代謝共役型グルタミン酸受容体拮抗剤

Japanese Patent JP2004510764

A

The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl-moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1-6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form -R2-R3-, which represents a bivalent radical of formula -Z4-CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula -CH2-CH2-CH2-CH2-; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate-induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.

WO/2012/116415	NOVEL SMALL-MOLECULES AS THERAPEUTICS
JPH0826002	[Title of Invention] 1- (2-Halogenocyclopropyl) Quinoline Carboxylic Acid Derivative
WO/2002/060875	NICOTINAMIDE BIARYL DERIVATIVES USEFUL AS INHIBITORS OF PDE4 ISOZYMES

Maville, Dominique Jean-Pierre
Marc Gaston, Benet
Coupa, Sofui
Poncelet, Alan Filip
Roussaille, Anne Simone Gioseph Dog

JP2002532423A

April 08, 2004

September 25, 2001

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JANSSEN PHARMACEUTICA NAAMLOZE VENNOOTSCHAP

A61K31/47; A61K31/4704; A61K31/4709; A61K31/473; A61K31/4741; A61K31/4743; A61K31/4745; A61K31/506; A61K31/5377; A61K31/541; A61P3/08; A61P5/00; A61P9/10; A61P25/00; A61P25/04; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P29/00; A61P43/00; C07D215/04; C07D215/12; C07D215/14; C07D215/18; C07D215/22; C07D215/227; C07D215/36; C07D215/38; C07D215/48; C07D215/50; C07D215/54; C07D215/60; C07D219/02; C07D221/10; C07D221/12; C07D221/16; C07D401/04; C07D401/06; C07D401/12; C07D405/04; C07D405/06; C07D405/12; C07D409/04; C07D409/06; C07D409/12; C07D413/12; C07D417/04; C07D417/06; C07D453/06; C07D471/04; C07D487/04; C07D491/04; C07D491/048; C07D491/052; C07D495/04; C07F7/08; C07F7/10; (IPC1-7): C07D215/04; A61K31/47; A61K31/4704; A61K31/4709; A61K31/473; A61K31/4741; A61K31/4743; A61K31/4745; A61K31/506; A61K31/5377; A61K31/541; A61P3/08; A61P5/00; A61P9/10; A61P25/00; A61P25/04; A61P25/08; A61P25/14; A61P25/16; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P29/00; A61P43/00; C07D215/14; C07D215/18; C07D215/22; C07D215/36; C07D215/38; C07D215/48; C07D215/54; C07D215/60; C07D219/02; C07D221/10; C07D221/12; C07D221/16; C07D401/06; C07D401/12; C07D405/04; C07D405/06; C07D405/12; C07D409/04; C07D409/06; C07D409/12; C07D413/12; C07D417/04; C07D417/06; C07D471/04; C07D487/04; C07D491/048; C07D491/052; C07D495/04

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Heikichi Odashima

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