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31. 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。

32. 发明授权

US06413982B1 4-substituted quinoline derivatives 失效
标题翻译： 4-取代喹啉衍生物
公开(公告)号：US06413982B1
公开(公告)日：2002-07-02
申请号：US09536922
申请日：2000-03-28
申请人： Jun Yuan , George D. Maynard , Alan Hutchison , Stanislaw Rachwal
发明人： Jun Yuan , George D. Maynard , Alan Hutchison , Stanislaw Rachwal
IPC分类号： A61L3147
CPC分类号： C07D401/04 , C07D401/14 , C07D413/04 , C07D487/04 , G01N33/9426 , G01N2333/70571
摘要： Disclosed are compounds of the Formula where R1, R2, R3, R4, X, Y1, and Y2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABAA receptors. Also provided are pharmaceutical compositions comprising these compounds, and methods of treating patients suffering from various central nervous system and peripheral diseases or disorders with these pharmaceutical compositions. This invention also relates to the use of such compounds in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. The compounds of this invention are also useful as probes for the localization of NK-3 receptors and GABAA receptors.
摘要翻译：公开了本文定义的化学式R 1，R 2，R 3，R 4，X，Y 1和Y 2的化合物。这些化合物以高亲和力结合NK-3受体和/或GABA A受体。还提供了包含这些化合物的药物组合物，以及用这些药物组合物治疗患有各种中枢神经系统和外周疾病或病症的患者的方法。本发明还涉及这样的化合物与一种或多种其它CNS剂组合用于增强其它CNS剂的作用的用途。本发明的化合物也可用作NK-3受体和GABA A受体定位的探针。

33. 发明授权

US06511987B1 Bicyclic and tricyclic heteroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US06511987B1
公开(公告)日：2003-01-28
申请号：US09709887
申请日：2000-11-10
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchinson
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchinson
IPC分类号： C07D47104
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。还公开了可用于制备这些化合物的中间体。

34. 发明授权

US08633193B2 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
标题翻译：吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物
公开(公告)号：US08633193B2
公开(公告)日：2014-01-21
申请号：US13014066
申请日：2011-01-26
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K31/519 , C07D487/04 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

35. 发明申请

US20110118273A1 PYRROLO-PYRIDINE, PYRROLO-PYRIMIDINE AND RELATED HETEROCYCLIC COMPOUNDS 失效
标题翻译：吡咯并吡啶，吡咯并吡啶和相关的杂环化合物
公开(公告)号：US20110118273A1
公开(公告)日：2011-05-19
申请号：US13014066
申请日：2011-01-26
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K31/519 , C07D487/04 , A61P29/00 , A61P37/00 , A61P37/06 , A61P11/06 , A61P17/06 , A61P25/28 , A61P25/00 , A61P11/00 , A61P9/10 , A61P13/12 , A61P27/02 , A61P31/18
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

36. 发明申请

US20080267887A1 Pyrrolo-Pyridine, Pyrrolo-Pyrimidine and Related Heterocyclic Compounds 失效
标题翻译：吡咯并 - 吡啶，吡咯并嘧啶和相关杂环化合物
公开(公告)号：US20080267887A1
公开(公告)日：2008-10-30
申请号：US11664565
申请日：2005-10-05
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： A61K9/12 , C07D471/04 , A61K31/437 , C07K14/705 , A61P9/10 , C12Q1/02 , C12N5/06 , A61K31/506
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其分子式如下：其中R 1，R 2，R 5，E，Z 1， Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

37. 发明授权

US07906528B2 Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
标题翻译：吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物
公开(公告)号：US07906528B2
公开(公告)日：2011-03-15
申请号：US11664565
申请日：2005-10-05
申请人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
发明人： Jun Yuan , Peter Hrnciar , Qin Guo , George D. Maynard
IPC分类号： C07D221/02 , C07D471/02 , C07D491/02 , C07D498/02 , A01N43/42 , A61K31/44
CPC分类号： C07D471/04
摘要： Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.
摘要翻译：吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。这些化合物是C5a受体的配体。本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出中性拮抗剂或反向激动剂活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。此外，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

38. 发明申请

US20060142324A1 Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands 审中-公开
公开(公告)号：US20060142324A1
公开(公告)日：2006-06-29
申请号：US11355439
申请日：2006-02-15
申请人： Jun Yuan , George Maynard , Alan Hutchison
发明人： Jun Yuan , George Maynard , Alan Hutchison
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , C07D495/04
摘要： Disclosed are compounds of formula (I) or pharmaceutically acceptable non-toxic salts or pharmaceutically acceptable solvates thereof wherein: (II) represents (a), (b), (c) or (d) and W, X, Y, A, B, C, D, E are variables as described herein. These compounds are highly selective agonists or antagonists at NK3 receptors or prodrugs thereof. The novel tachykinin NK-3 receptor antagonists contained in this invention have potential utility in the treatment of a broad array of disorders and diseases of the central nervous system (CNS) and periphery in mammals in which activation of NK-3 receptors is of importance.

39. 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。

40. 发明授权

US06281220B1 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：US06281220B1
公开(公告)日：2001-08-28
申请号：US09368543
申请日：1999-08-05
申请人： Jun Yuan , Alan Hutchison
发明人： Jun Yuan , Alan Hutchison
IPC分类号： A61K31437
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to deazapurine compounds of the formula wherein Ar, R1, R2, R3, R4, R5, X are as defined herein; these compounds selectively bind to CRF receptors and are useful in the treatment of stress related disorders.
摘要翻译：本发明涉及式（Ⅳ）的脱氮嘌呤化合物：Ar，R 1，R 2，R 3，R 4，R 5，X如本文所定义; 这些化合物选择性地结合CRF受体并且可用于治疗应激相关疾病。

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