Prof. J. Mittendorf

Honorarprofessor Dr. Joachim Mittendorf

Curriculum Vitae

1982 - 1987 Studies and degree in Chemistry at the University of Göttingen
1987 -1989 Ph. D. thesis with Prof. Dr. U. Schöllkopf in Organic Chemistry at the University of Göttingen supported by a Verband der Chemischen Industrie fellowship:
"A Novel Ring Expansion of Dihydropyrazines and Benzodihydroaromatics"
1989 - 1990 Postdoctoral research with Prof. K.P.C. Vollhardt at the University of California, Berkeley on a Feodor-Lynen-Fellowship of the Alexander von Humboldt Foundation
1990 - 1994 Senior Scientist in Medicinal Chemistry at Bayer AG, Wuppertal; Research Areas: Antimycotics (ß-amino acids), Virology (HIV protease inhibitors)
1994 - 1996 Senior Scientist in Pharma Process Development at Bayer AG, Wuppertal: Enantiomerically pure Dihydropyridines and ß-Amino Acids
1996 - 1999 Senior Scientist in Medicinal Chemistry at Bayer AG, Wuppertal; Research Areas: CNS (neuroprotectives for the treatment of stroke, traumatic brain injury), Asthma (tryptase inhibitors), Cardiovascular Diseases (coronary heart disease, hematology)
1999-             present Director and since 2016 VP of Medicinal Chemistry 2 at Bayer Pharma AG, Wuppertal; responsible for heart diseases
2002 - 2016 Project leader of Bayer pharma research IT platform “Pharmacophore Informatics”
Since Jan 2009 Honorarprofessor for Medicinal Chemistry, University of Leipzig, Germany
2010 - 2014 Chairmen of GDCH section Wuppertal-Hagen

