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    FUSED HETEROCYCLES
    134.
    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

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

    Inventor： 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: A61K31/407 ,  A61P29/00

    CPC classification number: A61K31/407 ,  C07D491/04 ,  C07D495/04

    Abstract: 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.

    Abstract translation: 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。

    Pyrrole and Pyrazole DAAO Inhibitors
    135.
    发明申请
    Pyrrole and Pyrazole DAAO Inhibitors 有权
    吡咯和吡唑DAAO抑制剂

    公开(公告)号：US20100016397A1

    公开(公告)日：2010-01-21

    申请号：US12566990

    申请日：2009-09-25

    Applicant: Q. Kevin Fang ,  Seth Hopkins ,  Michele Heffernan ,  Milan Chytil

    Inventor： Q. Kevin Fang ,  Seth Hopkins ,  Michele Heffernan ,  Milan Chytil

    IPC: A61K31/415 ,  C07D231/54 ,  C07D231/14 ,  A61K31/416 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28

    CPC classification number: C07D231/56 ,  C07D207/34 ,  C07D209/42 ,  C07D209/44 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D491/04

    Abstract: Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof: wherein R1 and R2 are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5; or R1 and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group; X and Y are independently selected from O, S, NH, and (CR6R7)n; R3 is hydrogen, alkyl or M+; M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof; Z is N or CR4; R4 is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5; R5 is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl; R6 and R7 are independently selected from hydrogen and alkyl; n is an integer from 1 to 6; at least one of R1, R2 and R4 is other than hydrogen; and at least one of X and Y is (CR6R7)n. D-serine or cycloserine may be coadministered along with the compound of formula I.

    Abstract translation: 提高D-丝氨酸浓度，降低D-丝氨酸氧化毒性浓度的方法，用于增强学习，记忆和/或认知，或用于治疗精神分裂症，阿尔茨海默病，共济失调或神经性疼痛，或防止神经功能特征丧失 的神经变性疾病涉及向需要治疗的受试者施用治疗有效量的式I化合物或其药学上可接受的盐或溶剂合物：其中R 1和R 2独立地选自氢，卤素，硝基，烷基，酰基， 烷基芳基和XYR5; 或R 1和R 2一起形成5,6,7或8元取代或未取代的碳环或杂环基团; X和Y独立地选自O，S，NH和（CR 6 R 7）n; R3是氢，烷基或M +; M是铝，钙，锂，镁，钾，钠，锌离子或它们的混合物; Z是N或CR4; R4选自氢，卤素，硝基，烷基，烷基芳基和XYR5; R 5选自芳基，取代的芳基，杂芳基和取代的杂芳基; R6和R7独立地选自氢和烷基; n是1至6的整数; R 1，R 2和R 4中的至少一个不是氢; 并且X和Y中的至少一个是（CR 6 R 7）n。 D-丝氨酸或环丝氨酸可以与式I化合物共同给药。

    Dopamine-Agonist Combination Therapy For Improving Sleep Quality
    136.
    发明申请
    Dopamine-Agonist Combination Therapy For Improving Sleep Quality 有权
    多巴胺激动剂联合治疗提高睡眠质量

    公开(公告)号：US20100004251A1

    公开(公告)日：2010-01-07

    申请号：US12541686

    申请日：2009-08-14

    Applicant: Timothy J. Barberich

    Inventor： Timothy J. Barberich

    IPC: A61K31/4985 ,  A61P25/00

    CPC classification number: A61K45/06 ,  A61K31/137 ,  A61K31/425 ,  A61K31/4985 ,  A61K2300/00

    Abstract: The present invention generally relates to pharmaceutical compositions comprising a dopamine agonist and sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. The pharmaceutical compositions of the invention are useful in the treatment of restless-leg syndrome and periodic-limb-movement disorder, as well as various sleep disorders. In addition, the present invention relates to a method of treating a patient suffering from restless-leg syndrome, periodic-limb-movement disorder, a sleep abnormality, or insomnia, comprising coadministering a therapeutically effective amount of a dopamine agonist and a therapeutically effective amount of a sedative agent. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine. In a preferred embodiment, the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone. In a preferred embodiment, the dopamine agonist is optically pure (S)-didesmethylsibutramine; and the sedative agent is optically pure (S)-zopiclone or optically pure (S)—N-desmethylzopiclone.

    Abstract translation: 本发明一般涉及包含多巴胺激动剂和镇静剂的药物组合物。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明。 在优选的实施方案中，镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明; 并且镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 本发明的药物组合物可用于治疗不宁腿综合征和周期性肢体运动障碍以及各种睡眠障碍。 此外，本发明涉及治疗患有不宁腿综合征，周期性肢体运动障碍，睡眠异常或失眠的患者的方法，包括共同施用治疗有效量的多巴胺激动剂和治疗有效量 的镇静剂。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明。 在优选的实施方案中，镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。 在优选的实施方案中，多巴胺激动剂是光学纯的（S） - 二甲基甲基西布曲明; 并且镇静剂是光学纯的（S） - 佐匹克隆或光学纯的（S）-N-去甲基佐匹克隆。

    Fused heterocycles
    137.
    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

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

    Inventor： 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: A61K31/40 ,  A61K31/34 ,  A61K31/19 ,  A01N43/38 ,  A01N43/08 ,  A01N37/00

    CPC classification number: A61K31/407 ,  C07D491/04 ,  C07D495/04

    Abstract: 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.

    Abstract translation: 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。

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