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    N-FORMYL DERIVATIVES OF PAROXETINE
    2.
    发明授权
    N-FORMYL DERIVATIVES OF PAROXETINE 有权
    PAROXETINE的N-甲酰基衍生物

    公开(公告)号：EP1440067B1

    公开(公告)日：2004-12-22

    申请号：EP02768169.1

    申请日：2002-10-15

    申请人： Synthon B.V.

    发明人： HOORN, Hans, Jan ,  PETERS, Theodorus, Hendricus, Antonius ,  PICHA, Frantisek

    IPC分类号： C07D405/12 ,  A61P39/00

    CPC分类号： C07D405/12 ,  C07D211/22

    摘要： The invention relates to a compound or composition comprising N-formyl paroxetine of formula (1) and 0 to 99.97% of a paroxetine compound, based on the combined weight of said N­-formyl paroxetine and said paroxetine compound, to a pharmaceutical composition, for treating a selective serotonin reuptake inhibitor-treatable disease or condition, comprising an effective amount of a paroxetine agent and at least one pharmaceutically acceptable excipient, wherein said paroxetine agent comprises of an N-formyl paroxetine compound of formula (1) and optionally a paroxetine compound, and to a process for producing a paroxetine compound which comprises treating an N-formyl paroxetine compound of formula (1) with a de-formylation agent, to a compound having the formula (2), to a process for determining the stability or purity of a paroxetine substance or composition, which comprises assaying a paroxetine substance or composition for the presence of an N-formyl paroxetine compound of formula (1), and to a process assaying the quality of paroxetine, which comprises forming a production lot of paroxetine pharmaceutical solid dosage forms wherein each dosage form comprises paroxetine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable exipient; removing a sample of said paroxetine pharmaceutical solid dosage forms from said production lot; assaying said sample for the presence and/or amount of N-formyl paroxetine; and selling or releasing said production lot if said sample passes said assay with respect to the presence or amount of N-formyl paroxetine.

    摘要翻译： 本发明涉及包含式（1）的N-甲酰基帕罗西汀和0-99.97％的帕罗西汀化合物的化合物或组合物，基于所述N-甲酰基帕罗西汀和所述帕罗西汀化合物的总重量，用于药物组合物， 治疗选择性5-羟色胺再摄取抑制剂可治疗的疾病或病症，其包含有效量的帕罗西汀剂和至少一种药学上可接受的赋形剂，其中所述帕罗西汀剂包含式（1）的N-甲酰基帕罗西汀化合物和任选的帕罗西汀化合物 并且涉及生产帕罗西汀化合物的方法，该方法包括用去甲酰化试剂处理式（1）的N-甲酰基帕罗西汀化合物到具有式（2）的化合物，确定稳定性或纯度的方法 其包括测定帕罗西汀物质或组合物中是否存在式（1）的N-甲酰基帕罗西汀化合物， 并涉及测定帕罗西汀质量的方法，其包括形成生产批量的帕罗西汀药物固体剂型，其中每个剂型包含帕罗西汀或其药学上可接受的盐和至少一种药学上可接受的赋形剂; 从所述生产批次中取出所述帕罗西汀药物固体剂型的样品; 测定所述样品中N-甲酰基帕罗西汀的存在和/或量; 以及如果所述样品通过所述测定关于N-甲酰基帕罗西汀的存在或量，则销售或释放所述生产批次。

    PROCESS FOR PREPARATION OF 2-AMINO-6-(ALKYL) AMINO-4,5,6,7-TETRAHYDROBENZOTHIAZOLES
    5.
    发明公开
    PROCESS FOR PREPARATION OF 2-AMINO-6-(ALKYL) AMINO-4,5,6,7-TETRAHYDROBENZOTHIAZOLES 有权
    制备2-氨基-6-（烷基）氨基-4,5,6,7-四氢苯并噻唑的方法

    公开(公告)号：EP1318986A1

    公开(公告)日：2003-06-18

    申请号：EP01979066.6

    申请日：2001-09-14

    申请人： Synthon B.V.

    发明人： POSPISILIK, Karel ,  HOORN, Hans, Jan ,  PETERS, Theodorus, Hendricus, Antonius ,  LEMMENS, Jacobus, Maria

    IPC分类号： C07D277/82

    CPC分类号： C07D277/82 ,  C07B2200/07

    摘要： A new process to obtain pramipexole and related products is described. The process involves the reaction of new compounds of formula (6), wherein R is hydrogen or acyl group, R3 and R4 are either the same and each of them represents an alkoxy group of 1-4 carbons or they together form a C2-C5 alkylenedioxy group or an oxo-group, with an alkylamine in the presence of a reducing agent or a hydrogen gas with hydrogenation catalyst. A process to obtain new compounds of formula (6) is also described.

    摘要翻译： 描述了一种获得普拉克索及相关产品的新工艺。 该方法涉及式（6）的新化合物的反应，其中R为氢或酰基，R 3和R 4相同并且它们中的每一个表示1-4个碳的烷氧基或它们一起形成C 2 -C 5 亚烷基二氧基或氧代基与烷基胺在还原剂或氢气存在下与氢化催化剂反应。 还描述了获得新的式（6）化合物的方法。

    N-FORMYL DERIVATIVES OF PAROXETINE
    8.
    发明公开
    N-FORMYL DERIVATIVES OF PAROXETINE 有权
    帕罗西汀N-甲酰基衍生物

    公开(公告)号：EP1440067A1

    公开(公告)日：2004-07-28

    申请号：EP02768169.1

    申请日：2002-10-15

    申请人： Synthon B.V.

    发明人： HOORN, Hans, Jan ,  PETERS, Theodorus, Hendricus, Antonius ,  PICHA, Frantisek

    IPC分类号： C07D405/12 ,  A61P39/00

    CPC分类号： C07D405/12 ,  C07D211/22

    摘要： The invention relates to a compound or composition comprising N-formyl paroxetine of formula (1) and 0 to 99.97% of a paroxetine compound, based on the combined weight of said N­-formyl paroxetine and said paroxetine compound, to a pharmaceutical composition, for treating a selective serotonin reuptake inhibitor-treatable disease or condition, comprising an effective amount of a paroxetine agent and at least one pharmaceutically acceptable excipient, wherein said paroxetine agent comprises of an N-formyl paroxetine compound of formula (1) and optionally a paroxetine compound, and to a process for producing a paroxetine compound which comprises treating an N-formyl paroxetine compound of formula (1) with a de-formylation agent, to a compound having the formula (2), to a process for determining the stability or purity of a paroxetine substance or composition, which comprises assaying a paroxetine substance or composition for the presence of an N-formyl paroxetine compound of formula (1), and to a process assaying the quality of paroxetine, which comprises forming a production lot of paroxetine pharmaceutical solid dosage forms wherein each dosage form comprises paroxetine or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable exipient; removing a sample of said paroxetine pharmaceutical solid dosage forms from said production lot; assaying said sample for the presence and/or amount of N-formyl paroxetine; and selling or releasing said production lot if said sample passes said assay with respect to the presence or amount of N-formyl paroxetine.