C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/08 (2006.01) A61K 31/135 (2006.01) A61K 31/395 (2006.01) C07C 225/22 (2006.01) C07C 259/10 (2006.01) C07D 207/34 (2006.01) C07D 211/32 (2006.01) C07D 211/34 (2006.01) C07D 211/36 (2006.01) C07D 211/46 (2006.01) C07D 211/58 (2006.01) C07D 211/62 (2006.01) C07D 211/94 (2006.01) C07D 295/108 (2006.01) C07D 295/135 (2006.01) C07D 295/24 (2006.01) C07D 307/66 (2006.01) C07D 317/66 (2006.01) C07D 319/18 (2006.01) C07D 333/36 (2006.01) C07D 405/02 (2006.01)
Patent
CA 2163747
The present invention relates to novel 5-HT4 receptor ligands which are 1-(5- halo-4-aminophenyl) (C2-6)alkan-1-one derivatives in which the 5-halo-4-aminophenyl group is substituted at its 2-position with (C1- 4)alkyloxy or phenyl(C1-4)alkyloxy and optionally substituted at its 3-position with (C1-4)alkyloxy or substituted at its 2- and 3-positions together with methylenedioxy or ethylenedioxy and the highest numbered carbon of the (C2-6)alkan-1-one is substituted with di(C1- 4)alkylamino, morpholin-1-yl or pyrrolidin-1-yl or optionally substituted piperidin-1-yl, piperidin-4-yl, azacyclohept-1-yl, azabicyclo[2.2.1]hept-3-yl, azabicyclo[2.2.2]oct-3-yl or azabicyclo[3.2.2]non-3-yl; and the pharmaceutically acceptable salts, individual isomers and mixtures of isomers and methods of using and making such derivatives.
L'invention concerne de nouveaux ligands du récepteur de 5-HT4 qui sont des dérivés de 1-(5-halo-4-aminophényl)(C2-6)alcane-1-one, dans lesquels le groupe 5-halo-4-aminophényle est substitué à sa position 2 par (C1-4)alkyloxy ou phényl(C1-4)alkyloxy et éventuellement substitué à sa position 3 par (C11-4)alkyloxy ou substitué à ses positions 2 et 3 par méthylènedioxy ou éthylènedioxy et le carbone à nombre le plus élevé de (C2-6)alcane-1-one est substitué par di(C1-4)alkylamino, morpholine-1-yl ou pyrrolidine-1-yle ou pipéridine-1-yle éventuellement substituée, pipéridine-4-yle, azacyclohept-1-yle, azabicyclo[2,2,1]hept-3-yle, azabicyclo[2,2,2]oct-3-yle ou azabicyclo[3,2,2]non-3-yle; sels pharmaceutiquement acceptables, isomères individuels et mélange d'isomères, ainsi que procédés d'utilisation et de préparation desdits dérivés.
Clark Robin Douglas
Eglen Richard Malcolm
Gardner John Otis
Jahangir Alam
Miller Aaron Bayne
Dennison Associates
Syntex (u.s.a.) Inc.
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