Astrazeneca Ab

Topivert Pharma Limited

Inflazome Limited

Respivert Limited

Dainippon Sumitomo Pharma Co., Ltd.

Astra Zeneca U.k. Limited

Astra Pharmaceuticals Limited

Sumitomo Dainippon Pharma Co., Ltd.

Sitryx Therapeutics Limited

Oxular Acquisitions Limited

Stephen Thom

Matthew Colin Thor Fyfe

Roger Victor Bonnert

Premji Meghani

David Miller

Thomas McInally

Jonathan Shannon

Angus Macleod

Stephen St-Gallay

Matthew Cooper

Timothy Jon Luker

Nicholas David Kindon

Anil Patel

Thomas Matthew Baker

Garry Pairaudeau

Jimmy Van Wiltenburg

Andrew Baxter

Rukhsana Tasneem Mohammed

Geraint Jones

Stuart Thomas Onions

Stephen Brough

Bryan Glyn Roberts

Gareth Harbottle

Anthony Ronald Cook

Hiroki Wada

Brian Springthorpe

Kazuhiro Ito

John King-Underwood

Peter John Murray

Yoshiaki Isobe

Catherine Elisabeth Charron

Matthew Wd Perry

Euan Alexander Fraser Fordyce

Jonathan Gareth Williams

Paul Andrew Willis

Lilian Alcaraz

Michael Knaggs

David Cousin

Austen Pimm

Mark Dickinson

Ian Strutt

Aaron Rigby

Nicholas James Bennett

Thomas Alanine

Vedran Hasimbegovic

Andrew Bailey

Colin Peter Sambrook-Smith

Jokin Carrillo Arregui

Tobias Mochel

Rukhsana Tanseem Mohammed

Anna-Karin Tidén

Richard Evans

Rukhsana Rasul

Michael Liam Cooke

Ian Millichip

Thomas Mcinally

Fritz-Frieder Frickel

Daniel Hamza

Roger Brown

Nicholas Kindor

David Harden

David Marriott

Paul Leeson

Daniel Schwizer

Phillip Abbott

Thomas Michael Waugh

Barry John Teobald

Satoshi Onuma

Sascha Breeger

Andrew Davies

Matthew Alexander Henry Stent

Claire Anne Walshe

Tom McInally

Claire Anne Marie Cariou

Judith McInally

Hayley Tegan Angela Watson

Gareth William Harbottle

Andrew Davis

Andrew Cook

The invention relates to compounds of formula (IW-1) and to their use in treating or preventing an inflammatory disease or a disease associated with an undesirable immune response: wherein R, R, Rand Rare as defined herein.

Itaconic acid derivatives and uses thereof intreating an inflammatory disease or a disease associated with an undesirable immune response

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl group substituted with a monovalent heteroaryl-containing group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

Sulfonamide carboxamide compounds

The present invention relates to sulfonylureas and sulfonylthioureas comprising as-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with at least one group containing an oxygen atom, and wherein said oxygen atom is attached to the heteroaryl ring via at least two other atoms. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

The present invention relates to compounds of formula (I) wherein Q is selected from O or S; Ris a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein Ris attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein Rmay optionally be substituted; and Ris a cyclic group substituted at the α-position, wherein Rmay optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

The present invention relates to sulfonylureas and sulfonylthioureas comprising a monocyclic imidazolyl group of formula (I):

Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors

The present invention relates to compounds of formula (I): Formula (I) wherein Q is selected from O or S; L is a saturated or unsaturated, optionally substituted C-Chydrocarbylene group optionally including one or more heteroatoms N, O or S; Ris &#x2014;NRR, &#x2014;OR, &#x2014;(C&#x2550;NR)R, &#x2014;(CO)R, &#x2014;CN, &#x2014;N, a quaternary ammonium group or an optionally substituted heterocycle; R, R, R, R, Rand Rare each independently hydrogen or a saturated or unsaturated, optionally substituted C-Chydrocarbyl group optionally including one or more heteroatoms N, O or S; wherein optionally L and R, or L and R, or Rand R, or L and R, or L and R, or L and R, or Rand R, or L and Rtogether with the atom(s) to which they are attached may form a 3- to 12-membered, saturated or unsaturated, optionally substituted cyclic group; and Ris a cyclic group substituted at the a-position, wherein Rmay optionally be further substituted; provided that the atom of L which is attached to the sulfur atom of the sulfonylurea group is a carbon atom and is not a ring atom of a heterocyclic or aromatic group. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

The present invention relates to processes of preparing N-((1,2,3,4,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)-1-iso-propyl-1H-pyrazole-3-sulfonamide and salts thereof. The present invention further relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.

Processes

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; Ris a saturated or unsaturated hydrocarbyl group, wherein the hydrocarbyl group may be straight-chained or branched, or be or include cyclic groups, wherein the hydrocarbyl group may optionally be substituted, and wherein the hydrocarbyl group may optionally include one or more heteroatoms N, O or S in its carbon skeleton; and Ris a cyclic group substituted at the a-position, wherein Rmay optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 

Compounds

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R' wherein Rcontains from 1 to 7 atoms other than hydrogen or halogen. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

Sulfonylureas and sulfonylthioureas as NLRPinhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is di-substituted at the 3- and 4-positions relative to the point of attachment of the sulfonyl group, wherein at least one of the di-substituents contains a nitrogen atom. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; Ris a saturated or unsaturated, optionally substituted C-Chydrocarbyl group, wherein the atom of Rwhich is attached to the sulfur atom of the sulfonylurea group is not a ring atom of a cyclic group; and Ris a cyclic group substituted at the &#x3b1;-position, wherein Rmay optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP. 

The present invention relates to compounds of formula (I): wherein Q is selected from O or S; Ris a non-aromatic heterocyclic group comprising at least one ring nitrogen atom, wherein Ris attached to the sulfur atom of the sulfonylurea group by a ring carbon atom, and wherein Rmay optionally be substituted; and Ris a cyclic group substituted at the &#x3b1;-position, wherein Rmay optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

The present invention relates to compounds of formula (I): wherein Q is O or S, Ris a 6-membered heteroaryl group containing at least one nitrogen atom in the 6-membered ring structure, wherein Rmay optionally be substituted, and Ris a cyclic group substituted at the &#x3b1;-position, wherein Rmay optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.

There are provided compounds of formula I, wherein Rto R, Rto R, R, L and Xto Xhave meanings given in the description, which compounds have anti-inflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Kinase inhibitors

There are provided compounds of: wherein T, A, Q, Z, R, R, R, n, r, Hetand Rhave meanings given in the description, which compounds are useful in synthesizing compounds that have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Growing community of inventors

Loughborough, United Kingdom

Stephen Thom