发明名称 Thiadiazolyl pyridazine derivatives, process of their preparation and pharmaceutical compositions in which the derivatives are comprised
摘要 The present invention relates to the compounds of the general formula I, N-oxide forms thereof, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Re1 represents hydrogen, alkyl group containing 1 to 6 carbon atoms, alkyloxy group having 1 to 6 carbon atoms, alkylthio group containing 1 to 6 carbon atoms, amino group, mono- or dialkylamino group having 1 to 6 carbon atoms in the alkyl moiety, Are1, Are1-NH-, cycloalkyl containing 3 to 6 carbon atoms, hydroxymethyl or benzyloxymethyl; Re2 and Re3 denote hydrogen, or taken together may form a bivalent radical of the general formula -CH=CH-CH=CH-; Re4, Re5 and Re6 are each independently selected from hydrogen, a halogen, alkyl group containing 1 to 6 carbon atoms, alkyloxy group having 1 to 6 carbon atoms, trifluoromethyl, nitro group, amino group, cyano group, azido group, alkyloxyalkyl group containing 1 to 6 carbon atoms in both the alkyloxy and alkyl moieties, alkylthio group having 1 to 6 carbon atoms, alkyloxycarbonyl containing 1 to 6 carbon atoms or Hete1; or when Re4 and Re5 are adjacent to each other they may be taken together to form a radical of the general formula -CH=CH-CH=CH-; A represents a bivalent radical of the formula NRe7, NRe7-Alke1-X-, NRe7-Alke1-X-Alke2-, O-Alke1-X-, O-Alke1-X-Alke2-, or S-Alke1-X-; wherein X denotes a direct bond, -O-, -S-, C=O, -NRe8 or Hete2; Re7 stands for hydrogen, alkyl containing 1 to 6 carbon atoms or Are2methyl; Re8 represents hydrogen, alkyl containing 1 to 6 carbon atoms or Are2methyl; Alke1 denotes alkanediyl containing 1 to 6 carbon atoms in the alkane moiety; Alk2 represents alkanediyl having 1 to 4 carbon atoms in the alkane moiety; Are1 and Are2 represent optionally substituted phenyl; phenyl; Hete1 and Hete2 denote optionally substituted heterocycles; having angiogenesis inhibiting activity; and their preparation. The invention further relates to compositions containing them as well as their use as medicaments.
申请公布号 CZ296000(B6) 申请公布日期 2005.12.14
申请号 CZ19990004508 申请日期 1998.06.22
申请人 JANSSEN PHARMACEUTICA N. V. 发明人 STOKBROEKX RAYMOND ANTOINE;CEUSTERS MARC ANDRE;VAN DER AA MARCEL JOZEF MARIA;LUYCKX MARCEL GEREBERNUS MARIA;VILLEMS MARC;TUMAN ROBERT W.
分类号 C07D417/04;C07D417/14;(IPC1-7):C07D417/04;A61K31/502;A61K31/433;A61P43/00;A61K31/501 主分类号 C07D417/04
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