2-Arylimino-2,3-dihydrothiazoles, and their use thereof as somatostatin receptor ligands

US6727269B1 · kind B1 · utility

Assignee

• Société de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S) SAS · FR

Inventors

• Christophe Moinet · Orvault, FR
• Carole Sackur · Paris, FR
• Christophe Thurieau · Paris, FR

Key dates

• Filing date: Jan 15, 2002
• Grant date: Apr 27, 2004
• Expiry date: Jan 16, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C40B40/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention concerns novel 2-arylimino-2,3-dihydrothiazole derivatives of general formula (I), their preparation methods and their use as medicines, in particular for treating pathological conditions or diseases wherein one (or several) somatostatin receptors is/are involved. Said pathological conditions include in particular acromegaly, pituitary adenoma or endocrine gastroenteropanceatic tumors including the carcinoid syndrome, and gastrointestinal bleeding. In general formula (I), R1 represents in particular an alkyl, aralkyl, cyclohexyl radical optionally substituted by an amino radical or R1 represents a —C(R11)(R12)—CO—R10 radical wherein R11 represents H, R12 represents in particular H, carbocyclic or heterocyclic alkyl, cycloalkyl or aralkyl and R10 represents in particular an aminoalkylamino radical; R2 represents a carcyclic or heterocyclic aryl radical optionally substituted; R3 represents in particular COR5 or a carbocyclic or heterocyclic alkyl, adamantyl, aryl radical optionally substituted, carbocyclic or heterocyclic aralkyl optionally substituted on the aryl group; and R5 represents a radical fixed by a nitrogen atom to the group CO.