Pulmagen Therapeutics (Asthma) Limited

Pulmagen Therapeutics Limited

Michael Colin Cramp

John Gary Montana

George Hynd

Harry Finch

Nicholas Charles Ray

Rosa Arienzo

Neville McLean

Peter Crackett

Yann Griffon

Trevor Keith Harrison

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

Michael Colin Cramp