# US 5,344,827 A · Steroid sulphatas inhibitors

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- Number: US 5,344,827 A
- Document ID: US5344827A
- Status: Granted
- Kind: A
- Application number: 08/143,071
- Filed: 1993-10-26
- Granted: 1994-09-06
- Earliest claimed: 1990-02-21
- Assignees: Imperial College of Science, Technology and Medicine
- Inventors: Michael J. Reed
- Web page: https://patentgrep.com/patent/US5344827A

## CPC

- C07J 51/00: Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
- A61P 5/30: Oestrogens
- A61P 35/00: Antineoplastic agents
- C07J: STEROIDS (seco-steroids C07C)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Novel steroid 3-thiophosphonates are disclosed which are useful as steroid sulphatase inhibitors.

## Claims

### Claim 1

A pharmaceutical preparation comprising in admixture a steroid sulphatase inhibitor and a parenterally administrable carrier wherein the steroid sulphatase inhibitor comprises an effective amount of a steroid-3-thiophosphonate of the formula ##STR5## where R=alkyl, and the ring system ABCD represents a substituted or umsubstituted saturated or unsaturated steroid nucleus, or a pharmaceutically acceptable salt thereof.

### Claim 2 (depends on 1)

A pharmaceutical preparation according to claim 1, wherein R in the formula of the steroid sulphatase inhibitor is C.sub.1 -C.sub.6 alkyl.

### Claim 3 (depends on 1)

A pharmaceutical preparation according to claim 1, wherein R in the formula of the steroid sulphatase inhibitor is methyl.

### Claim 4

A pharmaceutical preparation comprising, in unit dosage form, a steroid sulphatase inhibitor in admixture with an orally administrable carrier, wherein the said steroid sulphatase inhibitor is a steroid-3-thiophosphonate of the formula ##STR6## wherein R is alkyl, and the ring system ABCD represents a substituted or unsubstituted, saturated or unsaturated steroid nucleus, or a pharmaceutically acceptable salt thereof, said preparation containing from 100 to 500 mg of said steroid-3-thiophosphonate or salt per unit dose.

### Claim 5 (depends on 4)

A preparation according to claim 4, wherein R in the said formula is C.sub.1 -C.sub.6 alkyl.

### Claim 6 (depends on 5)

A preparation according to claim 5, wherein R is the said formula is methyl.