Non-steroidal polycyclic ring sulphamate derivatives, comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone, the preparation and their use as oestrone sulphatase inhibitors

Michael J Reed (Inventor), Barry Potter (Inventor)

Research output: Patent

Abstract

In particular the present invention relates to a non-steroidal sulphamate compound. Over the past two decades, considerable interest has been in the development of inhibitors of the aromatase pathway which converts the androgen precursor androstenedione to oestrone. However, there is evidence that oestrone sulphatase (E1-STS) pathway, i.e. the hydrolysis of oestrone sulphate to oestrone (E1S to E1), as opposed to the aromatase pathway, is the major source of oestrogen in breast tumours. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound has a polycyclic ring structure comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone. Preferably the compound has general formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; by wherein at least one of R1-R6 is a sulphamate group; and wherein the polycyclic ring structure is not tetrahydro-naphthol. Or preferably the compound of general formula (B), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein two or more of R1-R6 are linked together to form an additional cyclic structure.
Original languageEnglish
Patent numberNZ331326 (A)
IPCA61K31/37
Publication statusPublished - 27 Mar 2000

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Estrone
Derivatives
Salts
Naphthols
Aromatase Inhibitors
Aromatase
Androstenedione
Patents and inventions
Androgens
Tumors
Hydrolysis
Estrogens
sulfamic acid
estrone sulfatase

Cite this

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title = "Non-steroidal polycyclic ring sulphamate derivatives, comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone, the preparation and their use as oestrone sulphatase inhibitors",
abstract = "In particular the present invention relates to a non-steroidal sulphamate compound. Over the past two decades, considerable interest has been in the development of inhibitors of the aromatase pathway which converts the androgen precursor androstenedione to oestrone. However, there is evidence that oestrone sulphatase (E1-STS) pathway, i.e. the hydrolysis of oestrone sulphate to oestrone (E1S to E1), as opposed to the aromatase pathway, is the major source of oestrogen in breast tumours. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound has a polycyclic ring structure comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone. Preferably the compound has general formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; by wherein at least one of R1-R6 is a sulphamate group; and wherein the polycyclic ring structure is not tetrahydro-naphthol. Or preferably the compound of general formula (B), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein two or more of R1-R6 are linked together to form an additional cyclic structure.",
author = "Reed, {Michael J} and Barry Potter",
year = "2000",
month = "3",
day = "27",
language = "English",
type = "Patent",
note = "NZ331326 (A); A61K31/37",

}

TY - PAT

T1 - Non-steroidal polycyclic ring sulphamate derivatives, comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone, the preparation and their use as oestrone sulphatase inhibitors

AU - Reed, Michael J

AU - Potter, Barry

PY - 2000/3/27

Y1 - 2000/3/27

N2 - In particular the present invention relates to a non-steroidal sulphamate compound. Over the past two decades, considerable interest has been in the development of inhibitors of the aromatase pathway which converts the androgen precursor androstenedione to oestrone. However, there is evidence that oestrone sulphatase (E1-STS) pathway, i.e. the hydrolysis of oestrone sulphate to oestrone (E1S to E1), as opposed to the aromatase pathway, is the major source of oestrogen in breast tumours. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound has a polycyclic ring structure comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone. Preferably the compound has general formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; by wherein at least one of R1-R6 is a sulphamate group; and wherein the polycyclic ring structure is not tetrahydro-naphthol. Or preferably the compound of general formula (B), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein two or more of R1-R6 are linked together to form an additional cyclic structure.

AB - In particular the present invention relates to a non-steroidal sulphamate compound. Over the past two decades, considerable interest has been in the development of inhibitors of the aromatase pathway which converts the androgen precursor androstenedione to oestrone. However, there is evidence that oestrone sulphatase (E1-STS) pathway, i.e. the hydrolysis of oestrone sulphate to oestrone (E1S to E1), as opposed to the aromatase pathway, is the major source of oestrogen in breast tumours. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound has a polycyclic ring structure comprising two or more rings wherein at least two of the rings mimic the A and B rings of oestrone. Preferably the compound has general formula (A), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; by wherein at least one of R1-R6 is a sulphamate group; and wherein the polycyclic ring structure is not tetrahydro-naphthol. Or preferably the compound of general formula (B), wherein R1-R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1-R6 is a sulphamate group; and wherein two or more of R1-R6 are linked together to form an additional cyclic structure.

M3 - Patent

M1 - NZ331326 (A)

ER -