Estra-1,3,5(10)-triene-7alpha-thioethers

C - Chemistry – Metallurgy – 07 – J

Patent

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Details

C07J 31/00 (2006.01) A61K 31/56 (2006.01) A61K 31/59 (2006.01) C07J 41/00 (2006.01) C07J 43/00 (2006.01)

Patent

CA 2308773

The invention provides estrogens and antiestrogens of formula (I) having structure (I) wherein R is (II), (III), (IV), or (V); R1 and R2 are each, independently, alkyl of 1-6 carbon atoms, or are alkyl groups which are taken together to form a 5-7 membered satured heterocycle; X is hydroxy, alkoxy of 1- 6 carbon atoms, or -OC(O)R3; W is (VI), hydroxy, alkyl of 1-6 carbon atoms, halogen, -CF3, alkoxy of 1-6 carbon atoms, -CHO, cyano, alkylcarbonyl of 2-7 carbon atoms, alkoxycarbonyl of 2-7 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl group, trifluoromethoxy, hydroxyalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, -CN, -SO3H, or -CO2H; R3 is alkyl of 1-6 carbon atoms; Z is (VII), (VIII), (IX), or (X); Y is (XI), (XII), or (XIII); R4 is hydrogen, alkyl of 1- 6 carbon atoms, alkoyl of 2-7 carbon atoms, or benzoyl; Q is hydrogen, -OR5, or -NR6R7; R5 is hydrogen or alkyl of 1-6 carbon atoms; R6 and R7 are each, independently, alkyl of 1-6 carbon atoms, or are alkyl groups which are taken together to form a 5-7 membered saturated heterocycle; n = 4-12; and p = 2-6; or a pharmaceutically acceptable salt thereof.

L'invention concerne des oestrogènes et des anti-oestrogènes représentés par la formule (I) dont la structure est: (I), dans laquelle R est (II), (III), (IV) ou (V); R?1¿ et R?2¿ sont chacun indépendamment l'un de l'autre un alkyle comprenant 1-6 atomes de carbone ou des groupes alkyle qui forment ensemble un hétérocycle saturé comprenant 5-7 éléments; X est l'hydroxy, un alkoxy comprenant 1-6 atomes de carbone ou -OC(O)R?3¿; W est (VI), l'hydroxy, un alkyle comprenant 1-6 atomes de carbone, l'halogène, -CF¿3?, un alkoxy comprenant 1-6 atomes de carbones, -CHO, cyano, un alkylcarbonyle comprenant 2-7 atomes de carbone, un alkoxycarbonyle comprenant 2-7 atomes de carbone, amino, un alkylamino comprenant 1-6 atomes de carbone, un dialkylamino comprenant 1-6 atomes de carbone par groupe alkyle, trifluorométhoxy, un hydroxyalkyle comprenant 1-6 atomes de carbone, un alkoxyalkyle comprenant 2-12 atomes de carbone, -CN, -SO¿3?H, ou -CO¿2?H; R?3¿ est un alkyle comprenant 1-6 atomes de carbone; Z est (VII), (VIII), (IX) ou (X); Y est (XI), (XII), (XIII) ou (XIV); R?4¿ est l'hydrogène, un alkyle comprenant 1-6 atomes de carbone, un alcoyle comprenant 2-7 atomes de carbone ou un benzoyle; Q est l'hydrogène, -OR?5¿, ou NR?6¿R?7¿; R?5¿ est l'hydrogène ou un alkyle comprenant 1-6 atomes de carbone; R?6¿ et R?7¿ sont chacun indépendamment l'un de l'autre un alkyle comprenant 1-6 atomes de carbone ou R?6¿ et R?7¿ sont des groupes alkyle formant ensemble un hétérocycle saturé de 5-7 éléments; n = 4-12; et p = 2-6; ou un sel pharmaceutiquement acceptable de ce composé.

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