Publications

  1. Mittendorf, J. Liebigs Ann. Chem. 1988, 1201:
    Enantioselective synthesis of (R)- and (S)- 4-methylcycloserine by the bislactim ether method.
  2. Schöllkopf, U.; Mittendorf, J. Angew. Chem. 1989, 101, 633:
    From 2,5-dihydropyrazines to 2H-1,4-diazepines, and from benzodihydroarenes to benzocycloheptene derivatives, structural variants of the antidepressant protriptylene.
  3. Hartwig, W.; Mittendorf, J. Synthesis 1991, 939:
    Enantioselective synthesis of 2,3-diamino acids by the bislactim ether method.
  4. Boese, R.; Green, J. R.; Mittendorf, J.; Mohler, D. L.; Vollhardt, K. P. C.: Angew. Chem. 1992, 104, 1643:
    The first hexabutadiynylbenzene derivative: synthesis and structure.
  5. Schmidt, U.; Schumacher, A.; Mittendorf, J.; Riedl, B. Journal of Peptide Research 1998, 52, 143:
    Contribution to the synthesis of aureobasidin A. Synthesis of cyclopeptolides containing the sequence leucyl-N-methyl- -hydroxyvalyl-(2R)-oxy-(3R)-methyl-pentanoic acid.
  6. Hartwig, W.; Mittendorf, J Encyclopedia of Reagents for Organic Synthesis 2001:
    (2S)-(+)-2,5-Dihydro-2-isopropyl-3,6-dimethoxypyrazine.
  7. Mauler, F.; Mittendorf, J.; Horváth, E.; De Vry, J. Journal of Pharmacology and Experimental Therapeutics 2002, 302, 359:
    Characterization of the diarylether sulfonylester (-)-(R)-3-(2-hydroxymethylindanyl-4-oxy)phenyl-4-4-4-trifluoro-1-sulfonate (BAY 37-7271) as a potent cannabinoid receptor agonist with neuroprotective properties.
  8. Steinhagen, H.; Gerisch, M.; Mittendorf, J.; Schlemmer, K.-H.; Albrecht, B. Biorg. Med. Chem. Lett. 2002, 12, 3187 :
    Substituted uracil derivatives as potent inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
  9. Mittendorf, J: Benet-Buchholz, J.; Fey, P. Mohrs, K.-H. Synthesis 2003, 136:
    Efficient asymmetric synthesis of -amino acid BAY 10-8888 / PLD-118, a novel antifungal for the treatment of yeast infections.
  10. Mittendorf, J; Kunisch, F.; Matzke, M.; Militzer, H.-C.; Schmidt, A.; Schoenfeld, W. Biorg. Med. Chem. Lett. 2003, 13, 433:
    Novel antifungal -amino acids: Synthesis and activity against Candida albicans.
  11. Kuhl A; Hahn M G; Dumic M; Mittendorf J. Amino Acids 2005, 29, 89:
    Alicyclic beta-amino acids in Medicinal Chemistry.
  12. Hasenoehrl A.; Galic T.; Ergovic G.; Marsic N.; Skerlev M.; Mittendorf J.; Geschke U.; Schmidt A.; Schoenfeld W. Antimicrobial agents and chemotherapy 2006, 50, 3011:
    In vitro activity and in vivo efficacy of icofungipen (PLD-118), a novel oral antifungal agent, against the pathogenic yeast Candida albicans.
  13. Kast R; Schirok H; Figueroa-Perez S; Mittendorf J; Gnoth M J; Apeler H; Lenz J; Franz J K; Knorr A; Hutter J; Lobell M; Zimmermann K; Munter K; Augstein K H; Ehmke H; Stasch J P British Journal of Pharmacology 2007, 152, 1070:
    Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase.
  14. Schermuly R.; Stasch J.-P.; Pullamsetti S. S.; Middendorff R.; Mueller D.; Schlüter K.-D.; Dingendorf A.; Kolosionek E.; Kaulen C.; Dumitrascu R.; Weissmann N.; Mittendorf J.; Klepetko W.; Seeger W.;, Ghofrani H. A.; Grimminger F. Eur. Respir. J. 2008, 32, 881-891:
