University College London

Canbex Therapeutics Limited

Ucl Business Plc

Zeneca Limited

Ark Therapeutics Limited

Ludwig Institute for Cancer Research Limited

Genome Research Limited

Arktherapeutics Group, Plc

Ucl Cruciform Limited

David Lawrence Selwood

David Baker

Basil Hartzoulakis

Masahiro Okuyama

Ian Zachary

Gareth Pryce

Cristina Visintin

Haiyan Jia

Ashley Jarvis

Chris Chapman

Katie Ellard

Rosemary Lynch

Lili Cheng

Robert John Blade

Jamie Nally

Mark Stewart

Giti Garthwaite

Marcel Kling

Grant Wishart

Michelle Tickner

Yih Sang Pang

Xin Lu

Dana Davis

Michael Roland Duchen

Julia Marie Hill

Patrick John Thompson Vallance

James Mitchell Leiper

Justin Neil Darrel Warne

Sharon Rossiter

Patricia Kuwabara

Gyorgy Szabadkai

Adrian Hobbs

Marianne Lohr

Patrick John Vallance

The present invention relates to conjugates of cyclosporin with quinolium mitochondrial targeting groups, and their therapeutic uses.

Quinolinium conjugates of cyclosporin

The present invention provides a compound of formula I, a tautomer thereof, or a pharmaceutically acceptable salt or N-oxide thereof for use in the treatment or prevention of cardiovascular disease or of an inflammatory disease or condition: 

Agents for use in the treatment of cardiovascular and inflammatory diseases structurally based on 4(1 H)-quinolone

The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein: n is 0 or 1; R1 is selected from H, alkyl and aralkyl, wherein said alkyl and aralkyl groups may be optionally substituted by one or more OH groups; X is a group selected from &#x2014;C&#x2261;C&#x2014;(CH)&#x2014;; &#x2014;C(R)&#x2550;C(R)&#x2014;(CH)&#x2014;; and &#x2014;C(R)(R)C(R)(R)&#x2014;(CH)r-; where each of R, R, Rand Ris independently H or alkyl, and each of p, q and r is independently 1, 2, 3, 4 or 5; Y is a group selected from: CN; COOR; CONRR; SONRR; NRCOR; NRSOR; and a heterocyclic group selected from oxadiazolyl, thiazolyl, iso-thiazolyl, oxazolyl, iso-oxazolyl, pyrazolyl and imidazolyl; where each of R, Rand Ris independently H or alkyl; or Rand Rare linked, together with the nitrogen to which they are attached, to form a 5 or 6-membered heterocycloalkyl or heterocycloalkenyl group, said heterocycloalkyl or heterocycloalkenyl group optionally containing one or more further groups selected from O, N, CO and S, and where each of R, R, R, R, R, Rand Ris independently H or alkyl. 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, pain, or for controlling spasticity or tremors, for example, spasticity in MS. 

Benzamide derivatives useful in the treatment of muscular disorders and pain and for controlling spasticity and tremors

The present invention relates to a compound of formula (I) in crystalline form, wherein said compound is in the form of the free base or a pharmaceutically acceptable salt thereof, or a solvate of the free base or salt form thereof. The invention also relates to a pharmaceutical composition containing said crystalline form as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline form. 

Crystalline form of VSN16

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 process for preparing a compound of formula wherein: Ris cycloalkyl or alkyl, each of which may be optionally substituted; Y is &#x2014;CONRR, &#x2014;CN or COR; R, Rand Rare each independently H or alkyl; n is 1 to 6; wherein said process comprising the steps of: (i) treating a compound of formula (IV), where Ris alkyl, with a compound of formula (V) and forming a compound of formula (IIIb); (ii) treating said compound of formula (IIIb) with a compound of formula (I1) to form a compound of formula (I). 

Process for preparing carboxylic acid amides useful in the treatment of muscular disorders

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.

The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.

Arginine derivatives with NP-1 antagonistic activity

The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists. 

Arginine derivatives with NP-I antagonistic activity

Compounds of formula (I) have been found to be useful as inhibitors of DDAH. The present invention thus provides the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use in the treatment of a disease whose pathology is affected by DDAH 

Guanidine derivatives as inhibitors of DDAH

Compounds of Formula I and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.

Blockade of voltage dependent sodium channels

The invention relates to a polypeptide or part thereof which inhibits the apoptotic activity of the tumor suppressor protein p53, and includes screening methods to identify agents which interfere with the activity of the polypeptide.

Peptide inhibitors of IASPP

A peptide having part or all of the amino acid sequence QKRKRKKSRYKSWSVP (which is part of VEGF) has the ability to inhibit angiogenesis.

VEGF peptides and their use for inhibiting angiogenesis

Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple sclerosis.

Growing community of inventors

London, United Kingdom

David Lawrence Selwood