Medicinal Chemistry (Marc Nazaré)

Publications

Brennecke, B.; Wang, Q.; Zhang, Q.; Hu, H.-Y.; Nazare, M. An Activatable Lanthanide Luminescent Probe for Time-Gated Detection of Nitroreductase in Live Bacteria. Angew. Chem. Int. Ed.2020, early access, https://doi.org/10.1002/anie.202002391.

                                               
 

Webel, H. E.; Kimber, T. B.; Radetzki, S.; Neuenschwander, M.; Nazare, M.; Volkamer, A. Revealing cytotoxic substructures in molecules using deep learning. J. Comput. Aided Mol. Des.2020, https://doi.org/10.1007/s10822-020-00310-4.

Plastira, I.; Joshi, L.; Bernhart, E.; Schoene, J.; Specker, E.; Nazare, M., Sattler, W. Small-Molecule Lysophosphatidic Acid Receptor 5 (LPAR5) Antagonists: Versatile Pharmacological Tools to Regulate Inflammatory Signaling in BV-2 Microglia Cells. Front. Cell. Neurosci. 2019, 13, 531.

Schoene, J.; Gazzi, T.; Lindemann, P.; Christmann, M.; Volkamer, A.; Nazare, M. Probing 2H-Indazoles as Templates for SGK1, Tie2, and SRC Kinase Inhibitors. ChemMedChem 2019, 14, 1514-1527.

               

Zhang, Q.; Xu, S.; Lai, F.; Wang, Y.; Zhang, N.; Nazare, M.; Hu, H.-Y. Rapid Synthesis of γ-Halide/Pseudohalide-Substituted Cyanine Sensors with Programmed Generation of Singlet Oxygen. Org. Lett. 2019, 21, 2121-2125.

                                           
 

Schewe, M.; Sun, H.; Mert, Ü.; Mackenzie, A.; Pike, A. C. W.; Schulz, F.; Constantin, C.; Vowinkel, K. S.; Conrad, L. J.; Kiper, A. K.; Gonzalez, W.; Musinszki, M.; Tegtmeier, M.; Pryde, D. C.; Belabed, H.; Nazare, M.; de Groot, B. L.; Decher, N.; Fakler, B.; Carpenter, E. P.; Tucker, S. J.; Baukrowitz, T. A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels. Science 2019, 363, 875-880.

    
 

Brennecke, P.; Rasina, D.; Aubi, O.; Herzog, K.; Landskron, J.; Cautain, B.; Vicente, F.; Quintana, J.; Mestres, J.; Stechmann, B.; Ellinger, B.; Brea, J.; Kolanowski, J. L.; Pilarski, R.; Orzaez, M.; Pineda-Lucena, A.; Laraia, L.; Nami, F.; Zielenkiewicz, P.; Paruch, K.; Hansen, E.; von Kries, J. P.; Neuenschwander, M.; Specker, E.; Bartunek, P.; Simova, S.; Lesnikowski, Z.; Krauss, S.; Lehtiö, L.; Bilitewski, U.; Brönstrup, M.; Taskén, K.; Jirgensons, K.; Lickert, H.; Clausen, M. H.; Andersen, J. H.; Vicent, M. J.; Genilloud, O.; Martinez, A.; Nazare, M.; Fecke, W.; Gribbon P. EU-OPENSCREEN: A Novel Collaborative Approach to Facilitate Chemical Biology. SLAS Discov. 2019, 24, 398-413.

           

 

Marcinkowski, P.; Hoyer, I.; Specker, E.; Furkert, J.; Rutz, C.; Neuenschwander, M.; Sobottka, S.; Sun, H.; Nazare, M.; Berchner-Pfannschmidt, U.; von Kries, J.-P.; Eckstein, A.; Schülein, R.; Krause, G. A new highly thyrotropin receptor-selective small molecule antagonist wih potential for the treatment of Graves' orbitopathy. Thyroid 201929, 111-123.

