M. Burkard

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.

Dihydropyridines: a new class of angiotensin II antagonists

K. W. Hoover, M. Mangiapane, M. Burkard, 1994 .

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

J. Blake, J. Christensen, B. Brandhuber, 2018, ACS medicinal chemistry letters.

A new generation of bradykinin antagonists.

J. Stewart, E. Whalley, M. Burkard, 1996, Immunopharmacology.

Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer

J. Blake, J. Christensen, G. Vigers, 2020 .

Comparative profile of novel potent bradykinin antagonists at human B1 and B2 receptors.

E. Whalley, M. Francis, M. Burkard, 1996, Immunopharmacology.

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

J. Blake, Jianping Yin, Weiru Wang, 2015, Journal of medicinal chemistry.

Asymmetric Pictet–Spengler Reactions Employing N,N‐Phthaloyl Amino Acids as Chiral Auxiliary Groups

H. Waldmann, M. Burkard, G. Schmidt, 1995 .

Asymmetric control in the Pictet-Spengler reaction by means of N-protected amino acids as chiral auxiliary groups

H. Waldmann, M. Burkard, G. Schmidt, 1996 .

Selective RET kinase inhibition for patients with RET-altered cancers

A. Drilon, B. Tuch, V. Velcheti, 2018, Annals of oncology : official journal of the European Society for Medical Oncology.

The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients.

J. Fernandez-Banet, A. Pavlícek, J. Christensen, 2019, Cancer discovery.

Emergence and Targeting of Acquired and Hereditary Resistance to Multikinase RET Inhibition in Patients With RET-Altered Cancer

B. Tuch, T. Kohno, J. Blake, 2019, JCO precision oncology.

Bradykinin antagonists in human systems: correlation between receptor binding, calcium signalling in isolated cells, and functional activity in isolated ileum.

J. Stewart, L. W. Spruce, E. Whalley, 1997, Biochemical pharmacology.

New bradykinin antagonists having very high potency at B1 receptors.

J. Stewart, E. Whalley, M. Burkard, 1996, Immunopharmacology.

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

M. Volgraf, G. Vigers, Xingrong Liu, 2014, Bioorganic & medicinal chemistry letters.

8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.

K. Scearce-Levie, G. Vigers, Xingrong Liu, 2014, Journal of medicinal chemistry.

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.

K. Scearce-Levie, M. Volgraf, G. Vigers, 2014, Journal of medicinal chemistry.

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.

G. Vigers, Xingrong Liu, Darin J. Smith, 2013, Journal of medicinal chemistry.

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

J. Blake, Jianping Yin, Weiru Wang, 2014, Bioorganic & medicinal chemistry letters.

Dihydropyridines: A New Class of Angiotensin II Antagonists.

K. W. Hoover, M. Mangiapane, M. Burkard, 1994 .

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 .

Inducible bradykinin B1 receptor in isolated human ileum.

E. Whalley, M. Burkard, W. Selig, 1996, Immunopharmacology.

A new class of potent bradykinin antagonist dimers.

J. Stewart, E. Whalley, M. Burkard, 1996, Immunopharmacology.