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Inhibitors of 11 beta hydroxysteroid dehydrogenase Type 2 diabetes - 1 - 1 - and Pharmaceutical composition

机译:11种2型糖尿病β-羟类固醇脱氢酶的抑制剂-1-和药物组合物

摘要

Claim 1: A compound of formula (I): wherein: R 1 is aryl, heteroaryl, aralkyl, heteroaralkyl, lower alkyl, lower alkoxy-benzyl, lower alkoxy-carbonyl-lower alkyl, lower haloalkyl, hydroxy-lower alkyl, alkoxy lower-lower alkyl, (CH2) s-aryl, (CH2) s-heteroaryl or (CH2) s-cycloalkyl, wherein said aryl, heteroaryl, aralkyl, heteroaralkyl (CH2) s-aryl, (CH2) s-heteroaryl or (CH2) s-cycloalkyl is substituted or unsubstituted with one or more substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, cyano, lower alkoxycarbonyl, lower haloalkyl,Phenyl - (oxo low tar) and hydroxy low tar; P is 0 or 1; s is 0, 1 or 2; R2 is phenyl, which can be replaced or replaced without hesitation by one or more substitutes selected from halogenation, hydrogen group, low halogen group, low oxygen, trifluoromethy, carbamate, low tar, nitrate and cyanogen, 2. Diphenyl, one or more substitutes selected from the group of acetyl, halogenated, low acid and low oxygen carbides, sulfonamide, lower alkyl sulfuryl, low acid and low oxygen carbides, lower halogen subunit, substituted or unsubstituted naftil which can not be replaced or substituted by diphenyl;a 5 or 6 membered monocyclic heterocycle with 1-3 atoms selected from N, O and S, which may be unsubstituted or substituted with halogen, lower alkyl, substituted or unsubstituted phenyl, or lower haloalkyl, or substituted or unsubstituted benzothiophene , as long as the following compounds are excluded: 1,7,8,8-tetramethyl-2-phenyl-1,2,4,5,6,7-hexahydro-4,7-methane-indazol-3- one, 2,7,8,8-tetramethyl-1-phenyl-1,2,4,5,6,7-hexahydro-4,7-methane-indazol-3-one, 1,7,8,8-tetramethyl- 2-Naphthalen-2-yl-1,2,4,5,6,7-hexahydro-4,7-methane-indazol-3-one, 1,7,8,8-tetramethyl-2-p-tolyl- 1,2,4,5,6,7-hexahydro-4,7-methane-indazol-3-one,2 - (4-methyl-phenyl) - 1,7,8,8-tetramethyl-1,2,4,5,6,7-hexahydro-1,2,4,5,6,7-hexahydro-4,7-methane-indazol-3-ona and 1,7,8,8-tetramethyl-2-o-methanol-1,2,4,5,6,7-hexahydro-4,7-methane-indazol-3-ona.
机译:1.式(I)的化合物:其中:R 1是芳基,杂芳基,芳烷基,杂芳烷基,低级烷基,低级烷氧基-苄基,低级烷氧基-羰基-低级烷基,低级卤代烷基,羟基-低级烷基,低级烷氧基-低级烷基,(CH2)s-芳基,(CH2)s-杂芳基或(CH2)s-环烷基,其中所述芳基,杂芳基,芳烷基,杂芳烷基(CH2)s-芳基,(CH2)s-杂芳基或)s-环烷基被一个或多个选自卤素,低级烷基,低级烷氧基,氰基,低级烷氧羰基,低级卤代烷基,苯基-(氧代低焦油)和羟基低焦油的取代基取代或未取代; P为0或1; s是0、1或2; R 2是苯基,可以不加犹豫地被一种或多种选自卤代,氢基,低卤素基团,低氧,三氟甲基,氨基甲酸酯,低焦油,硝酸盐和氰基的取代基取代或取代。2.二苯基,一种或多种取代基选自乙酰基,卤代,低酸和低碳的碳化物,磺酰胺,低级烷基硫基,低酸和低碳的碳化物,低级卤素亚基,不可被二苯基取代或取代的取代或未取代的萘啶; a 5或具有1-3个选自N,O和S的原子的6元单环杂环,只要是以下化合物,即可被卤素,低级烷基,取代或未取代的苯基或低级卤代烷基或取代或未取代的苯并噻吩取代或取代不包括:1,7,8,8-四甲基-2-苯基-1,2,4,5,6,7-六氢-4,7-甲烷-吲唑-3- 1,2,7,8,8 -四甲基-1-苯基-1,2,4,5,6,7-六氢-4,7-甲烷-吲唑-3-one,1,7,8,8-te苯甲基-2-萘-2-基1,2,4,5,6,7-六氢-4,7-甲烷-吲唑-3-one,1,7,8,8-四甲基-2-p-甲苯基1,2,4,5,6,7-六氢-4,7-甲烷-吲唑-3-one,2-(4-甲基-苯基)-1,7,8,8-四甲基-1, 2,4,5,6,7-六氢-1,2,4,5,6,7-六氢-4,7-甲烷-吲唑-3-ona和1,7,8,8-四甲基-2-邻甲醇-1,2,4,5,6,7-六氢-4,7-甲烷-吲唑-3-ona。

著录项

  • 公开/公告号AR057101A1

    专利类型

  • 公开/公告日2007-11-14

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG;

    申请/专利号AR2006P103763

  • 发明设计人

    申请日2006-08-29

  • 分类号C07D231/54;A61K31/4184;A61P3/00;

  • 国家 AR

  • 入库时间 2022-08-21 20:08:59

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