Angiogenesis inhibiting pyridazinamines

作者: Raymond Antoine Jan Stokbroekx , Robert W Tuman , Der Aa Marcel Jozef Maria Van , Marc Willems , Marcel Gerebernus Maria Luyckx

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

参考文章(7)
Marcel Gerebernus Maria Luyckx, Joannes Josephus Maria Willems, Raymond Antoine Stokbroekx, Marcel Jozef Maria Van Der Aa, Anti-virally active pyridazinamines ,(1985)
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Marcel G. M. Luyckx, Raymond A. Stokbroekx, Gilbert A. J. Grauwels, Cyriel A. M. Van der Eycken, Intermediates for producing antipicornaviral pyridazinamines ,(1991)
Marcel G. M. Luyckx, Raymond A. Stokbroekx, Marcel J. M. Van der Aa, Gilbert A. J. Grauwels, Novel pyridazinamine derivatives ,(1988)