , A61K31/517 , A61K31/519 , A61K31/498 , C07D475/10 , C07D487/02
CPC分类号： C04B35/632 , C07D215/44 , C07D239/94 , C07D401/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D475/06
摘要： Capsaicin receptor agonists are provided. Such compounds are ligands that may be used to modulate VR1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to capsaicin receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供辣椒素受体激动剂。这样的化合物是可用于在体内或体外调节VR1活性的配体，并且特别可用于治疗对人，驯养的伴侣动物和家畜中的辣椒素受体激活有反应的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

13. 发明授权

US06403591B1 1-azatricyclic-4-benzylpiperazines 失效
标题翻译： 1-氮杂环己基-4-苄基哌嗪
公开(公告)号：US06403591B1
公开(公告)日：2002-06-11
申请号：US09894092
申请日：2001-06-28
申请人： Kevin Hodgetts , Stanislaw Rachwal , Daniel Rosewater , Andrew Thurkauf , Xiaoyan Zhang
发明人： Kevin Hodgetts , Stanislaw Rachwal , Daniel Rosewater , Andrew Thurkauf , Xiaoyan Zhang
IPC分类号： A61K31497
CPC分类号： C07D471/06 , C07D487/06 , G01N33/6896 , G01N33/9413 , G01N2333/70571 , G01N2800/2835
摘要： Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了可用于治疗和/或预防神经心理障碍的1-叠氮基-4-苄基哌嗪化合物，包括但不限于精神分裂症，躁狂症，痴呆，抑郁，焦虑，强迫行为，药物滥用，帕金森氏样运动与使用神经安定药相关的疾病和运动障碍。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A受体定位的探针。

14. 发明授权

US08580812B2 Heteroaryl amide analogues as P2X7 antagonists 失效
标题翻译：杂芳基酰胺类似物作为P2X7拮抗剂
公开(公告)号：US08580812B2
公开(公告)日：2013-11-12
申请号：US12595394
申请日：2008-04-09
申请人： David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
发明人： David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
IPC分类号： C07D221/02 , C07D491/02 , C07D498/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04 , C07D455/02 , C07D471/10 , C07D498/10 , C07D519/00
摘要： Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了式（I）的杂芳基酰胺类似物，其中变量如本文所述。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

15. 发明申请

US20100266509A1 HETEROARYL AMIDE ANALOGUES AS P2X7 ANTAGONISTS 失效
标题翻译：作为P2X7拮抗剂的异构体酰胺类似物
公开(公告)号：US20100266509A1
公开(公告)日：2010-10-21
申请号：US12595394
申请日：2008-04-09
申请人： David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
发明人： David C. Ihle , Qin Guo , Kevin Hodgetts , Jun Yuan
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/437 , C07D213/82 , A61K31/44 , C07D487/04 , A61K31/4985 , C07D413/14 , A61K31/519 , C07D401/14 , A61K31/497 , C07D498/10 , A61K31/438 , C07D403/14 , A61K9/12 , A61P29/00 , A61P25/00
CPC分类号： C07D471/04 , C07D455/02 , C07D471/10 , C07D498/10 , C07D519/00
摘要： Heteroaryl amide analogues are provided, of Formula (I), wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了式（I）的杂芳基酰胺类似物，其中变量如本文所述。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

16. 发明授权

US06509366B2 Substituted imidazoles as selective modulators of Bradykinin B2 receptors 失效
标题翻译：取代的咪唑作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06509366B2
公开(公告)日：2003-01-21
申请号：US09764805
申请日：2001-01-17
申请人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
发明人： Stanislaw Rachwal , Alan Hutchison , Kenneth Shaw , George D. Maynard , Xiao-shu He , Robert DeSimone , Kevin Hodgetts
IPC分类号： A61K314174
CPC分类号： C07D233/64 , C07D233/68 , C07D401/06
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7 R 7'是本文定义的变量，该化合物是缓激肽B2受体的调节剂。因此，这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血液 - 脑肿瘤屏障。

