Sterix Limited

Imperial College of Science, Technology and Medicine

Other

University of Bath of Claverton Down

Estryx Pharma Limited

Atul Purohit

Michael John Reed

Barry Victor Lloyd Potter

Lok Wai Lawrence Woo

Christian Bubert

Nigel Vicker

Matthew Paul Leese

Oliver Brook Sutcliffe

Toby Jackson

Dharshini Ganeshapillai

Bertrand Leblond

Paul Michael Wood

Hatem Hejaz

Su Xiangdong

Fabrice Jourdan

Joanna Mary Day

Wesley Heaton

Helen Victoria Bailey

Barry Victory Lloyd Potter

Gillian Reed, Legal Representative

Anita Singh

Su Xiangdon

Surinder Kuman Chander

Simon Paul Newman

Paul Foster

Delphine Sophie Marion Fischer

Gillian Margaret Allan

Harshani Rithma Ruchiranani Lawrence

Christopher Mark Sharland

Ana Maria Ramos Gonzalez

Christian Burbert

Meriel Kimberley

Aurélien Putey

Paul Alexander Foster

Sarah Louise Claire Tagg

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

There is provided a compound having Formula I wherein

Compound capable of inhibiting 17-beta hydroxysteriod dehydrogenase

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 involves tetrahydroisoquinoline compounds and their use in the inhibition and/or prevention of tumor growth.

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 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, &#x2014;S&#x2550;O, &#x2014;S(&#x2550;O), &#x2014;C&#x2550;O, &#x2014;S(&#x2550;O)NR, &#x2014;C&#x2550;ONR, and &#x2014;NR, wherein n and p are independently selected from 0 and 1; Y is (R)wherein each Ris independently selected from &#x2014;NR, &#x2014;CRR, &#x2014;S(&#x2550;O)and &#x2014;C&#x2550;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 &#x2014;R&#x2014;NR&#x2014; group.

Heterocyclic compounds as inhibitors of 17beta-HSD3

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 of Formula (III) wherein

17B-hydroxysteroid dehydrogenase inhibitors

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

The present invention provides a compound comprising a steroidal ring system and an optional group Rselected from any one of &#x2014;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 Rof the formula -L-R, wherein L is an optional linker group and Ris 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 Ris 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 R, wherein Ris a hydrocarbyl group.

Oestrogen derivatives as inhibitors of steroid sulphatase

A compound having Formula I wherein one of Rand Ris a group of the formula wherein Ris selected from H and hydrocarbyl, Ris a hydrocarbyl group and L is an optional linker group, or Rand Rtogether form a ring substituted with the group wherein Ris H or a substituent, and wherein X is selected from S, O, NRand C(R)(R), wherein Ris selected from H and hydrocarbyl groups, wherein each of Rand Rare independently selected from H and hydrocarbyl groups.

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.

Growing community of inventors

Slough, United Kingdom

Atul Purohit