757240-99-6Relevant academic research and scientific papers
QUINAZOLINE DERIVATIVES AS TAM FAMILY KINASE INHIBITORS
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Paragraph 0182; 0183, (2015/06/08)
Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the modulation of the activity of, e.g., the inhibition of, one or more members of the TAM family kinases.
The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1- hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist
Arnold, Nicola,Beattie, David,Bradley, Michelle,Brearley, Andrew,Brown, Lyndon,Charlton, Steven J.,Fairhurst, Robin A.,Farr, David,Fozard, John,Fullerton, Joe,Gosling, Martin,Hatto, Julia,Janus, Diana,Jones, Darryl,Jordan, Lynne,Lewis, Christine,Maas, Janet,McCarthy, Clive,Mercer, Mark,Oakman, Helen,Press, Neil,Profit, Rachel,Schuerch, Friedrich,Sykes, David,Taylor, Roger J.,Trifilieff, Alexandre,Tuffnell, Andrew
, p. 4341 - 4347 (2014/10/15)
The optimisation of two series of 4-hydroxybenzothiazolone derived β2-adrenoceptor agonists, bearing α-substituted cyclopentyl and β-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 α-substituted cyclopentyl analogue 2 as the optimal compound with a comparable profile to the inhaled once-daily long-acting β2-adrenoceptor agonist indacaterol. On the basis of these data 2 was promoted as the backup development candidate to indacaterol from the Novartis LABA project.
Long-chain formoterol analogues: An investigation into the effect of increasing amino-substituent chain length on the β2-adrenoceptor activity
Alikhani, Vahid,Beer, David,Bentley, David,Bruce, Ian,Cuenoud, Bernard M.,Fairhurst, Robin A.,Gedeck, Peter,Haberthuer, Sandra,Hayden, Claire,Janus, Diana,Jordan, Lynne,Lewis, Christine,Smithies, Kirsty,Wissler, Elke
, p. 4705 - 4710 (2007/10/03)
The synthesis of a series of long-chain formoterol analogues in which the terminal ether residue of the β-phenethyl-amino-substituent has been extended beyond the methyl ether residue present in the parent compound are described. Evaluation of these analo
