University College London

Canbex Therapeutics Limited

Ucl Business Plc

Gareth Pryce

David Lawrence Selwood

Masahiro Okuyama

David Baker

Cristina Visintin

David Selwood

The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is selected from OH, NHCHCHF, NHCH(Me)CHOH and NHCHCHOH; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO-alkyl, alkenyl, CN, NH, hydroxy, halo, alkoxy, CFand nitro; Y is a polar functional group selected from OH, NO, CN, COR, COOR, NRR, CONRR, SOH, SO&#x2014;R, SONRRand CF, where each of Rand Ris independently H or a hydrocarbyl group; A is phenyl or pyridyl; and B is (CH)where n is 0; with the proviso that: (i) when A is phenyl, and Z is OH, X&#x2014;Y is other than C&#x2261;C&#x2014;(CH)COH, C&#x2261;C&#x2014;(CH)COMe, (CH)COH. Uses of such compounds as medicaments for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors are provided.

Modulator

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is ORor NRRwherein each of Rand Ris independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO-alkyl, alkenyl, CN, NH, hydroxy, halo, alkoxy, CFand nitro; Y is a polar functional group selected from OH, NO, CN, COR, COOR, NRR, CONRR, SOH, SO&#x2014;R, SONRRand CF, where each of Rand Ris independently H or a hydrocarbyl group; A is an aryl or heteroaryl group, each of which may be optionally substituted; and B is (CH2)where n is 0, 1, 2, 3, 4 or 5; with the proviso that: (i) when A is phenyl, n is 0, and Z is OH, X&#x2014;Y is other than meta-C&#x2261;&#x2014;C&#x2014;(CH)COH, meta-C&#x2261;&#x2014;C&#x2014;(CH)OH, meta-C&#x2261;C&#x2014;(CH)COMe, meta-(CH)COH, ortho-CHCOH, ortho-(CH)COH and ortho-(CH)COH; and (ii) when A is phenyl, n is 0, and Z is OMe, X&#x2014;Y is other than meta-C&#x2261;C&#x2014;(CH)OH. Further aspects of the invention relate to the use of such compounds in the preparation of a medicament for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors.

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London, United Kingdom

Gareth Pryce