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    • 52. 发明授权
    • Intermediates for the preparation of substituted 1,2,3,4-tetrahydronaphthalene derivatives
    • 用于制备取代的1,2,3,4-四氢萘衍生物的中间体
    • US06534652B2
    • 2003-03-18
    • US09902123
    • 2001-07-10
    • Stefan BergSvante RossSeth-Olov Thorberg
    • Stefan BergSvante RossSeth-Olov Thorberg
    • C07D26530
    • C07D295/192C07C237/24C07C2602/10C07D295/135C07D295/155C07D295/205
    • The present invention relates to new piperidyl- or piperazinyl-substituted-1,2,3,4-tetrahydronaphthalene derivatives having the formula I wherein X is N or CH; Y is NR2CH2, CH2—NR2, NR2—CO, CO—NR2 or NR2SO2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted n is 0-4; R9 is C1-C6 alkyl, C3-C6 cycloalkyl OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined above, as (R)- enantiomers, (S)-enantiomers or racemates in the form of a free base or pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.
    • 本发明涉及具有式I的新的哌啶基或哌嗪基取代的-1,2,3,4-四氢萘衍生物,其中X是N或CH; Y是NR2CH2,CH2-NR2,NR2-CO,CO-NR2或NR2SO2,其中 R2是H或C1-C6烷基; R1是H,C1-C6烷基或C3-C6环烷基; R3是C1-C6烷基,C3-C6环烷基或(CH2)n-芳基,其中芳基是苯基或杂芳环 含有一个或两个选自N,O和S的杂原子,其可以是单取代或二取代的是0-4; R9是C1-C6烷基,C3-C6环烷基OCF3,OCHF2,OCH2F,卤素,CN,CF3, OH,C1-C6烷氧基,C1-C6烷氧基-C1-C6烷基,NR6R7,SO3CH3,SO3CF3,SO2NR6R7,含有一个或两个选自N和O的杂原子的未取代或取代的杂环或杂芳环, 是(C 1 -C 6)烷基; 或COR8; 其中R6,R7和R8如上定义,为游离碱形式的(R) - 对映异构体,(S) - 对映异构体或外消旋物或其药学上可接受的盐,其制备方法,含有所述治疗活性的药物组合物 化合物和所述活性化合物在治疗中的用途。