发明名称 Angiogenesis inhibiting thiadiazolyl pyridazine derivatives
摘要 This invention concerns compounds of formulathe N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar1, Ar1-NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula -CH=CH-CH=CH-; R4, R5 and R6 are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het1; or when R4 and R5 are adjacent to each other they may be taken together to form a radical of formula -CH=CH-CH=CH-; A is a bivalent radical of formula NR7, NR7-Alk1-X-, NR7-Alk1-X-Alk2-, O-Alk1-X-, O-Alk1-X-Alk2- or S-Alk1-X-; wherein X is a direct bond, -O-, -S-, C=O, -NR8- or Het2; R7 is hydrogen, C1-6alkyl or Ar2methyl; R8 is hydrogen, C1-6alkyl or Ar2methyl; Alk1 is C1-6alkanediyl; Alk2 is C1-4alkanediyl; Ar1 and Ar2 are optionally substituted phenyl; phenyl; Het1 and Het2 are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
申请公布号 US6602873(B2) 申请公布日期 2003.08.05
申请号 US20010864594 申请日期 2001.05.24
申请人 JANSSEN PHARAMACEUTICA, N.V. 发明人 STOKBROEKX RAYMOND ANTOINE;CEUSTERS MARC ANDRE;VAN DER AA MARCEL JOZEF MARIA;LUYCKX MARCEL GEREBERNUS MARIA;WILLEMS MARC;TUMAN ROBERT W.
分类号 C07D417/04;C07D417/14;(IPC1-7):A61K31/501 主分类号 C07D417/04
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