Pentacyclic compounds, intermediates, processes,...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) A61K 31/35 (2006.01) A61K 31/38 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07D 221/18 (2006.01) C07D 311/78 (2006.01) C07D 311/92 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 471/04 (2006.01) C07D 491/044 (2006.01) C07D 493/04 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2230974

The present invention relates to compounds of formulae (I) and (II) wherein X is -O-, -S-, or -NR5-; Y is -O-, -S-, -CH2-, -CH2CH2-, -CH=CH-, or -NR5-; B is -CH2- or -CO-; R1, R2, and R3 are each independently -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), -OSO2(C4-C6 alkyl), -OSO2CF3, Cl, or F; n is 1 or 2; W is CH2 or C=O; R4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4- morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; R5 is C1-C3 alkyl, -COC6H5, -CO(C1-C6 alkyl), -C(O)OC6H5, -C(O)O(C1-C6 alkyl), -SO2(C1-C6 alkyl), -SO2C6H5, or -SO2CF3; or a pharmaceutically acceptable salt thereof. Also provided by the present invention are intermediate compounds; processes for the preparation of compounds of formulae (I) and (II); and pharmaceutical methods and formulations employing the compounds of formulae (I) and (II).

L'invention concerne des composés de formules I et II dans lesquelles X représente -O-, -S-, ou -NR?5¿; Y représente -O-, -S-, CH¿2?-, -CH¿2?CH¿2?-, -CH=CH-, ou -NR?5¿-; B représente -CH?2¿- ou -CO-; R?1¿, R?2¿ et R?3¿ représentent chacun indépendamment -H, -OH, -O(alkyle C¿1?-C¿4?), -OCOC¿6?H¿5?, -OCO(alkyle C¿1?-C¿6?), -OSO¿2?(alkyle C¿4?-C¿6?), -OSO¿2?CF¿3?, Cl, ou F; n vaut 1 ou 2; W représente CH¿2? ou C=O; R?4¿ représente 1-pipéridinyle, 2-oxo-1-pipéridinyle, 1-pyrrolidinyle, méthyl-1-pyrrolodinyle, diméthyl-1-pyrrolidinyle, 2-oxo-1-pyrrolidinyle, 4-morpholino, diméthylamino, diéthylamino, ou 1-hexaméthylèneimino; R?5¿ représente alkyle C¿1?-C¿3?, -COC¿6?H¿5?, -CO(alkyle C¿1?-C¿6?), -C(O)OC¿6?H¿5?, -C(O)O(alkyle C¿1?-C¿6?), -SO¿2?(alkyle C¿1?-C¿6?), -SO¿2?C¿6?H¿5?, ou -SO¿2?CF¿3?; ou un sel pharmaceutiquement acceptable desdits composés. L'invention porte également sur des composés intermédiaires, des procédés de préparation des composés de formules I et II, des procédés et des formulations pharmaceutiques dans lesquels lesdits composés de formules I et II sont utilisés.

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