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    Substituted fused pyrazolecarboxylic acid arylamides and related compounds
    1.
    发明授权
    Substituted fused pyrazolecarboxylic acid arylamides and related compounds 失效
    取代的稠合吡唑甲酰芳基酰胺和相关化合物

    公开(公告)号：US06852730B2

    公开(公告)日：2005-02-08

    申请号：US10360963

    申请日：2003-02-07

    申请人： George Maynard ,  Jun Yuan ,  Stanislaw Rachwal

    发明人： George Maynard ,  Jun Yuan ,  Stanislaw Rachwal

    IPC分类号： G01N33/53 ,  A61K31/435 ,  A61K31/4439 ,  A61K31/519 ,  A61P25/00 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D401/12 ,  C07D471/04 ,  C07D487/04 ,  G01N33/60 ,  A61K31/437 ,  A61K31/55 ,  C07D487/14

    CPC分类号： C07D471/04 ,  C07B2200/05 ,  C07D487/04

    摘要： Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related 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 treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    摘要翻译： 杂环化合物如3,4,5,6-四氢-2,3,10-三氮杂 - 苯并[e]薁-1-羧酸芳基酰胺，5,7-二氢-6H-吡唑并[3,4-h] 喹啉-9-羧酸芳基酰胺，5,7-二氢-6H-吡唑并[3,4-h]喹唑啉-9-羧酸芳基酰胺，2,4,5,6-四氢-1,2,6,7- 四氮杂 - 引嗪并] -8-羧酸芳基酰胺和相关化合物。 这些化合物是用于GABAA脑受体的G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，因此可用于治疗焦虑，抑郁，睡眠和癫痫发作，用苯二氮卓类药物过量服用， 阿尔茨海默病的痴呆，并增强记忆力。 还提供药物组合物，包括包装的药物组合物。 还提供了可用于合成吡唑甲酰芳基酰胺的中间体。 本发明的化合物也可用作组织样品中GABA A受体定位的探针。

    Substituted fused pyrroleoximes and fused pyrazoleoximes
    3.
    发明申请
    Substituted fused pyrroleoximes and fused pyrazoleoximes 失效
    取代的稠合吡咯肟和稠合吡唑肟

    公开(公告)号：US20050059826A1

    公开(公告)日：2005-03-17

    申请号：US10858496

    申请日：2004-06-01

    申请人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    发明人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    IPC分类号： A61K31/4045 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  C07D209/42 ,  C07D231/56 ,  C07D401/12 ,  C07D275/04 ,  C07D261/20

    CPC分类号： C07D231/56 ,  C07D209/42 ,  C07D401/12

    摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. 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, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including 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R，Ar，A，n，R 1和R 2在本文中定义。 这些化合物是GABAA脑受体的高度选择性激动剂，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，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍， 过量与苯二氮卓类药物和增强记忆。 还公开了药物组合物，包括包装的药物组合物。

    Substituted Fused Pyrroleoximes and Fused Pyrazoleoximes
    4.
    发明申请
    Substituted Fused Pyrroleoximes and Fused Pyrazoleoximes 审中-公开
    取代的熔融吡咯肟和稠合吡唑油肟

    公开(公告)号：US20080032975A1

    公开(公告)日：2008-02-07

    申请号：US11872332

    申请日：2007-10-15

    申请人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    发明人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    IPC分类号： A61K31/416 ,  A61K31/404 ,  A61K31/4439 ,  A61K31/50 ,  A61K31/5377 ,  A61P25/00 ,  C07D209/42 ,  C07D231/54 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  G01N33/53

    CPC分类号： C07D231/56 ,  C07D209/42 ,  C07D401/12

    摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. 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, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including 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R，Ar，A，n，R 1和R 2是本文定义的。 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 诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和癫痫发作障碍，用苯二氮卓类药物服用过量，并增加记忆力。 还公开了药物组合物，包括包装的药物组合物。

    Aryl substituted tetrahydroindazoles
    5.
    发明授权
    Aryl substituted tetrahydroindazoles 失效
    芳基取代的四氢茚满

