Publication number: 20100286151
Abstract: The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; Z1 is H, C1-C4 alkyl or F; Z is CH2, CH(C1-C4 alkyl), C(C1-C4 alkyl)2 or a bond; A is a 5 membered heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, Cl C4 haloalkoxy, cyano; B is hydrogen or is a 5-6 membered heteroaryl, or phenyl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; being A and B linked via any atom; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.
Type:
Application
Filed:
January 30, 2008
Publication date:
November 11, 2010
Inventors:
Jonathan Bentley, Matteo Biagetti, Romano Di Fabio, Thorsten Genski, Sebastien Guery, Silvia Rosalia Kopf, Colin philip Leslie, Angelica Mazzali, Sergio Melotto, Domenica Antonia Pizzi, Fabio Maria Sabbatini, Catia Seri
Publication number: 20100160336
Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
Type:
Application
Filed:
December 16, 2009
Publication date:
June 24, 2010
Inventors:
Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
Publication number: 20100152195
Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituent
Type:
Application
Filed:
December 16, 2009
Publication date:
June 17, 2010
Inventors:
Luca Arista, Giorgio Bonanomi, Anna Maria Capelli, Federica Damiani, Romano Di Fabio, Gabriella Gentile, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Giovanna Tedesco, Silvia Terreni
Publication number: 20100152175
Abstract: There are provided according to the invention novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein: X represents a nitrogen atom; Y represents —C(H2)—, (—C(H2)—)2, —S(O2)— or —C(?O)—; Z represents —C(H2)—, —S(O2)—, —N(Rz)—, or an oxygen or sulphur atom; A represents hydrogen or —CH2OH; Rz represents hydrogen, C1-6 alkyl, C1-6 alkoxy, —COR7 or —SO2R7; R1 represents halogen, C1-6 alkyl, C1-6 alkoxy, ?O, haloC1-6 alkyl, haloC1-6 alkoxy, hydroxyl or —CH2OH; m represents an integer from 0 to 3; R2 represents halogen, ?O, C1-6 alkyl (optionally substituted by one or more hydroxyl groups), —COOR7, —CONR7R8, C1-6 alkoxy, haloC1-6 alkyl, haloC1-6 alkoxy or C1-6alkylOC1-6alkyl; n represents an integer from 0 to 3; p and q independently represent an integer from 0 to 2; R3 represents an -aryl, -heteroaryl, -heterocyclyl, -aryl-aryl, -aryl-heteroaryl, -aryl-heterocyclyl, -heteroaryl-aryl, -heteroaryl-heteroaryl, -heteroaryl-heterocyclyl, -heterocyclyl-aryl, -heterocyclyl-heteroaryl o
Type:
Application
Filed:
December 14, 2009
Publication date:
June 17, 2010
Applicant:
GlaxoSmithKline LLC
Inventors:
Giuseppe Alvaro, Daniele Andreotti, Sandro Belvedere, Romano Di Fabio, Alessandro Falchi, Riccardo Giovannini