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22 条记录 (耗时 0.022 秒)

    4-(Polyalkoxy phenyl)-2-pyrrolidones
    7.
    发明授权
    4-(Polyalkoxy phenyl)-2-pyrrolidones 失效
    4-（聚烷氧基苯基）-2-吡咯烷酮

    公开(公告)号：US4193926A

    公开(公告)日：1980-03-18

    申请号：US659082

    申请日：1976-02-18

    申请人： Ralph Schmiechen ,  Reinhard Horowski ,  Dieter Palenschat ,  Gert Paschelke ,  Helmut Wachtel ,  Wolfgang Kehr

    发明人： Ralph Schmiechen ,  Reinhard Horowski ,  Dieter Palenschat ,  Gert Paschelke ,  Helmut Wachtel ,  Wolfgang Kehr

    IPC分类号： C07D207/24 ,  C07D207/26 ,  C07D207/277 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D207/277 ,  C07D207/24 ,  C07D207/26

    摘要： 4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms at least one being other than methyl, a heterocyclic ring, or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl or an amino group; R' is H, alkyl, aryl or acyl; and X is O or S; possess neuropsychotropic activity. The compounds wherein X is O can be produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-amino-butyric acid or alkyl ester thereof. The pyrrolidones can be converted to the corresponding thiopyrrolidones by reaction with phosphorous pentasulfide in the presence of base.

    摘要翻译： 式（IMAGE）的4-（聚烷氧基苯基）-2-吡咯烷酮，其中R 1和R 2各自是至多18个碳原子的烃，至少一个不同于甲基，杂环或1-5个碳原子的烷基被 卤素，OH，COOH，烷氧基，烷氧基羰基或氨基; R'是H，烷基，芳基或酰基; X为O或S; 具有神经食物活性。 其中X为O的化合物可通过皂化和脱羧相应的2-吡咯烷酮-3-羧酸烷基酯或环化相应的3-苯基-4-氨基 - 丁酸或其烷基酯来制备。 吡咯烷酮可以通过在碱存在下与五硫化二磷反应而转化为相应的硫代吡咯烷酮。

    TRANSDERMAL THERAPEUTIC SYSTEM WITH TWO-PHASE RELEASE PROFILE
    10.
    发明申请
    TRANSDERMAL THERAPEUTIC SYSTEM WITH TWO-PHASE RELEASE PROFILE 审中-公开
    具有两相释放特性的超导治疗系统

    公开(公告)号：US20100143475A1

    公开(公告)日：2010-06-10

    申请号：US12311305

    申请日：2007-08-27

    申请人： Johannes Tack ,  Björn Schurad ,  Antje Müller-Schubert ,  Reinhard Horowski

    发明人： Johannes Tack ,  Björn Schurad ,  Antje Müller-Schubert ,  Reinhard Horowski

    IPC分类号： A61K31/48 ,  A61K9/00 ,  A61P25/16 ,  A61P25/14 ,  A61P25/00

    CPC分类号： A61K9/7061 ,  A61K31/48

    摘要： The present invention relates to a transdermal therapeutic system (TTS) consisting of an impermeable coating, a matrix containing an ergoline compound having the formula (I) or a physiologically compatible salt or derivative thereof, wherein R1 denotes an H atom or a halogen atom and R2 is an alkyl group having 1 to 4 carbon atoms and denotes a single or double bond, and a removable protective layer, wherein the ergoline compound or a physiologically compatible salt or derivative thereof is stabilised by an antioxidant and a basic polymer. The TTS is characterised in that the matrix contains at least one hydrocarbon having 8 to 18 carbon atoms in a straight or branched chain, which has a functional group at the end of the alkyl chain and/or Aloe Vera, so that in a first phase (0-5 hours after application) only 0-20% of the therapeutically desired steady-state plasma concentration of the ergoline compound is achieved and the therapeutically desired steady-state plasma concentration of the ergoline compound is only achieved in a second phase (5-20 hours after application).

    摘要翻译： 本发明涉及一种由不透水涂层组成的透皮治疗系统（TTS），含有式（I）的麦角灵化合物或其生理上相容的盐或衍生物的基质，其中R1表示H原子或卤素原子， R2是具有1至4个碳原子并且表示单键或双键的烷基和可除去的保护层，其中麦角灵化合物或其生理上相容的盐或其衍生物由抗氧化剂和碱性聚合物稳定。 TTS的特征在于，基质含有至少一个在直链或支链上具有8至18个碳原子的烃，其在烷基链和/或芦荟末端具有官能团，因此在第一相中 （施用后0-5小时）仅实现治疗期望的稳态血浆浓度的0〜20％的麦角灵化合物，并且仅在第二阶段（5）中实现麦角灵化合物的治疗期望的稳态血浆浓度 应用后-20小时）。