    Expression and Function of Soluble Guanylate Cyclase in Pulmonary Arterial Hypertension.
  15. Schirok, H.; Kast, R.; Figueroa-Perez, S.; Bennabi, S.; Gnoth, M. J.; Feurer, A.; Heckroth, H.; Thutewohl, M.; Paulsen, H.; Knorr, A.; Huetter, J.; Lobell, M.; Muenter, K.; Geiss, V.; Ehmke, H.; Lang, D.; Radtke, M.; Mittendorf, J.; Stasch, J.-P. ChemMedChem 2008, 3, 1893-1904:
    Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.
  16. Mittendorf, J.; Weigand S.; Alonso-Alija C.; Bischoff E.; Feurer A.; Gerisch M.; Kern A.; Knorr A.; Lang D.; Muenter K.; Radtke M.; Schirok H.; Schlemmer K.-H.; Stahl, E.; Straub A.; Wunder F.; Stasch J.-P. ChemMedChem2009, 4, 853-865.
  17. Baerfacker L.; Kuhl A.; Hillisch A.; Grosser R.; Figueroa-Pérez S.; Heckroth H.; Nitsche A.; Ergueden J.-K.; Gielen-Haertwig H.; Schlemmer K.-H.; Mittendorf, J.; Paulsen H.; Platzek J.; Kolkhof P. ChemMedChem2012, 7, 1385-1403: Discovery of BAY 94-8862: A Nonsteroidal Antagonist of the Mineralocorticoid Receptor for the Treatment of Cardiorenal Diseases.
  18. Griebenow N.; Schirok H.; Mittendorf J.; Straub A.; Follmann M.; Stasch J.-P.; Knorr A.; Schlemmer K.-H.; Redlich G. Biorg. Med. Chem. Lett. 2013,23, 1197-2000: Identification of acidic heterocycle-substituted 1H-pyrazolo[3,4-b]pyridines as soluble guanylate cyclase stimulators.
  19. Follmann M.; Griebenow N.; Hahn M. G.; Hartung J.; Mais F.-J.; Mittendorf J.; Schaefer M.; Schirok H. Stasch J.-P., Stoll F.; Straub A. Angew. Chem. Int. Ed. 2013, 52, 9442-9462: The Chemistry and Biology of Soluble Guanylate Cyclase Stimulators and Activators.
  20. Nussbaum, F.; Li, V. M.-J.; Allerheiligen, S.; Anlauf, S.; Baerfacker, L.; Bechem, M.; Delbeck, M.; Fitzgerald, M. F.; Gerisch, M.; Gielen-Haertwig, H.; Haning, H.; Karthaus, D.; Lang, D.; Lustig, K.; Meibom, D.; Mittendorf, J.; Rosentreter, U.; Schaefer, M.; Schaefer, S.; Schamberger, J.; Telan, L. A.; Tersteegen, A. ChemMedChem 2015, 10, 1163-1173: Freezing the Bioactive Conformation to Boost Potency: The Identification of BAY 85-8501, a Selective and Potent Inhibitor of Human Neutrophil Elastase for Pulmonary Diseases.
  21. Nussbaum, F.; Li, V. M.-J.; Meibom D.; Anlauf, S.; Bechem M.; Delbeck, M.; Gerisch, M.;Harrenga A.;  Karthaus, D.; Lang, D.; Lustig, K.; Mittendorf, J.; Schaefer, M.; Schaefer, S.; Schamberger, J. ChemMedChem 2016, 11, 199-206: Potent and Selective Human Neutrophil Elastase Inhibitors with Novel Equatorial Ring Topology: in vivo Efficacy of the Polar Pyrimidopyridazine BAY-8040 in a Pulmonary Arterial Hypertension Rat Model
  22. Meibom D.; Albrecht-Kuepper B.; Diedrichs N.; Huebsch W.; Kast R.; Kraemer T.; Krenz U.; Lerchen H.-G.; Mittendorf J.; Nell P. G.; Suessmeier F.; Vakalopoulos A.; Zimmermann K. ChemMedChem 2017, 12, 728-737: Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases.
  23. Follmann M.; Ackerstaff J.; Redlich G.; Wunder F.; Lang D.; Kern A.; Griebenow N.; Kroh  W.; Becker-Pelster E.-M.; Kretschmer A.; Geiss V.; Li V.; Straub A.; Mittendorf J.; Jautelat R.; Schirok H.; Schlemmer K.-H.; Lustig K.; Gerisch M.; Knorr A.; Tinel H.; Mondritzki T.; Truebel H.; Sandner P.; Stasch J.-P. J. Med. Chem.  2017, 60, 5146-5161: Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure

