Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121)

Autor: Philippe Muller, Pieter Van Remoortere, Rudy Edmond Willebrords, Fortin Jerome Michel Claude, Tom Valerius Josepha Gevers, Koen Andries, Christophe Meyer, Piet Wigerinck, Heidi Szel, Jean-François Bonfanti, Janssens Frans Eduard, Philip Timmerman, Frederic Marc Maurice Doublet, Peggy Janssens, Koen Wuyts, Laurence Queguiner

Publikováno v: Journal of medicinal chemistry

A preceding paper (Bonfanti et al. J. Med Chem. 2007, 50, 4572−4584) reported the optimization of the pharmacokinetic profile of substituted benzimidazoles by reducing their tissue retention. However, the modifications that were necessary to achiev

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8bccd604791964784d9bd96c5c4ca306
https://pubmed.ncbi.nlm.nih.gov/18254606

Synthesis and biodistribution of [11C]R116301, a promising PET ligand for central NK1 receptors

Autor: Xavier Langlois, Janssens Frans Eduard, C.G.M. Janssen, Albert D. Windhorst, Josée E. Leysen, F.M. Sommen, B. Verreet, Mirek Jurzak, Jacobus D. M. Herscheid, M. Van der Mey

Publikováno v: Van Der Mey, M, Janssen, C G M, Janssens, F E, Jurzak, M, Langlois, X, Sommen, F M, Verreet, B, Windhorst, A D, Leysen, J E & Herscheid, J D M 2005, ' Synthesis and biodistribution of [ 11 C]R116301, a promising PET ligand for central NK 1 receptors ', Bioorganic and Medicinal Chemistry, vol. 13, no. 5, pp. 1579-1586 . https://doi.org/10.1016/j.bmc.2004.12.019
Bioorganic and Medicinal Chemistry, 13(5), 1579-1586. Elsevier Limited

N1-(2,6-Dimethylphenyl)-2-(4-{(2R,4S)-2-benzyl-1-[3,5-di(trifluoromethyl) [carbonyl-11C]benzoyl]hexahydro-4-pyridinyl}piperazino)acetamide ([11C]R116301) was prepared and evaluated as a potential positron emission tomography (PET) ligand for investig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ebae1ade440e4079848c9bff21099622
https://research.vumc.nl/en/publications/491f21c4-da78-43a9-a940-de27e3a89995

Memorial Issue in Honor of Dr. Paul A. J. Janssen Preface

Autor: and Paul J. Lewi, Janssens Frans Eduard, Bruce E. Maryanoff, Robert A. Galemmo

Publikováno v: Journal of Medicinal Chemistry. 48:1685-1685

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f27dd6507638e518afa45f4cc128b221
https://doi.org/10.1021/jm040193r

New antihistaminic N-heterocyclic 4-piperidinamines. 2. Synthesis and antihistaminic activity of 1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-amines

Autor: Janssens Frans Eduard, Marcel Gerebernus Maria Luyckx, Marcel Janssen, Raymond Antoine Stokbroekx, Paul A. J. Janssen, Joseph Leo Ghislanus Torremans

Publikováno v: Journal of Medicinal Chemistry. 28:1934-1943

The synthesis of a series of 1-[(4-fluorophenyl)methyl]-N-(4-piperidinyl)-1H-benzimidazol-2-ami nes and the preliminary evaluation of their in vivo antihistamine activity are described. The title compounds were obtained starting from either 1, 4, 10,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e9803044322ec71cc5a997705b1d9b0
https://doi.org/10.1021/jm00150a029

ChemInform Abstract: Synthetic 1,4-Disubstituted-1,4-Dihydro-5H-tetrazol-5-one Derivatives of Fentanyl: Alfentanil (R 39209), a Potent, Extremely Short-Acting Narcotic Analgesic

Autor: J. Torremans, Paul A. J. Janssen, Janssens Frans Eduard

Publikováno v: ChemInform. 18

The synthesis of a series of N-1,4-disubstituted-1,4-dihydro-5H-tetrazol-5-one piperidinyl derivatives of fentanyl, carfentanil, and sufentanil is described. The 1-substituted tetrazolinones 2 were essentially prepared via the addition reaction of al

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e4a9e9cf0c3cfb15419b426b3f1ffae4
https://doi.org/10.1002/chin.198716217