发明名称 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40
摘要 The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
申请公布号 US9255073(B2) 申请公布日期 2016.02.09
申请号 US201313898950 申请日期 2013.05.21
申请人 AZIENDE CHIMICHE RIUNITE ANGELINI FRANCESCO A.C.R.A.F. S.p.A. 发明人 Guglielmotti Angelo;Furlotti Guido;Mangano Giorgina;Cazzolla Nicola
分类号 A61K31/415;A01N43/56;C07D231/56;C07D209/00;C07D231/54;C07D401/12;C07D295/088 主分类号 A61K31/415
代理机构 Oblon, McClelland, Maier & Neustadt, L.L.P. 代理人 Oblon, McClelland, Maier & Neustadt, L.L.P.
主权项 1. A method of inhibiting expression of MCP-1, CX3CR1, or p40, the method comprising; administering to a person in need thereof, an effective amount of a compound of formula (I):wherein A is a σ bond, —X1— or —X1—O—X2—, in which X1 and X2, which may be identical or different from each other, are an alkyl group having from 1 to 5 carbon atoms, optionally substituted with one or more alkyl groups having from 1 to 5 carbon; Y is H when A is a σ bond, or Y is H, —OH, or —N(R11)(R12) when A is X1— or —X1—O—X2—, in which R11 is hydrogen, an alkyl group having from 1 to 5 carbon atoms, or R11 together withR12 forms a 5- to 6-membered heterocycle,R12 is hydrogen, an alkyl group having from 1 to 5 carbon atoms, or R12 together withR11 forms a 5- to 6-membered heterocycle; R1 and R2, which may be identical or different from each other, are hydrogen or an alkyl group having from 1 to 5 carbon atoms; R3, R4 and R8, which may be identical or different from each other, are hydrogen, an alkyl group having from 1 to 5 carbon atoms, an alkoxy group having from 1 to 3 carbon atoms, a halogen atom, —OH, —N(R′)(R″), —N(R′)COR″, —CN, —CONR′R″, nitro, or trifluoromethyl; with R′ and R″, which may be identical or different from each other, being hydrogen or an alkyl group having from 1 to 5 carbon atoms; R5 is hydrogen, an alkyl group having from 1 to 5 carbon atoms, or R5 together with one from between R6 and R7 forms a ring having 5 or 6 carbon atoms; R6 and R7, which may be identical or different from each other, are hydrogen or an alkyl group having from 1 to 5 carbon atoms, or together form a group C═O, or one from between R6 and R7, together with R5, forms a ring having 5 or 6 carbon atoms, thereby inhibiting the expression of MCP-1, CX3CR1, or p40, wherein a disease treatable by said inhibition is at least one disease selected from the group consisting of a metabolic syndrome, obesity, diabetes, insulin resistance, rheumatoid arthritis, arthritis induced by viral infections, psoriatic arthritis, arthrosis, lupus nephritis, diabetic nephropathy, glomerulonephritis, polycystic kidney disease, interstitial lung disease, fibrosis, multiple sclerosis, Alzheimer's disease, HIV-associated dementia, atopic dermatitis, psoriasis, vasculitis, restenosis, atherosclerosis, myocardial infarction, angina, acute coronary disease, a complication following surgical intervention, Crohn's disease, ulcerative colitis, a coronary disorder, and lupus erythematosus.
地址 Rome IT