883195-34-4Relevant academic research and scientific papers
Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors
Fairhurst, Robin A.,Gerspacher, Marc,Imbach-Weese, Patricia,Mah, Robert,Caravatti, Giorgio,Furet, Pascal,Fritsch, Christine,Schnell, Christian,Blanz, Joachim,Blasco, Francesca,Desrayaud, Sandrine,Guthy, Daniel A.,Knapp, Mark,Arz, Dorothee,Wirth, Jasmin,Roehn-Carnemolla, Esther,Luu, Van Huy
, p. 3575 - 3581 (2015/08/06)
Abstract A cyclisation within a 4′,5-bisthiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors led to a novel 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole tricyclic sub-series. The synthesis and optimisation of this 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole sub-series and the expansion to a related tricyclic 4,5-dihydrothiazolo[4,5-h]quinazoline sub-series are described. From this work analogues including 11, 12, 19 and 23 were identified as potent and selective PI3Kα inhibitor in vivo tool compounds.
2-Carboxamide Cycloamino Ureas
-
Page/Page column 23, (2011/01/12)
The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol
PI3 KINASES
-
Page/Page column 138-139, (2008/06/13)
The invention relates to the novel compounds of formula (1), which, due to their pharmaceutical effect as PI3 kinase modulators, are suitable for use in the therapy and treatment of inflammatory or allergic diseases. Examples of these diseases are inflammatory and allergic respiratory diseases, inflammatory diseases of the gastro-intestinal system and of the locomotor apparatus, inflammatory and allergic skin diseases, inflammatory ophthalmic diseases, diseases of the nasal mucosa, inflammatory or allergic autoimmune reactive conditions, or renal inflammations.
