Amide and urea derivatives as 5-HT reuptake inhibitors and as 5-HT1B/1D ligands

US6509340B1 · kind B1 · utility

Assignee

• Merck Patentgesellschaft · DE

Inventors

• Christoph van Amsterdam · Darmstadt, DE
• Hartmut Greiner · Darmstadt, DE
• Henning Boettcher · Darmstadt, DE
• Gerd Bartoszyk · Weiterstadt, DE
• Juergen Harting · Darmstadt, DE
• Lisa Matzen · Mainz, DE
• Wilfried Rautenberg · Reinheim, DE

Key dates

• Filing date: Oct 3, 2001
• Grant date: Jan 21, 2003
• Expiry date: Oct 3, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/14
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Amide and urea derivatives of the formula IR1—(CH2)n—(Y)q—(Z)r—CO—NH—R2  (I)in which R1, n, Y, q, Z, r and R2 have the meanings indicated in Claim 1, are potent 5-HT1B/1D antagonists and exhibit 5-HT reuptake-inhibiting actions and are suitable for the treatment and prophylaxis of anxiety states, depressions, schizophrenia, compulsive ideas, tardive dyskinesias, learning disorders, age-dependent memory disorders, for positively affecting obsessive-compulsive behaviour (OCD), and also for the treatment and for the control of the sequelae of cerebral infarcts such as stroke and cerebral ischaemias.