            
 

Klein, W.; Rutz, C.; Eckhard, J.; Provinciael, B.; Specker, E.; Neuenschwander, M.; Kleinau, G.; Scheerer, P.; von Kries, J.-P.; Nazare, M.; Vermeire, K.; Schülein, R. Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway. PLoS ONE 201813, e0208641. 

                                                

Schulze, J.; Baukmann, H.; Wawrzinek, R.; Fuchsberger, F. F.; Specker, E.; Aretz, J.; Nazare, M.; Rademacher, C. CellFy: A Cell-Based Fragment Screen against C-Type Lectins. ACS Chem. Biol. 2018, 13, 3229-3235. 


                                          
 

Aretz, J.; Anumala, U. R.; Fuchsberger, F. F.; Molavi, N.; Ziebart, N.; Zhang, H.; Nazare, M.; Rademacher, C. Allosteric Inhibition of a Mammalian Lectin. J. Am. Chem. Soc. 2018, 140, 14924-14934.

                                       
 

Duro-Castano, A.; Lim, N. H.; Tranchant, I.; Amoura, M.; Beau, F.; Wieland, H.; Kingler, O.; Hermann, M.; Nazare, M.; Plettenburg. O.; Dive, V.; Vicent, M. J.; Nagase, H. In vivo Imaging of MMP-13 Activity Using a Specific Polymer-FRET Peptide Conjugate Detects Early Osteoarthritis and Inhibitor Efficacy. Adv. Funct. Mater. 2018, 28, 1802738.

                  

Ruess, D. A.; Heynen, G. J.; Ciecielski, K. J.; Ai, J.; Berninger, A.; Kabacaoglu, D.; Görgülü, K.; Dantes, Z.; Wörmann, S. M.; Diakopoulus, K. N.; Karpathaki, M. K.; Kowalska, M.; Kaya-Aksoy; E.; Song, L.; Zeeuw van der Laan, E. A.; López-Alberca, M. P.; Nazaré, M.; Reichert, M.; Saur, D.; Erkan, M. M.; Hopt, U. T.; Sainz Jr, B.; Birchmeier, W.; Schmid, R. M.; Lesina, M.; Algül, H. Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase. Nat. Med. 2018, 24, 954-960.

                                        

Schoene, J.; Bel Abed, H., Schmieder, P.; Christmann, M.; Nazare, M. A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorous-Silane System. Chem. Eur. J. 2018, 24, 9090-9100.

                                      
 

Bel Abed, H.; Weißing, N.; Schoene, J.; Paulus, J.; Sewald, N., Nazare, M. Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives. Tetrahedron Lett. 2018, 59, 1813-1815.

               


Wenskowsky L.; Schreuder, H.; Derdau, V.; Matter, H.; Volkmar, J.; Nazaré, M.; Opatz, T.; Petry, S. Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin. Angew. Chem. Int Ed. 2018, 57, 1044-1048.  

                                       
 

Liu, Y.; Zhang, L.; Nazare, M.; Yao, Q.; Hu, H.-Y. A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging. Acta Pharm. Sin. B 2018, 8, 401-408.

                                        
 

Anumala, U. R.; Waaler, J.; Nkizinkiko, Y.; Ignatev, A.; Lazarow, K.; Lindemann, P.; Olsen, P. A.; Murthy, S.; Obaji, E.; Majouga, A. G.; Leonov, S.; von Kries, J. P.; Lehtiö, L.; Krauss, S.; Nazaré, M. Discovery of a Novel Series of Tankyrase Inhibitors by a Hybridization Approach. J. Med. Chem. 2017, 60, 10013-10025.

                       
 

Griger, J.; Schneider, R.; Lahmann, I.; Schowel, V.; Keller, C.; Spuler, S.; Nazaré, M.; Birchmeier, C. Loss of Ptpn11 (Shp2) drives satellite cells into quiescence. eLife2017, 6, e21552.

