首页> 外国专利> New heterocyclically substituted aryl compounds are hypoxia-inducible factor inhibitors useful to treat and/or prevent e.g. cancer or tumor diseases, ischemic cardiovascular diseases, heart attack, arrhythmia, stroke, and psoriasis

New heterocyclically substituted aryl compounds are hypoxia-inducible factor inhibitors useful to treat and/or prevent e.g. cancer or tumor diseases, ischemic cardiovascular diseases, heart attack, arrhythmia, stroke, and psoriasis

机译:新的杂环取代的芳基化合物是可用于治疗和/或预防例如缺氧的缺氧诱导因子抑制剂。癌症或肿瘤疾病,缺血性心血管疾病,心脏病,心律不齐,中风和牛皮癣

摘要

Heterocyclically substituted aryl compounds and their salts, solvates or solvate of the salts are new. Heterocyclically substituted aryl compounds and their salts, solvates or solvate of the salts are new. Ring A : phenyl or pyridyl ring; ring B : e.g. 1H-pyrazole group, 1H-imidazole group, 1H-pyrrole group; a : connection point with the adjacent CH 2-group; aa : connection point with the ring (D); ring D : e.g. [1,2,4]oxadiazole group or [1,3,4]oxadiazole group; aaa : connection point with the ring (B); aaaa : connection point with the ring (E); ring E : phenyl or pyridyl ring; ring N : saturated 4-10-membered aza-heterocycle; X : e.g. a bond, -O- or -S-; R 1 : e.g. F, CN, (1-6C)-alkyl or OH; m : 0-4; R 2 : e.g. (1-6C)-alkyl or (1-6C)-alkylcarbonyl; n : 0 or 1; R 3 : CH 3, C 2H 5 or CF 3; R 4 : e.g. H, halo, CN, pentafluorothio or (1-6C)-alkyl; R 5 : F, Cl, CN, CH 3, CF 3 or OH; and p : 0-2. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. Independent claims are included for: (1) a medicament comprising (I) in combination with one or more inert, non-toxic auxiliary agent; and (2) the preparation of (I). [Image] ACTIVITY : Antiapoptotic; Cytostatic; Cardiant; Vasotropic; Antiarrhythmic; Cerebroprotective; Antipsoriatic; Ophthalmological; Antiinflammatory; Antiarthritic; Antirheumatic; Hemostatic; Vulnerary. MECHANISM OF ACTION : Hypoxia-inducible factor inhibitor. The ability of (I) to inhibit hypoxia-inducible factor was tested in HCT 116 cells using hypoxia-inducible factor luciferase assay. The results showed that 1-cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-yl}piperazine exhibited an IC 5 0 value of 0.6 nmole/l.
机译:杂环取代的芳基化合物及其盐,溶剂化物或盐的溶剂化物是新的。杂环取代的芳基化合物及其盐,溶剂化物或盐的溶剂化物是新的。环A:苯基或吡啶基环;环B:例如1H-吡唑基,1H-咪唑基,1H-吡咯基; a:与相邻的CH 2组的连接点; aa:与环的连接点(D); D环:例如[1,2,4]恶二唑基或[1,3,4]恶二唑基; aaa:与环的连接点(B); aaaa:与环的连接点(E); E环:苯基或吡啶基环;环N:饱和的4-10元氮杂杂环; X:例如键-O-或-S-; R 1>:例如F,CN,(1-6C)-烷基或OH; m:0-4; R 2>:例如(1-6C)-烷基或(1-6C)-烷基羰基; n:0或1; R 3>:CH 3,C 2H 5或CF 3; R 4>:例如H,卤素,CN,五氟硫基或(1-6C)-烷基; R 5>:F,Cl,CN,CH 3,CF 3或OH;并且p:0-2。完整定义在“定义(完整定义)”字段中给出。包括以下方面的独立权利要求:(1)包含(I)与一种或多种惰性,无毒助剂结合的药物; (2)制备(I)。活动:抗凋亡;细胞抑制卡迪恩变压性抗心律不整;脑保护对牛皮癣;眼科消炎(药;抗关节炎抗风湿;止血药伤药。作用机理:缺氧诱导因子抑制剂。使用低氧诱导因子荧光素酶测定法在HCT 116细胞中测试了(I)抑制低氧诱导因子的能力。结果表明1-环丙基-4- {4-[(5-甲基-3- {3- [4-(三氟甲氧基)苯基] -1,2,4-恶二唑-5-基} -1H-吡唑- 1-基)甲基]吡啶基-2-基}哌嗪的IC 5 0值为0.6 nmole / l。

著录项

  • 公开/公告号DE102009041242A1

    专利类型

  • 公开/公告日2011-12-15

    原文格式PDF

  • 申请/专利权人 BAYER SCHERING PHARMA AKTIENGESELLSCHAFT;

    申请/专利号DE20091041242

  • 发明设计人 ERFINDER WIRD SPÄTER GENANNT WERDEN;

    申请日2009-09-11

  • 分类号C07D413/14;C07D413/04;A61K31/4427;A61K31/4523;A61K31/496;A61P35;A61P9;

  • 国家 DE

  • 入库时间 2022-08-21 17:05:38

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