Oliver Schadt

I very much enjoy to help finding clever solutions for challenging and important problems which ultimately will lead to the identification of innovative and more effective medicines.


Perspective

As a scientist, and in particular as a Medicinal Chemist at Merck KGaA, Darmstadt, Germany, I have the unique opportunity to work at the exciting cross-functional interface between Chemistry, Biology, Pharmacology and Pharmacokinetics. Small molecule Drug discovery and development is a team sport and I very much enjoy to help finding clever solutions for challenging and important problems which ultimately will lead to the identification of innovative and more effective medicines. At the end of the day, it is extremely rewarding to have contributed to the identification and development of a molecule like Tepotinib, a compound that has the potential to change the life of patients. In the last 20 years, Merck KGaA, Darmstadt, Germany transformed to a science and technology driven company, which fosters curiosity and innovation, and I am proud to be part of our company's discovery engine.

I very much enjoy to help finding clever solutions for challenging and important problems which ultimately will lead to the identification of innovative and more effective medicines.

Oliver Schadt

Immuno-Oncology concepts from the perspective of Medicinal Chemistry.

Profile

Joined Merck KGaA, Darmstadt, Germany: 1999

Key research fields and topics:

  • Medicinal Chemistry
  • Pharmacology
  • Organic Chemistry
  • Compound Design and Optimization
  • Small Molecule Drug Discovery in Oncology
  • Small Molecule Drug Development in Oncology, Tepotinib, Kinases

CV & Scientific activities

CV: Education

CV: Education

1989 - 1994
Study of Chemistry at the Johann Wolfgang Goethe-University in Frankfurt
1995 - 1998
PhD thesis at the Institute of Pharmaceutical Chemistry at the Johann-Wolfgang Goethe-University in Frankfurt under the supervision of Professor Dr. Christian Noe.Title: “Ligands of the polyamine binding site of the NMDA receptor“
1999 - 2001
Postdoctoral fellowship, Department of Medicinal Chemistry, Merck KGaA, Darmstadt, Germany

CV: Professional Career

CV: Professional Career

2001 - 2010
Principle Scientist, Head of Laboratory Medicinal Chemistry, Merck KGaA, Darmstadt, Germany
2010 - 2016
Associate Director, Group Leader Medicinal Chemistry, Merck KGaA, Darmstadt, Germany
2016 - 2017
Director, Department Head Medicinal Chemistry, Merck KGaA, Darmstadt, Germany
since 2017
Director, Scientific Expert Medicinal Chemistry, Merck KGaA, Darmstadt, Germany

References

Scientific Publications

  • Tepotinib, Comprehensive Medicinal Chemistry III vol. 8 (2017), pp. 178–203
  • Characterization of RON protein isoforms in pancreatic cancer: implications for biology and therapeutics Oncotarget (2016), 7(29), 45959-45975
  • Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors, Bioorganic & Medicinal Chemistry Letters (2015), 25(7), 1597-1602
  • EMD 1214063 and EMD 1204831 Constitute a New Class of Potent and Highly Selective c-Met Inhibitors, Clinical Cancer Research (2013), 19(11), 2941-2951
  • Exploring the polyamine regulatory site of the NMDA receptor: a parallel synthesis approach, ChemMedChem (2013), 8(1), 82-94
  • New polyamine-sensitive inhibitors of the NMDA receptor: Syntheses and pharmacological evaluation, European Journal of Medicinal Chemistry (2007), 42(2), 175-197

Poster / Oral Presentations at Conferences

  • Identification of MSC2156119 (EMD1214063) as a potent and selective inhibitor of c-Met kinase, EFMC 2014
  • The c-Met inhibitors EMD 1214063 and EMD 1204831 are effective in combination with EGFR and VEGF inhibitors in NSCLC models, AACR 2012
  • Identification and preclinical characterization of EMD 1204831 – A selective c-Met kinase inhibitor in clinical phase 1, AACR 2011
  • EMD 1214063 – An exquisitely selective c-Met kinase inhibitor in clinical phase 1, AACR 2010
  • Preclinical characterization of EMD 1214063 – An exquisitely selective c-Met kinase inhibitor in clinical phase 1, EORTC 2010
  • Identification and optimization of pyridazinones as potent and exquisitely selective c-met kinase inhibitors, AACR 2009
  • Identification of a new class of highly potent and selective c-Met inhibitors, EORTC2009
  • 3-Phenyl-[1,2,4]oxadiazole Derivatives as Potent Inhibitors of c-Met-kinase, EuCheMS 2009
  • Novel 1-Acyl-pyrazoline Derivatives as Highly Selective Inhibitors of c-Met Kinase, ACS 2007

