利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

281 条记录 (耗时 0.042 秒)

    4-substituted quinoline derivatives
    33.
    发明授权
    4-substituted quinoline derivatives 失效
    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。

    Certain tricyclic substituted diazabicyclo (3.2.1) octane derivatives
    34.
    发明授权
    Certain tricyclic substituted diazabicyclo (3.2.1) octane derivatives 失效
    某些三环取代的二氮杂双环（3.2.1）辛烷衍生物

    公开(公告)号：US6156751A

    公开(公告)日：2000-12-05

    申请号：US393789

    申请日：1999-09-10

    申请人： Alan Hutchison ,  Jun Yuan ,  Raymond F. Horvath

    发明人： Alan Hutchison ,  Jun Yuan ,  Raymond F. Horvath

    IPC分类号： C07D487/08 ,  A61K31/495 ,  C07D247/00

    CPC分类号： C07D487/08

    摘要： This invention encompasses compounds of the formula: ##STR1## where either R.sub.1 or R.sub.2 represents ##STR2## and the other represents hydrogen or straight or branched chain lower alkyl having 1-6 carbon atoms; andX is oxygen, methylene, or NH;Y is represents various inorganic and organic substituents;Z is hydrogen, amino or NHR.sub.6 where R.sub.6 is lowere alkyl having 1-6 carbon atoms;T is hydrogen, halogen, hydroxy, or lower alkoxy having 1-6 carbon atoms; andA is methylene, carbonyl or CHOH.These compounds are selective partial agonists or antagonists at brain monoamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism. Furthermore compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neurolepticagents. These compounds show unexpectedly atypical antipsychotic profiles (clozapine-like) in the animal models described in this patent.

    摘要翻译： 本发明包括下式的化合物：其中R 1或R 2表示，另一个表示氢或具有1-6个碳原子的直链或支链低级烷基; X为氧，亚甲基或NH; Y代表各种无机和有机取代基; Z是氢，氨基或NHR 6，其中R6是具有1-6个碳原子的低级烷基; T是氢，卤素，羟基或具有1-6个碳原子的低级烷氧基; A是亚甲基，羰基或CHOH。 这些化合物是脑单胺受体亚型或其前药的选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。 此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。 这些化合物在本专利描述的动物模型中显示出意想不到的非典型抗精神病药谱（氯氮平样）。

    1-aryl-4-substituted isoquinolines
    35.
    发明授权
    1-aryl-4-substituted isoquinolines 失效
    1-芳基-4-取代的异喹啉

    公开(公告)号：US07915288B2

    公开(公告)日：2011-03-29

    申请号：US11587906

    申请日：2005-05-06

    申请人： Kyungae Lee ,  Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Scott Mitchell

    发明人： Kyungae Lee ,  Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Scott Mitchell

    IPC分类号： C07D217/02 ,  A61K31/47

    CPC分类号： C07D405/12 ,  A61K31/47 ,  C07D217/14 ,  C07D217/16 ,  C07D217/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14

    摘要： 1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II 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 1-aryl-4-substituted isoquinolines or 1-aryl-3,4-disubstituted isoquinolines, which are useful as probes for the localization of C5a receptors.

    摘要翻译： 式I和式II的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉类似物如下：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。 这些化合物是C5a受体的配体。 优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现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，本发明提供标记的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉，其可用作C5a受体定位的探针。

    2-aminoquinolinecarboxamides: neurokinin receptor ligands
    36.
    发明授权
    2-aminoquinolinecarboxamides: neurokinin receptor ligands 失效
    2-氨基喹啉甲酰胺：神经激肽受体配体

    公开(公告)号：US07041664B2

    公开(公告)日：2006-05-09

    申请号：US10868136

    申请日：2004-06-14

    申请人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    IPC分类号： C07D401/04 ,  A61K31/47

    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。

    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands
    37.
    发明授权
    Aryl fused 2,4-disubstituted pyridines: NK3 receptor ligands 失效
    芳基稠合的2,4-二取代吡啶：NK3受体配体

    公开(公告)号：US07037922B1

    公开(公告)日：2006-05-02

    申请号：US09914957

    申请日：2000-03-10

    申请人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George Maynard ,  Alan Hutchison

    IPC分类号： C07D471/04 ,  A61K31/435

    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.

    摘要翻译： 公开了式（I）化合物或其药学上可接受的无毒盐或其药学上可接受的溶剂合物，其中：（II）代表（a），（b），（c）或（d）和W，X，Y， B，C，D，E是本文所述的变量。 这些化合物是NK3受体或其前药的高选择性激动剂或拮抗剂。 本发明中包含的新型速激肽NK-3受体拮抗剂在治疗NK-3受体活化是重要的哺乳动物的中枢神经系统（CNS）和外周的疾病和疾病的广泛阵列中具有潜在的用途。

    Deazapurine derivatives: a new class of CRF1 specific ligands
    38.
    发明授权
    Deazapurine derivatives: a new class of CRF1 specific ligands 失效
    去氮嘌呤衍生物：一类新的CRF1特异性配体

    公开(公告)号：US06495688B2

    公开(公告)日：2002-12-17

    申请号：US09887206

    申请日：2001-06-21

    申请人： Jun Yuan ,  Alan Hutchison

    发明人： Jun Yuan ,  Alan Hutchison

    IPC分类号： C07D48704

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Disclosed are compounds of formula wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 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： 公开的化合物，其中Ar表示芳基或杂芳基; 并且R 1，R 2，R 3，R 4和R 5表示有机或无机取代基，所述化合物是人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血清后应激障碍 （PTSD）以及抑郁，头痛和焦虑。

    Deazapurine derivatives; a new class of CRF1 specific ligands
    39.
    发明授权
    Deazapurine derivatives; a new class of CRF1 specific ligands 失效
    去氮嘌呤衍生物 一类新的CRF1特异性配体

    公开(公告)号：US5847136A

    公开(公告)日：1998-12-08

    申请号：US881960

    申请日：1997-06-25

    申请人： Jun Yuan ,  Alan Hutchison

    发明人： Jun Yuan ,  Alan Hutchison

    IPC分类号： C07D471/04 ,  C07D487/04 ,  C07D487/02

    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。