专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

91. 发明授权

US6013799A Certain cycloalkyl imidazopyrimides, a new class of gaba brain receptor ligands 失效
标题翻译：某些环烷基咪唑并嘧啶，一类新的gaba脑受体配体
公开(公告)号：US6013799A
公开(公告)日：2000-01-11
申请号：US987575
申请日：1997-12-09
申请人： Kenneth Shaw , Alan Hutchison
发明人： Kenneth Shaw , Alan Hutchison
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable non-toxic salts thereof wherein: R.sub.9 and Y are substituents as defined herein; andR.sub.a and R.sub.b independently represent halogen, hydroxy, amino, mono or dialkylamino where each alkyl is straight or branched chain alkyl having 1-6 carbon atoms, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
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：R 9和Y是如本文所定义的取代基; 并且R a和R b独立地表示卤素，羟基，氨基，一或二烷基氨基，其中每个烷基是具有1-6个碳原子的直链或支链烷基，具有1-6个碳原子的直链或支链低级烷基，或直链或支链低级具有1-6个碳原子的烷氧基，该化合物是GABAa脑受体或其前药的高度选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量，以及提高警觉性。

92. 发明授权

US5962455A Certain substituted benzylamine derivatives a new class of neuropeptide Y1 specific ligands 失效
标题翻译：某些取代的苄胺衍生物是一类新的神经肽Y1特异性配体
公开(公告)号：US5962455A
公开(公告)日：1999-10-05
申请号：US897045
申请日：1997-07-18
申请人： Charles A. Blum , Alan Hutchison , John M. Peterson
发明人： Charles A. Blum , Alan Hutchison , John M. Peterson
IPC分类号： C07D295/12 , A61K31/4406 , A61K31/495 , A61K31/496 , A61P3/00 , A61P9/04 , A61P9/12 , A61P43/00 , C07D213/74 , C07D213/75 , C07D215/38 , C07D233/38 , C07D295/135 , C07D295/14 , C07D295/155 , C07D401/12 , C07D403/10
CPC分类号： C07D213/75 , C07D215/38 , C07D233/38 , C07D295/135 , C07D295/155 , C07C2101/14
摘要： This invention encompasses compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein X.sub.1, X.sub.2, X.sub.3 represent organic or inorganic substituents, n is 1, 2, or 3, m is 2, 3, or 4, R.sub.1 -R.sub.4 are hydrogen or organic substituents, and B is nitrogen, carbon, sulfur or oxygen, useful in the diagnosis and treatment of feeding disorders such as obesity and bulimia and cardiovascular diseases such as essential hypertension and congestive heart failure due to the binding of these compounds to mammalian Neuropeptide Y1 receptors.
摘要翻译：本发明包括下式的化合物及其药学上可接受的盐，其中X 1，X 2，X 3表示有机或无机取代基，n为1,2或3，m为2,3或4，R 1 -R 4为氢或有机取代基，B是氮，碳，硫或氧，可用于诊断和治疗诸如肥胖和贪食的进食障碍和心血管疾病，例如由于这些化合物与哺乳动物神经肽Y1受体的结合而引起的原发性高血压和充血性心力衰竭。

93. 发明授权

US5840888A Certain aryl and cycloalkyl fused imidazopyrazinediones; a new class of GABA brain receptor ligands 失效
标题翻译：某些芳基和环烷基稠合的咪唑并吡嗪二酮; 一类新的GABA脑受体配体
公开(公告)号：US5840888A
公开(公告)日：1998-11-24
申请号：US465693
申请日：1995-06-06
申请人： Kenneth Shaw , Alan Hutchison
发明人： Kenneth Shaw , Alan Hutchison
IPC分类号： C07D401/04 , C07D471/14 , C07D487/04 , C07D491/20 , A61K31/495
CPC分类号： C07D401/04 , C07D471/14 , C07D487/04
摘要： ##STR1## The present invention encompasses compounds of formula (I), and the pharmaceutical acceptable non-toxic salts thereof wherein: where X represents hydrogen or lower alkyl; W represents an aryl group unsubstituted or substituted with various organic and inorganic substituents; (a) represents (b); (c); (d) or (e) or (a) represents (f), where A, B, C, D, and E represent carbon or nitrogen substituted with hydrogen or various organic and inorganic substituents; and n is 0, 1, or 2; Y, R
3 , R
4 , R
12 , and R
13 are various organic and inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
摘要翻译：（a）（b）（c）（d）（e）（a）（f）（I）本发明包括式（I）的化合物及其药学上可接受的无毒盐，其中：其中X表示氢或低级烷基; W表示未被取代或被各种有机和无机取代基取代的芳基; （a）代表（b）; （C）; （d）或（e）或（a）表示（f），其中A，B，C，D和E表示被氢或各种有机和无机取代基取代的碳或氮; 并且n为0,1或2; Y，R 3，R 4，R 12和R 13是各种有机和无机取代基。这些化合物是GABAa脑受体或其前药的高度选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量和记忆增强。

