Diaryl-enynes as glycine transport inhibitors

Details Diaryl-enynes as glycine transport inhibitors Diaryl-enynes as glycine transport inhibitors

C - Chemistry, Metallurgy

07

C

C07C 229/00 (2006.01) A61K 31/21 (2006.01) C07C 229/36 (2006.01) C07C 323/41 (2006.01) C07D 207/325 (2006.01) C07D 307/52 (2006.01) C07D 317/58 (2006.01) C07D 333/20 (2006.01)

Patent

CA 2387660

Provided, among other things, is a compound of Formula (I), wherein, Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl- substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl- substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl- substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioarylalkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR', NRR', CO2R (where R and R' are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is selected from the group consisting of H, alkyl and benzyl; R3 is selected from the group consisting of CO2R, CONRR', CONH(OH), COSR, SO2NRR', PO(OR)(OR') and tetrazolyl, wherein R and R' are independently selected from the group consisting of H and alkyl; and a salt, solvate or hydrate thereof.

L'invention concerne, entre autres choses, un composé de la formule (I), dans laquelle Ar¿1? et Ar¿2? sont des groupes aryle sélectionnés indépendamment, facultativement substitués par jusqu'à cinq substituants choisis indépendamment dans le groupe comprenant alkyle, alcoxy, cycloalkyle, cycloalkyloxy, hétérocycloalkyle, hétérocycloalkyloxy, alcanoyle, thioalkyle, aralkyle, aralkyloxy, aryloxyalkyle, aryloxyalcoxy, alkyle à substitution cycloalkyle, alkyle à substitution cycloalkyloxy, alcoxy à substitution cycloalkyle, alcoxy à substitution cycloalkyloxy, alkyle à substitution hétérocycloalkyle, alkyle à substitution hétérocycloalkyloxy, alcoxy à substitution hétérocycloalkyle, alcoxy à substitution hétérocycloalkyloxy, thioaryle, aralkylthio, thioarylalkyle, aralkylthioalkyle, halo, NO¿2?, CF¿3?, CN, OH, alkylènedioxy, SO¿2?NRR', NRR', CO¿2?R (où R et R' sont sélectionnés indépendamment dans le groupe comprenant H et alkyle), ainsi qu'un second groupe aryle, lequel peut être substitué tel que ci-dessus; R¿1? est choisi dans le groupe comprenant H et alkyle; R¿2? est choisi dans le groupe comprenant H, alkyle et benzyle; R¿3? est choisi dans le groupe comprenant CO¿2?R, CONRR', CONH(OH), COSR, SO¿2?NRR', PO(OR)(OR') et tétrazolyle, où R et R' sont sélectionnés indépendamment dans le groupe comprenant H et alkyle; ainsi qu'un sel, un solvate ou un hydrate dudit composé.

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