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    Melanin concentrating hormone receptor ligands
    1.
    发明授权
    Melanin concentrating hormone receptor ligands 失效
    黑色素浓缩激素受体配体

    公开(公告)号：US06569861B2

    公开(公告)日：2003-05-27

    申请号：US09900679

    申请日：2001-07-06

    申请人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    发明人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    IPC分类号： A61K31495

    CPC分类号： C07D295/096

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

    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Q，X，Y，Z和R 1 R 9和R 12 -R 19如本文所定义。这些化合物是MCH 1受体的选择性调节剂，因此其可用于 治疗各种代谢，喂养和性功能障碍。 还公开了治疗这种病症以及包装的药物组合物的方法。

    Melanin concentrating hormone receptor ligands
    2.
    发明授权
    Melanin concentrating hormone receptor ligands 失效
    黑色素浓缩激素受体配体

    公开(公告)号：US06753336B2

    公开(公告)日：2004-06-22

    申请号：US10385973

    申请日：2003-03-11

    申请人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    发明人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    IPC分类号： A61K31451

    CPC分类号： C07D295/096

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

    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Q，X，Y，Z和R 1 R 9和R 12 -R 19如本文所定义。这些化合物是MCH 1受体的选择性调节剂，因此其可用于 治疗各种代谢，喂养和性功能障碍。 还公开了治疗这种病症以及包装的药物组合物的方法。

    Melanin concentrating hormone receptor ligands
    3.
    发明授权
    Melanin concentrating hormone receptor ligands 失效
    黑色素浓缩激素受体配体

    公开(公告)号：US07323478B2

    公开(公告)日：2008-01-29

    申请号：US10820344

    申请日：2004-04-08

    申请人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    发明人： Rajagopal Bakthavatchalam ,  Andrew Thurkauf ,  Alan Hutchison

    IPC分类号： A61K31/445

    CPC分类号： C07D295/096

    摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

    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Q，X，Y，Z和R 1 R 9和R 12， 本文定义了本文所述的方法。 这些化合物是MCH 1受体的选择性调节剂，因此可用于治疗各种代谢，喂养和性功能障碍。 还公开了治疗这种病症以及包装的药物组合物的方法。

    Substituted 4-(alkyl, dialkyl) or cycloaklyl)aminomethyl 2-phenylimidazoes: dopamine receptor subtype specific ligands
    4.
    发明授权
    Substituted 4-(alkyl, dialkyl) or cycloaklyl)aminomethyl 2-phenylimidazoes: dopamine receptor subtype specific ligands 失效
    取代的4-（烷基，二烷基）或环烯基）氨基甲基2-苯基咪唑：多巴胺受体亚型特异性配体

    公开(公告)号：US5646280A

    公开(公告)日：1997-07-08

    申请号：US457989

    申请日：1995-06-01

    申请人： Andrew Thurkauf ,  Alan Hutchison

    发明人： Andrew Thurkauf ,  Alan Hutchison

    IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D333/64 ,  A61K31/415 ,  C07D403/04 ,  C07D403/06

    CPC分类号： C07D233/64 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

    摘要： Disclosed are compounds and the pharmaceutically acceptable salts thereof useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism and useful in treating the extraparamidyl side effects associated with the use of conventional neuroleptic agents, which compounds have the formula: ##STR1## where R.sub.1, X, Y and T indepedently represent inorganic or organic groups such as hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy, or sulfonyl;R.sub.3 is hydrogen or lower alkyl or R.sub.3 and R.sub.4 together may form a ring structure; andR.sub.4 and R.sub.5 are the same or different and represent organic or inorganic groups where the groups may form a ring optionally substituted with various organic or inorganic substituents.

