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SUBSTITUTED OXAZOLE DERIVATIVES AND USE THEREOF AS TYROSINE KINASE INHIBITORS
专利权人:
AB S'JANS;SANTR NAS'ONAL' DE LJA RESHERSH S'ENTIFIK (SNRS);AB SJANS;EHNSTITJU KJURI
发明人:
GRIERSON David (FR),ГРИЕРСОН Давид (FR),BENDZhAKhAD Abdellakh (FR),БЕНДЖАХАД Абделлах (FR),MUSSI Alen (FR),МУССИ Ален (FR),KRUAZI Martin (FR),КРУАЗИ Мартин (FR),GRIERSON DAVID,BENDZHAKHAD ABDELLAKH,MUSSI ALEN,KRUAZI MARTIN
申请号:
RU2007140864/04
公开号:
RU0002445308C2
申请日:
2006.04.04
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
FIELD: medicine, pharmaceutics.SUBSTANCE: invention refers to a compound of formula I wherein the substitutes A, B, B', Q and R1-R5 in formula I are specified as follows: A and B' are one of the following groups: (i) (R6)N(CH2)n, wherein n is 0 or 1; (ii) (CH2)n, wherein n is 0, 1 or 2; (iii) C(O)(CH2)n, wherein n is 0 or 1; or provided each of A and B' represents nitrogen, together they can form a bivalent radical of formula: -(CH2)s-X1-(CH2)t- (a), wherein each s and t is independently 1 or 2, and X1 represents (CH2)n, wherein n is 0 or 1; B is one of the following groups: (i) (R6)N; (ii) oxygen; (iii) C=δ, wherein δ represents oxygen or sulphur; (iv) C(R6)=C(R7); each R6 and R7 independently represent hydrogen, C1-4-alkyl; R1 is specified in the following groups: (i) phenyl group substituted by one or more substitute such as: - halogen specified in F, CI, Br or I, or alkyl1 group; aryl1 or heteroaryl group1; cyano, NH-alkyl1, N(alkyl1)(alkyl1) and amino; - NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl group, or (ii) pyridinyl group which can be substituted by one substitute, such as halogen specified in I, F, Cl or Br; alkyl1 group; aryl1 group; cyano, NH-alkyl1, N(alkyl1)(alkyl1), and amino; -NHCO-R or NHCOO-R, or COO-R, or CONH-R, wherein R represents hydrogen or alkyl1 group; each R2, R3, R4 and R5 are independently specified in hydrogen or linear or branched alkyl group containing 1 to 10 carbon atoms; Q is specified in the following groups: (i) alkyl1; (ii) aryl1; (iii) heteroaryl1. The compounds of formula (I) are used for preparing a drug showing the c-kit inhibitor properties and aiming at treating a disease specified in neoplastic, allergic, inflammatory and autoimmune diseases.EFFECT: use of oxazole derivatives as tyrosine kinase inhibitors.13 cl, 1 tbl, 31 exИзобретение относится к соединению формулы I, где заместители А, В, В', Q и R1-R5 в формуле I определены следующим образом: А и В' являются одной из нижеуказанны
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