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NEW DERIVATIVES OF CYCLE UREA, THEIR PRODUCTION AND THEIR PHARMACEUTICAL APPLICATION AS KINASE INHIBITORS

机译:循环尿素的新衍生物,其生产及其在激酶抑制剂中的应用

摘要

The invention relates to novel products having formula (I), wherein: p denotes 0 to 2; R and R1 denote O or NH; R2 and R3 denote hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, or R2 and R3, together with the carbon atom to which they are bound, form a carbocyclic or heterocyclic radical, all of said radicals being optionally substituted; A1 denotes a single bond, alkyl, allyl and propynyl; Y and Y1 denote H, OCF3, S(O)nCF3, S(O)nAlk, SO2CHF2, SO2CF2CF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, SF5 and SO2NR5R6, whereby R5 and R6 are selected from among hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl and heteroaryl, which are optionally substituted, or R5 and R6, together with N to which they are bound, form a heterocyclic radical; A2 denotes Al, CO and SO2; B2 denotes a heterocyclic radical which is optionally substituted with one or more substituents which are selected from the values of Y2; Y2 denotes hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -O-alkenyl, -O-alkynyl, O-cycloalkyl, S(O)n-alkyl, -S(O)n-alkenyl, -S(O)n-alkynyl, S(O)n-cycloalkyl, -COOR13,-OCOR13, NR5R6, CONR5R6, S(O)n-NR5R6,-NR10-CO-R13, -NR10-SO2-R13, -NH-SO2-NR5R6, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13, all of said radicals being optionally substituted; and n denotes an integer of between 0 and 2. The aforementioned products are in all the isomeric forms and the salts thereof for use as medicaments.
机译:本发明涉及具有式(I)的新颖产物,其中:p表示0至2; R和R1表示O或NH; R 2和R 3表示氢,烷基,烯基,炔基,环烷基,芳基和杂芳基,或R 2和R 3与它们所键合的碳原子一起形成碳环或杂环基,所有所述基团任选地被取代; A1表示单键,烷基,烯丙基和丙炔基; Y和Y1表示H,OCF3,S(O)nCF3,S(O)nAlk,SO2CHF2,SO2CF2CF3,-O-CF2-CHF2,-O-CHF2,-O-CH2-CF3,SF5和SO2NR5R6,其中R5和R6选自氢,烷基,烯基,环烷基,环烯基,杂环烷基,芳基和杂芳基,它们是任选取代的,或R5和R6与它们所结合的N一起形成杂环基; A 2表示Al,CO和SO 2; B 2表示杂环基,其任选地被一个或多个选自Y 2的取代基取代; Y 2表示氢,卤素,羟基,氰基,烷基,烷氧基,环烷基,杂环烷基,芳基,杂芳基,-O-烯基,-O-炔基,O-环烷基,S(O)n-烷基,-S(O)n -烯基,-S(O)n-炔基,S(O)n-环烷基,-COOR13,-OCOR13,NR5R6,CONR5R6,S(O)n-NR5R6,-NR10-CO-R13,-NR10-SO2- R13,-NH-SO2-NR5R6,-NR10-CO-NR5R6,-NR10-CS-NR5R6,-NR10-COOR13,所有所述基团是任选取代的; n为0〜2的整数。上述产物为所有异构体形式及其盐,用作药物。

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