Patent Applications

  1. Boronic acid derivatives, WO 2016050358
  2. Boronic acid derivatives, WO 2016050356
  3. Boronic acid derivatives, WO 2016050355
  4. Boronic acid derivatives, WO 2016050359
  5. Preparation of a quinoline inhibitor of the macrophage stimulating 1 receptor, WO 2014194975
  6. Preparation of pyrido-pyrimidine derivatives as inhibitors of RON WO 2013022519
  7. Polymorphic forms of 3-(1-{3-[5-(1-methylpiperidin-4-ylmethoxy)pyrimidin-2-yl]benzyl}-6-oxo-1,6-dihydropyridazin-3-yl)-benzonitrile hydrochloride, WO 2010078897
  8. Preparation of benzylpyridazinones as Met kinase inhibitors, WO 2010078910
  9. Preparation of pyridazinones as Met kinase inhibitors, WO 2010078909
  10. Preparation of benzothiazolones as antitumor agents, WO 2010078905
  11. Preparation of 3-(3-pyrimidin-2-ylbenzyl)-[1,2,4]triazolo[4,3b]pyrimidines as protein tyrosine kinase inhibitors for cancer therapy, WO 2010072301
  12. Preparation of pyridazinones as antitumor agents, WO 2010072296
  13. Polymorphic forms of 6-(1-methyl-1H-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-ylethoxy)pyrimidin-2-yl]benzyl}-2Hpyridazin-3-one dihydrogen phosphate, WO 2010072295
  14. Preparation of 3-(3-pyrimidin-2-ylbenzyl)-[1,2,4]triazolo[4,3b]pyrimidines as protein tyrosine kinase inhibitors for cancer therapy, WO 2010069441
  15. Preparation of bicyclic triazoles as anti-tumor agents, WO 2010017870
  16. Preparation of triazolo[4,3-B]pyridazines as MET kinase inhibitors, WO 2009152920
  17. Preparation of dihydropyrazoles as anti-tumor agents, WO 2009143945
  18. Preparation of pyridazinones as anti-tumor agents, WO 2009129905
  19. Preparation of pyridazinones as Met kinase inhibitors, WO 2009083076
  20. Preparation of thiadiazinones as Met kinase inhibitors, WO 2009030333
  21. Preparation of 6-thioxopyridazines as antitumor agents, WO 2009024221
  22. Pyridazinone derivatives as Met kinase inhibitors and their preparation and use in the treatment of cancer, WO 2009006959
  23. Preparation of pyrimidinylpyridazinones as Met kinase inhibitors for treatment of tumors, WO 2009007074
  24. Preparation of benzo[d]oxazol-2(3H)-ones as Met kinase inhibitors, WO 2008148449
  25. Preparation of pyridazinones as Met kinase inhibitors, WO 2008145243
  26. Preparation of pyridazinones as Met kinase inhibitors, WO 2008145242
  27. Preparation of 3-phenyl-6-pyridazinones as Met kinase inhibitors, WO 2008017361
  28. Preparation of substituted 5-phenyl-3,6-dihydro-2-oxo-6H-1,3,4-thiadiazines as Met kinase inhibitors for treating tumors, WO 2007057092
  29. Preparation of substituted 3,6-dihydro-2-oxo-6H-1,3,4-thiadiazine derivatives as Met kinase inhibitors for treating tumors, WO 2007057093
  30. Preparation of 1-acyldihydropyrazoles as Met kinase inhibitors for treating tumors, WO 2007019933
  31. Preparation of pyridinyloxybenzylureas as RAF kinase inhibitors, WO 2004037789
  32. Preparation of pyridinyloxyphenylaminoacetamides as RAF kinase inhibitors, WO 2004019941
  33. Preparation of indole-3-carbonitriles as excitatory amino acid antagonists for the treatment of neurodegenerative diseases, WO 2003087086
  34. Preparation of aminoalkanoylaminobenzoxazoles as excitatory amino-acid antagonists, WO 2003076420
  35. Preparation of 3-biphenylpropionic acids as avb6-integrin receptor inhibitors, WO 2003066594
  36. Preparation of biphenyl thioamides serving as integrin receptor antagonists, WO 2003014088
  37. Preparation of 3-amino-3-phenylpropanoic acid amino acid derivatives as inhibitors of integrin avb6, WO 2002074730 A1 20020926
  38. Preparation of pyridinylaminoalkoxyphenylalkanoic acid derivatives and analogs as novel integrin avb3 inhibitors, WO 2001014338
  39. Preparation of pyridinyl- and pyrimidinylaminoalkoxyphenylbutyric acid derivatives and analogs as avb3 integrin inhibitors, WO 2001014337

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