FUSED HETEROCYCLES
    1.
    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

    IPC分类号: A61K31/407 A61P25/00

    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。

    FUSED HETEROCYCLES
    2.
    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

    IPC分类号: A61K31/407 A61P29/00

    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
    3.
    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

    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。

    Inhibitors of D-amino acid oxidase
    5.
    发明授权
    Inhibitors of D-amino acid oxidase 有权
    D-氨基酸氧化酶抑制剂

    公开(公告)号:US07902252B2

    公开(公告)日:2011-03-08

    申请号:US12506204

    申请日:2009-07-20

    IPC分类号: A61K31/403 C07D209/02

    摘要: The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

    摘要翻译: 本发明提供D-氨基酸氧化酶酶的新型抑制剂。 本发明的化合物可用于治疗或预防疾病和/或病症,其中D-丝氨酸水平和/或其氧化产物的调节在改善症状中是有效的。 本发明还提供增强学习,记忆和/或认知的方法。 例如,本发明提供了治疗或预防与神经变性疾病如阿尔茨海默病有关的记忆丧失和/或认知丧失的方法。 本发明还提供了用于预防神经变性疾病的神经元功能特征丧失的方法。 此外,提供了用于治疗或预防神经精神疾病(例如精神分裂症)和用于治疗或预防疼痛和共济失调的方法。

    INHIBITORS OF D-AMINO ACID OXIDASE
    6.
    发明申请
    INHIBITORS OF D-AMINO ACID OXIDASE 有权
    D-氨基酸氧化酶的抑制剂

    公开(公告)号:US20100029737A1

    公开(公告)日:2010-02-04

    申请号:US12506204

    申请日:2009-07-20

    摘要: The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

    摘要翻译: 本发明提供D-氨基酸氧化酶酶的新型抑制剂。 本发明的化合物可用于治疗或预防疾病和/或病症,其中D-丝氨酸水平和/或其氧化产物的调节在改善症状中是有效的。 本发明还提供增强学习,记忆和/或认知的方法。 例如,本发明提供了治疗或预防与神经变性疾病如阿尔茨海默病有关的记忆丧失和/或认知丧失的方法。 本发明还提供了用于预防神经变性疾病的神经元功能特征丧失的方法。 此外,提供了用于治疗或预防神经精神疾病(例如精神分裂症)和用于治疗或预防疼痛和共济失调的方法。