94. 发明授权

US5804685A Deazapurine derivatives: a new class of CRF1 specific ligands 失效
标题翻译：去氮嘌呤衍生物：一类新的CRF1特异性配体
公开(公告)号：US5804685A
公开(公告)日：1998-09-08
申请号：US476689
申请日：1995-06-07
申请人： Jun Yuan , Alan Hutchison
发明人： Jun Yuan , Alan Hutchison
IPC分类号： C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; and R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.
摘要翻译：公开了下式的化合物：其中Ar表示芳基或杂芳基; 并且R1，R2，R3，R4和R5代表有机或无机取代基，这些化合物是人CRF1受体的高选择性部分激动剂或拮抗剂，因此可用于诊断和治疗应激相关疾病例如post trumatic 压力障碍（PTSD）以及抑郁，头痛和焦虑。

95. 发明授权

US5792766A Imidazo�1,5-c! quinazolines; a new class of GABA brain receptor ligands 失效
标题翻译：咪唑并[1,5-c]喹唑啉; 一类新的GABA脑受体配体
公开(公告)号：US5792766A
公开(公告)日：1998-08-11
申请号：US614878
申请日：1996-03-13
申请人： Paul Chen , Alan Hutchison , Guolin Cai
发明人： Paul Chen , Alan Hutchison , Guolin Cai
IPC分类号： A61K31/519 , A61P25/22 , C07D401/14 , C07D403/14 , C07D487/04 , A61K31/505 , C07D403/07
CPC分类号： C07D487/04
摘要： Disclosed are compounds of compounds of the formula: ##STR1## or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H.sub.2 or sulfur Y is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups; W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; or W is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; and Z.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 where R.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine drugs, and enhancement of memory.
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：X是氧，H 2或硫，Y是氢或任选取代的烷基，烯基，（取代的）芳基烷基，芳基或杂芳基，或被烷基，环烷基，芳基或氨基取代的羰基; W是烷基，芳烷基或杂芳基烷基，其中每个芳基任选被至多两个基团取代; 或W是芳基，噻吩基，吡啶基或杂芳基，其各自任选被取代; 并且Z 1，Z 2，Z 3和Z 4独立地表示氮或C-R 1，其中R 1是氢，卤素，羟基，氨基或苯基或任选被卤素，羟基，低级烷基或低级烷氧基单取代或独立地被二取代的吡啶基，化合物是GABAa脑受体或GABAa脑受体的激动剂或反向激动剂前药的高选择性激动剂，拮抗剂或反向激动剂。这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量使用，并增强记忆功能。

96. 发明授权

US5750702A Certain pyrrolo pyridine-3-carboxamides; a new class of GABA brain receptor ligands 失效
标题翻译：某些吡咯并吡啶-3-甲酰胺; 一类新的GABA脑受体配体
公开(公告)号：US5750702A
公开(公告)日：1998-05-12
申请号：US683066
申请日：1996-07-16
申请人： Pamela Albaugh , Alan Hutchison
发明人： Pamela Albaugh , Alan Hutchison
IPC分类号： A61K31/404 , C07C233/58 , C07D209/08 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04 , C07D401/04
CPC分类号： C07D209/08 , A61K31/404 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl; X is hydrogen, hydroxy or lower alkyl; T is hydrogen, halogen, hydroxy, nitro, amino or alkyl; R.sub.3 is hydrogen or an organic group; R.sub.4 is hydrogen or substituted or unsubstituted organic substituent; R.sub.5 and R.sub.6 represent organic, and inorganic substituents; and n is 1, 2, 3, or 4, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
摘要翻译：本发明包括下式的结构：其中：W代表取代或未取代的苯基;或其药学上可接受的无毒盐，其中：W代表取代或未取代的苯基; X是氢，羟基或低级烷基; T是氢，卤素，羟基，硝基，氨基或烷基; R3是氢或有机基团; R4是氢或取代或未取代的有机取代基; R5和R6代表有机和无机取代基; 和n为1,2,3或4，这些化合物是用于GABAa脑受体的高选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。这些化合物可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆。

