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Your search keyword '"Kurt Gordon Pike"' showing total 5 results
Start Over Author "Kurt Gordon Pike" Publisher royal society of chemistry (rsc)
5 results on '"Kurt Gordon Pike"'

1. Correction: Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9. See DOI: 10.1039/c6md00159a

Author

Lisa O’ Fee, Julie A. Tucker, Julie Demeritt, Emmanuel de Billy, Matthew D. Cheeseman, Kevin Michael Foote, Stephen Green, Kurt Gordon Pike, Scott G. Lamont, Louise Goodwin, Paul D. Kemmitt, Christopher J. Lynch, Paul Workman, Lorenzo Zani, Swee Y. Sharp, Alan T. Henley, Nicola E. A. Chessum, Rosie Isaac, Paul Faulder, Keith Jones, Robert te Poele, Carl S. Rye, Angela Hayes, Florence I. Raynaud, and Joanna Boros

Subjects
Pharmacology, Stress (mechanics), Biochemistry, Chemistry, Drug Discovery, Organic Chemistry, Pharmaceutical Science, Molecular Medicine, Cyclin-dependent kinase 9, HSF1, Combinatorial chemistry
Abstract

Correction for ‘Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9’ by Carl S. Rye et al., Med. Chem. Commun., 2016, 7, 1580–1586.

Published
2016

2. Property based optimisation of glucokinase activators – discovery of the phase IIb clinical candidate AZD1656

Author

Graeme R. Robb, David S. Clarke, Kurt Gordon Pike, Craig Johnstone, Darren Mckerrecher, Linda Godfrey, Ingrid Wilson, Mark D. Fenwick, Rayner John Wall, Michael J. Waring, and Sam D. Groombridge

Subjects
Pharmacology, Biochemistry, Glucokinase, Chemistry, Drug Discovery, Organic Chemistry, Pharmaceutical Science, Molecular Medicine, Glucose homeostasis, Pharmaceutical sciences, Small molecule
Abstract

Glucokinase plays a central role in glucose homeostasis and small molecule activators of the glucokinase enzyme have been the subject of significant pharmaceutical research in the quest for agents capable of delivering improved glycaemic control. Here we describe our medicinal chemistry campaign to improve on our previously described development candidate in this area, AZD1092, focussed on removal of Ames liability and improved permeability characteristics. This work culminated in the superior compound AZD1656 which has progressed to phase 2 clinical trials.

Published
2012

3. Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092

Author

Kurt Gordon Pike, Graeme R. Robb, Craig Johnstone, Darren Mckerrecher, and Michael J. Waring

Subjects
Pharmacology, Oral agents, Biochemistry, Glucokinase, Drug Discovery, Organic Chemistry, Pharmaceutical Science, Molecular Medicine, Computational biology, Biology, Pharmaceutical sciences, Small molecule
Abstract

Small molecule activators of the glucokinase enzyme have the potential to deliver a level of glycaemic control that is superior to current oral agents and hence have great promise as new therapies for Type 2 Diabetes. As such, attempts to discover glucokinase activators suitable for clinical development have been the focus of many major pharmaceutical research programmes. Here we show how property-based matrix optimisation has been used to improve the multi-parameter technical profile of the AstraZeneca series of glucokinase activators culminating in the discovery of the development candidate AZD1092.

Published
2011

4. Overcoming retinoic acid receptor-α based testicular toxicity in the optimisation of glucokinase activators

Author

Graeme R. Robb, Kurt Gordon Pike, Darren Mckerrecher, Huw B. Jones, Brendan Leighton, Iain J. Brogan, Craig Johnstone, Michael J. Waring, and Matthew P. Coghlan

Subjects
Pharmacology, chemistry.chemical_classification, Glucokinase, Organic Chemistry, Retinoic acid, Pharmaceutical Science, Biology, Biochemistry, Small molecule, Retinoic acid receptor, Oral agents, chemistry.chemical_compound, Enzyme, chemistry, Drug Discovery, Molecular Medicine, Testicular toxicity, Pharmaceutical sciences
Abstract

Small molecule activators of the glucokinase enzyme have the potential to deliver a level of glycaemic control that is superior to current oral agents and hence have great promise as new therapies for Type 2 Diabetes. As such, attempts to discover glucokinase activators suitable for clinical development have been the focus of many major pharmaceutical research programmes. Here we describe how we have overcome a testicular toxicological liability in our pyridine acid lead series, which we show can be ascribed to antagonism of the retinoic acid receptor-α.

Published
2011

5. Aminative rearrangement of 2-alkoxy-3,4-dihydro-2H-pyrans: a novel stereocontrolled route to substituted pyrrolidinesElectronic supplementary information (ESI) available: experimental details and characterisation data for all new compounds. See http://www.rsc.org/suppdata/cc/b3/b316554j

Author

Graham R. Cumming, Kurt Gordon Pike, and Alan Armstrong

Subjects
Stereochemistry, Chemistry, Materials Chemistry, Metals and Alloys, Ceramics and Composites, Alkoxy group, General Chemistry, Catalysis, Surfaces, Coatings and Films, Electronic, Optical and Magnetic Materials
Abstract

Aziridination of 2-alkoxy-3,4-dihydro-2H-pyrans leads to rearrangement and stereocontrolled formation of 5-alkoxypyrrolidines which may be reduced to pyrrolidines or allylated stereoselectively.

Published
2004

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