MONOFLUOROALKYL DERIVATIVES
    16.
    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

    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。