Invention Grant
- Patent Title: Heteroarylacrylamides and their use as pharmaceuticals
- Patent Title (中): 杂芳基丙烯酰胺及其作为药物的用途
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Application No.: US12486117Application Date: 2009-06-17
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Publication No.: US08304438B2Publication Date: 2012-11-06
- Inventor: Hartmut Strobel , Paulus Wohlfart , Heinz-Werner Kleemann , Gerhard Zoller , David William Will
- Applicant: Hartmut Strobel , Paulus Wohlfart , Heinz-Werner Kleemann , Gerhard Zoller , David William Will
- Applicant Address: FR Paris
- Assignee: Sanofi
- Current Assignee: Sanofi
- Current Assignee Address: FR Paris
- Agency: Scully, Scott, Murphy & Presser, P.C.
- Priority: EP06026397 20061220
- Main IPC: C07D401/06
- IPC: C07D401/06 ; A61K31/44

Abstract:
The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, 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.
Public/Granted literature
- US20100016272A1 HETEROARYLACRYLAMIDES AND THEIR USE AS PHARMACEUTICALS Public/Granted day:2010-01-21
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