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    HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
    1.
    发明申请
    HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF 失效
    组胺H3逆转激动剂和拮抗剂及其使用方法

    公开(公告)号：US20120022050A1

    公开(公告)日：2012-01-26

    申请号：US13249166

    申请日：2011-09-29

    申请人： Milan Chytil ,  Sharon R. Engel ,  Qun Kevin Fang ,  Kerry L. Spear

    发明人： Milan Chytil ,  Sharon R. Engel ,  Qun Kevin Fang ,  Kerry L. Spear

    IPC分类号： A61K31/551 ,  A61P25/16 ,  A61P25/28 ,  A61K31/4188 ,  A61P25/00

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

    摘要翻译： 本文提供了稠合的咪唑基化合物，合成方法及其使用方法。 本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍和代谢紊乱。 本文提供的化合物抑制组胺H3受体的活性并调节各种神经递质如组胺，乙酰胆碱，去甲肾上腺素和多巴胺（例如在突触）的释放。 本文还提供了含有化合物及其使用方法的药物制剂。

    Histamine H3 inverse agonists and antagonists and methods of use thereof
    3.
    发明授权
    Histamine H3 inverse agonists and antagonists and methods of use thereof 有权
    组胺H3反向激动剂和拮抗剂及其使用方法

    公开(公告)号：US08063032B2

    公开(公告)日：2011-11-22

    申请号：US12704460

    申请日：2010-02-11

    申请人： Milan Chytil ,  Qun Kevin Fang ,  Kerry L. Spear

    发明人： Milan Chytil ,  Qun Kevin Fang ,  Kerry L. Spear

    IPC分类号： A61K31/33 ,  A61K31/55 ,  C07D257/10 ,  C07D487/12

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

    摘要翻译： 本文提供了稠合的咪唑基化合物，合成方法及其使用方法。 本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍和代谢紊乱。 本文提供的化合物抑制组胺H3受体的活性并调节各种神经递质如组胺，乙酰胆碱，去甲肾上腺素和多巴胺（例如在突触）的释放。 本文还提供了含有化合物及其使用方法的药物制剂。

    Histamine H3 inverse agonists and antagonists and methods of use thereof
    5.
    发明授权
    Histamine H3 inverse agonists and antagonists and methods of use thereof 失效
    组胺H3反向激动剂和拮抗剂及其使用方法

    公开(公告)号：US08404670B2

    公开(公告)日：2013-03-26

    申请号：US13249166

    申请日：2011-09-29

    申请人： Milan Chytil ,  Sharon R. Engel ,  Qun Kevin Fang ,  Kerry L. Spear

    发明人： Milan Chytil ,  Sharon R. Engel ,  Qun Kevin Fang ,  Kerry L. Spear

    IPC分类号： A61K31/33 ,  A61K31/55

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

    摘要翻译： 本文提供了稠合的咪唑基化合物，合成方法及其使用方法。 本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍和代谢紊乱。 本文提供的化合物抑制组胺H3受体的活性并调节各种神经递质如组胺，乙酰胆碱，去甲肾上腺素和多巴胺（例如在突触）的释放。 本文还提供了含有化合物及其使用方法的药物制剂。

    HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF
    6.
    发明申请
    HISTAMINE H3 INVERSE AGONISTS AND ANTAGONISTS AND METHODS OF USE THEREOF 有权
    组胺H3逆转激动剂和拮抗剂及其使用方法

    公开(公告)号：US20100204214A1

    公开(公告)日：2010-08-12

    申请号：US12704460

    申请日：2010-02-11

    申请人： Milan Chytil ,  Sharon R. Engel ,  Qun Kevin Fang ,  Kerry L. Spear

    发明人： Milan Chytil ,  Sharon R. Engel ,  Qun Kevin Fang ,  Kerry L. Spear

    IPC分类号： A61K31/551 ,  C07D487/04 ,  C07D471/14 ,  A61P25/00 ,  A61P25/28 ,  A61P25/16 ,  A61P3/00 ,  A61P3/04 ,  A61P1/00

    CPC分类号： C07D487/04 ,  C07D471/14

    摘要： Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

    摘要翻译： 本文提供了稠合的咪唑基化合物，合成方法及其使用方法。 本文提供的化合物可用于治疗，预防和/或治疗各种疾病，例如神经障碍和代谢紊乱。 本文提供的化合物抑制组胺H3受体的活性并调节各种神经递质如组胺，乙酰胆碱，去甲肾上腺素和多巴胺（例如在突触）的释放。 本文还提供了含有化合物及其使用方法的药物制剂。

