首页> 外国专利> Bicyclic Heterocycles 4 - amino substituted quinazoline Derivatives, medicaments containing these Compounds, their use in the treatment of diseases mediated by the activity of the tirosinquinasas and tiroquinasas and processes for their Preparation

Bicyclic Heterocycles 4 - amino substituted quinazoline Derivatives, medicaments containing these Compounds, their use in the treatment of diseases mediated by the activity of the tirosinquinasas and tiroquinasas and processes for their Preparation

机译:双环杂环4-氨基取代的喹唑啉衍生物,含有这些化合物的药物,其在治疗由替罗辛喹诺酮和替罗喹诺萨斯活性介导的疾病中的用途及其制备方法

摘要

Bicyclic Heterocyclic compounds of the General formula (1), tautomeros, their stereoisomers, their mixtures and their salts, especially their physiologically tolerable salts with inorganic or organic acids, which have an inhibitory effect on the signal transduction mediated by tiroquinas As to its use for the treatment of diseases, especially tumor diseases.As well as benign Prostate hyperplasia (BPH), pulmonary and respiratory diseases, and preparation.Claim 1: bicyclic Heterocycles of General formula (1) in which a mean ra RB H Atom; a radical 3-chloro-4 - phenyl Fluorine or a 3 - etinilfenilo RC Group, a radical selected from the group consisting of 1 - Methoxycarbonyl - piperidin-4-yl ILO, 1 - etiloxicarbonil - piperidin ILO - 4 - 1 - Trifluoroacetilpiperidin - 4 - cis-4 - (ILO, metoxicarbonilamino) - ciclohex - 1 - iloTrans-4 - (metoxicarbonilamino ciclohex - 1 - yl) - cis-4 - (etiloxicarbonilamino, ciclohex - yl) - trans - 1, 4 - (etiloxicarbonilamino ciclohex - 1 - yl) - cis-4 - (trifluoracetilamino, ciclohex - 1 - yl) -, trans - 4 - (trifluoracetilamino) - ciclohex - ILO - cis - 1, 4 - (Methoxycarbonyl - N - N - methyl - amino - 1 - yl) - ciclohex, trans-4 - (N - I Xicarbonil - N - methyl - amino - 1 - yl) - ciclohex, cis-4 - (N - etiloxicarbonil - N - methyl - amino) - ciclohex - 1 - iloTrans-4 - (N - etiloxicarbonil - N - methyl - amino - 1 - yl) - ciclohex, cis-4 - (N - trifluoracetil - N - methyl - amino - 1 - yl) - ciclohex, trans-4 - (N - trifluoracetil - N - methyl - amino) - ciclohex - 1 - ILO, cis-4 - phthalimido - Ciclohex - 1 - ILO and trans - 4 - phthalimido - ciclohex - 1 - ilo; RD a H Atom, a methoxy group or 2 - metoxietiloxi ethyloxy,, Eventually in the form of tautomeros, racematos, its enantiomers.Diastereoisomers and their mixtures, and eventually by adding acid salts, solvates and hydrates pharmacologically safe.
机译:通式(1)的双环杂环化合物,互变异构体,其立体异构体,它们的混合物及其盐,尤其是它们与无机酸或有机酸的生理上可耐受的盐,它们对噻吩喹诺斯介导的信号转导具有抑制作用。权利要求1:通式(1)的双环杂环,其中平均ra RB H原子;以及良性前列腺增生(BPH),肺和呼吸系统疾病以及制备。 -3-氯-4-苯基氟基团或3--etinilfenilo RC基团,选自1-甲氧羰基-哌啶-4-基ILO,1-乙噻卡西尔-哌啶ILO-4 -1-1-三氟乙哌啶- 4-顺式4-(ILO,甲氧羰基氨基)-ciclohex-1-iloTrans-4-(甲氧羰基氨基氨氯环己酮-1-yl)-顺式4-((etiloxicarbonilaminoamino,ciclohex-yl))-反式-1,4,-(eiloxicarbilaminoamino ciclohex -1-基)-顺式4-(三氟乙酰氨基,环己基-1-基)-,反式-4-(三氟乙氨基)-环己基-ILO-顺-1,4-(甲氧羰基-N-N-甲基-氨基- 1-基)-环己基,反式4-(N-席卡西尔-N-甲基-氨基-1-基)-环己基,顺式4-(N-依托昔卡地-N-甲基-氨基)-环己基-1- iloTrans-4-(N-埃替西卡西尔-N-甲基-氨基-1-yl)-环己酮,顺式4-(N-三氟乙腈-N-甲基-氨基-1-yl)-环己酮,反式4-(N -三氟乙腈-N-甲基-氨基)-环己烷-1-ILO,顺式4 -邻苯二甲酰亚胺基-环己酮-1-ILO和反式-4-邻苯二甲酰亚胺基-环己酮-1-ilo; RD为H原子,甲氧基或2-甲氧西洛西乙氧基,最终为互变异构体,消旋体,其对映异构体,非对映异构体及其混合物,并通过添加酸盐,溶剂化物和水合物在药理上是安全的。

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