260246-17-1Relevant articles and documents
Discovery of an Orally Bioavailable Pan αv Integrin Inhibitor for Idiopathic Pulmonary Fibrosis
Anderson, Niall A.,Campos, Sebastien,Butler, Sharon,Copley, Royston C. B.,Duncan, Ian,Harrison, Stephen,Le, Joelle,Maghames, Rosemary,Pastor-Garcia, Aleix,Pritchard, John M.,Rowedder, James E.,Smith, Claire E.,Thomas, Jack,Vitulli, Giovanni,Macdonald, Simon J. F.
supporting information, p. 8796 - 8808 (2019/10/16)
The heterodimeric transmembrane αv integrin receptors have recently emerged as potential targets for the treatment of idiopathic pulmonary fibrosis. Herein, we describe how subtle modifications of the central aromatic ring of a series of phenylbutyrate-based antagonists of the vitronectin receptors αvβ3 and αvβ5 significantly change the biological activities against αvβ6 and αvβ8. This resulted in the discovery of a pan αv antagonist (compound 39, 4-40 nM for the integrin receptors named above) possessing excellent oral pharmacokinetic properties in rats (with a clearance of 7.6 mL/(min kg) and a bioavailability of 97%).
SUBSTITUTED OXAZOLE- AND THIAZOLE-BASED CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS II
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Page/Page column 21-23, (2016/06/14)
The invention relates to oxazole and thiazole-based carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Baccatin derivatives and a process for producing the same
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, (2008/06/13)
The object of the invention is to develop baccatin derivatives useful for preparing taxoid compounds such as paclitaxel and a process for the producing the same. The invention provides baccatin derivatives represented by the general formula (I) as well as a process for producing baccatin derivatives represented by the general formula (I) above, which comprises allowing a baccatin represented by the general formula (II) to react with a β-ketoester in the absence of a catalyst or in the presence of a tin compound or an amine base, preferably under reduced pressure.