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    MONOFLUOROALKYL DERIVATIVES
    9.
    发明公开
    MONOFLUOROALKYL DERIVATIVES 有权
    单氟衍生物

    公开(公告)号：EP1183232A2

    公开(公告)日：2002-03-06

    申请号：EP00923110.1

    申请日：2000-04-17

    申请人： ELI LILLY AND COMPANY

    发明人： BENDER, David, Michael ,  CANTRELL, Buddy, Eugene ,  FRAY, Andrew, Hendley ,  JONES, Winton, Dennis ,  MILLER, William, David ,  MITCHELL, David ,  SIMON, Richard, Lee ,  ZARRINMAYEH, Hamideh ,  ZIMMERMAN, Dennis, Michael

    IPC分类号： C07C311/03 ,  C07C311/04 ,  C07C311/06 ,  C07C311/05 ,  C07C311/08 ,  C07D333/20 ,  C07D213/81 ,  C07D213/82 ,  C07C311/37 ,  A61K31/18 ,  A61K31/44 ,  A61K31/38

    CPC分类号： C07D213/81 ,  C07C307/06 ,  C07C311/03 ,  C07C311/04 ,  C07C311/05 ,  C07C311/06 ,  C07C311/08 ,  C07C311/39 ,  C07D209/34 ,  C07D213/38 ,  C07D213/61 ,  C07D213/82 ,  C07D261/18 ,  C07D295/192 ,  C07D333/20 ,  C07D333/38

    摘要： The present invention provides monofluoroalkyl derivatives of the formula (I) wherein: A represents SO2, CO2 or CONH; Ra represents (1-6C)alkyl, (2-6C)alkenyl, -(1-4C)alkyl(3-8C)cycloalkyl, or (1-4C)alkylaromatic; Rb represents H, (1-6C)alkyl, (2-6C)alkenyl, -(1-4C)alkyl(3-8C)cycloalkyl, or (1-4C)alkylaromatic; or R?a and Rb¿ together with the carbon atoms to which they are attached form a (3-8C) saturated carbocyclic ring, a (3-8C) saturated carbocyclic ring containing a heteroatom selected from the group consisting of sulfur or oxygen, or a (5-8C) carbocyclic ring containing one double bond; R1 represents an unsubstituted or substituted aromatic group, an unsubstituted or substituted heteroaromatic group, or an unsubstituted or substituted (5-8C)cycloalkyl group; R2 represents (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)fluoroalkyl, (1-6C)chloroalkyl, (2-6C)alkenyl, (1-4C)alkoxy(1-4C)alkyl, phenyl which is unsubstituted or substituted by halogen, (1-4C)alkyl or (1-4C)alkoxy, or when A represents SO¿2?, a group of formula R?3R4¿N in which R?3 and R4¿ each independently represents (1-4C)alkyl or , together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, morpholino, piperazinyl, hexahydroazepinyl or octahydroazocinyl group; or a pharmaceutically acceptable salt thereof, useful for potentiating glutamate receptor function in a mammal and thereof, useful for treating a wide variety of condutions, such as psychiatric and neurological disorder.

    摘要翻译： 本发明提供了式（I）的单氟烷基衍生物，其中：A代表SO 2，CO 2或CONH; Ra代表（1-6C）烷基，（2-6C）链烯基， - （1-4C）烷基（3-8C）环烷基或（1-4C）烷基芳香族基团; Rb代表H，（1-6C）烷基，（2-6C）烯基， - （1-4C）烷基（3-8C）环烷基或（1-4C）烷基芳族; 或R'a和Rb'与它们所连接的碳原子一起形成（3-8C）饱和碳环，含有选自硫或氧的杂原子的（3-8C）饱和碳环， 或含有一个双键的（5-8C）碳环; R1表示未取代或取代的芳族基团，未取代或取代的杂芳族基团或未取代或取代的（5-8C）环烷基; （1-6C）烷基，（3-6C）环烷基，（1-6C）氟烷基，（1-6C）氯烷基，（2-6C）烯基，（1-4C）烷氧基（1-4C）烷基， （1-4C）烷基或（1-4C）烷氧基取代的苯基，或当A代表SO 2 2时，式R 3 R 4 N的基团，其中R 3和R 4各自是 （1-4C）烷基或与它们所连接的氮原子一起形成氮杂环丁烷基，吡咯烷基，哌啶基，吗啉代，哌嗪基，六氢氮杂基或八氢吖辛因基; 或其药学上可接受的盐，用于增强哺乳动物及其哺乳动物中的谷氨酸受体功能，可用于治疗多种途径，如精神病和神经紊乱。