Isoquinoline derivatives with angiogenesis inhibiting activity

US6608071B2 · kind B2 · utility

Assignee

• Novartis AG · CH

Inventors

• Karl-Heinz Altmann · Reinach, CH
• Guido Bold · Gipf-Oberfrick, CH
• Paul W. Manley · Arlesheim, CH

Key dates

• Filing date: Feb 9, 2001
• Grant date: Aug 19, 2003
• Expiry date: Jun 29, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of formula I whereinr is from 0 to 2; n is from 0 to 2; m is from 0 to 4;A, B, D and E are each independently of the others N or CH, with the proviso that not more than two of those radicals are N;G is lower alkylene, —CH2—O—, —CH2—S—, —CH2—NH—, oxa (—O—), thia (—S—) or imino (—NH—), or is lower alkylene substituted by acyloxy or by hydroxy;Q is lower alkyl, especially methyl;R is H or lower alkyl;X is imino, oxa or thia;Y is lower alkyl or, especially, aryl, heteroaryl or unsubstituted or substituted cycloalkyl; andZ is amino, mono- or di-substituted amino, halogen, alkyl, substituted alkyl, hydroxy, etherified or esterified hydroxy, nitro, cyano, carboxy, esterified carboxy, alkanoyl, carbamoyl, N-mono- or N,N-di-substituted carbamoyl, amidino, guanidino, mercapto, sulfo, phenylthio, phenyl-lower alkylthio, alkylphenylthio, phenylsulfinyl, phenyl-lower alkylsulfinyl, alkylphenyl-sulfinyl, phenylsulfonyl, phenyl-lower alkanesulfonyl or alkylphenylsulfonyl, and where, if more than one radical Z is present (m≧2), the substituents Z are identical or differen…