- Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent, and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels in Vivo
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The human luteinizing hormone receptor (hLH-R) is a member of the glycoprotein hormone family of G-protein-coupled receptors (GPCRs), activated by luteinizing hormone (hLH) and essentially involved in the regulation of sex hormone production. Thus, hLH-R
- Wortmann, Lars,Lindenthal, Bernhard,Muhn, Peter,Walter, Alexander,Nubbemeyer, Reinhard,Heldmann, Dieter,Sobek, Lothar,Morandi, Federica,Schrey, Anna K.,Moosmayer, Dieter,Günther, Judith,Kuhnke, Joachim,Koppitz, Marcus,Lücking, Ulrich,R?hn, Ulrike,Sch?fer, Martina,Nowak-Reppel, Katrin,Kühne, Ronald,Weinmann, Hilmar,Langer, Gernot
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- Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors
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Discovery of a series of pyrazolopiperidine sulfonamide based γ-secretase inhibitors and its SAR evolution is described. Significant increases in APP potency on the pyrazolopiperidine scaffold over the original N-bicyclic sulfonamide scaffold were achieved and this potency increase translated in an improved in vivo efficacy.
- Ye, Xiaocong M.,Konradi, Andrei W.,Smith, Jenifer,Xu, Ying-Zi,Dressen, Darren,Garofalo, Albert W.,Marugg, Jennifer,Sham, Hing L.,Truong, Anh P.,Jagodzinski, Jacek,Pleiss, Michael,Zhang, Hongbin,Goldbach, Erich,Sauer, John-Michael,Brigham, Elizabeth,Bova, Michael,Basi, Guriqbal S.
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scheme or table
p. 2195 - 2199
(2010/07/05)
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- 5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES
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The invention provides N-cyclic sulfonamido compounds of Formula (I) wherein A, B, R1, R1a, R2, R2a, R3 and R3a are as described in the specification. Compounds of Formula (I) are useful in treating or preventing cognitive disorders, such as Alzheimer 's disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I), methods of preparing compounds of formula (I), and methods of treating cognitive disorders, such as Alzheimer's disease.
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Page/Page column 111
(2010/11/27)
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