首页> 外国专利> ANALOGUES OF QUINAZOLINE AS INHIBITORS OF RECEPTOR TYROSINE KINASES

ANALOGUES OF QUINAZOLINE AS INHIBITORS OF RECEPTOR TYROSINE KINASES

机译:喹唑啉类似物作为受体酪氨酸激酶抑制剂

摘要

FIELD: medicine.;SUBSTANCE: invention offers analogues of quinazoline of the formula I ;where A is bound at least with one of atoms of carbon in position 6 or 7 of the dicyclic ring; X represents N. A represents the group Q or Z including tautomeric group Z form where Q and Z, have the formulas resulted more low in which symbols and radicals, have the value specified in item 1 of the formula of the invention. R1 represents phenyl, substituted -(G)nOAr or -O(G)nAr and where phenyl is unessentially replaced by halogen or C1-C10alkyl; where G represents C1-C4alkylene, n is peer 0 or 1. And Ar represents phenyl either pyridyl or thiazolyl where Ar is unessentially substituted by 1-2 substituents chosen from halogen or C1-C10alkyl; R2 and R3 represent N. The bonds of the formula I are inhibitors of the receptor tyrosine kinases of type 1. The invention includes also a way of treatment of hyperproliferative diseases, such as a cancer, application of bonds of the formula 1 in manufacture of medical products and pharmaceutical composition on the basis of these bonds.;EFFECT: rising of efficiency of a composition and the method of treatment.;14 cl, 6 dwg, 63 ex
机译:领域:医学。;物质:发明提供式I的喹唑啉类似物。<图像文件=“ 00000004.GIF” he =“ 39” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 47” />;其中A在二环的6或7位上至少与一个碳原子键合; X代表N。A代表组Q <图像文件=“ 00000005.GIF” he =“ 31” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 53” />或Z <图像文件=“ 00000006.GIF “ he =” 34“ imgContent =” undefined“ imgFormat =” GIF“ wi =” 41“ />,包括互变异构基团Z形式,其中Q和Z导致公式的结果偏低,其中符号和部首具有在中指定的值本发明式的第1项。 R 1 代表被取代的-(G) n OAr或-O(G) n Ar所取代的苯基,其中苯基基本上被卤素或C 1 -C 10 烷基;其中G表示C 1 -C 4 亚烷基,n为对等体0或1。Ar表示吡啶基或噻唑基的苯基,其中Ar基本上被所选的1-2个取代基取代来自卤素或C 1 -C 10 烷基; R 2 和R 3 代表N。式I的键是1型受体酪氨酸激酶的抑制剂。本发明还包括一种治疗过度增殖性疾病的方法。 ;例如癌症,在这些键的基础上将式1的键应用于医疗产品和药物组合物的制造中;效果:提高组合物的效率和治疗方法。14cl,6 dwg, 63前

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