17. 发明申请

US20060089354A1 Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators 失效
标题翻译：羧酸，磷酸酯或膦酸酯取代的喹唑啉-4-基胺类似物作为辣椒素受体调节剂
公开(公告)号：US20060089354A1
公开(公告)日：2006-04-27
申请号：US10539031
申请日：2003-12-12
申请人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Stephane DeLombaert , Kevin Hodgetts , Xiaozhang Zheng
发明人： Rajagopal Bakthavatchalam , Charles Blum , Harry Brielmann , Timothy Caldwell , Stephane DeLombaert , Kevin Hodgetts , Xiaozhang Zheng
IPC分类号： A61K31/5377 , A61K31/519 , A61K31/4745 , A61K31/4709 , C07D487/02 , C07D413/02 , C07D401/02 , C07D471/02
CPC分类号： C07D417/14 , C07D239/94 , C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/10 , C07F9/65128 , C07F9/65583 , C07F9/6561
摘要： Acid-substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了酸取代的喹唑啉-4-基胺类似物。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了用于治疗这些病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

18. 发明申请

US20070191363A1 Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues 审中-公开
标题翻译：异丁烷基取代的联苯-4-羧酸芳酰胺类似物
公开(公告)号：US20070191363A1
公开(公告)日：2007-08-16
申请号：US10591383
申请日：2005-03-02
申请人： Kevin Hodgetts , Stephane De Lombaert
发明人： Kevin Hodgetts , Stephane De Lombaert
IPC分类号： A61K31/5377 , A61K31/4545 , A61K31/44 , C07D413/02 , C07D403/02
CPC分类号： C07D213/56 , C07D401/12 , C07D413/12
摘要： Heteroalkyl-substituted biphenyl-4-carboxylic acid arylamide analogues are provided, of the formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了下式的杂烷基取代的联苯-4-羧酸芳酰胺类似物：其中变量如本文所述。这些化合物是可用于在体内或体外调节特异性受体活性的配体，并且特别可用于治疗与人类，驯养伴侣动物和家畜中的病理受体激活相关的病症。还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

19. 发明申请

US20060229308A1 Substituted pyrirmidin-4-ylamine analogues as vanilloid receptor ligands 审中-公开
标题翻译：取代的嘧啶-4-基胺类似物作为香草素受体配体
公开(公告)号：US20060229308A1
公开(公告)日：2006-10-12
申请号：US10564583
申请日：2004-07-15
申请人： Charles Blum , Harry Brielmann , Kevin Hodgetts
发明人： Charles Blum , Harry Brielmann , Kevin Hodgetts
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/505 , C07D413/02
CPC分类号： C07D239/42 , C07D239/47 , C07D239/48 , C07D251/42 , C07D401/04
摘要： Substituted pyrimidyl-4-ylamine analogues are provided, of the Formula: (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate Vanilloid receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
摘要翻译：提供了取代的嘧啶-4-基胺类似物，其具有如下所述的变体：式（I）。这样的化合物是可用于在体内或体外调节香草素受体活性的配体，并且特别可用于治疗与人，驯养的伴侣动物和家畜中的病理受体激活相关的病症。还提供了使用这些化合物治疗这种病症的药物组合物和方法，以及使用这些配体进行受体定位研究的方法。

20. 发明授权

US06420365B1 Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors 失效
标题翻译：咪唑并吡啶类和相关衍生物作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06420365B1
公开(公告)日：2002-07-16
申请号：US09765159
申请日：2001-01-17
申请人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
发明人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
IPC分类号： A61K31435
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒性盐，其中A，B，C，D，Y，R 1，R 3，R 4，R 5和R 6是本文定义的变量，该化合物是缓激肽B2受体的调节剂。这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血脑屏障的渗透性，肿瘤屏障。

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