首页> 外国专利> Substituted tricyclic compounds useful as inhibitors of sPLA2 mediated release of fatty acids in mammals and the use of said compounds in the manufacture of compositions for alleviating LPathological effects of sPLA2 related diseases

Substituted tricyclic compounds useful as inhibitors of sPLA2 mediated release of fatty acids in mammals and the use of said compounds in the manufacture of compositions for alleviating LPathological effects of sPLA2 related diseases

机译:取代的三环化合物,可用作哺乳动物中sPLA2介导的脂肪酸释放的抑制剂,以及所述化合物在制备用于减轻sPLA2相关疾病的病理作用的组合物中的用途

摘要

It is recommended to use a tricyclic compound and use it to inhibit the release of fatty acids mediated by sPLA2 to treat diseases such as chemical shock. The above tricyclic compounds refer to formula (I),Where: A is phenyl opiridilo, where the nitrogen is in the position of 5, 6, 7 or 8; B or D is nitrogen, and the other is carbon; Z is cyclohexane, phenyl, pyridine, where the nitrogen is in the position of 1, 2 or 3; or a 6-ring heterocyclic ring with an heteroatom selected from the sulfur compound group. In position 1, 2 or 3, and nitration in position 1, 2, 3 or 4, line 1 is a simple or double link, R20 is selected from the group,(b) And (c),(a) Is (a) C5-20, alquenilo C5-20, C5-20, carbon-20 condensate, carbon thyroid or heterocyclic radicals, or (b) is (a) a member replaced by one or more non interfering substitutes selected independently; or (c) is (L) - R80; in (L) is an entire array of 1 to 12 atoms, 1. Choose from carbon, hydrogen, nitrogen and sulfur; in the combination of atoms in (L), choose from (I) carbide and hydrogen (II), (III) one sulfur, (I V) one oxygen, (IV) one or two nitrogen and one hydrogen, (V) carbon, one hydrogen, one sulfur, and (VI) carbon, one hydrogen and one oxygen;R80 is a group selected from (a) or (b);R21 is a non-interference substitute; R1 is - nh2-nh2-nh2-o-conh2; R2 is selected from a group consisting of - oh y-o (CH2) Tr5, wherein R5 is h-cn-nh2-conh2-conr10-nhs2r15; conhs2r15 is - C1-6 o-cf3 tar; benilo or fenilo is replaced by - CO2H or - co2-tar C1-4; and - (a group) acid,Where - (a) is an acid connector with a length of 1-7 and a t of 1-5; R3 is selected from non interfering alternatives, carbon thyroid radicals, carbon thyroid radicals and non interfering alternatives, Heteromorphic and heteromorphic radicals replaced by non interfering substitutes; or
机译:建议使用三环化合物并抑制由sPLA2介导的脂肪酸的释放,以治疗诸如化学休克等疾病。上述三环化合物是指式(Ⅰ),其中:A是苯基奥匹地洛,其中氮在5、6、7或8位; B或D为氮,另一个为碳; Z为环己烷,苯基,吡啶,其中氮位于1、2或3位;或具有选自硫化合物组的杂原子的6-环杂环。在位置1、2或3和位置1、2、3或4的硝化作用中,第1行是简单连接或双连接,R20选自(b)和(c),(a)为(a )C5-20,alquenilo C5-20,C5-20,碳20缩合物,甲状腺碳或杂环基,或(b)为(a)被一个或多个独立选择的无干扰取代基取代的成员;或(c)为(L)-R80;或在(L)中,是一个1到12个原子的整体阵列。1.从碳,氢,氮和硫中选择;在(L)中的原子的组合中,选自(I)碳化物和氢(II),(III)一种硫,(IV)一种氧,(IV)一种或两种氮和一种氢,(V)碳, 1个氢,1个硫和(VI)碳,1个氢和1个氧; R80为选自(a)或(b)的基团; R21为无干扰取代基; R1是-nh2-nh2-nh2-o-conh2; R2选自-OH-Y(CH2)Tr5,其中R5是h-cn-nh2-conh2-conr10-nhs2r15; conhs2r15是-C1-6 o-cf3焦油; benilo或fenilo被-CO2H或-co2-tar C1-4取代;和-(a)酸,其中-(a)是长度为1-7,t t为1-5的酸连接基; R 3选自非干扰性替代物,甲状腺碳自由基,甲状腺碳自由基和非干扰性替代物,被非干扰性替代物取代的亚同和杂构基团;要么

著录项

  • 公开/公告号AR018185A1

    专利类型

  • 公开/公告日2001-10-31

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号AR1999P101769

  • 发明设计人

    申请日1999-04-16

  • 分类号C07D209/82;C07D513/04;C07D471/04;C07D471/12;C07D487/04;C07D487/12;C07D491/04;C07D491/12;A61K31/40;A61K31/403;

  • 国家 AR

  • 入库时间 2022-08-22 01:26:19

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