N. Pegg

发表

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

[3.3] sigmatropy within 1-vinyl-2-alkenyl-7,7-dimethyl-exo-norbornan-2-ols: the first atropselective oxyanionic cope rearrangement

R. Rogers, L. Paquette, G. Maynard, 1990 .

Thrombin inhibitors based on [5,5] trans-fused indane lactams.

N. Ramsden, H. Jhoti, H. Finch, 1999, Bioorganic & medicinal chemistry letters.

Solid phase synthesis of aryl-ether dendrimers

M. Bradley, A. Basso, B. Evans, 2001 .

Targeting p300/CBP axis in lethal prostate cancer.

N. Tunariu, K. Knudsen, Jian Ning, 2021, Cancer discovery.

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

M. Belvin, E. Bradley, M. Ultsch, 2013 .

Direct oxygenation of enolates generated by anionic oxy-Cope rearrangement. Expedient preparation of polycyclic .alpha.-hydroxy ketones

L. Paquette, R. Taylor, T. Zydowsky, 1989 .

Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.

Steve Price, A. Nadin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

Solid-phase synthesis of aryl ethers on high loading dendrimer resin

M. Bradley, A. Basso, B. Evans, 2000 .

Solid‐Phase Synthesis of Amidine‐Based GP IIb‐IIIa Antagonists on Dendrimer Resin Beads

M. Bradley, A. Basso, B. Evans, 2000 .

Functionalization reactions of a medium-ring bridgehead enone that skirt transannular bond formation

L. Paquette, N. Pegg, 1991 .

5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.

J. Montana, C. Dix, H. Finch, 1998, Bioorganic & medicinal chemistry letters.

The synthesis of a conformationally restrained, combined thromboxane antagonist / synthase inhibitor using an intramolecular ‘Stille’- or ‘Grigg’-palladium-catalysed cyclisation strategy

H. Finch, B. Evans, N. Pegg, 1993 .

Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound

M. Congreve, P. Ward, S. Watson, 1996 .

3-substituted-1,2,4-oxadiazolin-5-one; A useful amidine precursor and protecting group

H. Finch, S. J. Coote, N. Pegg, 1995 .

Synthesis of grevillins, novel pyrandione pigments of fungi. Biogenetic interrelationships between grevillins, pulvinic acids, terphenylquinones and xylerythrins

G. Pattenden, N. Pegg, R. W. Kenyon, 1991 .

Synthesis of grevillins and their biogenetic interrelationship with terphenylquinones, xylerythrins and pulvinic acid

G. Pattenden, N. Pegg, R. W. Kenyon, 1987 .

A new synthesis of pulvinic acids

G. Pattenden, N. Pegg, A. G. Smith, 1986 .

Reaction of α-amino esters and α-amino ester imines with thiiranium ion intermediates. Application to the synthesis of new potential aminopeptidase inhibitors and mechanistic implications

C. Rayner, Duncan M. Gill, N. Pegg, 1997 .

Addition of amino esters to thiiranium ion intermediates: A novel approach to the synthesis of new potential aminopeptidase inhibitors

C. Rayner, Duncan M. Gill, N. Pegg, 1995 .

Lewis acid induced rearrangement of 2,3-epoxy sulfides; regiospecific trapping of thiiranium ion intermediates with nitrogen heterocycles and amides. Use of imines as nucleophilic equivalents for the selective monoalkylation of primary amines

C. Rayner, Duncan M. Gill, N. Pegg, 1996 .

Identification of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.

I. Chessell, A. Naylor, C. Bountra, 2004, Bioorganic & medicinal chemistry letters.

Synthetic [5,5] trans-fused indane lactones as inhibitors of thrombin.

H. Finch, E. McDonald, C. Mooney, 1999, Bioorganic & medicinal chemistry letters.

Title: Targeting p300/CBP in lethal prostate cancer. Running title: Targeting p300/CBP in lethal prostate cancer

N. Tunariu, K. Knudsen, Jian Ning, 2020 .

Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

P. Savy, Steve Price, A. Nadin, 2012, Journal of medicinal chemistry.

An open label phase I/IIa study to evaluate the safety and efficacy of CCS1477 as monotherapy and in combination in patients with advanced solid/metastatic tumors.

E. Cojocaru, J. Bono, W. West, 2019, Journal of Clinical Oncology.

SPIRO-PIPERIDINE NON-PEPTIDE NEUROKININ-1 RECEPTOR ANTAGONISTS

P. Ward, H. G. Davies, S. Watson, 1995 .

Potent Pre-Clinical and Early Phase Clinical Activity of EP300/CBP Bromodomain Inhibitor CCS1477 in Multiple Myeloma

T. Somervaille, J. Cavet, W. West, 2022, Blood.

Therapeutic Targeting of EP300/CBP By Bromodomain Inhibition in Acute Myeloid Leukemia

M. Copland, T. Somervaille, G. J. Spencer, 2022, Blood.

560TiP A phase I/IIa study to evaluate the safety and efficacy of CCS1477, a first in clinic inhibitor of p300/CBP, as monotherapy in patients with selected molecular alterations

R. Plummer, S. Crabb, L. Carter, 2021, Annals of Oncology.

An Open-Label Phase I/IIa Study to Evaluate the Safety and Efficacy of CCS1477, a First in Clinic Inhibitor of the p300/CPB Bromodomains, As Monotherapy in Patients with Advanced Haematological Malignancies

T. Somervaille, A. Davies, S. Knapper, 2019, Blood.

Synthesis of trans-fused [5,5] bicyclic lactones/lactams as templates for serine protease inhibition

J. Montana, H. Finch, H. A. Kelly, 1998 .

Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.

I. Chessell, C. Bountra, S. Bingham, 2009, Bioorganic & medicinal chemistry letters.

Characterisation of CCS1477: A novel small molecule inhibitor of p300/CBP for the treatment of castration resistant prostate cancer.

K. Knudsen, S. Paoletta, Jonathan Shannon, 2017 .