Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88 ^L265P Mutant Diffuse Large B Cell Lymphoma.

Autor: Degorce SL; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Anjum R; Bioscience, Oncology R&D , AstraZeneca, Boston , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Bloecher A; Bioscience, Oncology R&D , AstraZeneca, Boston , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Carbajo RJ; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Dillman KS; Bioscience, Oncology R&D , AstraZeneca, Boston , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Drew L; Bioscience, Oncology R&D , AstraZeneca, Boston , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Halsall CT; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Lenz EM; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Lindsay NA; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Mayo MF; Bioscience, Oncology R&D , AstraZeneca, Boston , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Pink JH; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Robb GR; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Rosen A; Bioscience, Oncology R&D , AstraZeneca, Boston , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Scott JS; Medicinal Chemistry, Oncology R&D , AstraZeneca , Cambridge Science Park , Unit 310 Darwin Building, Cambridge CB4 0WG , U.K., Xue Y; Discovery Sciences, R&D , AstraZeneca , Gothenburg SE-431 83 , Mölndal , Sweden.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2019 Nov 14; Vol. 62 (21), pp. 9918-9930. Date of Electronic Publication: 2019 Nov 01.

Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88 ^L265P Diffuse Large B-Cell Lymphoma.

Autor: Scott JS; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Degorce SL; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Anjum R; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Culshaw J; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Davies RDM; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Davies NL; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Dillman KS; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Dowling JE; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Drew L; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Ferguson AD; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Groombridge SD; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Halsall CT; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Hudson JA; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Lamont S; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Lindsay NA; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Marden SK; Pharmaceutical Sciences, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Mayo MF; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Pease JE; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Perkins DR; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Pink JH; Oncology, IMED Biotech Unit, AstraZeneca , Macclesfield SK10 4TG, United Kingdom., Robb GR; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Rosen A; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., Shen M; Oncology, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States., McWhirter C; Oncology, IMED Biotech Unit, AstraZeneca , Cambridge CB4 0FZ, United Kingdom., Wu D; Pharmaceutical Sciences, IMED Biotech Unit, AstraZeneca , Boston, Massachusetts 02451, United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2017 Dec 28; Vol. 60 (24), pp. 10071-10091. Date of Electronic Publication: 2017 Dec 11.

Regioselective Synthesis of 3-Hydroxy-4,5-alkyl-Substituted Pyridines Using 1,3-Enynes as Alkynes Surrogates.

Autor: Barday M; Department of Chemistry, University of Liverpool , Crown Street, Liverpool L69 7ZD, United Kingdom., Ho KY; Department of Chemistry, University of Liverpool , Crown Street, Liverpool L69 7ZD, United Kingdom., Halsall CT; Oncology Innovative Medicines Unit, AstraZeneca , Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom., Aïssa C; Department of Chemistry, University of Liverpool , Crown Street, Liverpool L69 7ZD, United Kingdom.

Publikováno v: Organic letters [Org Lett] 2016 Apr 15; Vol. 18 (8), pp. 1756-9. Date of Electronic Publication: 2016 Mar 31.