Abstract: A compound having Formula I 1

Abstract: 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.

Abstract: There is provided a compound of Formula I 1

Abstract: There is provided use of a compound in the manufacture of a medicament to inhibit superoxide dismutase (SOD) or for use in the therapy of a condition or disease associated with SOD wherein the compound is of Formula I 1

Abstract: A composition is described. The composition comprises i) a compound comprising a sulphamate group (“a sulphamate compound”); and ii) a biological response modifier.

Abstract: A method for controlling estrone or estrodiol production comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M. A method to target the estrogen metabolic pathway comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M.

Abstract: A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least one sulphamate group attached to at least one of the ring components, and wherein at least one oxime group is attached to or is part of at least one of the ring components.

Abstract: There is provided a compound of Formula I 1

Abstract: 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.

Abstract: 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 sulphamate group of the formula wherein each of R1 and R2 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° C. it would provide a Km value of less than 50 &mgr;M.

Abstract: 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.

Abstract: There is provided a compound comprising a steroidal ring system and a group R1 selected from any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula —L—R3, wherein L is an optional linker group and R3 is an aromatic hydrocarbyl group.

Abstract: 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.

Abstract: A compound is described. The compound has the formula (Ia) as presented in the FIG. 1; wherein: X is a ring having at least 4 atoms in the ring; K is hydrocarbyl group; Rh1 is an optional halo group; Rh2 is an optional halo group; at least one of Rh1 and Rh2 is present; Rs is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group. The compound is capable of inhibiting steroid sulphatase (STS) activity.

Abstract: 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 a bound thereto a sulphamate group.

Abstract: A sulphamate compound suitable for use as an inhibitor of oestrone sulphatase (E.C.3.1.6.2) is described. The compound is a polycyclic compound comprising at least two ring components, wherein the polycyclic compound comprises at least one sulphamate group attached to at least one of the ring components, and wherein at least one oxime group is attached to or is part of at least one of the ring components.

Abstract: There is provided a pharmaceutical composition comprising (i) a compound of the formula 1

Abstract: A method for controlling estrogen production comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M. A method to target the estrogen metabolic pathway comprising administering a ring system compound comprising a sulphamic acid ester group; wherein said compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3.1.6.2); and wherein if the sulphamic acid ester group of said compound is replaced with a sulphate group to form a sulphate compound and incubated with a steroid sulphatase enzyme (EC 3.1.6.2) at a pH 7.4 and 37° C. it provides a Km value of less than 50 &mgr;M.

Abstract: The invention pertains to methods for introducing an estrogenic compound into a subject in need thereof involving administering an effective amount of a ring system compound having the formula (II) wherein each of R1 and R2 is independently selected from H, alkyl, alkenyl, cycloalkyl and aryl, and at least one of R1 and R2 is H, or together represent alkylene optionally containing one or more hetero atoms or groups in the alkylene chain; and the ring system ABCD represents a substituted or unsubstituted, saturated or unsaturated steroid nucleus selected from the group consisting of oestrones, dehydroepiandrosterones, substituted oestrones, oestradiols, substituted oestradiols, oestriols, substituted dehydroepiandrosterones, or substituted oestriols; wherein the compound is an inhibitor of an enzyme having steroid sulphatase activity (EC 3,1,6,2), or a pharmceutically acceptable salt thereof.

Abstract: There is provided use of a material selected from (i) microtubule stabilizing agent; (ii) microtubule disrupter; (iii) a compound of the formula A-B wherein A is an oxyhydrocarbyl group and B is a cyclic group; and (iv) a compound of the formula C-D wherein C is an sulphamate group and D is a cyclic group, for the manufacture of a medicament for the inhibition of tumor necrosis factor &agr; (TNF&agr;) stimulated aromatase activity.