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US 6,288,050 B1Granted
Steroid sulfatase inhibitors and methods for making and using the same
AssigneesDuquesne University of the Holy Ghost, Kyowa Hakko Kogyo Co., Ltd.
InventorsPui-Kai Li, Chikara Murakata, Shiro Akinaga
Life of this patent
Estimating the term…
Abstract
Sulfatase inhibitor compounds useful in the treatment of estrogen dependent illnesses are disclosed. These compounds generally comprise a steroid nucleus substituted at the C17 position. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of a patient are also disclosed.
Claims11
A compound having the formula:
- wherein R1 and R2 are both hydrogen,
- wherein R3 is
A compound having the formula:
- wherein R1 and R2 are both hydrogen,
- wherein R3 is
- and R6 is an alkyl group having one to eight carbons.
A compound having the formula (3):
- wherein R3 is selected from
- R4 and R5 are independently selected from hydrogen, straight or branched chain alkyl groups having one to fourteen carbons, and straight or branched chain alkoxy groups having one to six carbons;
- R6 is selected from hydrogen and straight or branched chain alkyl groups having one to fourteen carbons;
- R7 is selected from
- —OR14, hydrogen and straight or branched chain alkyl groups having one to fourteen carbons, R12 and R13 are independently selected from hydrogen, alkyl groups having one to fourteen carbons and alkoxy groups having one to six carbons, and R14 is selected from hydrogen, and straight or branched chain alkyl groups having one to fourteen carbons;
- R8 is selected from hydrogen and straight or branched chain alkyl groups having one to six carbons;
- R9 is selected from straight or branched chain alkanoyl groups having one to fifteen carbons, straight or branched chain alkyl groups having one to fourteen carbons, CO(CH2)mCH3 and COR10;
- R10 is a straight or branched chain alkyl group having one to fourteen carbons, but the alkyl group is not a branched chain when the alkyl group is a C1 or C2 alkyl group;
- R11 is a branched chain alkyl group having three to fourteen carbons;
- m is 0 to 2;
- X and Y are both carbons and the bond between X and Y is either single or double, except when R3 is
- the bond between X and Y is single;
- and
- K is nitrogen and L is carbon and the bofeween K and L is either single or double.
11 more elements
A method of treating a patient for an estrogen dependent illness comprising administering to said patient an effective amount of a compound having the formula (3):
- wherein R3 is selected from
- R4 and R5 are independently selected from hydrogen, straight or branched chain alkyl groups having one to fourteen carbons, and straight or branched chain alkoxy groups having one to six carbons;
- R6 is selected from hydrogen and straight or branched chain alkyl groups having one to fourteen carbons;
- R7 is selected from
- —OR14, hydrogen and straight or branched chain alkyl groups having one to fourteen carbons, R12 and R13 are independently selected from hydrogen, alkyl groups having one to fourteen carbons and alkoxy groups having one to six carbons, and R14 is selected from hydrogen, and straight or branched chain alkyl groups having one to fourteen carbons;
- R8 is selected from hydrogen and straight or branched chain alkyl groups having one to six carbons;
- R9 is selected from straight or branched chain alkanoyl groups having one to fifteen carbons, straight or branched chain alkyl groups having one to fourteen carbons, CO(CH2)mCH3 and COR10;
- R10is a straight or branched chain alkyl group having one to fourteen carbons, but the alkyl group is not a branched chain when the alkyl group is a C1 or C2 alkyl group;
- R11, is a branched chain alkyl group having three to fourteen carbons;
- m is 0 to 2;
- X and Y are both carbons and the bond between X and Y is either single or double, except when R3 is
- the bond between X and Y is single;
- and
- K is nitrogen and L is carbon and the bond between K and L is either single or double.
11 more elements
Dependencies are inferred from the claim text.