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    • 3. 发明申请
    • 1,3-DIHYDROINDOL-2-ONE DERIVATIVES SUBSTITUTED IN POSITION 3 BY A NITROGEN GROUP AS VASOPRESSIN AND/OR OCYTOCINE AGONISTS AND/OR ANTAGONISTS
    • 由氮素组和/或OCYTOCINE激动剂和/或拮抗剂组成的氮基团取代的位置3中的1,3-二氢吲哚-2-酮衍生物
    • WO1995018105A1
    • 1995-07-06
    • PCT/FR1994001528
    • 1994-12-23
    • SANOFIWAGNON, JeanTONNERRE, BernardDI MALTA, AlainROUX, RichardAMIEL, Marie-SophieSERRADEIL-LEGAL, Claudine
    • SANOFI
    • C07D209/40
    • C07D401/04C07D209/34C07D209/38C07D209/40C07D401/12C07D401/14C07D405/12C07D409/12Y02P20/55
    • Compounds of formula (I), wherein R1 and R2 are each independently hydrogen, halogen, (C1-C7)alkyl, (C1-C7)alkoxy, trifluoromethyl; R3 is (C1-C7)alkyl, (C3-C7)cycloalkyl; cyclohexyl, cyclohexylmethyl, phenyl, benzyl; R4 is azido, a 2,2-dimethylhydrazino group; (C1-C7)alkylsulfonamido; phenylsulfonamido, dimethylaminosulfonamido, a NR7R8 group; a NR9R10 group; a NR9R11 group; a R12 heterocyclic radical, piperazin-1-yl; a lactoylamino group, a mandeloylamino group; a N'-(1-phenylethyl)ureido group; a N'-(1-naphth-1-ylethyl)ureido group; R5 is hydrogen or one of the values assigned to R6; R6 is halogen; (C1-C7)alkyl, trifluoromethyl, cyano, aminomethyl, nitro, an NR9R11 group; a heterocyclic radical selected from pyrrol-1-yl, DELTA 3-pyrrolin-1-yl, pyrrolidin-1-yl, morpholin-4-yl; an OR13 group; a SR13 group; guanidino, formyl, (C1-C7)alkylcarbonyl, carbamoyl; thiocarbamoyl, sulfamoyl, carboxy, (C1-C7)alkoxycarbonyl; phenoxycarbonyl, benzyloxycarbonyl, (C1-C7)alkylsulfonamido, phenylsulfonamido, dimethylaminosulfonamido, 2-(4methylphenyl)benzamido; or R5 and R6 together with the phenyl to which they are attached form a group (a); provided that X is -SO2-; X is SO2; CH2. The compounds of the invention have an affinity for vasopressin and/or ocytocine receptors.
    • 式(I)化合物,其中R 1和R 2各自独立地为氢,卤素,(C 1 -C 7)烷基,(C 1 -C 7)烷氧基,三氟甲基; R3是(C1-C7)烷基,(C3-C7)环烷基; 环己基,环己基甲基,苯基,苄基; R4是叠氮基,2,2-二甲基肼基; (C1-C7)烷基磺酰氨基; 苯基磺酰胺基,二甲基氨基磺酰氨基,NR7R8基团; NR9R10组; NR9R11组; R12杂环基,哌嗪-1-基; 乳酰氨基,戊二酰氨基; N' - (1-苯基乙基)脲基; N' - (1-萘-1-基乙基)脲基; R5是氢或分配给R6的值之一; R6是卤素; (C 1 -C 7)烷基,三氟甲基,氰基,氨基甲基,硝基,NR 9 R 11基团; 选自吡咯-1-基,DELTA 3-吡咯啉-1-基,吡咯烷-1-基,吗啉-4-基的杂环基; 一个OR13组; SR13组; 胍基,甲酰基,(C 1 -C 7)烷基羰基,氨基甲酰基; 硫代氨基甲酰基,氨磺酰基,羧基,(C 1 -C 7)烷氧基羰基; 苯氧基羰基,苄氧基羰基,(C1-C7)烷基磺酰氨基,苯基磺酰氨基,二甲基氨基磺酰胺基,2-(4-甲基苯基)苯甲酰氨基; 或R 5和R 6与它们所连接的苯基一起形成基团(a); 条件是X是-SO 2 - ; X是SO2; CH2。 本发明的化合物对加压素和/或卵母细胞受体具有亲和力。