首页> 外国专利> Substituted Tricyclic Compounds, Pharmaceutical formulation which comprises,Use of said Compound for producing a Medicament used to selectively inhibit sPLA2 and alleviate Pathological effects of related diseases

Substituted Tricyclic Compounds, Pharmaceutical formulation which comprises,Use of said Compound for producing a Medicament used to selectively inhibit sPLA2 and alleviate Pathological effects of related diseases

机译:取代的三环化合物,药物制剂,包括:所述化合物在制备用于选择性抑制sPLA2和减轻相关疾病的病理作用的药物中的用途

摘要

It describes new tricyclic compounds and the use of these compounds to inhibit the release of sPLA2 induced fatty acids into treatments for diseases such as septic shock. These compounds have formula (I),Where Z is cyclohexane or phenyl, R20 is selected as a group (a),(b) And (c),Among them: (a) C 5-20, alquenilo C5-20, c-5-20 tar, c-5-20, c-thyroid or heterocyclic excimer, or (b) a member of group a replaced by one or more non interfering substitutes independently selected; or (c) a single condition group composed of 1 to 12 carbon atoms, 1. Hydrogen, oxygen, nitrogen and sulfur; select delgroup atomic combination composed of (I) carbon and hydrogen (II) sulfur (III) monooxygen (I V) one or two nitrogen and hydrogen (V) carbon, hydrogen and sulfur (VI) one carbon, hydrogen and oxygen;R80 is a group of R80 selected from (a) or (b);R21 is a non-interference substitute selected from the group consisting of - oh y-o (CH2) Tr5, wherein R5 is h, - CN, - NH2, - CONH2, - conr9r10, - nhso2r15, - conhs2r15, r15-c1-6 or - CF3, substituted by - CO2H or - co2-c1-4; and (ya) group;It is a single acid group composed of 1-7 and t-1-5 acid linkers; R3 consists of non interfering substitutes, carbon thyroid radicals, and carbon thyroid substitutes, Aperiodic and aperiodic radicals are replaced by noise substitutes; or their racemates, solutions, polymers, optically isomerized isomers, disordered derivatives or salts acceptable to drugs.
机译:它描述了新的三环化合物以及这些化合物在抑制sPLA2诱导的脂肪酸释放到诸如败血性休克等疾病的治疗中的用途。这些化合物具有式(I),其中Z为环己烷或苯基,R20选自基团(a),(b)和(c),其中:(a)C 5-20,alquenilo C5-20,c -5-20焦油,c-5-20,c-甲状腺或杂环准分子,或(b)被一个或多个独立选择的无干扰替代物取代的a组成员; (c)由1至12个碳原子组成的单一条件基团; 1.氢,氧,氮和硫;或选择由(I)碳和氢(II)硫(III)单氧(IV)之一或两个氮和氢(V)碳,氢和硫(VI)碳,氢和氧组成的delgroup原子组合; R80为R80是选自(a)或(b)的R80基团; R21是选自以下的无干扰取代基:-oh yo(CH2)Tr5,其中R5是h,-CN,-NH2,-CONH2,-conr9r10 ,-nhso2r15,-conhs2r15,r15-c1-6或-CF3,被-CO2H或-co2-c1-4取代;它是由1-7和t-1-5酸连接基组成的单一酸基。 R3由无干扰的取代基,甲状腺碳自由基和甲状腺碳取代基组成,非周期性和非周期性自由基被噪声替代所取代;或其药物的外消旋体,溶液,聚合物,光学异构体,无序衍生物或盐。

著录项

  • 公开/公告号AR018593A1

    专利类型

  • 公开/公告日2001-11-28

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号AR1999P101771

  • 发明设计人

    申请日1999-04-16

  • 分类号C07D209/82;C07D209/88;C07D209/86;A61K31/40;A61P11/00;A61P19/00;A61P25/00;

  • 国家 AR

  • 入库时间 2022-08-22 00:46:31

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