Duquesne University of the Holy Ghost

Kyle W Selcer

Pui-Kai Li

Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.

Compounds for the treatment of estrogen-dependent illnesses and methods for making and using the same

Compounds for the treatment of estrogen-dependent illnesses and methods of making and using the same

Sulfatase inhibitor compounds having the formula: ##STR1## wherein X, Y, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification. The compounds are useful in the treatment of estrogen dependent illnesses. Methods for synthesizing these compounds are also disclosed.

Steroid sulfatase inhibitors and methods for making and using the same

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, NH.sub.2, NO.sub.2, C.tbd.N and N.dbd.C.dbd.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) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1 -C.sub.6 -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.

Derivatives of estra 1,3,5(10)triene-17-one, 3-amino compounds and their

Derivatives of estra 1,3,5(10)triene-17-one,3-amino compounds and their

This invention discloses compounds useful as steroid inhibitors. The compounds comprise the formula (5) ##STR1## wherein (a) R.sub.1 is hydrogen and R.sub.2 is selected from the group consisting of SO.sub.2 CF.sub.3, SO.sub.2 NH.sub.2, SO.sub.2 (C.sub.1 -C.sub.6 -alkyl), COCF.sub.3, CONH.sub.2, CO(C.sub.1-C.sub.6 -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. Preferably the steroid nucleus is selected from the group consisting of estrone, dehydropeiandrosterone and pregnenolone. The invention also discloses methods of treating a patient therapeutically and prophylactically for estrogen dependent diseases with the compounds of this invention.

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Murrysville, PA, United States of America

Kyle W Selcer