Patents

  1. Mittendorf J.; Hartwig W. Eur. Pat. Appl. 1993, EP 529469 A2: Preparation of 2,3-diamino acids from azidomethyldiketopiperazine derivatives.      
  2. Mittendorf J.; Kunisch F.; Plempel M.; Eur. Pat. Appl. 1993, EP 538691 A1: Preparation of aminotetrahydrothiophenecarboxylates as medical fungicides.  
  3. Mittendorf J.; Kunisch F.; Babczinski P.; Plempel M.; Eur. Pat. Appl. 1993, EP 538689 A1: Preparation of 3-amino-2,3-dihydro-6H-pyran-2-carboxylates as medical fungicides.  
  4. Kunisch F.; Mittendorf J,; Plempel M. Eur. Pat. Appl. 1993, EP 538688 A1: Preparation and antimycotic activity of substituted tetrahydrofurans.
  5. Kunisch F.; Mittendorf J.; Plempel M.; Militzer H.-C. Eur. Pat. Appl. 1993, EP 538692 A1: Preparation and antimycotic activity of partially known substituted pyrrolidines.
  6. Mittendorf J.; Kunisch F.; Matzke M.; Militzer H.-C.; Endermann R.; Metzger K.; Bremm K.-D.; Plempel M.; Eur. Pat. Appl. 1993, EP 571870 A1: Preparation of 1-amino-2-carboxycyclopentanes as antimycotics and antibacterials.
  7. Uhr H.; Kunisch F.; Wachtler M.; Kugler M.; Mittendorf J. Ger. Offen. 1995, DE 4403838 A1: Preparation of 1,3,2-benzodithiazole 1-oxides as microbicides.     
  8. Militzer, H.-C.; Matzke M.; Mittendorf J.; Schmidt A.; Ziegelbauer K.; Schoenfeld W. Ger. Offen. 1996, DE 4443890 A1: Antimicrobial cyclohex-4-enecarboxylic acids and their preparation.    
  9. Mittendorf J.; Fey P.; Junge B.; Kaulen J.; van Laak K.; Meier H.; Schohe-Loop R. Eur. Pat. Appl. 1996, EP 716081 A1: Highly selective process for the preparation of enantiomerically pure phenyl-substituted 1,4-dihydropyridine-3,5-dicarboxylic acid derivatives.  
  10. Fey P.; van Laak K.; Mittendorf J. Ger. Offen. 1996, DE 4446337 A1: Preparation of 3-cyanobenzaldehydes.  
  11. Matzke M.; Militzer H.-C.; Mittendorf J.; Kunisch F.; Schmidt A.; Schoenfeld W.; Ziegelbauer K. Eur. Pat. Appl. 1997, EP 754678 A2: Improvement of physiological tolerance of pharmaceutically active beta amino acids.  
  12. Kunisch F.; Matzke M.; Militzer H.-C.; Mittendorf J.; Babczinski P.; Schmidt A.; Schoenfeld W.; Ziegelbauer K. Ger. Offen. 1997, DE 19604225 A1: Condensation of beta amino acids and beta aminocyclohexenoic acids for use as antimicrobial agents.
  13. Mittendorf J.; Eur. Pat. Appl. 1997, EP 805145 A1: Efficient and highly enantioselective process for the preparation of enantiomerically pure cyclopentane-beta-amino acids. 
  14. Mittendorf J.; Dressel J.; Matzke M.; Franz J.; Spreyer, P.; Voehringer V.; Schuhmacher J.; Friedl A.; Horvath E.; Mauler F.; de Vry J.; Jork R. Ger. Offen. 1998, DE 19706903 A1: Use of agonists of central cannabinoid CB1 receptors in neurodegenerative diseases.  
  15. Mittendorf J.; Dressel J.; Matzke M.; Keldenich J.; Mohrs K.; Raddatz S.;  Franz J.; Spreyer, P.; Voehringer V.; Schuhmacher J.; Rock M. H.; Friedl A.; Horvath E.; Mauler F.; de Vry J.; Jork R. Ger. Offen. 1998, DE 19740785 A1: Preparation of arylsulfonamides and related compounds as cannabinoid CB1 and CB2 receptor agonists.      
  16. Mittendorf J.; Dressel J.; Matzke M.; Keldenich J.; Mauler F.; de Vry J.; Franz J.; Spreyer, P.; Voehringer V.; Schuhmacher J.; Rock M. H.; Horvath E.; Friedl A.; Ger. Offen. 2000, DE 19837627 A1: Preparation of alkylsulfonyloxyphenoxyindanylmethanol amino acid esters and related compounds as CB1 and CB2 cannabinoid receptor agonists.     
  17. Mittendorf J.; Dressel J.; Matzke M.; Keldenich J.; Mauler F.; de Vry J.; Franz J.; Spreyer, P.; Voehringer V.; Schuhmacher J.; Rock M. H.; Horvath E.; Friedl A.; Mohrs K.; Raddatz S.; Jork R. Ger. Offen. 2000, DE 19837638 A1: Preparation of aryl trifluorobutylsulfonates as CB1 receptor antagonists.
  18. Mittendorf J.; Henning R.; Raddatz S.; Schlemmer K.-H., Hiraoka M.; Kadono H.; Mogi M.; Moriwaki T.; Murata T.; Sakakibara S.; Shimada M.; Yoshida N.; Yoshino T. PCT Int. Appl. 2000, WO2000020401 A1: Preparation of bis-benzimidazoles as tryptase inhibitors.
  19. Haerter M.; Albrecht B.; Gerisch M.; Handke G.; Huetter J.; Jensen A.; Krahn T.; Mittendorf J.; Oehme F.; Schlemmer K.-H.; Steinhagen H. PCT Int. Appl. 2002, WO2002006247 A1: Preparation of fused amidoalkyluracils as poly(ADP-ribose) synthetase inhibitors.     
