Pulmagen Therapeutics (Asthma) Limited

Pulmagen Therapeutics Limited

Rosa Arienzo

John Gary Montana

George Hynd

Harry Finch

Nicholas Charles Ray

Michael Colin Cramp

Neville McLean

Barbara Avitabile-Woo

Mathias Domostoj

Peter Crackett

Yann Griffon

Trevor Keith Harrison

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 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 C-Calkyl 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. 

Compounds of formula [1] are CRTH2 antagonists, useful in the treatment of conditions having an inflammatory components; in which: R-Rare various substituents; A is &#x2014;CHR&#x2014;, &#x2014;C(O)&#x2014;, &#x2014;S(O)n&#x2014;, &#x2014;O&#x2014;, or &#x2014;NR&#x2014; wherein n is an integer from 0-1 and Ris selected from various substituents; B is a direct bond or a divalent radical; Rand Rare selected from cvarious substituents; X is a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid group, or a group of formula C&#x2550;(O)NHSORor SONHC(&#x2550;O)R; and Y is aryl, heteroaryl, aryl-fused-heterocycloalkyl, heteroaryl-fused-cycloalkyl, heteroaryl-fused-heterocycloalkyl or aryl-fused-cycloalkyl group. 

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Essex, United Kingdom

Rosa Arienzo