K. Robarge

发表

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.

Dolores Diaz, Jianping Yin, Michael Burkard, 2016, Journal of medicinal chemistry.

From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus.

B Kohl, R. Mcdowell, B. Kohl, 1997, Journal of medicinal chemistry.

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

C. Ly, S. Sideris, S. Malek, 2011, Journal of medicinal chemistry.

Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor

M. Belvin, K. Hoeflich, J. Chan, 2010, Xenobiotica; the fate of foreign compounds in biological systems.

Preparation and biological activity of novel tricyclic GPIIb/IIIa antagonists.

I. Aliagas, R. Webb, T. Somers, 1998, Bioorganic & medicinal chemistry.

Stability of Alkoxycarbonylamidine Prodrugs

Z. Shahrokh, M. Powell, K. Robarge, 1998, Pharmaceutical Research.

Pharmacokinetics, Pharmacodynamics and Tolerability of a Potent, Non-peptidic, GP IIb/IIIa Receptor Antagonist following Multiple Oral Administrations of a Prodrug Form

S. Bunting, M. Beresini, K. Robarge, 1998, Thrombosis and Haemostasis.

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.

D. Sutherlin, Leslie B. Lee, F. D. de Sauvage, 2010, Bioorganic & medicinal chemistry letters.

Electrophile-mediated cyclizations in carbohydrate chemistry: synthesis of highly functionalized ribofuranose and ribopyranose compounds

K. Robarge, F. Freeman, 1985 .

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.

S. Sideris, S. Malek, J. Lyssikatos, 2013, Bioorganic & medicinal chemistry letters.

From Peptide to Non-Peptide. Part 2. The de novo Design of Potent, Non- Peptidal Inhibitors of Platelet Aggregation Based on a Benzodiazepinedione Scaffold.

Mark Reynolds, M. Venuti, E. Thorsett, 1994 .

A Selective, Slow Binding Inhibitor of Factor VIIa Binds to a Nonstandard Active Site Conformation and Attenuates Thrombus Formation in Vivo*

D. Banner, M. Ultsch, D. Sutherlin, 2005, Journal of Biological Chemistry.

Electrophile-mediated cyclizations of 6-O-benzyl-1,2-di- deoxy-3,4-O-isopropylidene-d-ribo-hex-1-enitol to derivatives of 2,5-anhydro-6-O-benzyl-3,4-O-isopropylidene-d-altro-hexitol

K. Robarge, F. Freeman, 1985 .

Accelerated inverse electron demand Diels-Alder reactions of 1-oxa-1,3-butadienes: [4 + 2] cycloaddition reactions of .beta.,.gamma.-unsaturated .alpha.-keto esters

D. Boger, K. Robarge, 1988 .

From Peptide to Non-Peptide. 2. The de Novo Design of Potent, Non-peptidal Inhibitors of Platelet Aggregation Based on a Benzodiazepinedione Scaffold

Thomas Rawson, E. Thorsett, T. Gadek, 1994 .

Mono-N-alkylation of anthranilamides via quinazolinones. An efficient synthesis of G5598, a benzodiazepine dione gpIIbIIIa antagonist

R. Webb, M. Reynolds, K. Robarge, 1994 .

Stereoselectivity in electrophile-mediated intramolecular cyclizations of hept-2-enitols

K. Robarge, F. Freeman, 1989 .

Divergent de novo synthesis of carbohydrates based on an accelerated inverse electron demand Diels-Alder reaction of 1-oxa-1,3-butadienes

D. Boger, K. Robarge, 1988 .

Epimerization at C-2 during the Wittig reaction of 2,3,5-tri-O-benzyl-d-ribose and methylidenetriphenylphosphorane

K. Robarge, F. Freeman, 1986 .

Stereoselectivity in the electrophile-mediated cyclization of 2,3,5-tri-O-benzyl-1,2-dideoxy-d-arabino-hex-1-enitol. A stereocontrolled synthesis of 1-amino-2,5-anhydro-3,4,6-tri-O-benzyl-1-deoxy-d-glucitol

K. Robarge, F. Freeman, 1987 .

Electrophile-mediated cyclizations in carbohydrate chemistry: synthesis of highly functionalized ribofuranose and ribopyranose compounds

K. Robarge, F. Freeman, 1985 .

ELECTROPHILE-MEDIATED CYCLIZATIONS OF 6-O-BENZYL-1,2-DIDEOXY-3,4-O-ISOPROPYLIDENE-D-RIBO-HEX-1-ENITOL TO DERIVATIVES OF 2,5-ANHYDRO-6-O-BENZYL-3,4-O-ISOPROPYLIDENE-D-ALTRO-HEXITOL

K. Robarge, F. Freeman, 1985 .

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

Marie Evangelista, BinQing Wei, M. Ultsch, 2016, ACS medicinal chemistry letters.

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.

BinQing Wei, M. Ultsch, C. Eigenbrot, 2014, Bioorganic & medicinal chemistry letters.

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.

M. Belvin, A. Daemen, BinQing Wei, 2016, Nature chemical biology.

Discovery and preclinical development of vismodegib

L. Rubin, D. Sutherlin, F. D. de Sauvage, 2014, Expert opinion on drug discovery.

Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance.

Z. Modrušan, D. Sutherlin, T. Januario, 2011, Cancer research.

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

BinQing Wei, M. Ultsch, C. Eigenbrot, 2015, Bioorganic & medicinal chemistry letters.

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

BinQing Wei, M. Ultsch, C. Eigenbrot, 2014, Bioorganic & medicinal chemistry letters.

GDC-0449-a potent inhibitor of the hedgehog pathway.

K. Kotkow, L. Rubin, D. Sutherlin, 2009, Bioorganic & medicinal chemistry letters.

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

H. Wong, E. Plise, Y. Shin, 2009, Xenobiotica; the fate of foreign compounds in biological systems.

Structure-based Optimization of Hydroxylactam as Potent, Cell-Active Inhibitors of Lactate Dehydrogenase.

BinQing Wei, M. Ultsch, C. Eigenbrot, 2022, Bioorganic & medicinal chemistry letters.

Preclinical Disposition of GDC-0973 and Prospective and Retrospective Analysis of Human Dose and Efficacy Predictions

M. Belvin, K. Hoeflich, M. Merchant, 2012, Drug Metabolism and Disposition.

Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.

Adam R. Johnson, W. Ouyang, A. Barnard, 2015, Bioorganic & medicinal chemistry letters.

Corrigendum to “GDC-0449—A potent inhibitor of the hedgehog pathway” [Bioorg. Med. Chem. Lett. 19 (2009) 5576]

K. Kotkow, L. Rubin, D. Sutherlin, 2010 .

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

P. Savy, Steve Price, M. Ultsch, 2014, Bioorganic & medicinal chemistry letters.

Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development

S. Gould, M. Belvin, Peter Yin, 2014 .