    摘要翻译： 公开了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的化合物及其药学上可接受的盐，并且可用于治疗与使用常规的精神抑制剂相关的甲喋呤副作用，其中 化合物具有下式：其中R 1，X，Y和T独立地表示无机或有机基团，例如氢，卤素，羟基，低级烷基，低级烷氧基或磺酰基; R3是氢或低级烷基或R3和R4一起可以形成环结构; 并且R 4和R 5相同或不同并且表示有机或无机基团，其中基团可以形成任选被各种有机或无机取代基取代的环。

    Certain cycloalkyl and azacycloalkyl pyrrolopyrimidines; a new class of GABA brain receptor ligands
    5.
    发明授权
    Certain cycloalkyl and azacycloalkyl pyrrolopyrimidines; a new class of GABA brain receptor ligands 失效
    某些环烷基和氮杂环烷基吡咯并嘧啶; 一类新的GABA脑受体配体

    公开(公告)号：US5585490A

    公开(公告)日：1996-12-17

    申请号：US30468

    申请日：1993-04-05

    申请人： Andrew Thurkauf ,  Alan Hutchison ,  Vinod Singh

    发明人： Andrew Thurkauf ,  Alan Hutchison ,  Vinod Singh

    IPC分类号： C07D471/14 ,  C07D487/04 ,  C07D491/14 ,  C07D487/10 ,  C07D487/20

    CPC分类号： C07D471/14 ,  C07D487/04 ,  C07D491/14

    摘要： This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1 or 2, and R.sub.1, R.sub.2, X, Y and W are variables.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 type drugs, and enhancement of alertness.

    摘要翻译： PCT No.PCT / US91 / 07195 Sec。 371日期：1993年4月5日 102（e）日期1993年4月5日PCT 1991年10月8日提交PCT本发明包括下式的化合物：其中n为0,1或2，R1，R2， X，Y和W是变量。 这些化合物是用于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并提高警觉性。

    High affinity small molecule C5a receptor modulators
    6.
    发明授权
    High affinity small molecule C5a receptor modulators 失效
    高亲和力小分子C5a受体调节剂

    公开(公告)号：US06723743B1

    公开(公告)日：2004-04-20

    申请号：US09672071

    申请日：2000-09-28

    申请人： Andrew Thurkauf ,  Xiao-shu He ,  He Zhao ,  John Peterson ,  Xiaoyan Zhang ,  Robbin Brodbeck ,  James Krause ,  George Maynard ,  Alan Hutchison

    发明人： Andrew Thurkauf ,  Xiao-shu He ,  He Zhao ,  John Peterson ,  Xiaoyan Zhang ,  Robbin Brodbeck ,  James Krause ,  George Maynard ,  Alan Hutchison

    IPC分类号： A61K31415

    CPC分类号： C07D207/327 ,  C07C233/11 ,  C07C233/22 ,  C07C233/65 ,  C07C233/66 ,  C07C233/73 ,  C07C233/78 ,  C07C235/46 ,  C07C235/48 ,  C07C235/54 ,  C07C235/60 ,  C07C235/62 ,  C07C235/66 ,  C07C237/20 ,  C07C323/62 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2603/18 ,  C07D213/38 ,  C07D213/82 ,  C07D215/12 ,  C07D217/04 ,  C07D217/06 ,  C07D217/14 ,  C07D217/16 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D235/02 ,  C07D235/14 ,  C07D235/18 ,  C07D317/58 ,  C07D333/24 ,  C07D333/28 ,  C07D333/54 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04

    摘要： This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors, preferably human C5a receptors, Preferred compounds of the invention possess one or more, and preferably two or more, three or more, four or more, or all of the following properties in that they are; 1) multi-aryl in structure (having a plurality of un-fused or fused aryl groups), 2) heteroaryl in structure, 3) orally available in vivo (such that a sub-lethal or preferably a pharmaceutically acceptable oral dose can provide a detectable in vitro effect such as a reduction of C5a-induced neutropenia), 4) comprised of fewer than four, preferably fewer than three, or fewer than two, or no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar concentrations and preferably at sub-nanomolar concentrations. Specifically exemplified representative compounds include, but are not limited to optionally substituted arylimidazoles, optionally substituted arylpyridyls, optionally substituted aryl-substituted cycloalkylimidazoles, optionally substituted arylpyrazoles, optionally substituted benzimidazoles, optionally substituted aryl-substituted tetrahydroisoquinolines, and optionally substituted biaryl carboxamides. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.