97. 发明申请

US20080009477A1 Arylalkyl Ureas As Cb1 Antagonists 审中-公开
标题翻译：芳基烷基脲作为Cb1拮抗剂
公开(公告)号：US20080009477A1
公开(公告)日：2008-01-10
申请号：US11718421
申请日：2005-11-01
申请人： Alan Hutchison , Jun Yuan
发明人： Alan Hutchison , Jun Yuan
IPC分类号： A61K31/55 , A61K31/17 , A61K31/337 , A61K31/352 , A61K31/40 , A61P1/00 , A61P11/06 , A61P25/00 , G01N33/52 , A61P3/04 , A61P19/00 , A61P1/16 , A61K31/551 , A61K31/4164 , A61K31/435 , A61K31/439
CPC分类号： A61K31/17 , Y10T436/171538
摘要： CB1 antagonists are provided. Such compounds may be used to modulate CB1 activity in vivo or in vitro, and are particularly useful in the treatment of conditions responsive to CB1 receptor modulation in humans, domesticated companion animals and livestock animals, including appetite disorders, obesity and addictive disorders. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using ligands for receptor localization studies and various in vitro assays.
摘要翻译：提供了CB1拮抗剂。这样的化合物可用于体内或体外调节CB1活性，并且特别可用于治疗对人类，驯养的伴侣动物和家畜的CB1受体调节的病症，包括食欲障碍，肥胖症和成瘾性疾病。还提供了用于治疗这些疾病的药物组合物和方法，以及使用配体进行受体定位研究和各种体外测定的方法。

98. 发明申请

US20060142301A1 Substituted 1-benzyl-4-substituted piperazine analogues 失效
标题翻译：取代的1-苄基-4-取代的哌嗪类似物
公开(公告)号：US20060142301A1
公开(公告)日：2006-06-29
申请号：US11100355
申请日：2005-04-06
申请人： Alan Hutchison , Bertrand Chenard , James Tarrant , Guiying Li , Manuka Ghosh , George Luke , John Peterson , Wallace Pringle , Mary-Margaret O'Donnell , Kyungae Lee , Linda Gustavson , Dario Doller
发明人： Alan Hutchison , Bertrand Chenard , James Tarrant , Guiying Li , Manuka Ghosh , George Luke , John Peterson , Wallace Pringle , Mary-Margaret O'Donnell , Kyungae Lee , Linda Gustavson , Dario Doller
IPC分类号： A61K31/496 , A61K31/497 , C07D403/02
CPC分类号： C07D213/74 , C07D213/82 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译：提供了式I化合物，其中变量如本文所述：这样的化合物可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗各种代谢，进食和性障碍在人类，驯养的伴侣动物和家畜中。还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

99. 发明授权

US06906075B2 Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues 失效
标题翻译：黑色素浓缩激素受体配体：取代的苯并咪唑类似物
公开(公告)号：US06906075B2
公开(公告)日：2005-06-14
申请号：US10339111
申请日：2003-01-09
申请人： Robert W. DeSimone , Cheryl Steenstra , Linda Gustavson , Rajagopal Bakthavatchalam , Alan Hutchison
发明人： Robert W. DeSimone , Cheryl Steenstra , Linda Gustavson , Rajagopal Bakthavatchalam , Alan Hutchison
IPC分类号： A61K31/4184 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/55 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P15/00 , A61P43/00 , C07D235/10 , C07D235/14 , C07D401/04 , C07D403/04 , C07D403/10 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D513/04 , C07D521/00 , C07D401/10 , A61K31/445 , A61K31/495
CPC分类号： C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D401/04 , C07D403/04 , C07D403/10 , C07D409/12 , C07D409/14 , C07D417/12 , C07D513/04
摘要： Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译：提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是取代的苯并咪唑类似物）。这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。

100. 发明授权

US06894044B2 2-aminoquinolinecarboxamides: neurokinin receptor ligands 失效
标题翻译： 2-氨基喹啉甲酰胺：神经激肽受体配体
公开(公告)号：US06894044B2
公开(公告)日：2005-05-17
申请号：US10115409
申请日：2002-04-03
申请人： Jun Yuan , George D. Maynard , Alan Hutchison
发明人： Jun Yuan , George D. Maynard , Alan Hutchison
IPC分类号： A61K31/47 , A61P25/00 , A61P25/28 , C07D215/50 , C07D401/04 , C07D453/06 , C07D491/10 , A61K31/4709
CPC分类号： A61K31/47 , C07D215/50 , C07D401/04 , C07D453/06 , C07D491/10 , Y10S206/828
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.
摘要翻译：公开了下式的化合物或其药学上可接受的盐或药学上可接受的溶剂化物，其中R 1，R 2，R 3，X，本文定义Q 1和Q 2 2，这些化合物是神经激肽受体特别是NK-3受体的配体，并且可用于治疗广泛范围的疾病或病症，包括但不限于抑郁症，焦虑症，精神病，肥胖症，疼痛，帕金森病，阿尔茨海默病，神经变性疾病，运动障碍，呼吸系统疾病，炎性疾病，神经病，免疫疾病，偏头痛，胆汁功能异常和皮炎。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式