Pyrimido [5, 4-d] pyrimidines, pharmaceuticals containing these compounds, their use and processes for their preparation

US5977102A · kind A · utility

Assignee

• Dr. Karl Thomae GmbH · DE

Inventors

• Frank Himmelsbach · Mittelbiberach, DE
• Georg Dahmann · Biberach an der Riß, DE
• Thomas von Ruden · Planegg, DE
• Thomas Metz · Kennewick, US

Key dates

• Filing date: Mar 5, 1997
• Grant date: Nov 2, 1999
• Expiry date: Mar 5, 2017

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Pyrimido[5,4-d]pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of oncoses, and their preparation. Exemplary compounds are: PA1 (a) 4-(5-indolylamino)-6-morpholinopyrimido[5,4-d]pyrimidine; PA1 (b) 4-(5-indolylamino)-6-[trans-(4-hydroxycyclohexyl)amino]pyrimido[5,4-d]pyri midine; PA1 (c) 4-[(3-chloro-4-fluorophenyl)amino]-6-[4-(morpholinocarbonylmethyl)-1-piper azinyl]pyrimido[5,4-d]pyrimidine; PA1 (d) 4-[(3-chloro-4-fluorophenyl)amino]-6-[(4-morpholinyl)amino]pyrimido[5,4-d] pyrimidine; PA1 (e) 4-[(3-chloro-4-fluorophenyl)amino]-6-(4-picolylamino)pyrimido[5,4-d]pyrimi dine; PA1 (f) 4-[(3-chloro-4-fluorophenyl)amino]-6-[1-trifluoroacetyl-4-piperidinylamino ]pyrimido[5,4-d]pyrimidine; PA1 (g) 4-[(3-chloro-4-fluorophenyl)amino]-6-(endo-tropinylamino)pyrimido[5,4-d]py rimidine; and, PA1 (h) 4-[(3-chloro-4-fluorophenyl)amino]-6-(exo-tropinylamino)pyrimido[5,4-d]pyr imidine.