Abstract: The invention discloses compounds of the formula wherein A, B, X, Y and Z are defined. The compounds of the invention show activity against a range of bacteria, and are useful in the treatment or prophylaxis of a bacterial infection in an animal.

Abstract: The present invention relates to novel derivatives of estradiol, in particular to deuterated derivatives of estradiol sulfamates. The present invention also relates to compositions comprising said novel derivatives, as well as to uses of said novel derivatives and compositions comprising said derivatives.

Abstract: There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C?O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (?O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C?O)0-1R12][(C?O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C?O)0-1R12][(C?O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R?14, wherein R12 and R13

Abstract: The present invention relates to a solid pharmaceutical composition including the active principle 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. The present invention also relates to polymorphs of the 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate compound.

Abstract: The present invention relates to a solid pharmaceutical composition including the active principle 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate. The present invention also relates to polymorphs of the 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta[c]chromen-3-yl sulfamate compound.

Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0

Abstract: There is provided a compound of Formula I wherein X, Y and Z are each independently of each other an optional linker group; R1 is a ring system; R2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2) and halogens; R3 and R4 are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.

Abstract: The present invention involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.

Abstract: There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C?O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (?O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C?O)0-1R12][(C?O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C?O)0-1R12][(C?O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R?14, wherein R12 and R13

Abstract: 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.

Abstract: The present invention relates to steroid sulphatase and/or aromatase inhibitors of Formula III or Formula IV, wherein A is selected from H, OH, halogen and hydrocarbyl; D, E and F are each independently of each other an optional linker group; P, Q and R are independently of each other a ring system, wherein R4 and R5 are independently selected from H, alkyl, cycloalkyl, alkenyl, acyl and aryl, or combinations thereof, or together represent alkylene, wherein the or each alkyl or cycloalkyl or alkenyl or optionally contain one or more hetero atoms or groups, and which can be used in medicine.

Abstract: There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.

Abstract: There is provided a compound having Formula (I) wherein each of rings A and B is selected from five or six membered carbon rings optionally containing one or more hetero atoms selected from N, S, and O and optionally having fused thereto a further ring; X is an optional group selected from O, S, —S?O, —S(?O)2, —C?O, —S(?O)2NR8, —C?ONR9, and —NR10, wherein n and p are independently selected from 0 and 1; Y is (R11)1-3 wherein each R11 is independently selected from —NR12, —CR13R14, —S(?O)2 and —C?O; Z is selected from (i) six or seven membered ring containing carbon and at least one nitrogen, which may be optionally substituted wherein the substituents may together form further ring fused thereto; and (ii) a —R15—NR16— group.

Abstract: A compound having Formula I wherein one of R1 and R2 is a group of the formula wherein R4 is selected from H and hydrocarbyl, R5 is a hydrocarbyl group and L is an optional linker group, or R1 and R2 together form a ring substituted with the group wherein R3 is H or a substituent, and wherein X is selected from S, O, NR6 and C(R7)(R8), wherein R6 is selected from H and hydrocarbyl groups, wherein each of R7 and R8 are independently selected from H and hydrocarbyl groups.

Abstract: There is provided a compound of Formula I wherein R3, R4, R5, R6 and R7 are independently selected from H and —Y—R8; wherein each R8 is independently selected from —OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2), H-bond acceptors, and halogens; wherein at least one of R3, R4, R5, R6 and R7 is —Y—R8 wherein R8 is selected from substituted and unsubstituted heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further substituted; wherein R9 is selected from H, —OH and —OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is —Y—R8; OR (b) R9 is —OSO2NR1R2 or —OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is —Y—R8.

Abstract: There is provided a compound of Formula I wherein X is a ring system; R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; R2 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein when X is a steroidal structure and both of R1 and R2 are sulphamate groups, the steroidal ring system (X) represents an oestrogen; and wherein said compound is capable of inhibiting steroid sulphatase (STS) activity and/or is capable of acting as a modulator of cell cycling and/or as a modulator of apoptosis and/or as a modulator of cell growth.

Abstract: There is provided a compound of Formula I wherein R3, R4, R5, R6 and R7 are independently selected from H and —Y—R8; wherein each R8 is independently selected from —OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2), H-bond acceptors, and halogens; wherein at least one of R3, R4, R5, R6 and R7 is —Y—R8 wherein R8 is selected from substituted and unsubstituted heterocyclic rings and amino substituted phenyl groups, wherein X is a bond or a linker group; wherein Y is an optional linker group; and wherein ring A is optionally further substituted; wherein R9 is selected from H, —OH and —OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R3, R4, R5, R6 and R7 is —Y—R8; OR (b) R9 is —OSO2NR1R2 or —OH and four of R3, R4, R5, R6 and R7 are H and one of R3, R4, R5, R6 and R7 is —Y—R8. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.

Abstract: There is provided a compound of Formula (III) wherein R1 is a selected from an alkyloxyalkyl group, a nitrile group, alkylaryl group, alkenylaryl group, alkylheteroaryl group, alkenylheteroaryl group, ?N—O—alkyl or ?N—O—H group, branched alkenyl, alkyl-alcohol group, amide or alkylamide or —CHO so that R1 together with R3 provide the enol tautomer or R1 together with R3 form a pyrazole, wherein (a) R4 is ?N—O-alkyl or ?N—O—H group, (b) the pyrazole is substituted with one of alkyl-OH group, alkyl ester group, alkyloxyalkyl group, branched alkyl group, and an amide and/or (c) the 2-position is substituted with a group selected from —OH and —O-hydrocarbyl or a heteroaryl ring; R2 is selected from —OH and a sulphamate group; and R3 is selected from —OH or ?O; wherein the ring system may be further substituted with one or more hydroxyl, alkyl, alkoxy, alkinyl or halo substituents.

Abstract: There is provided a compound having Formula I wherein G is a fluorocarbyl group, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group.

Abstract: The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, 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 selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl group.