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Aminotiofeno compound and its use for the preparation of a Pharmaceutical composition

机译:氨基噻吩化合物及其在制备药物组合物中的用途

摘要

A compound of Aminotiofeno has the following formula (1): in which R1 represents nr4r5; R2 represents CONH2 or so2nh2; R3 represents Three substituents selected from the group formed by c1-4 alkyl, halogen, NF3, or alkyl alkyl -, S -, CN; Cho, SO2 and NO2 - alkyl; R4 represents H OR C1-2 alkyl; R5 represents C (=) nhr6, cor7 or R6 represents; or,S or N; R6 represents H or alkyl c1-2 alkyl; R7 represents C1 - 2; l is a Linking Group D - e - D where D represents a link or a c1-4 alkyl; e represents - C = C (g) - (i), with, nhco, COO, n o, S, or S, and G and R independently represent H or alkyl c1-2; or a Pharmaceutical Salt ACE Ptable themUnder the condition of the compound of formula (1) is not [2 - (Aminocarbonyl) amino] - 5 - [(4-chlorophenyl) methyl] - 3 - tiofenocarboxamida oxi. Use of said Compound for preparing a Pharmaceutical composition to be used in the treatment of diseases with inhibitors of the phosphorylation of IKB Protein by Enzyme aminotiofenos IKK - B type.In doing so, these inhibitors block the type of aminotiofenos Pathological Activation of transcription factor NF Kb in Diseases involving excessive Activation of NF Kb.These compounds are of use in the treatment of inflammatory disorders and separation of tissues, particularly rheumatoid arthritis, Asthma, chronic obstructive pulmonary disease, Osteoarthritis, autoimmune diseases, rejection of Tissue and Organs, Alzheimer's disease, resteno SIS, Diabetes and glomerulonephritis.
机译:氨基噻吩化合物具有下式(1):其中R1代表nr4r5; R2代表CONH2或so2nh2; R 3代表选自C 1-4烷基,卤素,NF 3或烷基烷基-,S-,CN形成的组中的三个取代基; Cho,SO 2和NO 2-烷基; R4代表H或C1-2烷基; R5代表C(=)nhr6,cor7或R6代表;或,S或N; R6代表H或烷基的C1-2烷基; R7代表C1-2; l为连接基团D-e-D,其中D表示连接基或c1-4烷基; e代表-C = C(g)-(i),其中nhco,COO,no,S或S,G和R独立地代表H或烷基c1-2;或在式(1)化合物的条件下可药用的盐ACE化合物不是[2--(氨基羰基)氨基]-5-[(4-氯苯基)甲基]-3-tiofenocarboxamida oxi。所述化合物在制备药物组合物中的用途,所述药物组合物用于通过酶INK-B型抑制IKB蛋白磷酸化的抑制剂来治疗疾病。在此过程中,这些抑制剂阻断了氨基噻吩的类型转录因子NF的病理激活涉及NF Kb过度活化的疾病中的Kb这些化合物可用于治疗炎症性疾病和组织分离,尤其是类风湿性关节炎,哮喘,慢性阻塞性肺疾病,骨关节炎,自身免疫性疾病,组织和器官排斥,阿尔茨海默氏病,resteno SIS,糖尿病和肾小球肾炎。

著录项

  • 公开/公告号AR040145A1

    专利类型

  • 公开/公告日2005-03-16

    原文格式PDF

  • 申请/专利权人 SMITHKLINE BEECHAM CORPORATION;

    申请/专利号AR2003P101991

  • 发明设计人

    申请日2003-06-04

  • 分类号C07D333/36;A61K31/381;A61P17/00;A61P19/02;A61P19/10;A61P37/00;

  • 国家 AR

  • 入库时间 2022-08-21 22:18:53

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