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SUBSTITUTED DIALKYL (OXIDE)-Λ4-SULFANILIDENE NICOTINAMIDE DERIVATIVES AS KINASE INHIBITORS
专利权人:
INK.;ALLERGAN
发明人:
BORAL Sugato (US),БОРАЛ Сугато (US),VONG Shimiao (US),ВОНГ Шимиао (US),MALOUN Tomas (US),МАЛОУН Томас (US),VURSTER Dzhuli (US),ВУРСТЕР Джули (US),SHEN Tsze (US),ШЭНЬ Цзе (US),ROBINSON Majkl (US),РОБИН
申请号:
RU2016127377
公开号:
RU0002711749C2
申请日:
2014.12.10
申请国别(地区):
RU
年份:
2020
代理人:
摘要:
FIELD: medicine; pharmaceuticals.SUBSTANCE: invention relates to a compound of formula Ior a pharmaceutically acceptable salt thereof, where Z isor ,where X is absent, or X is selected from a group consisting of NH and CH2; R is selected from a group consisting of hydrogen, amino and lower alkyl, R1 is selected from a group consisting of hydrogen and halogen, R2 is hydrogen, R3 and R4 are independently selected from a group consisting of hydrogen, C1-C8 alkyl, (CR5R6)aC(O)OR7, (CR5R6)aOR7, (CR5R6)aC(O)N(R7)2, (CR5R6)aN(R7)2, wherein N(R7)2 can be taken together to form 3–7-member heterocyclic ring optionally substituted with one or more R5, wherein, if one of R3 and R4 is (CR5R6)aC(O)OR7, the other can not be (CR5R6)aC(O)OR7; or R3 and R4 can be taken together with a sulfur atom to form 4–7-member heterocyclic ring optionally substituted with one or more R9, R5 is selected from a group consisting of hydrogen, hydroxy and CH2CH2OCH2CH2OH; R6 is hydrogen; R7 is selected from a group consisting of hydrogen, C1-C8 alkyl, fluorine; R9 is selected from a group consisting of hydrogen, C1-C8 alkyl; Ar1 and Ar2 are independently selected from a group consisting of, , , , , ,where R8 is selected from a group consisting of hydrogen, C1-C4 alkyl, amino, hydroxyl, alkoxy, halogen and CF3, and equals 0 or integer from 1 to 4.EFFECT: compounds are able to modulate the tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.19 cl, 10 tbl, 42 exИзобретение относится к соединению формулы Iили его фармацевтически приемлемой соли, где Z представляет собойили ,где X отсутствует, или X выбран из группы, состоящей из NH и CH2; R выбран из группы, состоящей из водорода, амино и низшего алкила, R1 выбран из группы, состоящей из водорода и галогена, R2 представляет собой водород, R3 и R4 независимо выбраны из группы, состоящей из водорода, C1-C8 алкила, (CR5R6)aC(O)OR7, (CR5R6)aOR7, (CR5R6)aC(O)N(R7)2, (CR5R6)aN(R7)2, причем N(R7)2 мог
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