2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol and estrogen formulations
AssigneeWyeth
InventorsJames Harrison Pickar, Barry Samuel Komm
Life of this patent
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Abstract
The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structure below: and related methods of treatment for providing tissue selective estrogenic activity while minimizing undesirable side effects of estrogen treatment or therapy, such as excessive estrogenic uterine stimulation.
Claims2
A method of preventing excessive estrogenic uterine stimulation in a mammal, the method comprising administering to a mammal in need thereof an estrogen and an effective amount of a compound having the structure:
- wherein:
- R1 is selected from H, OH or the C1-C4 esters or alkyl ethers thereof, or halogen;
- R2, R3, R4, R5, and R6 are independently selected from H, OH or the C1-C4 esters or alkyl ethers thereof, halogen, cyano, C1-C6 alkyl, or trifluoromethyl, with the proviso that, when R1 is H, R2 is not OH;
- X is selected from H, C1-C6 alkyl, cyano, nitro, trifluoromethyl, or halogen;
- n is 2 or 3;
- Y is the moiety:
- R7 and R8 are selected independently from H, C1-C6 alkyl, or combined by —(CH2)p—, wherein p is an integer of from 2 to 6, so as to form a ring, the ring being optionally substituted by up to three substituents selected from the group of hydrogen, hydroxyl, halo, C1-C4 alkyl, trihalomethyl, C1-C4 alkoxy, trihalomethoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, hydroxy (C1-C4)alkyl, —CO2H, —CN, —CONH(C1-C4)alkyl, —NH3, C1-C4 alkylamino, di(C1 -C4)alkylamino, —NHSO2(C1-C4)alkyl, —NHCO(C1-C4)alkyl, and —NO2;
- or a pharmaceutically acceptable salt thereof.
A method of preventing excessive estrogenic uterine stimulation in a mammal in need thereof, comprising administering to said mammal an effective amount of a combination of conjugated estrogens and 2-(4-hydroxy-phenyl)-3-methyl-1-[4-(3-piperidin-1-yl-prop-1-ynyl)-benzyl]-1H-indol-5-ol, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.