ANGIOGENESIS INHIBITING PYRIDAZINAMINES

摘要

This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH2 groups of the moiety which may also contain one double bond, may be substituted with C1-6alkyl, amino, aminocarbonyl, mono- or di(C1-6alkyl)amino, C1-6alkyloxycarbony, C1-6alkylcarbonylamino, hydroxy or C1-6alkyloxy; and/or 2 C-atoms of said CH2 groups may be bridged with C2-4alkanediyl; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, mono- or di(C1-6alkyl)amino, Ar, ArNH-, C3-6cycloalkyl, hydroxymethyl or benzyloxymethyl; R2 and R3 are hydrogen, or taken together may form a bivalent radical of formula -CH=CH-CH=CH-; in case X represents CH then L is a radical L1, L2 or L3; or in case X represents N then L is a radical L2 or L3; L1 is Ar-C1-6alkyloxy, Ar-oxy, Ar-thio, Ar-carbonylamino, di-Ar-methyloxy-, N-Ar-piperazinyl, N-Ar-homopiperazinyl, 2-benzimidazolinonyl, Ar-NR4-, Ar-Alk-NR4-, Ar-NR4-Alk-NR5- or Het-NR4-; L2 is Ar, Ar-carbonyl, Ar-CH=CH-CH2-, naphtalenyl or Het; L3 is C1-6alkyl substituted with one or two radicals selected from Ar, Ar-oxy, or Ar-thio, further optionally substituted with cyano or hydroxy; 2,2-dimethyl-1,2,3,4-tetrahydro-naphtalenyl; 2,2-dimethyl-1H-2,3-dihydroindenyl;Ar-piperidinyl or Ar-NR4-Alk-; R4 and R5 are each independently selected from hydrogen or C1-6alkyl; Alk is C1-6alkanediyl; their preparation, compositions containing them and their use as a medicine.