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JAK KINASE-MODULATING QUINAZOLINE DERIVATIVES AND METHODS OF APPLYING THEREOF
专利权人:
EHMBIT BAJOSAJENSIZ KORPOREJSHN
发明人:
ABRAKhAM Sanni (US),АБРАХАМ Санни (US),ChAO Tsi (US),ЧАО Ци (US),KhADD Majkl Dzh. (US),ХАДД Майкл Дж. (US),KhOLLADEhJ Mark U. (US),ХОЛЛАДЭЙ Марк У. (US),LJu Gan (US),ЛЮ Ган (US),SETTI Ehduardo (US),СЕ,ABRAKHAM SANNI,АБРАХАМ Санни,CHAO TSI,ЧАО Ци,KHADD MAJKL DZH.,ХАДД Майкл Дж.,KHOLLADEHJ MARK U.,ХОЛЛАДЭЙ Марк У.,LJU GAN,ЛЮ Ган,SETTI EHDUARDO,СЕТТИ Эдуардо
申请号:
RU2011139321/04
公开号:
RU0002529019C2
申请日:
2010.02.26
申请国别(地区):
RU
年份:
2014
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to compounds of formula (I) , where R1 and R2 have the following values: (i) R1 and R2 together form =O; (ii) R1 and R2 together with carbon atom, which they are bound with, form duoxacycloalkyl; R1 represents hydrogen or halogen; and R2 represents halogen; (iv) R1 represents C1-6alkyl, where alkyl is optionally substituted with cyano, -RxS(O)qRv or -RxNRyRz; and R2 represents hydrogen; (v) R1 represents -OR12 or -NR13R14; and R2 represents hydrogen, deutero or phenyl, which is optionally substituted with halogen; R3 represents hydrogen, halogen, C1-6alkyl, cyano, halogen C1-6alkyl, C3-10cycloalkyl or C1-6alkoxy; R4 and R5 represent hydrogen; R6 is independently selected from halogen, C1-6alkyl, halogenC1-6alkyl, -RxOR18 and -RxS(O)qRv; R7 independently represents halogen or -RxORw; R12 is selected from hydrogen and C1-6alkyl, R13 represents hydrogen; R14 is selected from hydrogen, C3-10cycloalkyl, -C(O)Rv and -C(O)ORw; R18 represents hydrogen, C1-6alkyl, or pyperidinyl, where R18 is optionally substituted with 1-3 Q1 groups, each Q1 is independenly selected from hydroxyl, C1-6alkoxy, C1-6alkoxycarbonyl, carboxyl and morpholinyl; Rx independently represents C1-6alkylene or simple bond; Rv and Rw represent hydrogen or C1-6alkyl; Ry and Rz represent hydrogen; n has value 0-4; p has value 0-5; and each q independently has value 0, 1 or 2. Invention also relates to compounds of formula (II) , where substituents have values, given in the invention formula, to pharmaceutical composition, possessing inhibiting activity with respect to JAK kinases, containing compounds of formula (I) or (II), methods of treating JAK-modulated disease, and application of compounds of formula (I) or (II).EFFECT: compounds of formula (I) or (II) as inhibitors of JAK kinases.32 cl, 6 dwg, 2 tbl, 84 exИзобретение относится к соединениям формулы (I), где R1 и R2 имеют следующие значения: (i) R1 и R2 вместе образуют =O; (ii) R1 и R2, вместе с атомом
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