The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl; R.sup.3 is (1-4C)alkoxy; and R.sup.1 is di-\x9b(1-4C)alkyl!amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-\x9b(1-4C)alkoxy-(2-4C)alkyl!amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R.sup.1 substituents comprising a CH.sub.2 (methylene) group which is not attached to a N or O atom optionally bears on said CH.sub.2 group a hydroxy substituent; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
该发明涉及公式I的
喹唑啉衍
生物,其中n为1、2或3,每个R.sup.2独立地为卤素、三
氟甲基或(1-4C)烷基;R.sup.3为(1-4C)烷氧基;R.sup.1为二-(1-4C)烷基
氨基-(2-4C)烷氧基、
吡咯烷-1-基-(2-4C)烷氧基、
哌啶-1-基-(2-4C)烷氧基、吗啉-1-基-(2-4C)烷氧基、
哌嗪-1-基-(2-4C)烷氧基、4-(1-4C)烷基
哌嗪-1-基-(2-4C)烷氧基、
咪唑-1-基-(2-4C)烷氧基、二-(1-4C)烷氧基-(2-4C)烷基
氨基-(2-4C)烷氧基、噻吗吗啉-1-基-(2-4C)烷氧基、1-氧代噻吗吗啉-1-基-(2-4C)烷氧基或1,1-二氧代噻吗吗啉-1-基-(2-4C)烷氧基,其中上述任何R.sup.1取代基包括未连接到N或O原子的CH.sub.2(亚甲基)基,该CH.sub.2基上可选择地具有一个羟基取代基;或其药学上可接受的盐;它们的制备方法,含有它们的药物组合物,以及利用化合物的受体
酪氨酸激酶抑制性能治疗增殖性疾病如癌症。