Phthalazines with angiogenesis inhibiting activity

US6258812A · kind A · 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: Oct 20, 1999
• Grant date: Jul 10, 2001
• Expiry date: Oct 20, 2019

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, ##STR1## wherein r is 0 to 2, n is 0 to 2; m is 0 to 4; R.sub.1 and R.sub.2 (i) are in each case a lower alkyl, or (ii) together form a bridge in subformula I* ##STR2## (I*) or (iii) together form a bridge in subformula I** ##STR3## (I**), wherein one or two of the ring members T.sub.1, T.sub.2, T.sub.3, and T.sub.4 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, --CH.sub.2 --O--, --CH.sub.2 --S--, --CH.sub.2 --NH--, oxa, thia, or imino; Q is methyl; c 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 …