Morpholinylquinazolines

US9126952B2 · kind B2 · utility

Assignee

• Merck Patent GmbH · DE

Inventors

• Werner Mederski · Zwingenberg, DE
• Thomas Fuchss · Bensheim, DE
• Frank Zenke · Darmstadt, DE

Key dates

• Filing date: Feb 17, 2011
• Grant date: Sep 8, 2015
• Expiry date: Oct 4, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D417/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of the formulae (I), (II) and (III)in which R1, R2, R3, R4, Y, W1, W2, L, A, Alk, Cyc, Ar, Het1, Het2, Hal and n have the meaning indicated in Claim 1, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.