Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity

2017-11-07T14:15:56+00:00

81) Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity. McCoull W, Barton P, Broo A, Brown A, Clarke D, Coope G, Davies RDM, Dossetter AG , Kelly E,  Knerr L, Macfaul P, Holmes J,  Martin N,  Moore JE, Morgan D, Newton C, Osterlund K, Robb G, Rosevere E, Selmi N, Stokes S, Svensson T,

Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity2017-11-07T14:15:56+00:00

“Investigation of the Origins of Regiochemical Control in [4+2] Cycloadditions of 2-Pyrones and Alkynylboronates”

2017-11-07T14:15:16+00:00

82) “Investigation of the Origins of Regiochemical Control in [4+2] Cycloadditions of 2-Pyrones and Alkynylboronates” Kirkham, J. D.; Leach, A. G.; Row, E. C.; Harrity, J. P. A. Synthesis, 2012, 44, 1964-1973.

“Investigation of the Origins of Regiochemical Control in [4+2] Cycloadditions of 2-Pyrones and Alkynylboronates”2017-11-07T14:15:16+00:00

Free-Wilson and Structural Approaches to Co-optimizing Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors

2017-11-07T14:14:31+00:00

83) Free-Wilson and Structural Approaches to Co-optimizing Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors Frederick W. Goldberg, Andrew G. Leach, James S. Scott, Wendy L. Snelson, Sam D. Groombridge, Craig S. Donald, Stuart N. L. Bennett, Cristian Bodin, Pablo Morentin Gutierrez, and Amy C. Gyte. J. Med. Chem., 2012, 55

Free-Wilson and Structural Approaches to Co-optimizing Human and Rodent Isoform Potency for 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Inhibitors2017-11-07T14:14:31+00:00

Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists

2017-11-07T14:12:34+00:00

84) Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists James S. Scott, Alan M. Birch, Katy J. Brocklehurst, Hayley S. Brown, Kristin Goldberg, Sam D. Groombridge, Julian A. Hudson, Andrew G. Leach, Philip A. MacFaul, Darren McKerrecher, Ruth Poultney, Paul Schofield and Per H. Svensson Med. Chem. Commun.,

Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists2017-11-07T14:12:34+00:00

Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1

2017-11-07T14:12:08+00:00

85) Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1 Alleyn T. Plowright, Peter Barton, Stuart Bennett, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Robert D. M. Davies, Anne Ertan, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Per H. Svensson, Andrew

Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 12017-11-07T14:12:08+00:00

A monomeric form of iNOS can rationalise observed SAR for inhibitors of dimerisation: quantum mechanics and docking compared

2017-11-07T14:11:38+00:00

86) A monomeric form of iNOS can rationalise observed SAR for inhibitors of dimerisation: quantum mechanics and docking compared Andrew G. Leach, Lise-Lotte Olsson and Daniel J. Warner Med. Chem. Commun., 2013,4, 180-186

A monomeric form of iNOS can rationalise observed SAR for inhibitors of dimerisation: quantum mechanics and docking compared2017-11-07T14:11:38+00:00

Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353

2017-11-07T14:11:12+00:00

87) Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD2353 Michael J. Waring, Alan M. Birch, Susan Birtles, Linda K. Buckett, Roger J. Butlin, Leonie Campbell, Pablo Morentin Gutierrez, Paul D. Kemmitt, Andrew G. Leach, Philip A. MacFaul, Charles O'Donnell and Andrew V. Turnbull Med. Chem. Commun., 2013,4,

Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 – the discovery of AZD23532017-11-07T14:11:12+00:00

Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors

2017-11-07T14:10:47+00:00

88) Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors Frederick W. Goldberg, Alan M. Birch, Andrew G. Leach, Sam D. Groombridge, Wendy L. Snelson, Pablo Morentin Gutierrez, Clare D. Hammond, Susan Birtles and Linda K. Buckett Med. Chem. Commun., 2013,4, 165-174.

Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors2017-11-07T14:10:47+00:00

Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt

2017-11-07T14:10:13+00:00

89) Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases Addie, M.; Ballard, P.; Buttar, D.; Crafter, C.; Currie, G.; Davies, B. R.; Debreczeni, J.; Dry, H.; Dudley, P.; Greenwood, R.; Johnson, P. D.; Kettle, J. G.; Lane, C.; Lamont, G.; Leach, A. G.; Luke, R. W. A.; Morris, J.; Ogilvie, D.;

Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt2017-11-07T14:10:13+00:00
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