首页> 外国专利> Compounds that are agonists of alpha2 - 1 receptor agonists preferably alpha 1a / l

Compounds that are agonists of alpha2 - 1 receptor agonists preferably alpha 1a / l

机译:作为α2-1受体激动剂的激动剂的化合物优选为α1a/ l

摘要

1. Claim 1: compound (1) of general formula,a. X is - S (o) n-O-C (o);A is C1-6alkyl, aryl heteroaryl, hydroxyC1-6alkyl, or - (CH2) p-NRaRb; R1, R2, R3 and R4 are each independently selected from the group consisting of H, halogen, halogen C1-6alkyl, C1-6alkyl, hydroxy, C1-6alkoxy, C1-6alkylthio, (C1-6alkyl ) sulfinyl, (C1-6) alkyl sulfonyl, (C1-6 alkyl) sulfonylamino, (C1-6) alkyl aminosulfonyl, cyano, nitro, -NRaRb, phenyl, benzyl and benzyloxy, where said phenyl rings are optionally substituted by C1-alkyl -6, halogen, cyano, nitro, halogen C1-6alkyl or C1-6 alkoxy; R5 is H, C1-6alkyl, C1-6alkoxy, C1-6alkoxyalkyl, C1-6alkylthio, C1-6alkyl sulfinyl, (C1-6alkyl) sulfonyl, hydroxyC1-6alkyl,C1-6 hydroxy methanol, halogen, C1-6 halogen, C1-6, cyanogen, nrarb, NRC,(C1-6) alkylene -NRaRb, or R5 and A together form a C2-3 alkylene radical; R6 is H or C1-6 alkyl; R 'and R' 'each independently is H or C1-6 alkyl; Ra, Rb, and Rc are each independently selected from the group consisting of H, C1-6alkyl, hydroxyC1-6alkyl, C2-6alkenyl, cycloalkyl (C3-6 )alkyl (C1-6), and arylsulfonyl, or Ra and Rb together with the N to which they are attached may also form a 5- to 7-membered non-aromatic heterocyclic ring, optionally incorporating an additional heteroatom in the ring, selected from N, O, or S; m is 1 or 2; n is 0, 1, or 2 with the proviso that when n is 0, R5 is not -NRaRb; and p is 0, 1, or 2;Or a mixture of an individual isomer, an racemic isomer and a non racemic isomer, a predicted isomer, or a pharmaceutically acceptable salt or solution of these isomers.
机译:1.权利要求1:通式a的化合物(1)。 X为-S(o)n-O-C(o); A为C1-6烷基,芳基杂芳基,羟基C1-6烷基或-(CH2)p-NRaRb; R1,R2,R3和R4各自独立地选自H,卤素,卤素C 1-6烷基,C 1-6烷基,羟基,C 1-6烷氧基,C 1-6烷硫基,(C 1-6烷基)亚磺酰基,(C 1-6) )烷基磺酰基,(C 1-6烷基)磺酰基氨基,(C 1-6)烷基氨基磺酰基,氰基,硝基,-NR aRb,苯基,苄基和苄氧基,其中所述苯环任选地被C 1-烷基-6,卤素,氰基取代,硝基,卤素C 1-6烷基或C 1-6烷氧基; R5为H,C1-6烷基,C1-6烷氧基,C1-6烷氧基烷基,C1-6烷硫基,C1-6烷基亚磺酰基,(C1-6烷基)磺酰基,羟基C1-6烷基,C1-6羟基甲醇,卤素,C1-6卤素,C1 -6,氰,nrarb,NRC,(C1-6)亚烷基-NRaRb或R5和A一起形成C2-3亚烷基。 R6是H或C1-6烷基; R'和R''各自独立地为H或C1-6烷基; Ra,Rb和Rc各自独立地选自由H,C1-6烷基,羟基C1-6烷基,C2-6烯基,环烷基(C3-6)烷基(C1-6)和芳基磺酰基组成的组,或Ra和Rb一起它们所连接的N还可以形成5至7元的非芳族杂环,任选地在环中结合选自N,O或S的另外的杂原子; m为1或2; n为0、1或2,条件是当n为0时,R5不是-NRaRb; p为0、1或2;或单个异构体,外消旋异构体和非外消旋异构体的混合物,预测的异构体或这些异构体的可药用盐或溶液。

著录项

  • 公开/公告号AR038341A1

    专利类型

  • 公开/公告日2005-01-12

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN -LA ROCHE AG.;

    申请/专利号AR2003P100287

  • 申请日2003-01-31

  • 分类号C07D403/06;C07D403/14;C07D413/14;C07D495/04;A61K31/403;A61K31/4178;A61K31/495;A61P3/04;A61P11/02;A61P13/00;A61P15/10;A61P25/22;A61P25/24;A61P25/28;A61P27/16;C07D403/06;C07D209/30;C07D233/06;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:54

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