Schoene, J.; Bel Abed, H.; Christmann, M.; Nazaré, M. A straightforward approach to N-substituted-2H-indazol-2-amines through reductive cyclization. Tetrahedron Lett. 2017, 58, 1633-1635.
                                                                               

Sun, H.; Horatscheck, A.; Martos, V.; Bartetzko, M.; Uhrig, U.; Lentz, D.; Schmieder, P.; Nazaré, M. Direct Experimental Evidence for Halogen-Aryl π Interactions in Solution from Molecular Torsion Balances. Angew. Chem. Int. Ed. 2017, 129, 6554-6558.

                                                      
                                       

Carter, D. M.; Specker, E.; Przygodda, J.; Neuenschwander, M.; von Kries, J.P.; Heinemann, U.; Nazaré, M.; Gohlke, U. Identification of a Novel Benzimidazole Pyrazolone Scaffold that Inhibits KDM4 Lysine Demethylases and Reduces Proliferation of Prostate Cancer Cells. SLAS Discov. 2017, 22, 801-812.
 

Robertson, M. J.; Horatscheck, A.; Sauer, S.; von Kleist, L.; Baker, J. R.; Stahlschmidt, W.; Nazaré, M.; Whiting, A.; Chau, N.; Robinson, P. J.; Haucke, V.; McCluskey, A. 5-Aryl-2-(naphtha-1-yl)sulfonamido-thiazol-4(5H)-ones as clathrin inhibitors. Org. Biolmol. Chem. 2016, 14, 11266-11278.

                                            
 

Geiger, M.-A.; Orwick-Rydmark, M.; Märker, K.; Franks, W. T.; Akhmetzyanov, D.; Stöppler, D.; Zinke, M.; Specker, E.; Nazaré, M.; Diehl, A.; van Rossum, B.-J.; Aussenac, F.; Prisner, T.; Akbey, Ü.; Oschkinat, H. Temperature dependence of cross-effect dynamic nuclear polarization in rotating solids: advantages of elevated temperatures. Phys. Chem. Chem. Phys. 201618, 30696-30704. 

                                     
 

Bel Abed, H.; Schoene, J.; Christmann, M.; Nazare, M. Organophosphorus-mediated N-N bond formation: facile access to 3-amino-2H-indazoles. Org. Biomol. Chem. 2016, 14, 8520-8528.

                              
 

Kozian, D. H.; von Haeften, E.; Joho, S.; Czechtizky, W.; Anumala, U. R.; Roux, P.; Dudda, A.; Evers, A.; Nazare, M. Modulation of Hexadecyl-LPA-Mediated Activation of Mast Cells and Microglia by a Chemical Probe for LPA5. ChemBioChem 201617, 861-865.

                                                     
 

Aretz, J.; Kondoh, Y.; Honda, K.; Anumala, U. R.; Nazaré, M.; Watanabe, N.; Osada, H.; Rademacher, C. Chemical fragment arrays for rapid druggability assessment. Chem. Commun. 2016, 52, 9067-9070. 


                                       
 

Hu, H.-Y.; Lim, N.-H.; Juretschke, H.-P.; Ding-Pfennigdorf, D.; Florian, P.; Kohlmann, M., Kandira, A.; von Kries, J. P.; Saas, J.; Rudolphi, K. A.; Wendt, K. U.; Nagase, H.; Plettenburg, O.; Nazaré, M.; Schultz, C. In vivo visualization of osteoarthritic hypertrophic lesions. Chem. Sci. 20156, 6256-6261.

                                
 

Hu, H.-Y.; Lim, N.-H.; Ding-Pfennigdorff, D.; Saas, J.; Wendt, U.; Ritzeler, O.; Nagase, H.; Plettenburg, O.; Schultz, C.; Nazaré, M. DOTAM Derivatives as Active Cartilage-targeting Drug Carriers for the Treatment of OA. Bioconj. Chem. 201526, 383-388.
                   
                                   

Halland, N.; Schmidt, F.; Weiss, T.; Saas, J.; Li, Z.; Czech, J.; Dreyer, M.; Hofmeister, A.; Mertsch, K.; Dietz, U.; Strübing, C.; Nazaré, M. Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors. ACS Med. Chem. Lett. 20156, 73-78.

