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    Aryl and heteroaryl substituted pyridino derivatives GABA brain receptor ligands
    11.
    发明授权
    Aryl and heteroaryl substituted pyridino derivatives GABA brain receptor ligands 失效
    芳基和杂芳基取代的吡啶衍生物GABA脑受体配体

    公开(公告)号：US06297256B1

    公开(公告)日：2001-10-02

    申请号：US09596031

    申请日：2000-06-15

    Applicant: Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

    Inventor： Guolin Cai ,  Gang Liu ,  Pamela A. Albaugh

    IPC: G07D40104

    CPC classification number: C07D401/14 ,  C07D495/04

    Abstract: Disclosed are aryl and heteroaryl substitated pyridino compounds. 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 further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    Abstract translation: 公开了芳基和杂芳基取代的吡啶基化合物。 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受体定位的探针。

    Aryl fused substituted 4-oxy-pyridines
    15.
    发明授权
    Aryl fused substituted 4-oxy-pyridines 失效
    芳基稠合取代的4-氧 - 吡啶

    公开(公告)号：US06828329B2

    公开(公告)日：2004-12-07

    申请号：US09892024

    申请日：2001-06-26

    Applicant: Guolin Cai ,  Pamela Albaugh ,  Jun Yuan

    Inventor： Guolin Cai ,  Pamela Albaugh ,  Jun Yuan

    IPC: A61K3144

    CPC classification number: C07D215/233 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D471/04 ,  C07D495/04

    Abstract: Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are 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 further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    Abstract translation: 公开了下式的化合物：其中X，Q，W和如本文所定义。 这些化合物是GABAA脑受体的激动剂，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，唐氏综合征，睡眠和癫痫发作，过量与 苯二氮卓类药物和增强记忆力。 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受体定位的探针。

    Oxomidazopyridine-carboxamides
    16.
    发明授权
    Oxomidazopyridine-carboxamides 失效
    恶唑并吡啶 - 甲酰胺

    公开(公告)号：US06723332B2

    公开(公告)日：2004-04-20

    申请号：US09864846

    申请日：2001-05-24

    Applicant: Guolin Cai ,  Pamela A. Albaugh ,  Kenneth Shaw

    Inventor： Guolin Cai ,  Pamela A. Albaugh ,  Kenneth Shaw

    IPC: A01N2534

    CPC classification number: C07D471/04

    Abstract: Disclosed are compounds of the formula: wherein: A, B, C, E, F, and G are substituents as defined herein, which compounds bind to the benzodiazepine site of GABAA receptors and are therefore useful in treatment of central nervous system (CNS) diseases.

    Abstract translation: 公开了下式的化合物：其中：A，B，C，E，F和G是如本文所定义的取代基，该化合物结合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

    2,4-substituted quinoline derivatives
    17.
    发明授权
    2,4-substituted quinoline derivatives 失效
    2,4-取代喹啉衍生物

    公开(公告)号：US06559163B2

    公开(公告)日：2003-05-06

    申请号：US09931549

    申请日：2001-08-16

    Applicant: Guolin Cai ,  Jun Yuan ,  Kevin Currie ,  Pamela Albaugh ,  Alan Hutchison

    Inventor： Guolin Cai ,  Jun Yuan ,  Kevin Currie ,  Pamela Albaugh ,  Alan Hutchison

    IPC: A61K314709

    CPC classification number: C07D231/12 ,  C07D215/52 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04

    Abstract: Disclosed are compounds of the formula or pharmaceutically acceptable salts thereof wherein: represents: and A, B, G, D, E, Ra, Rb, W, and Z are defined herein. These compounds are 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 further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    Abstract translation: 公开了式或其药学上可接受的盐的化合物，其中：表示：并且A，B，G，D，E，Ra，Rb，W和Z在本文中定义。 这些化合物是GABAA脑受体的激动剂，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，唐氏综合征，睡眠和癫痫发作，过量与 苯二氮卓类药物和增强记忆力。 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受体定位的探针。

    Substituted 4-oxo-quinoline-3-carboxamides
    18.
    发明授权
    Substituted 4-oxo-quinoline-3-carboxamides 失效
    取代的4-氧代 - 喹啉-3-甲酰胺

    公开(公告)号：US06413956B1

    公开(公告)日：2002-07-02

    申请号：US09565529

    申请日：2000-05-05

    Applicant: Pamela A. Albaugh ,  Kevin S. Currie ,  Dan Rosewater ,  Guolin Cai

    Inventor： Pamela A. Albaugh ,  Kevin S. Currie ,  Dan Rosewater ,  Guolin Cai

    IPC: C07D40112

    CPC classification number: C07D401/12 ,  C07D215/56 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D487/04

    Abstract: Disclosed are compounds of Formula I: or the pharmaceutically acceptable salts thereof where, R1, R2, and W 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 further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

    Abstract translation: 公开了式I的化合物或其药学上可接受的盐，其中R1，R2和W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，唐氏综合征，睡眠和发作障碍， 过量与苯二氮卓类药物和增强记忆。 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受体定位的探针。

    4-(4-piperidylmethylamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands
    19.
    发明授权
    4-(4-piperidylmethylamino) substituted heteroaryl fused pyridines: GABA brain receptor ligands 失效
    4-（4-哌啶基甲基氨基）取代的杂芳基稠合吡啶：GABA脑受体配体

    公开(公告)号：US06380209B1

    公开(公告)日：2002-04-30

    申请号：US09583147

    申请日：2000-05-30

    Applicant: Guolin Cai ,  Gang Liu

    Inventor： Guolin Cai ,  Gang Liu

    IPC: A61K314375

    CPC classification number: C07D471/04 ,  C07D495/04

    Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; and W is (un)substituted alkyl, aryl, or heteroaryl, 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. The compounds of the invention are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

    Abstract translation: 公开了下式的化合物或其药学上可接受的无毒盐，其中：R是氢，烷基或（未）取代的烷氧基或氨基; 和W是（未取代的）取代的烷基，芳基或杂芳基，该化合物是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。 本发明的化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍，以及用苯二氮卓类药物过量并提高警觉性。

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