Pyrido-, pyrimido-, pyridazo- and pyrazo- pyridazines having angiogenesis inhibiting activity

US6514974B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Guido Bold · Gipf-Oberfrick, CH
• Jorg Frei · Hölstein, CH
• Peter Traxler · Allschwil, CH
• Karl-Heinz Altmann · Reinach, CH
• Helmut Mett · Karlstadt, DE
• David Stover · Sylvia Park, US
• Jeanette Marjorie Wood · Biel-Benken, CH

Key dates

• Filing date: May 17, 2001
• Grant date: Feb 4, 2003
• Expiry date: May 17, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of formula I, wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R1 and R2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* or (iii) together form a bridge in subformula I** wherein one or two of the ring members T1, T2, T3, and T4 are nitrogen, and the remainder are in each case CH; A, B, D, and E are N or CH, wherein not more than 2 of these radicals are N; G is lower alkylene, acyloxy- or hydroxy-lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa, thia, or imino; Q is methyl; R is H or lower alkyl; X is imino, oxa, or thia; Y is aryl, pyridyl, or (un)substituted cycloalkyl; and Z is mono- or disubstited amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-disubstituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenylsulfinyl, phenylsulfonyl, phenyl-lower alkylsulfonyl, or alkylphenylsulfony; and wherein the bonds characterized by a wavy line are eit…