                      
 

Boldron, C.; Besse, A.; Bordes, M.-F.; Tissandié, S.; Yvon, X.; Gau, B.; Badorc, A.; Rousseaux, T.; Barré, G.; Meneyrol, J.; Zech, G.; Nazaré, M.; Fossey, V.; Pflieger, A.-M.; Bonnet-Lignon, S.; Millet, L.; Briot, C.; Dol, F.; Herault, J.-P.; Savi, P.; Lassalle, G. Y.; Delesque, N.; Herbert, J.-M.; Bono, F. N-[6-(4-butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methyl-piperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible and Directly Acting P2Y12 Antagonist. J. Med. Chem. 201457, 7293-7316.

                     
 

Wilde, F.; Specker, E.; Neuenschwander, M.; Nazaré, M.; Bodtke, A.; Link, A. Tractable synthesis of multipurpose screening compounds with under-represented molecular features for an open access screening platform. Mol. Divers. 201418, 483-495.

                                            
 

Fälker, K.; Nazaré; M., Wonerow, P.; Kozian, D. H. Targeting Platelet G Protein-Coupled Receptors for Antithrombotic TherapyDrug Dev. Res201374, 440–449.

Zech, G.; Hessler, G.; Evers, A.; Weiss, T.; Florian, P.; Just, M.; Czech, J.; Czechtizky, W.; Görlitzer, J.; Ruf, S.; Kohlmann, M.; Nazaré, M. Identification of High Affinity P2Y12 Antagonists Based on a Phenylpyrazole Glutamic Acid Piperazine Backbone. J. Med. Chem. 2012, 55, 8615-8629.

                          
 

Kozian, D. H., Evers, A.; Florian, P.; Wonerow, P.; Joho, S.; Nazaré, M. Selective Non-Lipid Modulator of LPA5 Activity in Human PlateletsBioorg. Med. Chem. Lett. 2012, 22, 5239-5243.

                          

 

Matter, H.; Nazaré, M.; Güssregen, S. Halogen-π Interactions as Important Contribution to Binding Affinity in Medicinal Chemistry. Frontiers in Crystal Engineering III: The Importance of pi-Interaction in Crystal Engineering. Tiekink, E. R. T.; Zuckerman-Schpector, J. Eds.; Wiley2012, pp 187-209.

Nazaré, M; Matter, H.; Will, D. W.; Wagner, M.; Urmann, M.; Czech, J.; Schreuder, H.; Bauer, A.; Ritter, K.; Wehner, V. Fragment Deconstruction of Small, Potent Factor Xa Inhibitors: Exploring the Superadditivity Energetics of Fragment Linking in Protein-Ligand Complexes. Angew. Chem. Int. Ed. 201251, 905-911.

                                       
 

Alonso, J.; Halland, N.; Nazaré, M.; R’kyek, O.; Urmann, M.; Lindenschmidt, A. A Direct, Regioselective Palladium-Catalyzed Synthesis of N-Substituted Benzimidazoles and Imidazopyridines. Eur. J. Org. Chem. 2011, 234-237.


                             
 

Halland, N.; Nazaré, M.; Alonso, J.; R'kyek, O.; Lindenschmidt, A. A general and mild domino approach to substituted 1-aminoindoles. Chem. Commun. 201147, 1042-1044.
                     
                  
 

R'kyek, O.; Halland, N.; Lindenschmidt, A.; Alonso, J.; Lindemann, P.; Urmann, M.; Nazaré, M. A General Palladium-Catalyzed Sonogashira Coupling of Aryl and Heteroaryl Tosylates. Chem. Eur. J. 2010, 16, 9986-9989.

                                
 

Halland, N.; Nazaré, M.; R'kyek, O.; Alonso, J.; Urmann, M.; Lindenschmidt, A. A General and Mild Palladium-Catalyzed Domino Reaction for the Synthesis of 2H-Indazoles. Angew. Chem. Int. Ed. 200948, 6879-6882.

