Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.

Autor: Wellaway CR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Baldwin IR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Bamborough P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Barker D; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Bartholomew MA; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Dümpelfeld B; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, 69117 Heidelberg, Germany., Evans JP; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Fazakerley NJ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Homes P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Keeling SP; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Lewell XQ; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., McNab FW; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Morley J; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Needham D; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Neu M; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., van Oosterhout AJM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Pal A; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Reinhard FBM; Cellzome GmbH, A GlaxoSmithKline Company, Meyerhofstraße 1, 69117 Heidelberg, Germany., Rianjongdee F; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Robertson CM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Rowland P; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Shah RR; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Sherriff EB; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Sloan LA; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Teague S; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Thomas DA; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Wellaway N; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Wojno-Picon J; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K., Coe DM; GSK, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, U.K.

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2022 Jan 13; Vol. 65 (1), pp. 633-664. Date of Electronic Publication: 2021 Dec 20.

Targeting PI3K family with small-molecule inhibitors in cancer therapy: current clinical status and future directions.

Autor: Li, Hongyao^1,2,3 (AUTHOR), Wen, Xiang³ (AUTHOR), Ren, Yueting^3,4 (AUTHOR), Fan, Zhichao^1,2,3 (AUTHOR), Zhang, Jin⁵ (AUTHOR) zhangjin1989@szu.edu.cn, He, Gu³ (AUTHOR) hegu@scu.edu.cn, Fu, Leilei^1,2 (AUTHOR) leilei_fu@163.com

Publikováno v: Molecular Cancer. 8/10/2024, Vol. 23 Issue 1, p1-42. 42p.

DAMPAK IMPLEMENTASI PERDAGANGAN BEBAS PADA SEKTOR EKONOMI DI INDONESIA.

Autor: Mentari Pombu, Yerlen Sri, Yeni, Hari

Publikováno v: Syntax Idea. Jan2024, Vol. 6 Issue 1, p1-9. 9p.

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.