Derivatives of estra 1,3,5(10)triene-17-one,3-amino compounds and their use
First Claim
1. A method of therapeutically treating a patient for estrogen dependent comprising diseases providing a compound having the formula (5) ##STR29## wherein R1 is hydrogen and R2 is selected from the group consisting of SO2 CF3, SO2 NH2, SO2 (C1 -C6 -alkyl) COCF3, CONH2, and CO(C1 -C6 -alkyl) and the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone,incorporating said compound in a suitable pharmaceutical carrier;
- administering a therapeutically effective dosage of said compound incorporated in said carrier to a patient; and
employing said method in therapeutically treating a patient for estrogen related diseases selected from the group consisting of breast cancer, ovarian cancer, vaginal cancer, endometrial cancer and endometriosis.
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Abstract
This invention discloses compounds useful as steroid sulfatase inhibitors. The compounds comprise the formula (1) ##STR1## wherein (a) R is selected from the group consisting of hydrogen, a lower alkyl group, an alkoxy group, halogen, NH2, NO2, C.tbd.N and N═C═S; and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The compounds also comprise the formula (5) ##STR2## wherein (a) R1 is hydrogen and R2 is selected from the group consisting of SO2 CF3, SO2 NH2, SO2 (C1 -C6 -alkyl), COCF3, CONH2, CO(C1 -C6 -alkyl); and (b) the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiol, estradiolester, pregnenolone, substituted estrones, substituted dehydroepiandrosterone, substituted estradiols, substituted estradiolesters and substituted pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.
65 Citations
38 Claims
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1. A method of therapeutically treating a patient for estrogen dependent comprising diseases providing a compound having the formula (5) ##STR29## wherein R1 is hydrogen and R2 is selected from the group consisting of SO2 CF3, SO2 NH2, SO2 (C1 -C6 -alkyl) COCF3, CONH2, and CO(C1 -C6 -alkyl) and the ring system ABCD is a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone,
incorporating said compound in a suitable pharmaceutical carrier; -
administering a therapeutically effective dosage of said compound incorporated in said carrier to a patient; and employing said method in therapeutically treating a patient for estrogen related diseases selected from the group consisting of breast cancer, ovarian cancer, vaginal cancer, endometrial cancer and endometriosis. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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19. A method of prophylactically treating a patient to provide protection as an estrogen depleting agent, the method comprising providing a compound having the formula (5) ##STR33## wherein (a) R1 is hydrogen and R2 is selected from the group consisting of SO2 CF3, SO2 NH2, SO2 (C1 -C6 -alkyl), COCF3, CONH2, and CO(C1 -C6 -alkyl);
- and (b) the ring system ABCD represents a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone,
incorporating said compound in a suitable pharmaceutical carrier; administering a prophylactically effective dosage of said estrogen depleting compound incorporated in said carrier to a patient; and employing said method in prophylactically treating a patient to provide protection as an estrogen depleting agent against an estrogen dependent disease selected from the group consisting of breast cancer, ovarian cancer, vaginal cancer, endometrial cancer and endometriosis. - View Dependent Claims (20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38)
- and (b) the ring system ABCD represents a steroid nucleus selected from the group consisting of estrone, dehydroepiandrosterone, estradiols, estradiolesters, pregnenolone, substituted estrones, substituted dehydroepiandrosterones, substituted estradiols, substituted estradiolesters and substituted pregnenolone,
Specification