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Design and Development of a Macrocyclic Series Targeting Phosphoinositide 3-Kinase δ.

Autor: Spencer JA; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom.; Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Baldwin IR; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Barton N; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Chung CW; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Convery MA; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Edwards CD; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Jamieson C; Department of Pure and Applied Chemistry, University of Strathclyde, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Mallett DN; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Rowedder JE; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Rowland P; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Thomas DA; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom., Hardy CJ; GSK Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, United Kingdom.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2020 Jun 03; Vol. 11 (7), pp. 1386-1391. Date of Electronic Publication: 2020 Jun 03 (Print Publication: 2020).

Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease.

Autor: Down K; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Amour A; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Baldwin IR; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Cooper AW; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Deakin AM; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Felton LM; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Guntrip SB; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Hardy C; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Harrison ZA; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Jones KL; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Jones P; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Keeling SE; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Le J; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Livia S; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Lucas F; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Lunniss CJ; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Parr NJ; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Robinson E; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Rowland P; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Smith S; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Thomas DA; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Vitulli G; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Washio Y; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K., Hamblin JN; Refractory Respiratory Inflammation DPU, and ‡Allergic Inflammation DPU, Respiratory Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Molecular Discovery Research, ∥Biological Sciences, and ⊥Computational Chemistry, Platform Technology & Science, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.; Experimental Medicine Unit, and ∇Epinova DPU, ImmunoInflammation Therapeutic Area, GlaxoSmithKline R&D , Gunnels Wood Road, Stevenage, SG1 2NY, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2015 Sep 24; Vol. 58 (18), pp. 7381-99. Date of Electronic Publication: 2015 Sep 03.

3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.

Autor: Miller DD; GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK., Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Apr 15; Vol. 21 (8), pp. 2255-8. Date of Electronic Publication: 2011 Mar 01.