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    Fluoro-substituted inhibitors of D-amino acid oxidase
    7.
    发明授权
    Fluoro-substituted inhibitors of D-amino acid oxidase 有权
    氟取代的D-氨基酸氧化酶抑制剂

    公开(公告)号：US07884124B2

    公开(公告)日：2011-02-08

    申请号：US11772798

    申请日：2007-07-02

    申请人： Michele L. R. Heffernan ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Mustapha Soukri ,  Steven W. Jones ,  Kerry L. Spear ,  Mark A. Varney

    发明人： Michele L. R. Heffernan ,  Robert J. Foglesong ,  Seth C. Hopkins ,  Mustapha Soukri ,  Steven W. Jones ,  Kerry L. Spear ,  Mark A. Varney

    IPC分类号： A61K31/40 ,  C07D487/02 ,  C07D491/02 ,  C07D495/02 ,  C07D497/02

    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通式：其中A是NH或S.Q是选自CR1和N的成员.X和Y是独立地选自O，S，CR2，N和NH的成员。 R 1，R 2和R 4是独立地选自H和F的成员，条件是选自R 1，R 2和R 4中的至少一个是F.R 6是选自O-X +和OH的成员，其中X +是正离子，其中 是选自无机正离子和有机正离子的成员。

    Processes for the synthesis of olanzapine
    8.
    发明授权
    Processes for the synthesis of olanzapine 失效
    奥氮平合成方法

    公开(公告)号：US07863442B2

    公开(公告)日：2011-01-04

    申请号：US11976978

    申请日：2007-10-30

    申请人： Kiran Kumar Kothakonda ,  Daqing Che ,  Bhaskar Reddy Guntoori

    发明人： Kiran Kumar Kothakonda ,  Daqing Che ,  Bhaskar Reddy Guntoori

    IPC分类号： C07D495/02

    CPC分类号： C07D495/04

    摘要： There is provided a process for the preparation of olanzapine comprising: i) reacting 4-amino-2-methyl-10H-thieno-[2,3-b][1,5]benzodiazepine and N-methylpiperazine in a C1 to C4 alcoholic solvent or mixture thereof at suitable temperature and for a suitable time, ii) cooling the reaction mixture, and iii) isolating the precipitated olanzapine.

    摘要翻译： 提供了一种制备奥氮平的方法，其包括：i）使4-氨基-2-甲基-10H-噻吩并[2,3-b] [1,5]苯并二氮杂和N-甲基哌嗪在C1至C4醇中反应 溶剂或其混合物在合适的温度和合适的时间，ii）冷却反应混合物，和iii）分离沉淀的奥氮平。

    THIOPHENE DERIVATIVES AND ITS APPLICATIONS
    9.
    发明申请
    THIOPHENE DERIVATIVES AND ITS APPLICATIONS 有权
    噻吩衍生物及其应用

    公开(公告)号：US20100237771A1

    公开(公告)日：2010-09-23

    申请号：US12486307

    申请日：2009-06-17

    申请人： Shinn-Horng CHEN

    发明人： Shinn-Horng CHEN

    IPC分类号： H01J1/63 ,  C07D409/02 ,  C07D495/02

    CPC分类号： C09K11/06 ,  C07D333/08 ,  C07D333/18 ,  C07D495/04 ,  H01L51/0037 ,  H01L51/0052 ,  H01L51/0068 ,  H01L51/5012 ,  H05B33/20

    摘要： A thiophene derivative, which has a chemical structure of formula (1): wherein, X is a substituted or non-substituted C6-C20 aromatic or C1-C20 aliphatic group; R1 and R2 are independently H, a C1-C10 linear, branched, or cyclic aliphatic group, or connected with the carbon atoms of formula (1) to form a first heterocyclic ring; R3 and R4 are independently H, a C1-C10 linear, branched, or cyclic aliphatic group, or connected with the carbon atoms of formula (1) to form a second heterocyclic ring; and b is an integer ranging from 1 to 10, with a proviso that X is not when all of R1, R2, R3 and R4 are H.

    摘要翻译： 具有式（1）的化学结构的噻吩衍生物：其中X是取代或未取代的C 6 -C 20芳族或C 1 -C 20脂族基团; R1和R2独立地为H，C1-C10直链，支链或环状脂族基团，或与式（1）的碳原子连接形成第一个杂环; R3和R4独立地为H，C1-C10直链，支链或环状脂族基团，或与式（1）的碳原子连接形成第二个杂环; 并且b是1至10的整数，条件是当R 1，R 2，R 3和R 4全部为H时，X不是。