EP 1968958 A1 20080917 - SUBSTITUTED THIAZOLES AND THEIR USE FOR PRODUCING DRUGS
Title (en)
SUBSTITUTED THIAZOLES AND THEIR USE FOR PRODUCING DRUGS
Title (de)
SUBSTITUIERTE THIAZOLE UND IHRE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN
Title (fr)
THIAZOLES SUBSTITUES ET LEUR UTILISATION POUR PRODUIRE DES MEDICAMENTS
Publication
Application
Priority
- EP 2006012483 W 20061222
- DE 102005062990 A 20051228
Abstract (en)
[origin: DE102005062990A1] N-thiazolylalkyl-substituted propiolamide derivatives (I) are new. N-thiazolylalkyl-substituted propiolamide derivatives of formula (I) and their pure stereoisomers, particularly enantiomers or diastereomers, including racemates and mixtures in any proportion, and their salts and solvates, are new. R 1>and R 2>e.g alkyl, alkenyl, alkynyl, cycloalkyl, aryl (all optionally substituted), H, F, Cl, Br, I, NO 2, CN or carboxy; R 3>and R 10>e.g. alkyl, alkenyl, alkynyl, cycloalkyl, aryl (all optionally substituted), H or carbamoyl; R 4>-R 9>e.g. alkyl, alkenyl, alkynyl, cycloalkyl, aryl (all optionally substituted), H, F, Cl, Br, I, NO 2, CN or carboxy; and R 11>(hetero)aryl (optionally substituted). The full definitions are given in the DEFINITIONS (Full Definitions) field. An independent claim is included for the preparation of (I). [Image] [Image] ACTIVITY : Analgesic; Antimigraine; Antidepressant; Nootropic; Neuroprotective; Antiparkinsonian; Anticonvulsant; Tranquilizer; Antitussive; Uropathic; Antidiarrheal; Antipruritic; Antiasthma; Cerebroprotective; Ophthalmological; Antialcoholic; Antismoking. MECHANISM OF ACTION : mGluR5 receptor regulator; mGluR5 receptor inhibitor. N-(3-((thiazol-2-yl)amino)propyl)-3-phenylpropiolamide (Ia) has IC 50against porcine mGluR5 receptor of 0.99 mu M.
IPC 8 full level
C07D 277/42 (2006.01); A61K 31/426 (2006.01); A61K 31/427 (2006.01); A61K 31/428 (2006.01); A61P 25/00 (2006.01); C07D 417/04 (2006.01); C07D 417/12 (2006.01); C07D 487/04 (2006.01)
CPC (source: EP US)
A61P 1/04 (2017.12 - EP); A61P 1/08 (2017.12 - EP); A61P 1/12 (2017.12 - EP); A61P 1/14 (2017.12 - EP); A61P 3/04 (2017.12 - EP); A61P 7/12 (2017.12 - EP); A61P 9/10 (2017.12 - EP); A61P 11/00 (2017.12 - EP); A61P 11/04 (2017.12 - EP); A61P 11/06 (2017.12 - EP); A61P 13/02 (2017.12 - EP); A61P 15/10 (2017.12 - EP); A61P 17/04 (2017.12 - EP); A61P 21/00 (2017.12 - EP); A61P 21/04 (2017.12 - EP); A61P 23/02 (2017.12 - EP); A61P 25/00 (2017.12 - EP); A61P 25/04 (2017.12 - EP); A61P 25/06 (2017.12 - EP); A61P 25/08 (2017.12 - EP); A61P 25/10 (2017.12 - EP); A61P 25/12 (2017.12 - EP); A61P 25/14 (2017.12 - EP); A61P 25/16 (2017.12 - EP); A61P 25/18 (2017.12 - EP); A61P 25/22 (2017.12 - EP); A61P 25/24 (2017.12 - EP); A61P 25/26 (2017.12 - EP); A61P 25/28 (2017.12 - EP); A61P 25/32 (2017.12 - EP); A61P 25/34 (2017.12 - EP); A61P 25/36 (2017.12 - EP); A61P 27/00 (2017.12 - EP); A61P 27/02 (2017.12 - EP); A61P 29/00 (2017.12 - EP); C07D 277/42 (2013.01 - EP US); C07D 417/04 (2013.01 - EP US); C07D 417/12 (2013.01 - EP US); C07D 487/04 (2013.01 - EP US)
Citation (search report)
See references of WO 2007079961A1
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
DE 102005062990 A1 20070705; CA 2633734 A1 20070719; EP 1968958 A1 20080917; JP 2009522223 A 20090611; US 2008269295 A1 20081030; US 8318774 B2 20121127; WO 2007079961 A1 20070719
DOCDB simple family (application)
DE 102005062990 A 20051228; CA 2633734 A 20061222; EP 06829856 A 20061222; EP 2006012483 W 20061222; JP 2008547892 A 20061222; US 14720308 A 20080626