4-(phenylamino)-[1,4]dioxano[2,3-g]quinazoline Derivatives and Process for Preparing the Same

4-(페닐아미노)-[1,4]디옥사노[2,3-g]퀴나졸린 유도체 및그의 제조방법

Abstract

PURPOSE: Provided are 4-(phenylamino)-(1,4)dioxano(2,3-Q)quinazoline inhibiting the activity of tyrosine kinase which is a receptor of the epidermic growth factor and used for prevention and treatment of cancers, its pharmaceutically acceptable salts, hydrates, solvates and a preparation method thereof. The compounds. CONSTITUTION: 4-(phenylamino)-(1,4)dioxano(2,3-Q)quinazoline is represented by the formula (I) and its preparation method comprises mixing one equivalent of quinazoline derivative of the formula(II) with two equivalent of substituted aniline of the formula(III); and adding HCl then allowing them to react at 20-80 deg.C. In the above formulae, R1 is hydrogen, halogen, hydroxy, C1-6 alkyl, alkoxy, thioalkoxy, and alkoxyamino, C3-6 cycloalkyl, cycloalkoxy and thioalkoxy, (aryl or heteroaryl)oxy, thio(aryl or heteroaryl)oxy, nitro, amino, N-mono(C1-6) alkylamino, N,N-di(C1-6) alkylamino,formamido, iodo, acetiodo, hydroxyamino, hydrazino, trifluoromethyl, trifluroro- methoxy, alkenyl, alkynyl, aryl or heterocycle group; R2 and R3 are the same or different and represent -(CH2)m-R4 wherein m is 0 or 1; R4 is hydrogen, halogen, C1-6 hydroxy, C1-6 alkyl, alkoxy, thioalkoxy,and alkoxyamino, C3-6 cycloalkyl, cycloalkoxy and thioalkoxy, (aryl or heteroaryl)oxy, thio(aryl or heteroaryl)oxy, nitro, amino, N-mono(C1-6) alkylamino, N,N-di(C1-6) alkylamino,formamido, iodo, acetiodo, hydroxyamino, hydrazino, trifluoro-methyl, trifluroro methoxy, alkenyl, alkynyl, aryl or heterocycle, carboxy, alkoxycarbonyl, amido, N-monoalkyl (C1-6) amido, N,N-dialkyl(C1-6)amido, thioamido, N,N-dialkyl(C1-6)thioamido, guanidino, ureido, C1-6sulfaido, C1-6alkylsulfonyl, morphorino, 4-C1-6alkylpiperidino, mono(hydroxy(C1-6)alkyl)amino, mono(pyrrolidine (C1-6)alkyl)amino, di(pyrrolidine (C1-6) alkyl)amino or -N(R5)(CHR6R7), wherein R5 is hydrogen or C1-6 alkyl; R6 is (CH2)nOH, wherein n is an integer 1-4; R7 is hydrogen, C1-5 alkyl, hydroxyalkyl, thiohydroxyalkyl, phenyl C1-5 alkyl, 4-hydroxyphenyl (C1-5) alkyl or heteroaryl alkyl group; and n is 1,2 or 3.
본 발명은 표피성장인자 수용체의 티로신 키나제를 억제하는 4-(페닐아미노)-[1,4]디옥사노[2,3- g ]퀴나졸린 유도체, 그의 약학적으로 허용되는 염과 수화물, 용매화물 및 이들의 제조방법에 관한 것이다. 본 발명의 4-(페닐아미노)-[1,4]디옥사노[2,3- g ]퀴나졸린 유도체는 물에 대한 높은 용해도를 가지고, 표피성장인자 수용체의 티로신 키나제의 활성과 암세포의 성장을 억제하므로, 암과 같은 과다증식 질병의 치료에 널리 활용될 수 있을 것이다.

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