414910-20-6Relevant articles and documents
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
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
, p. 10321 - 10341 (2019/11/21)
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
A consecutive process for C-C and C-N bond formation with high enantio-and diastereo-control: Direct reductive amination of chiral ketones using hydrogenation catalysts
Gilbert, Sophie H.,Viseur, Virginie,Clarke, Matthew L.
supporting information, p. 6409 - 6412 (2019/06/07)
High diastereoselectivity was observed in the Rh-catalysed reductive amination of 3-arylcyclohexanones to form tertiary amines. This was incorporated into a one-pot enantioselective conjugate addition and diastereoselective reductive amination, including an example of assisted tandem catalysis.
4-PIPERIDIN-N-(PYRIMIDIN-4-YL)CHROMAN-7-SULFONAMIDE DERIVATIVES AS SODIUM CHANNEL INHIBITORS
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Page/Page column 38; 41, (2018/10/19)
The invention provides 4-piperidin-chroman-7-sulfonamide derivatives and salts thereof that are sodium channel modulators, as well as compositions containing such a compound or salt and therapeutic methods for using such a compound, salt, or composition.
THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
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Page/Page column 283; 285, (2017/08/01)
The invention provides a compound of formula: or a salt thereof, wherein the variables RAA, n, ring A, ring B, R1a, R1b, R2, R3, R4, R5, R6, R7, R8, and R9 have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
BENZOXAZEPINES AS INHIBITORS OF P13K/MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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Page/Page column 162, (2012/06/15)
The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds. 9936396.1
BENZOXAZEPINES AS INHIBITORS OF MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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Page/Page column 37, (2010/12/26)
The invention is directed to inhibitors of mTOR and pharmaceutically acceptable salts or solvates thereof, as well as methods of using them. The inhibitors are generally of structural formula wherein the combination of R1 and R2 are
BENZOXAZEPINES AS INHIBITORS OF PI3K/m TOR AND METHODS OF THEIR USE AND MANUFACTURE
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Page/Page column 127, (2010/12/26)
The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention al
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and Efficacious γ-Secretase Inhibitors
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.
scheme or table, p. 2195 - 2199 (2010/07/05)
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.
5-(ARYLSULFONYL)-PYRAZOLOPIPERIDINES
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Page/Page column 131, (2010/11/27)
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.
Enantioselective synthesis of 2-aryl-4-piperidones via rhodium/ phosphoramidite-catalyzed conjugate addition of arylboroxines
Jagt, Richard B. C.,De Vries, Johannes G.,Feringa, Ben L.,Minnaard, Adriaan J.
, p. 2433 - 2435 (2007/10/03)
(Chemical Equation Presented) The highly enantioselective synthesis of 2-aryl-4-piperidones by rhodium/phosphoramidite-catalyzed conjugate addition of arylboroxines to 2,3-dihydro-4-pyridones is described. Both enantiomers of a variety of products with sterically and electronically different R substituents were obtained in high isolated yield and with excellent enantioselectivity up to 99%.