5 research outputs found
Recommended from our members
Pyrazole derivatives for treating conditions mediated by activation of the adenosine a2b or a3 receptor
Compounds of formula (I) in free or salt form, wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating a condition mediated by activation of the adenosine Alb receptor or the adenosine A3 receptor, particularly an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described
Recommended from our members
5-phenyl-4-methyl-thiazol-2-yl-amine derivatives as inhibitors of phosphatidylinositol 3 kinase enzymes (pi3) for the treatment of inflammatory airway diseases
Compounds of Formula (I) in free or salt form, wherein Ra, Rb, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by mediated by phosphatidylinositol 3-kinase such as inflammatory airway diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described
Recommended from our members
Derives du 5-phenylthiazol et leurs utilisations comme inhibiteurs de la pi3 kinase
L'invention porte sur des composés de formule (I) sous forme libre ou de sels. Dans ladite formule, R1,R2,R3,R4, et R5, sont tels que définis dans la spécification et utilisables pour le traitement de maladies médiées par la phosphatidylinositol 3-kinase. L'invention porte également sur des préparations pharmaceutiques les contenant et sur leurs procédés de préparation
Recommended from our members
A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of ß2-adrenoceptor agonists as inhaled long-acting bronchodilators
The chiral synthesis of a 4-hydroxybenzothiazolone based series of ß2-adrenoceptor agonists is described. Using this methodology a library of N-substituted analogues were prepared for the rapid identification of leads with the potential to be fast onset and long-acting inhaled bronchodilators with improved therapeutic margins. The design of the library to achieve the targeted profile was based upon lipophilicity and metabolism based hypotheses. This approach identified ß-phenethyl, a-substituted cyclopentyl and monoterpene N-substituents to be of particular interest for further evaluation, as exemplified by structures 19, 29 and 33, respectively. © 2010 Elsevier Ltd. All rights reserved
Recommended from our members
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1- hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting ß2-adrenoceptor agonist
The optimisation of two series of 4-hydroxybenzothiazolone derived ß2-adrenoceptor agonists, bearing a-substituted cyclopentyl and ß-phenethyl amino-substituents, as inhaled long-acting bronchodilators is described. Analogues were selected for synthesis using a lipophilicity based hypothesis to achieve the targeted rapid onset of action in combination with a long duration of action. The profiling of the two series led to identification of the a-substituted cyclopentyl analogue 2 as the optimal compound with a comparable profile to the inhaled once-daily long-acting ß2-adrenoceptor agonist indacaterol. On the basis of these data 2 was promoted as the backup development candidate to indacaterol from the Novartis LABA project. © 2014 Elsevier Ltd. All rights reserved