C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 409/12 (2006.01) A61K 31/381 (2006.01) A61K 31/44 (2006.01) C07D 295/08 (2006.01) C07D 295/092 (2006.01) C07D 333/50 (2006.01)
Patent
CA 2497627
The present invention provides a compound of the formula (I) wherein R1 is -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), or -OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1- C6 alkyl), -OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is S- or -HC=CH-; and Y is O-, -S-, -NH-, -NMe-, or -CH2-;or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.
L'invention concerne un composé, sel pharmaceutiquement acceptable compris, de formule (I), dans laquelle R?1¿ est -H, -OH, -O(C¿1?-C¿4? alkyle), -OCOC¿6?H¿5?, -OCO(C¿1?-C¿6? alkyle), ou -OSO¿2?(C¿2?-C¿6? alkyle); R?0¿, R?2¿ et R?3¿ sont chacun indépendamment -H, -OH, -O(C¿1?-C¿4? alkyle), -OCOC¿6?H¿5?, -OCO(C¿1?-C¿6? alkyle), -OSO¿2?(C¿2?-C¿6? alkyle) ou halo; R?4¿ est 1-pipéridinyle, 1-pyrrolidinyle, méthyle-1-pyrrolidinyle, diméthyle-1-pyrrolidinyle, 4-morpholino, diméthylamino, diéthylamino, diisopropylamino, or 1-hexaméthylèneimino; n vaut 2 ou 3; X est S- ou -HC=CH-; et Y est O-, -S-, -NH-, -NMe-, ou -CH¿2?-. L'invention concerne également des compositions pharmaceutiques de ce composé, éventuellement en combinaison avec de l'oestrogène et de la progestine, des procédés visant à inhiber une maladie associée à un déficit d'oestrogène, et des procédés visant à inhiber une maladie associée à une réponse physiologique aberrante à l'oestrogène endogène.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
LandOfFree
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