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    • 47. 发明申请
    • COMPOUNDS HAVING ACTIVITY AT NK3 RECEPTOR AND USES THEREOF IN MEDICINE
    • 在NK3受体中具有活性的化合物及其在医学中的用途
    • WO2006050991A1
    • 2006-05-18
    • PCT/EP2005/012207
    • 2005-11-10
    • SMITHKLINE BEECHAM CORPORATIONBRADLEY, Daniel MarcusPORTER, Roderick, AlanSMITH, Paul WilliamSTEAD, Rachel Elizabeth AnneVONG, Antonio, Kuok, Keong
    • BRADLEY, Daniel MarcusPORTER, Roderick, AlanSMITH, Paul WilliamSTEAD, Rachel Elizabeth AnneVONG, Antonio, Kuok, Keong
    • C07D215/52A61K31/47A61P25/18A61P25/24
    • C07D409/04C07D215/52
    • The invention also relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R 1 is phenyl or cyclohexyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; R 2 is C 1-6 alkyl or C 3-6 cycloalkyl; n is 1 or 2; R 3 is hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl; X is -(C=O)- or -SO 2 -; R 4 is C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkyl, C 1-6 haloalkoxy, amino, monoC 1-6 alkylamino or diC 1-6 alkylamino, or R 4 is heterocyclyl or carbocyclyl, either of which is optionally substituted independently by one or more halogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 alkoxy or C 1-6 haloalkoxy; R 5 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms; and y is 0, 1 or 2; wherein when y is 1 or 2, Y is a halogen atom, and wherein when y is 2 the halogen atoms may be the same or different. Also disclosed are use of the compounds in treating diseases and conditions mediated by activation of the NK 3 receptor, compositions containing the derivatives and processes for their preparation.
    • 本发明还涉及式(I)化合物,其药学上可接受的盐,溶剂合物或前药:其中R 1是苯基或环己基,其任一个任选被1,2或3个卤素 原子,其原子可以相同或不同; R 2是C 1-6烷基或C 3-6环烷基; n为1或2; R 3是氢,C 1-6烷基或C 3-6环烷基; X是 - (C = O) - 或-SO 2 - 。 R 4是C 1-6烷基,C 1-6卤代烷基,C 1-6烷氧基,C C 1-6烷氧基C 1-6烷基,C 1-6卤代烷氧基,氨基,一C 1-6烷基氨基 或二C 1-6烷基氨基或R 4是杂环基或碳环基,其中任一个可以任选被一个或多个卤素C 1-6独立地取代, C 1-6烷基,C 1-6卤代烷基,C 1-6烷氧基或C 1-6卤代烷氧基; R 5是苯基或噻吩基,其任一个任选被1,2或3个卤素原子取代; y为0,1或2; 其中当y为1或2时,Y为卤素原子,当y为2时,卤素原子可以相同或不同。 还公开了这些化合物在治疗由活化NK 3受体介导的疾病和病症中的用途,含有衍生物的组合物及其制备方法。
    • 50. 发明申请
    • GLYT1 TRANSPORTER INHIBITORS AND USES THEREOF IN TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS
    • GLYT1运输商抑制剂及其在治疗神经病学和神经病学疾病中的应用
    • WO2004113301A1
    • 2004-12-29
    • PCT/EP2004/006593
    • 2004-06-17
    • GLAXO GROUP LIMITEDBRANCH, Clive, LeslieCOULTON, StevenPORTER, Roderick, Alan
    • BRANCH, Clive, LeslieCOULTON, StevenPORTER, Roderick, Alan
    • C07D215/58
    • C07D209/08C07D209/44C07D215/58C07D217/06
    • Compounds of formula (I), salts, solvates and physiologically functional derivatives thereof are provided: formula (I) wherein R 1 and R 2 is independently selected from hydrogen, optionally substituted C 1-6 alkyl, optionally substituted C 3-6 cycloalkyl, optionally substituted aryl, optionally substituted arylC 1-4 alkyl and optionally substituted arylC 3-6 cycloalkyl, wherein R 1 and R 2 are not both hydrogen, or R 1 and R 2 , together with the nitrogen atom to which they are attached, are linked to form an optionally substituted 4-, 5-, 6- or 7-membered saturated ring, wherein one or more of the carbon atoms is optionally replaced by a heteroatom independently selected from N, O and S; R 3 is an optionally substituted group of formula (a): wherein m and n are independently 0, 1, 2 or 3 and m+n is 2, 3 or 4; each Z is independently -CH 2 -, -NH-, -O- or -S-; and each Y is independently CH or N; R 4 and R 5 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 6 cycloalkyl, optionally substituted aryl and optionally substituted arylC 1 -C 4 alkyl; and R 6 , R 7 , R 8 and R 9 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl and optionally substituted arylC 1 -C 4 alkyl, or R 6 and R 7 together form an optionally substituted C 3 -C 6 cycloalkyl group, or R 8 and R 9 together form an optionally substituted C 3 -C 6 cycloalkyl group. Methods of preparation and uses of the compounds in medicine for the treatment of a disorder mediated by GlyT1, for example schizophrenia, are also disclosed.
    • 提供式(I)化合物,其盐,溶剂化物和生理功能衍生物:式(I)其中R 1和R 2独立地选自氢,任选取代的C 1-6烷基,任选取代的C 3-6环烷基, 任选取代的芳基,任选取代的芳基C 1-4烷基和任选取代的芳基C 3-6环烷基,其中R 1和R 2不是氢或R 1和R 2都与氮原子一起 被连接以形成任选取代的4-,5-,6-或7-元饱和环,其中一个或多个碳原子任选被独立地选自N,O和S的杂原子取代; R 3是式(a)的任选取代的基团:其中m和n独立地是0,1,2或3,m + n是2,3或4; 每个Z独立地是-CH 2 - , - NH - , - O-或-S-; 并且每个Y独立地是CH或N; R 4和R 5独立地选自氢,任选取代的C 1 -C 6烷基,任选取代的C 3 -C 6环烷基,任选取代的芳基和任选取代的芳基C 1 -C 4烷基; R 6,R 7,R 8和R 9独立地选自氢,任选取代的C 1 -C 6烷基和任选取代的芳基C 1 -C 4烷基,或R 6和R 7独立地选自氢, 一起形成任选取代的C 3 -C 6环烷基,或R 8和R 9一起形成任选取代的C 3 -C 6环烷基。 还公开了用于治疗由GlyT1介导的病症(例如精神分裂症)的医药中化合物的制备和用途的方法。