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Invention Grant
US08048893B2 Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them 失效
吡唑基衍生物，该方法的制备方法和中间体作为药物产品和含有它们的药物组合物

Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them
Abstract:
The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
Abstract(Chinese):

本发明涉及式（I）的新衍生物，其中A是（C 1 -C 6）烷基，（C 3 -C 6）烯基，（C 3 -C 6）炔基，（C 3 （C 5 -C 7）氮杂双环烷基或（C 5 -C 9）氮杂双环链烯基;（C 1 -C 7）氮杂环烷基，（C 5 -C 9） A-R1使得R 1的氮和吡唑1位的氮必须分开至少两个碳原子，R3是H，卤素，OH，SH，NH2，ORc，SRc，SORa， SO 2 R a，NHCHO，NR a R b，NHC（O）R a，NHC（S）R a或NHSO 2 R a，R 4是芳基或杂芳基; 其中R 5为H，卤素，CF 3，CHF 2，CH 2 F，直链或支链（C 1 -C 6）烷基或（C 3 -C 7）环烷基，与其外消旋体，对映异构体和非对映异构体及其混合物，其互变异构体及其药学上可接受的 盐。

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