Diazapane derivatives useful as antagonists of neurokinin 1 receptor and methods for their formation

US6452001B2 · kind B2 · utility

Assignee

• Hoffmann-La Roche Inc. · US

Inventors

• Guido Galley · Rheinfelden (Baden), DE
• Annick Goergler · Basel, CH
• Thierry Godel · Basel, CH
• Reinhard Heck · Oftersheim, DE

Key dates

• Filing date: May 14, 2001
• Grant date: Sep 17, 2002
• Expiry date: May 14, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention relates to compounds of the formula whereinR1, R2 are independently from each other aryl or heteroaryl, wherein the heteroaryl group contains one or two heteroatoms, selected from N, O, or S, and wherein the aryl or heteroaryl groups are optionally substituted by 1 to 3 substituents, which are independently from each other halogen, CF3, lower alkoxy or lower alkyl;R3 is hydrogen, lower alkyl, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl;R4 is ═O, ═N(CH2)nCH3 or ═N(CH2)nN(R)2;R3 and R4 may be together with the N and C atoms to which they are attached the group —CR5═N—N═; R5 is hydrogen, —(CH2)nN(R)2, —(CH2)n-heteroaryl or is a —(CH2)n-non aromatic heterocycle, which heterocycles are optionally substituted by halogen, CF3, lower alkoxy or lower alkyl;R is hydrogen or lower alkyl;n is 0, 1, 2 or 3;and pharmaceutically acceptable acid addition salts and enantiomeric forms thereof. The compounds are useful in the treatment of diseases, related to the NK-1 receptor.