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    • 7. 发明申请
    • 5-ALKYLOXY-INDOLIN-2-ONE DERIVATIVES, PREPARATION THEREOF AND APPLICATION THEREOF IN THERAPY AS SELECTIVE LIGANDS OF V2 VASOPRESSIN RECEPTORS
    • 5-烷基-L-吲哚-2-酮衍生物,其制备方法及其在治疗中的应用作为V2 VASOPRESSIN受体的选择性配体
    • WO2008087278A3
    • 2008-09-18
    • PCT/FR2007002028
    • 2007-12-10
    • SANOFI AVENTISFOULON LOICROCHARD PIERRICKSERRADEIL-LE GAL CLAUDINEVALETTE GERARD
    • FOULON LOICROCHARD PIERRICKSERRADEIL-LE GAL CLAUDINEVALETTE GERARD
    • C07D209/34A61K31/404C07D401/12C07D403/10C07D403/12C07D487/04
    • C07D209/34C07D401/12C07D403/10C07D403/12C07D487/04
    • The invention relates to compounds of the formula (I) in which: R 0 is (C 1 -C 4 )alkyl, mono or polyfluoro-(C 1 C 4 )alkyl, cyclopropyl or -CH2- cyclopropyl, (C 2 -C 4 )alkenyl or (C 2 -C 4 )alkynyl; R 1 is H, (C 1 -C 5 )alkyl, mono or polyfluoro-(C 1 C 5 )alkyl, hydroxy-(C 2 -C 5 )alkyl, -(CH 2 )m-(C 3 -C 5 )cycloalkyl; Z 1 is H or halogen, (C 1 C 4 )alkyl, mono or polyfluoro-(C- 1 -C 4 )alkyl, (C 1 - C 4 )alkoxy, mono or PoIy[IuOrO-(C 1 -C 4 )Alkoxy, cyclopropyl or -CH 2 -yclopropyle, optionally substituted; Z 2 is a halogen atom or a T 1 W group, in which T 1 is a -(CH 2 ) n - group, and W is one or more of H, (C 1 - C 4 )alkyl, mono or polyfluoro-(C- 1 -C 4 )alkyl or cyclopropyl optionally substituted, or W is -C(O)OR 19 , or W is -C(O)NR 6 R 7 , or W is a -NR 8 C(O)R 9 group, or W is -NR 10 R 11 , or W is a -OR 12 group; R 4 is (CrC4)alkyl, mono or polyfluoro-(C 1 C 4 )alkyl, OH, (C 1 - C 4 )alkoxy, (C2-C4) alkenyl, nitro, COORCl, benzyloxy, or R 4 is - C(O)NR 13 R 14 , or R 4 is -NR 15 R 16 , or R 4 is -NR 17 C(O)R 18 ; R 3 and R 5 are H or halogen, (CrC4)alkyl, mono or polyfluoro-(CrC4)alkyl, (C 1 - C 4 )alkoxy or mono or polyfluoro-(C 1 C 4 )alkoxy; m = 0, 1 or 2; n = 0 or 1; said compounds being in their base, hydrate or solvate state, in the form of cis/trans isomers, or mixtures thereof. The invention also relates to a method for the preparation of the compounds of the formula (I) and to the use thereof in therapy.
    • 本发明涉及式(I)的化合物,其中:R 0是(C 1 -C 4 -C 4)烷基,单或多氟 - (C 1 -C 4)烷基,环丙基或-CH 2 - 环丙基,(C 2 -C 4)烷基,(C 1 -C 4) )烯基或(C 1 -C 2 -C 4)炔基; R 1是H,(C 1 -C 5)烷基,单或多氟 - (C 1 -C 1)烷基, 烷基,羟基 - (C 2 -C 5 -C 5)烷基, - (CH 2 CH 2)m - (C 3 -C 5 )环烷基; Z 1是H或卤素,(C 1 -C 4)烷基,单或多氟 - (C 1 -C 12) (C 1 -C 4)烷基,(C 1 -C 4)烷基,(C 1 -C 4)烷基,(C 1 -C 4) 烷氧基,环丙基或-CH 2 - 环丙基,任选取代的; Z 2是卤素原子或T 1 W基团,其中T 1是 - (CH 2/2) ),W是H,(C 1 -C 4)烷基,单或多氟((C 1 -C 4) 任选取代的C 1 -C 6烷基或环丙基,或W是-C(O)OR 19,或W是-C (O)NR 6 R 7或W是-NR 8 C(O)R 9基团 ,或W是-NR 10 R 11,或W是-OR 12基团; R 4是(C 1 -C 4)烷基,单或多氟 - (C 1 -C 4)C 4烷基,OH,(C 1 H 4) (C 2 -C 4)烷基,(C 2 -C 4)烯基,硝基,COORCl,苄氧基或R 4是-C(O)NR 13 R 14或R 4是-NR 15 R 16,或R 14, 4是-NR 17 C(O)R 18; R 3和R 5是H或卤素,(C 1 -C 4)烷基,单或多氟 - (C 1 -C 4)烷基,(C 1 -C 4) (C 1 -C 4)烷氧基或单或多氟 - (C 1 -C 4)烷氧基; m = 0,1或2; n = 0或1; 所述化合物是其顺式/反式异构体形式的其碱,水合物或溶剂合物状态,或其混合物。 本发明还涉及制备式(I)化合物的方法及其在治疗中的用途。