    公开(公告)号：US06656941B2

    公开(公告)日：2003-12-02

    申请号：US09947702

    申请日：2001-09-06

    申请人： George Maynard ,  Pamela Albaugh ,  Stanislaw Rachwal ,  Linda Gustavson

    发明人： George Maynard ,  Pamela Albaugh ,  Stanislaw Rachwal ,  Linda Gustavson

    IPC分类号： A61K3150

    CPC分类号： C07D231/56 ,  C07D401/12 ,  G01N2333/70571

    摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables R1, R2, R3, n, and Ar are defined herein. 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, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

    摘要翻译： 公开了下式的化合物及其药学上可接受的盐，其中变量R1，R2，R3，n和Ar如本文所定义。 这些化合物是GABAA脑受体的高度选择性激动剂，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，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍， 过量与苯二氮卓类药物和增强记忆。

    Substituted fused pyrroleimines and pyrazoleimines
    6.
    发明授权
    Substituted fused pyrroleimines and pyrazoleimines 失效
    取代的稠合吡咯亚胺和吡唑亚胺

    公开(公告)号：US06743817B2

    公开(公告)日：2004-06-01

    申请号：US09947710

    申请日：2001-09-06

    申请人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    发明人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    IPC分类号： A61K31403

    CPC分类号： C07D231/56 ,  C07D209/42 ,  C07D401/12

    摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. 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, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including 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R，Ar，A，n，R 1和R 2在本文中定义。 这些化合物是GABAA脑受体的高度选择性激动剂，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，因此可用于诊断和治疗焦虑症，抑郁症，唐氏综合症，睡眠和癫痫发作障碍， 过量与苯二氮卓类药物和增强记忆。 还公开了药物组合物，包括包装的药物组合物。

    Substituted fused pyrroleoximes and fused pyrazoleoximes
    7.
    发明授权
    Substituted fused pyrroleoximes and fused pyrazoleoximes 失效
    取代的稠合吡咯肟和稠合吡唑肟

    公开(公告)号：US07282498B2

    公开(公告)日：2007-10-16

    申请号：US10858496

    申请日：2004-06-01

    申请人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    发明人： George Maynard ,  LingHong Xie ,  Stanislaw Rachwal

    IPC分类号： C07D413/12 ,  C07D403/12 ,  C07D231/54 ,  A61K31/416 ,  A61K31/5377

    CPC分类号： C07D231/56 ,  C07D209/42 ,  C07D401/12

    摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. 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, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including 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R，Ar，A，n，R 1和R 2是本文定义的。 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 诊断和治疗焦虑症，抑郁症，唐氏综合征，睡眠和癫痫发作障碍，用苯二氮卓类药物服用过量，并增加记忆力。 还公开了药物组合物，包括包装的药物组合物。

    4-substituted quinoline derivatives
    8.
    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。

    4-Substituted quinoline derivatives
    9.
    发明授权
    4-Substituted quinoline derivatives 失效
    4-取代的喹啉衍生物

    公开(公告)号：US06624175B2

    公开(公告)日：2003-09-23

    申请号：US10140693

    申请日：2002-05-07

    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： A61K3147

    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。

    Substituted imidazoles as selective modulators of Bradykinin B2 receptors
    10.
    发明授权
    Substituted imidazoles as selective modulators of Bradykinin B2 receptors 失效
    取代的咪唑作为缓激肽B2受体的选择性调节剂

    公开(公告)号：US06509366B2

    公开(公告)日：2003-01-21

    申请号：US09764805

    申请日：2001-01-17

    申请人： Stanislaw Rachwal ,  Alan Hutchison ,  Kenneth Shaw ,  George D. Maynard ,  Xiao-shu He ,  Robert DeSimone ,  Kevin Hodgetts

    发明人： Stanislaw Rachwal ,  Alan Hutchison ,  Kenneth Shaw ,  George D. Maynard ,  Xiao-shu He ,  Robert DeSimone ,  Kevin Hodgetts

    IPC分类号： A61K314174

    CPC分类号： C07D233/64 ,  C07D233/68 ,  C07D401/06

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis, and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.

    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Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7 R 7'是本文定义的变量，该化合物是缓激肽B2受体的调节剂。 因此，这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛 经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血液 - 脑肿瘤屏障。