Bifunctional Imine Reductase Cascades for the Synthesis of Saturated N -Heterocycles.

Autor: Ramsden JI; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Zucoloto da Costa B; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Heath RS; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Marshall JR; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Derrington SR; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Mangas-Sanchez J; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Montgomery SL; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K., Mulholland KR; Chemical Development, Pharmaceutical Technology and Development, Operations, AstraZeneca, Silk Road Business Park, Macclesfield SK10 2NA, U.K., Cosgrove SC; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K.; School of Chemical and Physical Sciences and Keele Centre for Glycoscience, Keele University, Keele ST5 5BG, U.K., Turner NJ; Manchester Institute of Biotechnology, Department of Chemistry, University of Manchester, 131 Princess Street, Manchester M1 7DN, U.K.

Publikováno v: ACS catalysis [ACS Catal] 2024 Sep 19; Vol. 14 (19), pp. 14703-14710. Date of Electronic Publication: 2024 Sep 19 (Print Publication: 2024).

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).

Autor: Pike KG; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Barlaam B; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Cadogan E; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Campbell A; Pharmaceutical Sciences , AstraZeneca , Silk Road Business Park, Macclesfield SK10 2NA , U.K., Chen Y; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States., Colclough N; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Davies NL; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., de-Almeida C; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Degorce SL; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K.; Oncology, IMED Biotech Unit , AstraZeneca, Centre de Recherches, Z. I. la Pompelle , BP 1050, 51689 Reims Cedex 2 , France., Didelot M; Oncology, IMED Biotech Unit , AstraZeneca, Centre de Recherches, Z. I. la Pompelle , BP 1050, 51689 Reims Cedex 2 , France., Dishington A; Oncology, IMED Biotech Unit , AstraZeneca , Alderley Park , Macclesfield , Cheshire SK10 4TG , U.K., Ducray R; Oncology, IMED Biotech Unit , AstraZeneca, Centre de Recherches, Z. I. la Pompelle , BP 1050, 51689 Reims Cedex 2 , France., Durant ST; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Hassall LA; Oncology, IMED Biotech Unit , AstraZeneca , Alderley Park , Macclesfield , Cheshire SK10 4TG , U.K., Holmes J; Oncology, IMED Biotech Unit , AstraZeneca , Alderley Park , Macclesfield , Cheshire SK10 4TG , U.K., Hughes GD; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., MacFaul PA; Oncology, IMED Biotech Unit , AstraZeneca , Alderley Park , Macclesfield , Cheshire SK10 4TG , U.K., Mulholland KR; Chemical Development , AstraZeneca , Silk Road Business Park , Macclesfield SK10 2NA , U.K., McGuire TM; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Ouvry G; Oncology, IMED Biotech Unit , AstraZeneca, Centre de Recherches, Z. I. la Pompelle , BP 1050, 51689 Reims Cedex 2 , France., Pass M; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Robb G; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Stratton N; Discovery Sciences , AstraZeneca , Alderley Park , Macclesfield , Cheshire SK10 4TG , U.K., Wang Z; Pharmaron Beijing Co., Ltd. , 6 Taihe Road BDA , Beijing 100176 , P.R. China., Wilson J; Oncology, IMED Biotech Unit , AstraZeneca , Building 310, Cambridge Science Park, 319 Milton Road , Cambridge CB4 0WG , U.K., Zhai B; Pharmaron Beijing Co., Ltd. , 6 Taihe Road BDA , Beijing 100176 , P.R. China., Zhao K; Pharmaron Beijing Co., Ltd. , 6 Taihe Road BDA , Beijing 100176 , P.R. China., Al-Huniti N; Oncology, IMED Biotech Unit , AstraZeneca , 35 Gatehouse Drive , Waltham , Massachusetts 02451 , United States.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2018 May 10; Vol. 61 (9), pp. 3823-3841. Date of Electronic Publication: 2018 May 02.

An ( R )-Imine Reductase Biocatalyst for the Asymmetric Reduction of Cyclic Imines.

Autor: Hussain S; School of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, Manchester, M1 7DN (UK)., Leipold F; School of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, Manchester, M1 7DN (UK)., Man H; Department of Chemistry, University of York, Heslington, York, YO10 5DD (UK)., Wells E; Department of Chemistry, University of York, Heslington, York, YO10 5DD (UK)., France SP; School of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, Manchester, M1 7DN (UK)., Mulholland KR; Chemical Development, AstraZeneca, Silk Rd Business Park, Macclesfield SK10 2NA (UK)., Grogan G; Department of Chemistry, University of York, Heslington, York, YO10 5DD (UK)., Turner NJ; School of Chemistry, University of Manchester, Manchester Institute of Biotechnology, 131 Princess Street, Manchester, M1 7DN (UK).

Publikováno v: ChemCatChem [ChemCatChem] 2015 Feb; Vol. 7 (4), pp. 579-583. Date of Electronic Publication: 2015 Jan 21.

Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.

Autor: Bromidge SM; SmithKline Beecham Pharmaceuticals, Discovery Research, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. Steve_Bromidge-1@sbphrd.com, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gaster LM, Ham P, Jones GE, King FD, Mulholland KR, Saunders DV, Wyman PA, Blaney FE, Clarke SE, Blackburn TP, Holland V, Kennett GA, Lightowler S, Middlemiss DN, Trail B, Riley GJ, Wood MD

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2000 Mar 23; Vol. 43 (6), pp. 1123-34.

The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.

Autor: Gaster LM; SmithKline Beecham Pharmaceuticals, Discovery Research, New Frontiers Science Park (North), Third Avenue, Harlow, Essex CM19 5AW, England., Blaney FE, Davies S, Duckworth DM, Ham P, Jenkins S, Jennings AJ, Joiner GF, King FD, Mulholland KR, Wyman PA, Hagan JJ, Hatcher J, Jones BJ, Middlemiss DN, Price GW, Riley G, Roberts C, Routledge C, Selkirk J, Slade PD

Publikováno v: Journal of medicinal chemistry [J Med Chem] 1998 Apr 09; Vol. 41 (8), pp. 1218-35.