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    FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE
    1.
    发明申请
    FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE 有权
    D-氨基酸氧化酶的荧光取代抑制剂

    公开(公告)号：US20080004327A1

    公开(公告)日：2008-01-03

    申请号：US11772798

    申请日：2007-07-02

    申请人： Michele Heffernan ,  Robert Foglesong ,  Seth Hopkins ,  Mustapha Soukri ,  Steven Jones ,  Kerry Spear ,  Mark Varney

    发明人： Michele Heffernan ,  Robert Foglesong ,  Seth Hopkins ,  Mustapha Soukri ,  Steven Jones ,  Kerry Spear ,  Mark Varney

    IPC分类号： A61K31/407 ,  C07D491/02

    CPC分类号： C07D495/04 ,  C07D491/04

    摘要： This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O−X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.

    摘要翻译： 本发明提供了D-氨基酸氧化酶酶的新型抑制剂以及包含本发明化合物的药物组合物。 本发明还提供了治疗和预防神经系统疾病如神经精神和神经退行性疾病以及疼痛，共济失调和惊厥的方法。 本发明的化合物具有以下一般结构：其中A是NH或S.Q是选自CR 1和N的成员.X和Y是独立地选自O，S，CR < > 2，N和NH。 R 1，R 2和R 4都是独立地选自H和F的成员，条件是选自R 1，R 2， R 1，R 2，R 4和R 4是F.R 6是选自O - >其中X + +为​​正离子，其为选自无机正离子和有机正离子的成员。

    FUSED HETEROCYCLES
    3.
    发明申请
    FUSED HETEROCYCLES 失效
    熔融杂环

    公开(公告)号：US20080004328A1

    公开(公告)日：2008-01-03

    申请号：US11833903

    申请日：2007-08-03

    申请人： James Dorsey ,  Michele Heffernan ,  Qun Fang ,  Robert Foglesong ,  Seth Hopkins ,  Cyprian Ogbu ,  Mustapha Soukri ,  Kerry Spear

    发明人： James Dorsey ,  Michele Heffernan ,  Qun Fang ,  Robert Foglesong ,  Seth Hopkins ,  Cyprian Ogbu ,  Mustapha Soukri ,  Kerry Spear

    IPC分类号： A61K31/407

    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R 1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。 R 2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。 R 3是选自H，C 1 -C 6取代或未取代的烷基，取代或未取代的芳基烷基和取代的 或未取代的杂芳基烷基。 R 4是选自OH和O - O + X +的成员，其中X + +是正离子，其中 是选自有机正离子和无机阳离子的成员。 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。