Chiesi Farmaceutici S.p.a.

Pulmagen Therapeutics (Inflammation) Limited

Pulmagen Therapeutics (Asthma) Limited

Pulmagen Therapeutics (Synergy) Limited

Argenta Discovery Limited

Pulmagen Therapeutics Limited

Harry Finch

Christine Edwards

John Gary Montana

George Hynd

Craig Fox

Rosa Arienzo

Nicholas Charles Ray

Monique Bodil Van Niel

Justian Craig Fox

Mary Frances Fitzgerald

Janusz Jozef Kulagowski

Karen Williams

Andrew Forrest

Mohammed Sajad

Michael Colin Cramp

Chi-Kit Woo

Neville McLean

Monique Bondil Van Niel

Elizabeth O'Connor

Bohdan Waszkowycz

Richard James Bull

Jamie Knight

Trevor Keith Harrison

Yann Griffon

Peter Crackett

John Montana

Vidya Ramdas

Mathias Domostoj

Barbara Avitabile-Woo

Janus Kulagowski

Marco Van Den Heuvel

Jose Antonio Bravo

Elizabeth O'CONNOR

Paul Matthew Blaney

David Middlemiss

Yan A Griffon

Disclosed are compounds having [1,2,4]triazolo[4,3-a]pyridine groups and pharmaceutically acceptable salts thereof. The compounds are p38 MAPK inhibitors, useful as anti-inflammatory agents in the treatment of, inter alia, diseases of the respiratory tract.

Kinase inhibitors

Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C&#x2014;Ror N; &#x2014;X&#x2014;X&#x2014; is CR&#x2550;N&#x2014; or &#x2014;NR&#x2014;CO&#x2014;; and R-R, R, Rand Rare as defined in the claims. 

Pyrimidine derivatives and their use in the treatment of respiratory diseases such a COPD

Compounds of formula (I) are inhibitors of neutrophil elastase, wherein A is C&#x2014;Ror N; &#x2014;X&#x2014;X&#x2014; is CR&#x2550;N&#x2014; or &#x2014;NR&#x2014;CO&#x2014;; and R-R, Rand Rare as defined in the claims. 

Pyrimidine derivatives and their use in the treatment of respiratory diseases such as COPD

There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery.

Inhaled combination therapy

A pharmaceutical composition adapted for pulmonary administration by inhalation is described, wherein the composition comprises a glitazone and one or more pharmaceutically acceptable carriers and/or excipients, wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer, and wherein the glitazone is pioglitazone or rosiglitazone or a pharmaceutically acceptable salt thereof, and wherein the glitazone is in the form of microparticles.

Respiratory disease treatment

The subject invention provides compounds of formula (I): Including monomers and multimers thereof that are inhibitors of human neutrophil elastase (HNE) activity and are useful in the treatment of diseases or conditions in which HNE plays a part.

Tetrahydropyrrolopyrimidinediones and their use in therapy

There is provided a pharmaceutical composition that is adapted for pulmonary administration by inhalation, which composition comprises a glitazone, such as pioglitazone or rosiglitazone, and one or more pharmaceutically acceptable carriers and/or excipients, and wherein the glitazone content of the composition consists of at least 95% by weight of the 5R enantiomer and less than 5% by weight of the 5S enantiomer. There is also provided a use and kit.

Compounds of formula (I) are inhibitors of p38 MAP kinase, useful as anti-inflammatory agents in the treatment of inter alia, diseases of the respiratory tract wherein; Ris C-Calkyl, C-Ccycloalkyl, phenyl which is optionally substituted, 5- or 6 membered monocyclic heteroaryl which is optionally substituted, or a radical of formula (II) wherein n is 1 or 2, and Rand Rare independently H or C-Calkyl, or Rand Rtaken together with the nitrogen to which they are attached form a 6-membered heterocyclic ring optionally containing a further heteroatom selected from N and O; Y is &#x2014;O&#x2014; or &#x2014;S(O)&#x2014; wherein p is 0, 1 or 2; A is an optionally substituted divalent arylene radical, or a mono- or bicyclic heteroarylene radical, or a C-Cdivalent cycloalkylene radical having 5 or 6 ring atoms, or a piperidinylene radical wherein the ring nitrogen is linked to RNHC(&#x2550;O)W&#x2014;; W is a bond, &#x2014;NH&#x2014; or &#x2014;C(R)(R), wherein Rand Rare independently H, methyl, ethyl, amino, hydroxyl or halo; and Ris a radical as defined in the claims. 

Triazolopyridine derivatives and their therapeutic use

The compound of formula (I) is an inhibitor of human neutrophil elastase, useful for inhalation treatment of pulmonary inflammation. 

Pyrrolopyrimidinedione and its therapeutic use

Combination of methylxanthine compounds and steroids to treat chronic respiratory diseases

Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is &#x2014;SO&#x2014; or *&#x2014;SONR&#x2014; wherein the bond marked with an asterisk is attached to Ar; Ris hydrogen, fluoro, chloro, CN or CF; Ris hydrogen, fluoro or chloro; Ris hydrogen, CCalkyl or C-Ccycloalkyl; Aris phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C-Ccycloalkyl, &#x2014;O(C-Calkyl) or CCalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Aris phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C-C-Ccycloalkyl, &#x2014;O(C-Calkyl) or CCalkyl, the latter two groups being optionally substituted by one or more fluoro atoms. 

Indoles and their therapeutic use

Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: Ris halogen or cyano; Ris hydrogen or methyl; Rand Rare independently &#x2014;OR, C-Calkyl or C-Ccycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; Ris hydrogen or halogen; Ris CCalkyl or C-Ccycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is &#x2014;CH&#x2014;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; one of Y and Yis hydrogen and the other is OR, &#x2014;C(&#x2550;O)R, NRSORor a heterocyclic group selected from those referred to in the specification; and R, Rand Rare as defined in the specification.

Quinolines and their therapeutic use

Compounds of formula (I) are agonists of PPAR&#x3b3;, useful for the treatment of respiratory disease; formula (I): wherein R, Ror Reach independently represents halo, cyano, nitro, amino, alkyl, haloalkyl, alkoxy, haloalkoxy, carboxylic acid or an ester or amide thereof; Rrepresents hydrogen or alkyl; m, n or p independently represents 0, 1, 2 or 3. 

Sulfonamide compounds for the treatment of respiratory disorders

Growing community of inventors

Essex, United Kingdom

Harry Finch