发明名称 THIADIAZOLYL PYRIDAZINE DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM
摘要 This invention concerns compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein R<1> is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar<1>, Ar<1>-NH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R<2> and R<3> are hydrogen, or taken together may form a bivalent radical of formula -CH=CH-CH=CH-; R<4>, R<5> and R<6> are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, nitro, amino, cyano, azido, C1-6alkyloxyC1-6alkyl, C1-6alkylthio, C1-6alkyloxycarbonyl or Het<1>; or when R<4> and R<5> 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 NR<7>, NR<7>-Alk<1>-X-, NR<7>-Alk<1>-X-Alk<2>-, O-Alk<1>-X-, O-Alk<1>-X-Alk<2>- or S-Alk<1>-X-; wherein X is a direct bond, -O-, -S-, C=O, -NR<8>- or Het<2>; R<7> is hydrogen, C1-6alkyl or Ar<2>methyl; R<8> is hydrogen, C1-6alkyl or Ar<2>methyl; Alk<1> is C1-6alkanediyl; Alk<2> is C1-4alkanediyl; Ar<1> and Ar<2> are optionally substituted phenyl; phenyl; Het<1> and Het<2> are optionally substituted heterocycles; having angiogenesis inhibiting activity; their preparation, compositions containing them and their use as a medicine.
申请公布号 PL191409(B1) 申请公布日期 2006.05.31
申请号 PL19980337657 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;WILLEMS MARC;TUMAN ROBERT W.
分类号 C07D417/04;A61K;A61K31/41;A61K31/501;A61P17/06;A61P27/02;A61P29/00;A61P35/00;A61P43/00;C07D;C07D417/14 主分类号 C07D417/04
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