首页> 外国专利> No Binding to peptidilicos inhibitors of vla-4 dependent cells useful in the treatment of autoimmune and inflammatory diseases, respiratory

No Binding to peptidilicos inhibitors of vla-4 dependent cells useful in the treatment of autoimmune and inflammatory diseases, respiratory

机译:没有与可用于治疗自身免疫和炎性疾病,呼吸道疾病的vla-4依赖性细胞的肽酶抑制剂结合

摘要

Structure refers to non Peptide compounds of formula (1.0.0), a is aryl, heteroaryl, a1nhconha2, a1nhcooa2, among others; A1 and A2 are h, aryl, heteroaryl, heterocycle; b is a Group (1.1.(2) 1.1.6), among others; and it is a Link, or CH = CH, A1A is cr1r1a; when H is a monovalent Substituent R1 and R1 when A1A is a Link, is a divalent Substituent; X is o, S (0) Q, and is nr14; SO2, co, CS,CHRA; M is 0 - 2; n is 1 - 2, p is 1 - 2; Q is 0 - 2; R is tetrazolilo, CO (CH2) kcoor5, conhso2r5, so2nr14r15, co nhso2r6 Group (3.0.0); K is 0 - 2; R2 and R3 are h, alkyl - C1 alquenilo C2 - C6, C4, among others.A Preferred Compound is acid, 3 - [2 - (3 - methyl - 1 - {2 - [4 - (3 - o-tolyl - ureido) phenyl] - acetylamino - Butyl) - oxazole 4,5-dihydro - - 5 - yl] - propionic acid, among others.It also relates to a Pharmaceutical composition comprising Plus theophylline, sulfasalazine, aminosalicylates, Cyclosporin, Rapamycin, clofosfamida, methotrexate, interferons.Compound 1 is an inhibitor of the binding of very late antigen (4 Integrin vla-4 Integrin), of leukocytes (o4u00df1) (cd49d / CD29) to proteins and cell adhesion molecule-1 (vcam-1)The Domain hepii / IIICS region (s-1) of Fibronectin and osteopontin, inhibit cell adhesion by what may be useful in the treatment of autoimmune and inflammatory diseases, respiratory
机译:结构是指式(1.0.0)的非肽化合物,a是芳基,杂芳基,a1hhconha2,a1nhcooa2等; A1和A2为h,芳基,杂芳基,杂环; b是一个群组(1.1。(2)1.1.6)等;并且它是一个链接,或CH = CH,A1A是cr1r1a;当H是一价取代基时,R1和R1,当A1A是连接基时,是二价取代基; X为o,S(0)Q为nr14; SO2,co,CS,CHRA; M是0-2; n是1-2,p是1-2; Q是0-2; R为四唑基,CO(CH2)kcoor5,conhso2r5,so2nr14r15,co nhso2r6基团(3.0.0); K为0-2; R 2和R 3是h,烷基-C 1烷基C 2 -C 6,C 4等。优选的化合物是酸3- [2-(3-甲基-1- {2--4-(3-邻甲苯基-脲基)苯基]-乙酰氨基-丁基)-恶唑4,5-二氢--5-酰基]-丙酸等。它还涉及药物组合物,其包含茶碱,柳氮磺吡啶,氨基水杨酸酯,环孢菌素,雷帕霉素,氯氟沙星,甲氨蝶呤干扰素。化合物1是白细胞(o4 u00df1)(cd49d / CD29)的极晚期抗原(4 Integrin vla-4 Integrin)与蛋白质和细胞粘附分子-1(vcam-1)结合的抑制剂。纤连蛋白和骨桥蛋白的Hepii // IIICS域(s-1)可以通过治疗自身免疫和炎性疾病,呼吸道疾病来抑制细胞粘附

著录项

  • 公开/公告号PE07622000A1

    专利类型

  • 公开/公告日2000-08-24

    原文格式PDF

  • 申请/专利权人 PFIZER PRODUCTS INC.;

    申请/专利号PE19990000583

  • 申请日1999-06-25

  • 分类号C07D241/08;A61K31/41;A61K31/495;C07D261/04;C07D261/08;C07D263/10;C07D263/32;C07D405/06;C07D413/12;

  • 国家 PE

  • 入库时间 2022-08-22 01:55:25

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