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Page 1
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.
Cumming IA, Degorce SL, Aagaard A, Braybrooke EL, Davies NL, Diène CR, Eatherton AJ, Felstead HR, Groombridge SD, Lenz EM, Li Y, Nai Y, Pearson S, Robb GR, Scott JS, Steward OR, Wu C, Xue Y, Zhang L, Zhang Y. Cumming IA, et al. Among authors: robb gr. Bioorg Med Chem. 2022 Jun 1;63:116729. doi: 10.1016/j.bmc.2022.116729. Epub 2022 Apr 2. Bioorg Med Chem. 2022. PMID: 35439688
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: robb gr. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, Wu D. Scott JS, et al. Among authors: robb gr. J Med Chem. 2017 Dec 28;60(24):10071-10091. doi: 10.1021/acs.jmedchem.7b01290. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29172502
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Degorce SL, Anjum R, Dillman KS, Drew L, Groombridge SD, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Scott JS, Stokes S, Xue Y. Degorce SL, et al. Among authors: robb gr. Bioorg Med Chem. 2018 Feb 15;26(4):913-924. doi: 10.1016/j.bmc.2018.01.008. Epub 2018 Jan 17. Bioorg Med Chem. 2018. PMID: 29398441
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Pike KG, Barlaam B, Cadogan E, Campbell A, Chen Y, Colclough N, Davies NL, de-Almeida C, Degorce SL, Didelot M, Dishington A, Ducray R, Durant ST, Hassall LA, Holmes J, Hughes GD, MacFaul PA, Mulholland KR, McGuire TM, Ouvry G, Pass M, Robb G, Stratton N, Wang Z, Wilson J, Zhai B, Zhao K, Al-Huniti N. Pike KG, et al. J Med Chem. 2018 May 10;61(9):3823-3841. doi: 10.1021/acs.jmedchem.7b01896. Epub 2018 May 2. J Med Chem. 2018. PMID: 29683659
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, Goldberg K, Hassall LA, Hughes GD, MacFaul PA, McGuire TM, Pass M, Patel A, Pearson S, Petersen J, Pike KG, Robb G, Stratton N, Xin G, Zhai B. Barlaam B, et al. ACS Med Chem Lett. 2018 Jul 13;9(8):809-814. doi: 10.1021/acsmedchemlett.8b00200. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128072 Free PMC article.
59 results