                          
 

Matter, H.; Nazaré, M.; Guessregen, S.; Will, D. W.; Schreuder, H.; Bauer, A.; Urmann, M.; Ritter, K.; Wagner, M.; Wehner, V. Evidence for C-Cl/C-Br...π interactions as an important contribution to protein-ligand binding affinity. Angew. Chem. Int. Ed. 200948, 2911-2916.

                                                        
 

Nazaré, M., Will, D. W.; Matter, H.; Schreuder, H.; Ritter,K.; Urmann, M.; Essrich, M.; Bauer, A.; Wagner, M.; Czech, J.; Laux, V.; Wehner, V. Probing the Sub-pockets of Factor Xa by SAR and X-ray Crystallography: Factor Xa inhibitors based on a 2-Carboxyindole Scaffold. J. Med. Chem. 2005, 48, 4511-4525.

                                             
 

Matter, H.; Will, D. W.; Nazaré, M.; Schreuder, H.; Laux, V.; Wehner, V. Structural Requirements for Factor Xa Inhibition by 3-Oxybenzamides with Neutral P1 Substituents: Combining X-ray Crystallography, 3D-QSAR and Tailored Scoring Functions. J. Med. Chem. 2005, 48, 3290-3312.

                                               

Nazaré, M.; Schneider, C.; Lindenschmidt, A.; Will, D. W. A flexible, palladium-catalyzed indole and azaindole synthesis by direct annulation of chloroanilines and chloroaminopyridines with ketones. Angew. Chem. Int. Ed. 2004, 43, 4526-4528.

                           
 

Nazaré, M.; Essrich, M.; W. Will, D. W.; Matter, H.; Ritter, K.; Urmann, M.; Bauer, A.; Schreuder, H.; Czech, J.; Lorenz, M.; Laux, V.; Wehner, V. Novel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Group. Bioorg. Med. Chem. Lett. 200414, 4197-4201.

                                                      
 

Nazaré, M.; Essrich, M.; W. Will, D. W.; Matter, H.; Ritter, K.; Urmann, M.; Bauer, A.; Schreuder, H.; Dudda, A.; Czech, J.; Lorenz, M.; Laux, V.; Wehner, V. Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents. Bioorg. Med. Chem. Lett. 200414, 4191-4195.

                                                                 
 

Nazaré, M.; Matter, H.; Klingler, O.; Al-Obeidi, F.; Schreuder, H.; Zoller, G.; Czech, J.; Lorenz, M.; Dudda, A.; Peyman, A.; Nestler, H.-P.; Urmann, M.; Bauer, A.; Laux, V.; Wehner, V.; Will, D. W. Novel Factor Xa Inhibitors Based on a Benzoic Acid Scaffold and Incorporating a Neutral P1 Ligand. Bioorg. Med. Chem. Lett. 2004, 14, 2801-2805.

                                                               
 

Nazaré, M.; Waldmann, H. Enantiospecific synthesis of the (9S,18R)-diastereomer of the leukocyte adhesion inhibitor cyclamenol A. Chem. Eur. J. 2001, 7, 3363-3376.                                                              

Nazaré, M.; Waldmann, H.  Synthesis of the (9S,18R) diastereomer of cyclamenol A. Angew. Chem. Int. Ed. 2000, 39, 1125-1128.

Nazaré, M.; Waldmann, H. Synthesis of the (9S,18R)-seco acid of the leukocyte adhesion inhibitor cyclamenol A. Tetrahedron Lett2000, 41, 625-628.

Schlede, U.; Nazaré, M.; Waldmann, H. Efficient enantioselective synthesis of a ß-hydroxyepoxide building block for the construction of macrocyclic natural products. Tetrahedron Lett1998, 39, 1143-1144.

