| US 7,550,482 B2 | ||
| Tetrahydroquinolones and their use as modulators of metabotropic glutamate receptors | ||
| Valerjans Kauss, Riga (Latvia); Ieva Jaunzeme, Riga (Latvia); Aigars Jirgensons, Riga (Latvia); Ivars Kalvinsh, Salaspils (Latvia); Maksims Vanejevs, Riga (Latvia); Markus Henrich, Wetzlar (Germany); Wojciech Danysz, Nidderau (Germany); Claudia Jatzke, Frankfurt am Main (Germany); Christopher Graham Raphael Parsons, Nidderau (Germany); and Tanja Weil, Heidelberg (Germany) | ||
| Assigned to Merz Pharma GmbH & Co. KGAA, Frankfurt Main (Germany) | ||
| Filed on Aug. 24, 2005, as Appl. No. 11/210,569. | ||
| Application 11/210569 is a continuation in part of application No. 11/066899, filed on Feb. 25, 2005. | ||
| Claims priority of provisional application 60/548788, filed on Feb. 27, 2004. | ||
| Prior Publication US 2005/0288284 A1, Dec. 29, 2005 | ||
| Int. Cl. C07D 215/38 (2006.01); A61K 31/44 (2006.01) | ||
| U.S. Cl. 514—313 [546/177; 546/178] | 11 Claims |
1. A compound selected from those of Formula I
 wherein
R1 represents aryl or heteroaryl;
R2 and R3, which may be the same or different, represent hydrogen or C1-6alkyl;
R4 and R5, which may be the same or different, represent hydrogen or C1-6alkyl;
it being understood that:
aryl represents an unsubstituted phenyl ring or a phenyl ring that is substituted with 1, 2, 3, 4 or 5 substituents, that
may be the same or different, which substituents are selected from C1-6alkyl, which is optionally substituted with one or more fluorine, chlorine or bromine atoms, C1-6alkoxy, which is optionally substituted with one or more fluorine, chlorine or bromine atoms, cycloC3-12alkyl, hydroxyl, F, Cl, Br, I, CN, nitro, di-C1-6alkylamino, N-cycloC3-12alkyl-N-C1-6alkylamino, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, 4-C1-6alkyl-piperazinyl, tetrazolyl, oxazolyl, furyl, thiophenyl, pyrrolyl, isoxazolyl, thiazolyl, imidazolyl, oxadiazolyl, pyridinyl,
pyrimidyl, and phenyl;
heteroaryl represents a (hetero)aromatic 5-, 6- or 7-membered ring having from 1 to 4 heteroatoms, said heteroatoms being
independently selected from oxygen, nitrogen and sulfur, wherein said ring is unsubstituted or substituted with 1, 2 or 3
substituents, that may be the same or different, which substituents are selected from C1-6alkyl, which is optionally substituted with one or more fluorine, chlorine or bromine atoms, C1-6alkoxy, which is optionally substituted with one or more fluorine, chlorine or bromine atoms, cycloC3-12alkyl, hydroxyl, F, Cl, Br, I, CN, nitro, di-C1-6alkylamino, N-cycloC3-12alkyl-N—C1-6alkylamino, azetidinyl, pyrrolidinyl, piperidinyl, morpholinyl, 4-C1-6alkyl-piperazinyl, tetrazolyl, oxazolyl, furyl, thiophenyl, pyrrolyl, isoxazolyl, thiazolyl, imidazolyl, oxadiazolyl, pyridinyl,
pyrimidyl, and phenyl;
and optical isomers and pharmaceutically acceptable salts thereof.
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