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N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Hennequin LF, Allen J, Breed J, Curwen J, Fennell M, Green TP, Lambert-van der Brempt C, Morgentin R, Norman RA, Olivier A, Otterbein L, Plé PA, Warin N, Costello G. Hennequin LF, et al. J Med Chem. 2006 Nov 2;49(22):6465-88. doi: 10.1021/jm060434q. J Med Chem. 2006. PMID: 17064066
Discovery of 9-(1-anilinoethyl)-2-morpholino-4-oxo-pyrido[1,2-a]pyrimidine-7-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Giordanetto F, Green S, Inghardt T, Hennequin L, Hancox U, Lambert-van der Brempt C, Morgentin R, Pass S, Plé P, Saleh T, Ward L. Barlaam B, et al. Among authors: lambert van der brempt c. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3928-35. doi: 10.1016/j.bmcl.2014.06.040. Epub 2014 Jun 21. Bioorg Med Chem Lett. 2014. PMID: 24992874
Discovery of (R)-8-(1-(3,5-difluorophenylamino)ethyl)-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6-carboxamide (AZD8186): a potent and selective inhibitor of PI3Kβ and PI3Kδ for the treatment of PTEN-deficient cancers.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Pasquet MJ, Péru A, Plé P, Saleh T, Vautier M, Walker M, Ward L, Warin N. Barlaam B, et al. Among authors: lambert van der brempt c. J Med Chem. 2015 Jan 22;58(2):943-62. doi: 10.1021/jm501629p. Epub 2015 Jan 7. J Med Chem. 2015. PMID: 25514658
Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.
Barlaam B, Anderton J, Ballard P, Bradbury RH, Hennequin LF, Hickinson DM, Kettle JG, Kirk G, Klinowska T, Lambert-van der Brempt C, Trigwell C, Vincent J, Ogilvie D. Barlaam B, et al. Among authors: lambert van der brempt c. ACS Med Chem Lett. 2013 May 31;4(8):742-6. doi: 10.1021/ml400146c. eCollection 2013 Aug 8. ACS Med Chem Lett. 2013. PMID: 24900741 Free PMC article.
Discovery of a series of 8-(2,3-dihydro-1,4-benzoxazin-4-ylmethyl)-2-morpholino-4-oxo-chromene-6-carboxamides as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Péru A, Plé P, Saleh T, Ward L, Warin N. Barlaam B, et al. Among authors: lambert van der brempt c. Bioorg Med Chem Lett. 2016 May 1;26(9):2318-23. doi: 10.1016/j.bmcl.2016.03.034. Epub 2016 Mar 11. Bioorg Med Chem Lett. 2016. PMID: 26996374
Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3Kβ/δ inhibitors for the treatment of PTEN-deficient tumours.
Barlaam B, Cosulich S, Degorce S, Ellston R, Fitzek M, Green S, Hancox U, Lambert-van der Brempt C, Lohmann JJ, Maudet M, Morgentin R, Plé P, Ward L, Warin N. Barlaam B, et al. Among authors: lambert van der brempt c. Bioorg Med Chem Lett. 2017 May 1;27(9):1949-1954. doi: 10.1016/j.bmcl.2017.03.027. Epub 2017 Mar 14. Bioorg Med Chem Lett. 2017. PMID: 28347666
19 results