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KINASE INHIBITORS
专利权人:
Kezi Farmacheutichi S.p.A.
发明人:
VAN NIL Monik Bodil (IT),ВАН НИЛ Моник Бодил (IT),REJ Nikolas Charlz (IT),РЭЙ Николас Чарльз (IT),ALKARAZ Lilian (IT),АЛЬКАРАЗ Лилиан (IT),PANCHAL Terri Aaron (IT),ПАНЧАЛ Терри Аарон (IT),DZHENNINGS E,VAN NIL Monik Bodil,ВАН НИЛ Моник Бодил,REJ Nikolas Charlz,РЭЙ Николас Чарльз,ALKARAZ Lilian,АЛЬКАРАЗ Лилиан,PANCHAL Terri Aaron,ПАНЧАЛ Терри Аарон,DZHENNINGS Endryu Stiven Robert,ДЖЕННИНГС Эндрю Стив
申请号:
RU2014123031
公开号:
RU0002623734C2
申请日:
2012.12.05
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: pharmacology.SUBSTANCE: invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof which have an inhibitory activity against p38 MAP kinase. In formula (I), W is NH, Y is selected from the -O (CR3R4)n- group, where n is 0, R1 is (IIb) group , X1 is -(CH)-, R9 is C1-C6alkyl, C3-C6cycloalkyl or phenyl optionally substituted with halogen atoms, R12 is a hydrogen atom, A is a bivalent cycloalkylene radical having 5, 6 or 7 ring atoms, wherein the said cycloalkylene ring is attached to W and Y and fused to a phenyl ring, wherein such phenyl ring is optionally substituted with one or two R27 groups, R27 is selected from halogen, R2 is a radical of formula (IVb) or (IVc) where R17 is selected from a single electron pair, hydrogen or aryl, where any such aryl may be optionally substituted by a C1-C6alkyl or C3-C7cycloalkyl; or R17th is a group of general formula (V) R20 is selected from the group consisting of -CH3 or -C2H5; R21 is -CH3 or -C2H5; R18 is selected from the group consisting of a single electron pair, hydrogen, aryl, heteroaryl, -(C1-6alkyl), -(C3-C7cycloalkyl), -(C3-C7heterocycloalkyl), (C5-C7heterocycloalkyl)-(C1-C6alkyl) and (C5-C7heterocycloalkyl)-(C3-C6cycloalkyl) group, R19 Is selected from -CF3, z1, z2, z3 and z4 are independently selected from the group consisting of C, N, O, -CH- and -NH- groups, in such combination that the resulting ring is an aromatic system, T is -CR28=; R28 is halogen; R22 is H or halogen. The invention also relates to a pharmaceutical composition comprising the said compounds, a method for treatment of diseases which benefit from p38 MAP kinase inhibition, and their application for manufacture of a medicament for treatment of such diseases.EFFECT: increased efficiency of compounds application.14 cl, 2 tbl, 35 exИзобретение относится к соединениям формулы (I) или их фармацевтически приемлемым солям, которые обладают ингибирующей активностью в отношении МАР-киназы р38. В формуле (I) W предста
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