                

Patents

Krauss, S.; Nazare, M.; Anumala, U. R.; Lehtio, L.; Waaler, J.; Holsworth, D.; Wegert, A.; Leenders, R. G. G. Preparation of triazole derivatives as tankyrase inhibitors useful in treatment and prevention of diseases. WO 2018118868

Scheidereit, C.; Willenbrock, M.; Lindemann, P.; Radetrki, S.; Von Kries, J. P.; Nazare, M.; Preparation of polycyclic nitrogen heterocycles as selective inhibitors of genotoxic stress-induced IKK/NF-kB pathways for the treatment of diseases. WO 2018087389

Bader, M.; Specker, E.; Matthes, S.; Schuetz, A.; Mallow, K., Grohmann, M. Nazare, M. Preparation of xanthine derivatives as tryptophan hydroxylase inhibitors for the treatment of serotonin-related disorders. WO 2018019917

Krause, G.; Hoyer, I.; Specker, E.; Furkert, J.; Marcinkowski, P.; Von Kries, J.-P.; Neuenschwander, M.; Nazare, M. Synthesis of antagonists of the thyroid-​stimulating hormone receptor (TSHR). WO 2017186793

Bader, M.; Specker, E.; Matthes, S.; Schuetz, A.; Mallow, K.; Grohmann, M.; Nazaré, M. Xanthine derivatives, their use as a medicament, and pharmaceutical preparations comprising the same. WO 2016135199

Hu, H.-Y; Nazare, M.; Han Lim, N.; Ding-Pfennigdorff, D.; Plettenburg, O.; Ritzeler, O; Juretschke, H.-P.; Saas, J.; Bartnik, E.; Florian, P.; Wendt, U.; Schultz, C.; Nagase, H. DOTAM derivatives for therapeutic use. WO 2015075699

Nazaré, M.; Halland, N.; Schmidt, F.; Kleemann, H.-W.; Weiss, T.; Saas, J.; Struebing, C.; N-(4-(Azaindazol-6-yl)-phenyl)-sulfonamides and their use as pharmaceuticals. WO 2014140065

Petry, S; Nazaré, M.; Schmidt, T.; Matter, H.; Fluorescence-labelled fatty acids binding to fatty acid-binding compd. to elicit FRET (Foerster resonance energy transfer) and uses thereof. WO 2014037394

Nazaré, M.; Kozian, D.; Bossart, M., Czechtizky, W., Evers, A. Benzo[1,3]dioxine derivatives and their use as LPAR5 antagonists. WO 2013171318.

Nazaré, M.; Kozian, D.; Evers, A.; Czechtizky, W. Pyrazole derivatives and their use as LPAR5 antagonists. WO 2013171317.

Nazaré, M.; Kozian, D.; Evers, A.; Czechtizky, W. Pyridine derivatives and their use as LPAR5 antagonists. WO 2013171316.

Nazaré, M.; Halland, N.; Schmidt, F.; Weiß, T.; Dietz, U.; Hofmeister, A. N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl] sulfonamide derivatives as kinase inhibitors. WO 2013041119.

Nazaré, M.; Zech, G.; Just, M.; Weiss, T.; Hessler, G.; Kohlmann, M. Preparation of heterocyclic pyrazole-carboxamides as P2Y12 antagonists for treating cardiovascular diseases and other disorders. WO 2009080226.

Nazaré, M.; Zech, G.; Goerlitzer, J.; Just, M.; Weiss, T.; Hessler, G.; Czechtizky, W.; Ruf, S. Preparation of pyrazole-carboxamide derivatives as P2Y12 antagonists for treating cardiovascular disorders. WO 2009080227.

R'Kyek, O.; Nazaré, M.; Lindenschmidt, A.; Urmann, M.; Halland, N.; Alonso, J. A process for the palladium-catalyzed coupling of terminal alkynes with aryl tosylates. WO 2009003589.

R'Kyek, O.; Nazaré, M.; Lindenschmidt, A.; Alonso, J.; Urmann, M.; Halland, N.; A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates. WO 2009003590.

