Heteroarylcyclopropanecarboxamides and their use as pharmaceuticals

US8299102B2 · kind B2 · utility

Assignee

• Sanofi · FR

Inventors

• Hartmut Strobel · Liederbach, DE
• Paulus Wohlfart · Frankfurt am Main, DE
• Gerhard Zoller · Blankenloch, DE
• David William Will · Schwalbach, DE

Key dates

• Filing date: Jun 17, 2009
• Grant date: Oct 30, 2012
• Expiry date: Jul 1, 2031

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D487/08
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The present invention relates to heteroarylcyclopropanecarboxamides of the formula I,in which Het, X, Ra, Rb, Rc, Rd, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.