  20. Feurer A.; Bennabi S.; Heckroth H.; Schirok H.; Mittendorf J.; Kast R.; Stasch J.-P.; Gnoth M. J.; Muenter K.; Lang D.; Figueroa Perez S.; Ehmke, H. PCT Int. Appl. 2004, WO20040039796 A1: Preparation of phenylaminopyrimidines as Rho-Kinase II inhibitors for the treatment of cardiovascular diseases.
  21. Bennabi S.; Heckroth H.; Schirok H.; Mittendorf J.; Kast R.; Stasch J.-P.; Gnoth M. J.; Muenter K.; Lang D.; Figueroa Perez S.; Bauser M.; Feurer A.; Ehmke, H. PCT Int. Appl. 2005, WO2005058891 A1: Preparation of pyrrolopyridinyloxyphenylamides and related compounds as cardiovascular agents. 
  22. Schirok H.; Radtke M.; Mittendorf J.; Kast R.; Stasch J.-P.; Gnoth M. J.; Muenter K.; Lang D.; Figueroa Perez S.; Thutewohl M.; Bennabi S.; Ehmke, H. PCT Int. Appl. 2005, WO2005007790 A1: Preparation of heteroaryloxy-substituted phenylamino pyrimidines as Rho kinase inhibitors.
  23. Schirok H.; Stasch J.-P.; Kast R.; Muenter K.; Gnoth M. J.; Figueroa Perez S.; Thutewohl M.; Bennabi S.; Radtke M.; Lang D.; Mittendorf J.; Ehmke, H. PCT Int. Appl. 2005, WO2005108397 A1: Preparation of substituted phenylaminopyrimidines for use as cardiovascular agents.
  24. Schirok H.; Stasch J.-P.; Kast R.; .; Figueroa Perez S.; Muenter K.; Gnoth M. J.; Radtke M.; Lang D.; Mittendorf J. Ger. Offen. 2006, DE 102004060752 A1: Preparation of 4-phenoxy-7-azaindoles as rho kinase II inhibitors.  
  25. Schirok H.; Griebenow N.; Fuerstner C.; Mittendorf J.; Stasch J.-P.; Wunder F.; Schlemmer K.-H.; Heitmeier S.; Stoll F. PCT Int. Appl. 2007, WO2007124854 A1: Fused pyrazole derivatives as cardiovascular agents, their preparation, pharmaceutical compositions, and use in therapy.
  26. Fuerstner C.; Schirok H.; Griebenow N.; Mittendorf J.; Stasch J.-P.; Wunder F.; PCT Int. Appl. 2007, WO2007128454 A1: Preparation of 3-tetrazolylpyrazolopyridines as cardiovascular agents.   
  27. Schirok H.; Mittendorf J.; Stasch J.-P.; Wunder F.; Stoll F.; Schlemmer K.-H. PCT Int. Appl. 2008, WO2008031513 A1: Azabicyclic derivatives as stimulators of guanylate cyclase, their preparation, pharmaceutical compositions, and use for the treatment of cardiovascular disorders.     
  28. Schirok H.; Mittendorf J.; Stasch J.-P.; Wunder F.; PCT Int. Appl. 2008, WO2008061657 A1: Preparation of imidazo[2,1-c]-1,2,4-triazoles as guanylate cyclase activators for treatment of cardiovascular diseases.  
  29. Straub A.; Suessmeier F.; Wunder F; Stasch J.-P.; Li V. M.-J.; Mittendorf J. PCT Int. Appl. 2010, WO 2010079120 A1: Preparation of fused pyrazoles and imidazoles as cardiovascular agents.
  30. Follmann M.; Stasch J.-P.; Redlich G.; Ackerstaff J.; Griebenow N.; Kroh W.; Knorr A.; Becker E.-M.; Wunder F.; Li V. M.-J.; Hartmann E.; Mittendorf J.; Schlemmer K.-H.; Jautelat R.; Bierer D. PCT Int. Appl. 2011, WO 2011147809 A1: Substituted 5-fluoro-1H-pyrazolopyridine derivatives as guanylate cyclase inhibitor and their preparation and use in the treatment of cardiovascular diseases.
  31. Follmann M.; Stasch J.-P.; Redlich G.; Ackerstaff J.; Griebenow N.;  Wunder F.; Li V. M.-J.; Mittendorf J.; Jautelat R. PCT Int. Appl. 2012, WO 2012010576 A1: Carbamate-substituted diaminopyrimidines as guanylate cyclase inhibitors and their preparation and use in the treatment of cardiovascular diseases.
  32. Follmann M.; Stasch J.-P.; Redlich G.; Ackerstaff J.; Griebenow N.; Knorr A.; Wunder F.; Li V. M.-J.; Mittendorf J.; Schlemmer K.-H.; Jautelat R. PCT Int. Appl. 2012, WO 2012059549 A1: Substituted 6-fluoro-1H-pyrazolo[4,3-b]pyridines as guanylate cyclase inhibitors and their preparation and use in the treatment of cardiovascular diseases.
  33. Hahn M.; Follmann M.; Huebsch W.; Becker E.-M.; Stasch J.-P.; Keldenich J.; Delbeck M.; Tinel H.; Wunder F.; Mittendorf J.; Terebesi I.; Lang D.; Martin R. PCT Int. Appl. 2014, WO 2014012934 A1: Preparation of 5-aminotetrahydroquinoline-2-carboxylic acids for use in treatment and/or prevention of cardiovascular and cardiopulmonary disorders.
letzte Änderung: 03.11.2017

Contact

Prof. Dr. J. Mittendorf
Bayer AG
Pharmaceuticals
Medicinal Chemistry Wuppertal
Aprather Weg 18a
D-42113 Wuppertal

Telefon: +49 (0) 2 02 36-43 52
E-Mail