    FUSED HETEROCYCLES
    7.
    发明申请
    FUSED HETEROCYCLES 审中-公开
    熔融杂环

    公开(公告)号：US20100022612A1

    公开(公告)日：2010-01-28

    申请号：US12537925

    申请日：2009-08-07

    申请人： James M. Dorsey ,  Michele L. R. Heffernan ,  Qun Kevin Fang ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Cyprian O. Ogbu ,  Mustapha Soukri ,  Kerry L. Spear

    发明人： James M. Dorsey ,  Michele L. R. Heffernan ,  Qun Kevin Fang ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Cyprian O. Ogbu ,  Mustapha Soukri ,  Kerry L. Spear

    IPC分类号： A61K31/407 ,  A61P29/00

    CPC分类号： A61K31/407 ,  C07D491/04 ,  C07D495/04

    摘要： This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3 is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.

    摘要翻译： 本发明提供具有下式的稠合杂环：其中R1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R3是选自H，C1-C6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R4是选自OH和O-X +的成员，其中X +是选自有机正离子和无机阳离子的正离子。 取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。 索引n是从1到4的整数。

    Fused heterocycles
    8.
    发明授权
    Fused heterocycles 失效
    融合杂环

    公开(公告)号：US07579370B2

    公开(公告)日：2009-08-25

    申请号：US11833903

    申请日：2007-08-03

    申请人： Michele L. R. Heffernan ,  James M. Dorsey ,  Qun Kevin Fang ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Cyprian O. Ogbu ,  Mustapha Soukri ,  Kerry L. Spear

    发明人： Michele L. R. Heffernan ,  James M. Dorsey ,  Qun Kevin Fang ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Cyprian O. Ogbu ,  Mustapha Soukri ,  Kerry L. Spear

    IPC分类号： A61K31/40 ,  A61K31/34 ,  A61K31/19 ,  A01N43/38 ,  A01N43/08 ,  A01N37/00

    CPC分类号： A61K31/407 ,  C07D491/04 ,  C07D495/04

    摘要： This invention provides fused heterocycles having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.

    摘要翻译： 本发明提供具有下式的稠合杂环：其中R1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R3是选自H，C1-C6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R4是选自OH和O-X +的成员，其中X +是选自有机正离子和无机阳离子的正离子。 取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。 索引n是从1到4的整数。

    FUSED HETEROCYCLES
    9.
    发明申请
    FUSED HETEROCYCLES 审中-公开
    熔融杂环

    公开(公告)号：US20100029741A1

    公开(公告)日：2010-02-04

    申请号：US12537896

    申请日：2009-08-07

    申请人： James M. Dorsey ,  Michele L. R. Heffernan ,  Qun Kevin Fang ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Cyprian O. Ogbu ,  Mustapha Soukri ,  Kerry L. Spear

    发明人： James M. Dorsey ,  Michele L. R. Heffernan ,  Qun Kevin Fang ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Cyprian O. Ogbu ,  Mustapha Soukri ,  Kerry L. Spear

    IPC分类号： A61K31/407 ,  A61P25/00

    CPC分类号： A61K31/407 ,  C07D491/04 ,  C07D495/04

    摘要： This invention provides methods of improving cognitive function by administering to a subject a therapeutically effective amount of a fused heterocycle having the formula: in which R1 is a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R2 is a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R3 is a member selected from the group consisting of H, C1-C6 substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. R4 is a member selected from OH and O−X+, in which X+ is positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.

    摘要翻译： 本发明提供了通过向受试者施用治疗有效量的具有下式的稠合杂环来提高认知功能的方法：其中R1是选自H，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R2是选自H取代或未取代的烯基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R3是选自H，C1-C6取代或未取代的烷基，取代或未取代的芳基烷基和取代或未取代的杂芳基烷基的成员。 R4是选自OH和O-X +的成员，其中X +是选自有机正离子和无机阳离子的正离子。 取代或未取代的芳基烷基和取代或未取代的杂芳基烷基部分具有下式：其中Ar是选自取代或未取代的芳基和取代或未取代的杂芳基的成员。 索引n是从1到4的整数。