    摘要翻译： 本发明涉及作为哺乳动物补体C5a受体调节剂的低分子量，非肽，非拟肽，有机分子，优选用作高亲和力C5a受体配体的调节剂，还涉及作为拮抗剂或反向激动剂的这些配体 的补体C5a受体，优选人C5a受体。本发明的优选化合物具有一个或多个，优选两个或更多个，三个或更多个，四个或更多个或全部以下性质： 1）结构上的多芳基（具有多个未稠合或稠合芳基），2）结构上的杂芳基，3）在体内可口服（使得亚致死或优选药学上可接受的口服剂量可提供 可检测的体外效应，例如C5a诱导的中性粒细胞减少的减少），4）由少于4个，优选少于3个，或少于2个或不存在的酰胺键组成，以及5）能够以纳摩尔浓度抑制白细胞趋化性， 优选亚纳摩尔浓度。 具体示例的代表性化合物包括但不限于任选取代的芳基咪唑，任选取代的芳基吡啶基，任选取代的芳基取代的环烷基咪唑，任选取代的芳基吡唑，任选取代的苯并咪唑，任选取代的芳基取代的四氢异喹啉和任选取代的双芳基甲酰胺。 本发明还涉及包含这些化合物的药物组合物。 它还涉及这些化合物在治疗各种炎性和免疫系统疾病中的应用。 此外，本发明涉及使用这些化合物作为C5a受体定位的探针。

    Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
    10.
    发明授权
    Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes 失效
    Gabaa受体亚型和使用咪唑并喹啉和吡咯并嘧啶结合gabaa受体亚型筛选药物化合物的方法

    公开(公告)号：US5597920A

    公开(公告)日：1997-01-28

    申请号：US876050

    申请日：1992-04-30

    申请人： Kenneth Shaw ,  Alan Hutchison ,  Andrew Thurkauf ,  John Tallman

    发明人： Kenneth Shaw ,  Alan Hutchison ,  Andrew Thurkauf ,  John Tallman

    IPC分类号： G01N33/53 ,  A61K31/495 ,  A61K31/505 ,  A61P25/08 ,  A61P25/20 ,  A61P25/28 ,  C07B59/00 ,  C07D487/04 ,  G01N33/534 ,  G01N33/566 ,  G01N33/94 ,  C07D487/06 ,  C07D487/02

    CPC分类号： G01N33/9426 ,  C07B59/002 ,  G01N33/566 ,  G01N33/948 ,  G01N2500/20

    摘要： The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent hydrogen, halogen, alkyl or alkoxy substituents;R5 is hydrogen or lower alkyl;X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; andZ is hydrogen or fluorine.The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas I and II radiolabeled with tritium or isotopes of iodine.The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas I or II.The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula I or II.The compounds provided herein bind selectively to a novel subtype of the GABAa binding site. Selective interaction of ligands at this unique receptor population results in pharmacological specificity which may lead to superior anxiolytics, cognition enhancers, anticonvulsants and sedative hypnotics.

    摘要翻译： 本发明提供了利用式I和II化合物筛选药物化合物的方法，其中式I和II是其中R 1，R 2，R 3和R 4表示氢， 卤素，烷基或烷氧基取代基; R5是氢或低级烷基; X和Y表示氢，卤素，烷基或烷氧基取代基; Z是氢或氟。 本发明还提供用氚或碘的同位素放射性标记的式I和II的氚或碘同位素放射性标记的化合物。 本发明还提供了与式I或II化合物特异性结合的新型GABAa受体亚型。 本发明还提供了与式I或II化合物原位结合的GABAa受体亚型。 本文提供的化合物选择性结合GABAa结合位点的新亚型。 配体在这种独特的受体群体上的选择性相互作用导致药理学特异性，这可能导致优异的抗焦虑药，认知增强剂，抗惊厥药和镇静催眠药。