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118 条记录 (耗时 0.057 秒)

    Bicyclic and tricyclic heteroaromatic compounds
    52.
    发明申请
    Bicyclic and tricyclic heteroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US20060217384A1

    公开(公告)日：2006-09-28

    申请号：US11442812

    申请日：2006-05-30

    申请人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    发明人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    IPC分类号： C07D487/04 ,  A61K31/503 ,  A61K31/4745

    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 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）疾病和用作GABA < 组织样品中的受体。 还公开了可用于制备这些化合物的中间体。

    Fused pyrrolecarboxamides; GABA brain receptor ligands
    53.
    发明授权
    Fused pyrrolecarboxamides; GABA brain receptor ligands 失效
    熔融吡咯烷酰胺; GABA脑受体配体

    公开(公告)号：US07109351B1

    公开(公告)日：2006-09-19

    申请号：US09651207

    申请日：2000-08-30

    申请人： Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    发明人： Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    IPC分类号： C07D209/42 ,  A61K31/40

    CPC分类号： A61K51/047 ,  C07D209/42 ,  C07D209/52 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D417/14 ,  C07D471/04 ,  G01N2333/70571

    摘要： Substituted pyrrolecarboxamide compounds are disclosed. These 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 and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. 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： 公开了取代的吡咯甲酰胺化合物。 这些化合物是高度选择性的激动剂，拮抗剂或反义激动剂，用于GABA A A受体或GABA A A受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于 诊断和治疗焦虑，抑郁，阿尔茨海默氏痴呆，睡眠和癫痫发作障碍，与苯二氮卓类药物过量并用于记忆增强。 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 A受体定位的探针。

    Heteroaryl fused aminoalkyl imidazole derivates: selective modulators of GABAA receptors
    54.
    发明申请
    Heteroaryl fused aminoalkyl imidazole derivates: selective modulators of GABAA receptors 失效
    杂芳基稠合氨基烷基咪唑衍生物：GABA A受体的选择性调节剂

    公开(公告)号：US20060160842A1

    公开(公告)日：2006-07-20

    申请号：US11295173

    申请日：2005-12-06

    申请人： Robert DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  Daniel Rosewater

    发明人： Robert DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  Daniel Rosewater

    IPC分类号： C07D471/02 ,  A61K31/4745

    CPC分类号： C07D235/14 ,  C07D401/06 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D471/04

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, 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, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and 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A，B，C，D，X，R 1，R 2， R 3，R 4，R 5和R 6是本文定义的变量，这些化合物是高度选择性的激动剂 ，GABAa脑受体的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，因此可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作障碍，抑郁症，苯并二氮卓过量 药物，提高记忆力和警觉性。

    Bicyclic and tricyclic hetroaromatic compounds
    55.
    发明授权
    Bicyclic and tricyclic hetroaromatic compounds 失效
    双环和三环杂芳族化合物

    公开(公告)号：US07053093B2

    公开(公告)日：2006-05-30

    申请号：US10352519

    申请日：2003-01-28

    申请人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    发明人： Jun Yuan ,  Pamela Albaugh ,  Kenneth Shaw ,  Alan Hutchison

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K25/24 ,  A61P25/22

    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 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）疾病和用作GABA < 组织样品中的受体。 还公开了可用于制备这些化合物的中间体。

    Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands
    57.
    发明申请
    Heteroaryl substituted fused bicyclic heteroaryl compounds as GABAA receptor ligands 审中-公开
    杂芳基取代的稠合双环杂芳基化合物作为GABA A受体配体

    公开(公告)号：US20060014746A1

    公开(公告)日：2006-01-19

    申请号：US11214345

    申请日：2005-08-29

    申请人： Alan Hutchison ,  George Maynard ,  Pamela Albaugh ,  Linghong Xie ,  Jun Yuan ,  Scott Mitchell ,  Vinod Singh ,  Manuka Ghosh ,  Guiying Li ,  Nian Liu

    发明人： Alan Hutchison ,  George Maynard ,  Pamela Albaugh ,  Linghong Xie ,  Jun Yuan ,  Scott Mitchell ,  Vinod Singh ,  Manuka Ghosh ,  Guiying Li ,  Nian Liu

    IPC分类号： C07D487/04 ,  C07D471/02 ,  A61K31/519 ,  A61K31/503 ,  A61K31/4745

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D513/04

    摘要： This invention relates to heteroaryl substituted fused bicyclic heteroaryl compounds, such as heteroaryl substituted imidazopyridines, imidazopyrazines, imidazopyridizines, imidazopyrimidines, and imidazothiazoles, which may be described by Formula I or Formula II: The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Processes for preparing compounds of Formula I and Formula II are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I or Formula II in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.

    摘要翻译： 本发明涉及可以由式I或式II描述的杂芳基取代的稠合双环杂芳基化合物，例如杂芳基取代的咪唑并吡啶，咪唑并吡嗪，咪唑并吡啶，咪唑并嘧啶和咪唑并噻唑。本发明特别涉及以高选择性结合的这些化合物 并且对GABA A A受体的苯并二氮杂位点具有高亲和力。 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某些中枢神经系统（CNS）疾病中的用途。 公开了制备式I和式II化合物的方法。 本发明还涉及式I或式II的苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。

    Certain pyrrolopyridine derivatives: novel CRF1 specific ligands
    59.
    发明授权
    Certain pyrrolopyridine derivatives: novel CRF1 specific ligands 失效
    某些吡咯并吡啶衍生物：新型CRF1特异性配体

    公开(公告)号：US06670371B2

    公开(公告)日：2003-12-30

    申请号：US10096239

    申请日：2002-03-12

    申请人： Raymond F. Horvath ,  Alan Hutchison

    发明人： Raymond F. Horvath ,  Alan Hutchison

    IPC分类号： A61K31437

    CPC分类号： C07D471/04 ,  C07D471/14

    摘要： Disclosed are compounds of the formula: wherein Ar is optionally substituted aryl or heteroaryl R1 is hydrogen or alkyl; R7 is hydrogen or alkyl; R2 is hydrogen, halogen, alkyl or alkoxy; or R1 and R2 taken together with the ring to which they are attached form a 5-9 membered saturated or aromatic ring optionally having a hetero atom selected from oxygen, sulfur or nitrogen; R3 and R4 are independently hydrogen, alkyl, cycloalkyl, aryl or heteroaryl groups; or R3 and R4 together with the nitrogen atom to which they are attached form a 5-8 membered ring; and R5 is hydrogen, halogen, straight or branched chain lower alkyl having 1-6 carbon atoms, or straight or branched chain lower alkoxy or thioalkoxy having 1-6 carbon atoms, which compounds are highly selective partial agonists or antagonists at human Corticotropin-Releasing Factor 1 (CRF1) receptors and 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是任选取代的芳基或杂芳基R 1是氢或烷基; R 7是氢或烷基; R 2是氢，卤素，烷基或烷氧基; 或者R 1和R 2与它们所连接的环一起形成任选具有选自氧，硫或氮的杂原子的5-9元饱和或芳环; R 3和R 4独立地是氢，烷基，环烷基，芳基或杂芳基 团体 或R 3和R 4与它们所连接的氮原子一起形成5-8元环; 和R 5是氢，卤素，具有1-6个碳原子的直链或支链低级烷基，或具有1-6个碳原子的直链或支链低级烷氧基或硫代烷氧基，该化合物是人促皮激素释放因子的高选择性部分激动剂或拮抗剂 1（CRF1）受体，可用于诊断和治疗应激相关疾病如后遗传性应激障碍（PTSD）以及抑郁，头痛和焦虑。