Alonso, J.; Lindenschmidt, A.; Nazaré, M.; Urmann, M.; Halland, N.; R'Kyek, O. A regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles. WO 2009000413.

Alonso, J.; Lindenschmidt, A.; Nazaré, M.; R'Kyek, O.; Urmann, M.; Halland, N. A regioselective metal catalyzed synthesis of annulated benzimidazoles and azabenzimidazoles.; WO 2009000412.

Halland, N.; Nazaré, M.; Lindenschmidt, A.; Alonso, J.; R'Kyek, O.; Urmann, M. A transition metal catalyzed synthesis of 2H-indazoles. WO 2009000411.

Nazaré, M.; Zech, G.; Just, M.; Weiss, T.; Hessler, G.; Czech, J. Quinoline-carboxamide derivatives as P2Y12 antagonists and their preparation, pharmaceutical compositions and use in the treatment of cardiovascular diseases. WO 2008128647.

Halland, N.; Nazaré, M.; Lindenschmidt, A.; Rkyek, O.; Urmann, M.; Alonso, J. A transition metal catalyzed synthesis of N-aminoindoles. WO 2008125207.

Alonso, J.; Lindenschmidt, A.; Nazaré, M.; Halland, N.; Rkyek, O.; Urmann, M. A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles from halonitroarenes and amides. WO 2008009348.

Wagner, M.; Urmann, M.; Wehner, V.; Lorenz, M.; Bauer, A.; Nazaré, M.; Matter, H.; Preparation of heteroarylcarboxylic acid sulfamoylalkyl amides as factor Xa inhibitors. WO 2006122661.

Urmann, M.; Nazaré, M.; Matter, H.; Wehner, V.; Bauer, A.; Wagner, M., Beta-aminoacid-derivatives as factor Xa inhibitors. WO 2005095440.

Bauer, A.; Wagner, M.; Nazaré, M.; Wehner, V.; Urmann, M.; Matter, H. Pyrrole-derivatives as factor Xa inhibitors. WO 2005085239.

Nazaré, M.; Laux, V.; Bauer, A.; Wagner, M. Triazole-derivatives as factor Xa inhibitors. WO 2004101555.

Nazaré, M.; Wehner, V.; Laux, V.; Urmann, M.; Bauer, A.; Matter, H. Indazole-derivatives as factor Xa inhibitors.  WO 2004101556.

Nazaré, M.; Wehner, V.; Will, D. W.; Ritter, K.; Urmann, M.; Matter, H. Azaindole-derivatives as factor Xa inhibitors.WO 2004101563.

Nazaré, M.; Wagner, M.; Wehner, V.; Matter, H.; Urmann, M.; Ritter, K.  Benzimidazole-derivatives as factor Xa inhibitors. WO 2004101553.

Nazaré, M.; Wehner, V.; Ritter, K.; Laux, V.  New Indole-derivatives as factor Xa inhibitors WO 2004101554.

Nazaré, M.; Bauer, A.; Wehner, V.; Will, D. W.; H. Matter, H.; Wagner, M.; Schreuder, H.  Imidazole-derivatives as factor Xa inhibitors. WO 200405636.

Nazaré, M.; Wehner, V.; Will, D. W.; Matter, H.  Pyrazole-derivatives as factor Xa inhibitors. WO2004056815.

Nazaré, M.; Essrich, M.; Will, D. W.; Matter, H.; Ritter, K.; Wehner, V.  Preparation of indole-2-carboxamides as factor Xa inhibitors. WO 2003044014.

Nazaré, M.; Will, D. W.; Peyman, A.; Matter, H.; Zoller, G.; Gerlach, U.  Oxybenzamides derivatives as factor Xa inhibitors. WO 2002051831.

Peyman, A.; Will, D. W.; Gerlach, U.; Nazaré, M.; Zoller, G.; Nestler, H.-P.; Matter, H.; Al-Obeidi, F.  Preparation of guanidines and amidines as Factor Xa and/or VIIa inhibitors. WO 2002046159.

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