Estra-1,3,5(10),16-tetraene derivatives
AssigneesKyowa Hakko Kogyo Co., Ltd., Duquesne University of the Holy Ghost
InventorsYoji Ino, Nobuyoshi Amishiro, Taisuke Nakata, Hiroyuki Ishida, Shiro Akinaga, Chikara Murakata, Pui-Kai Li
Life of this patent
Estimating the term…
Abstract
Estra-1,3,5(10),16-tetraene derivatives represented by the following formula (I): (wherein R1 is as defined by the present specification.
Claims16
An estra-1,3,5(10),16-tetraene derivative represented by formula (I):
- wherein R1 represents alkoxy (the alkyl moiety of said alkoxy is straight-chain alkyl having 1, 2, or 4-14 carbon atoms or branched-chain alkyl having 1 to 14 carbon atoms), or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms, with the proviso that when one of R2 and R3 is hydrogen, the other is not CH2CH2CH3, CH2CH(CH3)2, or C(CH3)3), or a pharmaceutically acceptable salt thereof.
A method for inhibiting steroid sulfatase in a person requiring such treatment, which comprises administering a therapeutically effective amount of an estra-1,3,5(10),16-tetraene derivative represented by formula (I):
- wherein R1 represents alkoxy (the alkyl moiety of said alkoxy is straight-chain alkyl having 1, 2, or 4-14 carbon atoms or branched-chain alkyl having 1 to 14 carbon atoms), or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms, with the proviso that when one of R2 and R3 is hydrogen, the other is not CH2CH2CH3, CH2CH(CH3)2, or C(CH3)3), or a pharmaceutically acceptable salt thereof.
A method for treating a person having breast cancer associated with the overproduction of estrone produced from estrone sulfate, which comprises administering a therapeutically effective amount of an estra-1,3,5(10),16-tetraene derivative represented by formula (I):
- wherein R1 represents alkoxy (the alkyl moiety of said alkoxy is straight-chain alkyl having 1, 2, or 4-14 carbon atoms or branched-chain alkyl having 1 to 14 carbon atoms), or NR2R3 (wherein R2 and R3 are the same or different, and each represents hydrogen, straight-chain lower alkyl having 1 to 3 carbon atoms, or branched-chain lower alkyl having 3 to 8 carbon atoms, with the proviso that when one of R2 and R3 is hydrogen, the other is not CH2CH2CH3, CH2CH(CH3)2, or C(CH3)3), or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.