Sterix Limited

Other

Ipsen Pharma S.a.s.

Estryx Pharma Limited

Lok Wai Lawrence Woo

Barry Victor Lloyd Potter

Michael John Reed

Atul Purohit

Christian Bubert

Oliver Brook Sutcliffe

Toby Jackson

Paul Michael Wood

Bertrand Leblond

Christian Diolez

Gérard Coquerel

Alain Rolland

Matthew Paul Leese

Hatem Hejaz

Francis Diancourt

Damien Martins

Delphine Delahaye

Gillian Reed, Legal Representative

Paul Foster

Barry Victory Lloyd Potter

Aurélien Putey

Christian Burbert

There is provided a compound of formula I  wherein t is 1 or 2wherein R'is a unsubstituted or substituted phenyl group;wherein each of Rto Ris independently selected from &#x2014;H, NO, halo, &#x2014;O&#x2014;(C-C)haloalkyl, (C-C)haloalkyl, (C-C)alkyl, &#x2014;CN, &#x2014;OH, &#x2014;OPh, &#x2014;OBn, -Ph, &#x2014;OSONRR, &#x2014;SOR, &#x2014;SONRR, &#x2014;O&#x2014;(C-C)alkyl, &#x2014;(C&#x2550;O)NRRand &#x2014;CO(O)R;

Compound

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.

Solid pharmaceutical composition containing 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta (C)chromen-3-yl  sulfamate and polymorphs thereof

There is provided a compound of Formula I wherein X, Y and Z are each independently of each other an optional linker group; Ris a ring system; Ris selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (&#x2014;CN), nitro (&#x2014;NO) and halogens; Rand Rare independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.

Phenyl-sulfamates as aromatase inhibitors

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 Rand Rare 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.

Sulfamic acid ester compounds useful in the inhibition of steroid sulphatase activity and aromatase activity

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

Steroidal compounds for inhibiting steroid sulphatase

There is provided a compound of Formula I wherein R, R, R, Rand Rare independently selected from H and &#x2014;Y&#x2014;R; wherein each Ris independently selected from &#x2014;OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (&#x2014;CN), nitro (&#x2014;NO), H-bond acceptors, and halogens; wherein at least one of R, R, R, Rand Ris &#x2014;Y&#x2014;Rwherein Ris 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 Ris selected from H, &#x2014;OH and &#x2014;OSONRR; wherein Rand Rare independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R, R, R, Rand Ris &#x2014;Y&#x2014;R; OR (b) Ris &#x2014;OSONRRor &#x2014;OH and four of R, R, R, Rand Rare H and one of R, R, R, Rand Ris &#x2014;Y&#x2014;R.

There is provided a compound of Formula I wherein X is a ring system; Ris any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; Ris 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 Rand Rare 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. There is also provided a compound of Formula VIII wherein Ris any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; 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.

Oestrogen-17-sulphamates as inhibitors of steroid sulphatase

There is provided a compound of Formula I wherein R, R, R, Rand Rare independently selected from H and &#x2014;Y&#x2014;R; wherein each Ris independently selected from &#x2014;OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (&#x2014;CN), nitro (&#x2014;NO), H-bond acceptors, and halogens; wherein at least one of R, R, R, Rand Ris &#x2014;Y&#x2014;Rwherein Ris 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 Ris selected from H, &#x2014;OH and &#x2014;OSONRR; wherein Rand Rare independently selected from H and hydrocarbyl; wherein (a) X is a bond and at least one of R, R, R, Rand Ris &#x2014;Y&#x2014;R; OR (b) Ris &#x2014;OSONRRor &#x2014;OH and four of R, R, R, Rand Rare H and one of R, R, R, Rand Ris &#x2014;Y&#x2014;R. These compounds inhibit steroid sulphatase and aromatase activity and are useful in the treatment of endocrine-dependent tumors.

1,2,4-triazol-1-yl bisphenyl derivatives for use in the treatment of endocrine-dependent tumors

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

Steroidal compounds as steroid sulphatase inhibitors

There is provided a compound of Formula I wherein each T is independently selected from H, hydrocarbyl, &#x2014;F&#x2014;R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CHand C&#x2550;O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

Polycyclic sulphamate compounds suitable for use as inhibitors of aromatase and/or sulphatase

There is provided a compound of formula XII, wherein G is H or a substituent, and wherein Ris a sulphamate group.

There is provided a compound of Formula Iwherein each T is independently selected from H, hydrocarbyl, &#x2014;F&#x2014;R, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CHand C&#x2550;O; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

Growing community of inventors

Slough, United Kingdom

Lok Wai Lawrence Woo