Astex Therapeutics Limited

Heptares Therapeutics Limited

Cancer Research Technology Limited

The Institute of Cancer Research: Royal Cancer Hospital

Michael Alistair O'Brien

Miles Stuart Congreve

Maria Grazia Carr

Andrew James Woodhead

Alison Jo-Anne Woolford

Valerio Berdini

Adrian Liam Gill

Giles Albert Brown

Christopher William Murray

Paul Graham Wyatt

Gary Trewartha

Theresa Rachel Early

Benjamin Gerald Tehan

Mark Pickworth

Julie Elaine Cansfield

Barry John Teobald

Martyn Frederickson

Eva Figueroa Navarro

Mark David Rackham

Gianni Chessari

Robert Downham

Theresa Rachel Phillips

Andrew Madin

Gordon Saxty

Charlotte Mary Griffiths-Jones

Gilbert Besong

Richard David Taylor

David Livermore

Emma Vickerstaffe

Owen Callaghan

Kathryn White

Rajdeep Kaur Nijjar

Andrew Pike

Steven Howard

Neil Thomas Thompson

John Francis Lyons

Lynsey Helen Fazal

Alison Jo-Ann Woolford

Valerio 436 Cambridge Science Park Berdini

Maria Grazia 436 Cambridge Science Park Carr

Paul Graham 436 Cambridge Science Park Wyatt

Theresa Rachel 436 Cambridge Science Park Early

AdrianL 436 Cambridge Science Park Gill

Gary 436 Cambridge Science Park Trewartha

This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof, wherein Q, R, R, Rand Rare as defined herein. 

Bicyclic AZA compounds as muscarinic M1 receptor and/or M4 receptor

Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor

This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula 1, or a salt thereof wherein Q, R, R, Rand Rare as defined herein. 

Bicyclic aza compounds as muscarnic M1 receptor and/or M4 receptor antagonists

Bicyclic aza compounds as muscarinic M1 receptor and/or M4 receptor agonists

The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, Rand Rare as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain. 

Piperidin-1-yl and azepin-1-yl carboxylates as muscarinic M4 receptor agonists

Bicyclic AZA compounds as muscarinic M1 receptor and/or M4 receptor agonists

The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein Ris hydroxy or hydrogen; Ris hydroxy; methoxy or hydrogen; provided that at least one of Rand Ris hydroxy; Ris selected from hydrogen; halogen; cyano; optionally substituted Chydrocarbyl and optionally substituted Chydrocarbyloxy; Ris selected from hydrogen; a group &#x2014;(O)&#x2014;Rwhere n is 0 or 1 and Ris an optionally substituted acyclic Chydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-Chydrocarbyl-amino; or Rand Rtogether form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NRRforms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

Hydroxybenzamide derivatives and their use as inhibitors of HSP90

This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1), or a salt thereof, wherein Q, R, R, Rand Rare as defined herein. 

The present invention provides muscarinic Mreceptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, Rand Rare as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain. 

The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3.  In formula (0):

3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinase and glycogen synthase kinase-3 modulators

The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Bicyclic heterocyclic compounds as FGFR inhibitors

The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof, and combinations thereof with other anti-cancer agents, for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. 

The invention provides a compound for use in medicine, the compound being a compound of the formula (VI) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; Ris hydrogen, hydroxy, or O&#x2014;R; Ris hydroxy, methoxy or O&#x2014;R; provided that at least one of Rand Ris O&#x2014;R; Ris L-R; SOH; a glucuronide residue; a mono-, di- or tripeptide residue; or Lis a bond, C&#x2550;O, (C&#x2550;O)O, (C&#x2550;O)NRor S(O)NR; x is 1 or 2; Ris hydrogen or a an optionally substituted Chydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that Ris not hydrogen when Lis a bond, C&#x2550;O or (C&#x2550;O)O; and provided also that O&#x2014;Rdoes not contain an O&#x2014;O moiety; and excluding compounds wherein Ris hydroxy and Ris methoxy; Rand Rare the same or different and each is a group R; and R, R, Rand Rare defined in the claims. The compounds of formula (VI) are pro-drugs of parent compounds wherein Rand/or Rare hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.

Pharmaceutical compounds

The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.

Therapeutic combinations of hydroxybenzamide derivatives as inhibitors of HSP90

The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.

Imidazo[1,2-a]pyridine compounds for use in treating cancer

Growing community of inventors

Hitchin, United Kingdom

Michael Alistair O'Brien