Astex Therapeutics Limited

Cancer Research Technology Limited

The Institute of Cancer Research: Royal Cancer Hospital

Glaxo Group Limited

University of Dundee

Smithkline Beecham Corporation

Paul Graham Wyatt

Valerio Berdini

Gary Trewartha

Maria Grazia Carr

Adrian Liam Gill

Alison Jo-Anne Woolford

Michael Alistair O'Brien

Andrew James Woodhead

Theresa Rachel Early

Gordon Saxty

Ian James Collins

Robert George Boyle

David Winter Walker

Steven Woodhead

David Charles Rees

Mladen Vinkovic

Steven Howard

Alan D Borthwick

John Liddle

Deirdre Mary Bernadette Hickey

Andrew McMurtrie Mason

Robert Downham

Anna Katrin Szardenings

Eva Figueroa Navarro

Neil Derek Miller

Steven Leslie Sollis

Marinus Leendert Verdonk

John Caldwell

David George Hubert Livermore

Hannah Fiona Sore

Robin Arthur Ellis Carr

Alastair Donald

Tatiana Faria Da Fonseca

Richard Jonathan Hatley

Fabrizio Nerozzi

Stephen Brand

Ian Gilbert

Neil Norcross

Laura Cleghorn

Stephen Thompson

Victoria Smith

Tracy Bayliss

Justin Harrison

Ruth Brenk

Miles Stuart Congreve

Neil Thomas Thompson

John Francis Lyons

Marc O'Reilly

Jayne Elizabeth Curry

Kyla Merriom Thompson

Michael Alistair O'brien

Matthew Simon Squires

Harren Jhoti

Steven John Woodhead

Alison Jo-Ann Woolford

Valerio 436 Cambridge Science Park Berdini

The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.

N-myristoyl transferase inhibitors

The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between Rand NRRand a maximum chain length of 4 atoms extending between E and NRR, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom &#x3b1; with respect to the NRRgroup and provided that the oxo group when present is located at a carbon atom &#x3b1; with respect to the NRRgroup; Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

Pyrazole derivatives as protein kinase modulators

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 provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR; J-Jis N&#x2550;C(R), (R)C&#x2550;N, (R)N&#x2014;C(O), (R)C&#x2014;C(O), N&#x2550;N or (R)C&#x2550;C(R); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Qis a bond or a saturated Chydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRor NRCO where Ris hydrogen or methyl, or Ris a Calkylene chain linked to R or a carbon atom of Qto form a cyclic moiety; and wherein the carbon atoms of the linker group Qmay optionally bear one or more substituents selected from fluorine and hydroxy; Qis a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Qis other than a bond; G is hydrogen, NRR, OH or SH provided that when E is aryl or heteroaryl and Qis a bond, then G is hydrogen; Ris hydrogen or an aryl or heteroaryl group, with the proviso that when Ris hydrogen and G is NRR, then Q is a bond; and R, R, R, Rand Rare as defined in the claims. 

Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein

The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR; J-Jis N&#x2550;C(R), (R)C&#x2550;N, (R)N&#x2014;C(O), (R)C&#x2014;C(O), N&#x2550;N or (R)C&#x2550;C(R); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Qis a bond or a saturated Chydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRor NRCO where Ris hydrogen or methyl, or Ris a Calkylene chain linked to Ror a carbon atom of Qto form a cyclic moiety; and wherein the carbon atoms of the linker group Qmay optionally bear one or more substituents selected from fluorine and hydroxy; Qis a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Qis other than a bond; G is hydrogen, NRR, OH or SH provided that when E is aryl or heteroaryl and Qis a bond, then G is hydrogen; Ris hydrogen or an aryl or heteroaryl group, with the proviso that when Ris hydrogen and G is NRR, then Qis a bond; and R, R, R, Rand Rare as defined in the claims. 

Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases 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 of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R', E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase. 

Pyrazole compounds that modulate the activity of CDK, GSK and aurora kinases

The invention provides compounds of the formula (I) having protein kinase B inhibiting activity:  Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (Ic) or salts, tautomers or N-oxides thereof. 

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of the formula (I) or a pharmaceutically acceptable salt thereof.

Substituted diketopiperazines as oxytocin antagonists

The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): or salts or tautomers or N-oxides or solvates thereof;wherein

Combinations of pyrazole kinase inhibitors

A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.

The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.

4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide acid addition salts as kinase inhibitors

The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between Rand NRRand a maximum chain length of 4 atoms extending between E and NRR, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NRRgroup and provided that the oxo group when present is located at a carbon atom a with respect to the NRRgroup; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; Ris an aryl or heteroaryl group; and R, R, Rand Rare as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents. 

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Perth, United Kingdom

Paul Graham Wyatt