摘要:
A composition is described. The composition comprises i) a compound comprising a sulphamate group (“a sulphamate compound”); and ii) a biological response modifier.
摘要:
Disclosed and claimed are compounds suitable for use as an inhibitor of oestrone sulphatase in a subject in need thereof, as well as compositions containing such compounds and methods for using such compounds. Such compounds can be a sulphamate compound that has the Formula (X) and wherein X is a sulphamate group, and Y is CH2 and optionally any other H attached directly to the ring system is substituted by another group
摘要:
Steroid sulphatase inhibitors and pharmaceutical compositions containing them for use in the treatment of oestrone dependent tumors, especially breast cancer. The steroid sulphatase are sulphamate esters of formula (I): ##STR1## where R.sub.1 and R.sub.2 are each H, alkyl, alkenyl, cycloalkyl or aryl, or together represent an alkylene group optionally containing a heteroatom e.g. --O-- or --NH--; and --O- polycycle represents the residue of a polycyclic alcohol such as a sterol, preferably a 3-sterol.
摘要:
A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), 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 X is any one of S, NH, a substituted N, CH2, or a substituted C.
摘要:
The present invention provides a composition comprising (i) a compound comprising a sulphamate group (“a sulphamate compound”); and (ii) an apoptosis inducer.
摘要:
The instant invention relates to sulphamate compounds of formula I, wherein A represents a ring structure, B represents a ring structure, D a ring structure, C is a bond, E is a link joining ring structure B to the ring structure D, X represents a suitable first group, and Y represents a suitable second group; wherein one ring of the compound is a phenolic ring; and wherein any one of ring structures A, B and D has bound thereto a sulphamate group.
摘要:
There is provided use of a cyclic compound or a pharmaceutically active salt thereof in the manufacture of a medicament to prevent and/or inhibit and/or arrest cell cycling, wherein the cyclic compound comprises at least one ring, wherein Group I and Group II, independently of each other, are attached to a ring of the cyclic compound; wherein Group I is a hydrocarbyl or an oxyhydrocarbyl group; and wherein Group II is a group of the formula X is P or S; when X is P, Y is ═O or S, Z is —OH and R is hydrocarbyl or H; when X is S, Y is ═O, Z is ═O, and R is hydrocarbyl or N(R1)(R2), wherein each of R1 and R2 is independently selected from H or a hydrocarbyl group.
摘要:
Disclosed and claimed are methods for oral contraception, or a hormone replacement therapy, or for treating breast cancer, in a patient in need thereof involving administering to the patient, at a dosage of no greater than 200 &mgr;g/day per 70 kg subject, a compound having Formula (I): wherein X in combination with K form a steroidal ring and R5 is a sulphamate group that has of the formula: wherein each of R1 and R2 is H.
摘要:
Phosphate esters of formula: ##STR1## for use in the inhibition of steroid sulfatase enzyme, wherein R is as defined in the specification and the -O-polycycle represents a residue of a sterol.
摘要:
A method of inhibiting steroid sulphatase activity in a subject in need of same is described. The method comprises administering to said subject a steroid sulphatase inhibiting amount of a ring system compound; which ring system compound comprises a ring to which is attached a sulphamate group of the formula ##STR1## wherein each of R.sub.1 and R.sub.2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (E.C.3.1.6.2); and if the sulphamate group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (E.C.3.1.6.2) at a pH 7.4 and 37.degree. C. it would provide a K.sub.m value of less than 50 .mu.M.