- 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
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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.
- Gilbert, Sophie H.,Viseur, Virginie,Clarke, Matthew L.
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supporting information
p. 6409 - 6412
(2019/06/07)
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- 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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p. 10321 - 10341
(2019/11/21)
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- 4-PIPERIDIN-N-(PYRIMIDIN-4-YL)CHROMAN-7-SULFONAMIDE DERIVATIVES AS SODIUM CHANNEL INHIBITORS
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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.
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- THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF
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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.
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- BENZOXAZEPINES AS INHIBITORS OF P13K/MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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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
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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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- BENZOXAZEPINES AS INHIBITORS OF MTOR AND METHODS OF THEIR USE AND MANUFACTURE
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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
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Page/Page column 37
(2010/12/26)
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- BENZOXAZEPINES AS INHIBITORS OF PI3K/m TOR AND METHODS OF THEIR USE AND MANUFACTURE
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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
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Page/Page column 127
(2010/12/26)
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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 131
(2010/11/27)
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- Enantioselective synthesis of 2-aryl-4-piperidones via rhodium/ phosphoramidite-catalyzed conjugate addition of arylboroxines
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(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%.
- Jagt, Richard B. C.,De Vries, Johannes G.,Feringa, Ben L.,Minnaard, Adriaan J.
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p. 2433 - 2435
(2007/10/03)
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- Chemical compounds
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Formula (1) wherein R represents a halogen atom or a C1-4 alkyl group; R1 represents a C1-4 alkyl group; R2 represents hydrogen or a C1-4 alkyl group; R3 represents hydrogen, or a C1-4 alkyl group; R4 represents a trifluorometyl group; R5 represents hydrogen, a C1-4 alkyl group or C(0)R6; R6? represents C1-4 alkyl, C3-7 cycloalkyl, NH(C1-4 alkyl) or N(C1-4alkyl)2; m is zero or an integer from 1 to 3; n is an integer from 1 to 3 and pharmaceutically acceptable salts and solvates thereof; to processes for their preparation and their use in the treatment of conditions mediated bytachykinins.
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Page/Page column 12
(2010/02/05)
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