1193-20-0Relevant academic research and scientific papers
Ketoreductase/Transaminase, One-Pot, Multikilogram Biocatalytic Cascade Reaction
Burns, Michael,Bi, Wenying,Kim, Hui,Lall, Manjinder S.,Li, Chao,O'Neill, Brian T.
, p. 941 - 946 (2021/03/01)
A biocatalytic cascade to produce tert-butyl ((2R,4R)-2-methyltetrahydro-2H-pyran-4-yl)carbamate 6 has been demonstrated at the multikilogram scale. In this reaction, a racemic ketone is resolved by reducing the undesired ketone using a ketone reductase (KRED). The reduction is stereospecific for the 2-position of substrate (2S)-ketone leaving the (2R)-ketone unreacted. After the (2S)-ketone has been depleted, a transaminase is added to catalyze the enantioselective transamination of the ketone, resulting in formation of the (2R, 4R)-amine 6. The product is recovered from the aqueous reaction after Boc protection.
CYCLIC SUBSTITUTED IMIDAZO[4,5-C]QUINOLINE DERIVATIVES
-
Page/Page column 48; 49, (2018/09/28)
The present invention provides novel cyclic substituted imidazo[4,5- c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof, wherein R1, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
NOVEL IMIDAZO[4,5-C]QUINOLINE DERIVATIVES AS LRRK2 INHIBITORS
-
Page/Page column 53; 54; 55, (2018/09/28)
The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R1, R2 and R3 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
NOVEL COMPOUNDS
-
Page/Page column 47, (2015/12/17)
Disclosed are novel retinoid-related orphan receptor gamma (RORγ) modulators and their use in the treatment of diseases mediated by RORγ.
NOVEL 4-(HETEROCYCLOALKYL)BENZENE-1,3-DIOL COMPOUNDS AS TYROSINASE INHIBITORS, PROCESS FOR THE PREPARATION THEREOF AND USE THEREOF IN HUMAN MEDICINE AND ALSO IN COSMETICS
-
Page/Page column 20-21, (2010/06/20)
The present invention relates to novel 4- (heterocycloalkyl) benzene- 1,3-diol compounds corresponding to general formula (I) below: to the compositions containing same, to the process for the preparation thereof and to the use thereof in pharmaceutical or cosmetic compositions for use in the treatment or prevention of pigmentary disorders
ANTI-HIV COMPOUNDS
-
Page/Page column 63; 67-68, (2009/08/14)
Thiazole derivatives represented by Formula (I) are disclosed, where R1, R2, R3, A, X, Y, Z, R6 and R7 are disclosed herein. These thiazole derivatives and pharmaceutical compositions comprising these derivatives are useful in the treatment of HIV mediated diseases and conditions.
The Role of the Nitrogen Atom in the Hydrogenation of Piperidinones and Methylenepiperidines
Senda, Yasuhisa,Okamura, Kazue,Kuwahara, Mayumi,Ide, Masatoshi,Itoh, Hiroki,Ishiyama, Jun-Ichi
, p. 799 - 803 (2007/10/02)
Dimethylpiperidinones and dimethylmethylenepiperidines have been hydrogenated over several Group 8, 9 and 10 transition metal catalysts and the stereochemistry of the products compared with those of the carbocyclic analogues.The results obtained suggest that intramolecular interactions between the nitrogen lone pair and the unsaturated bond play a major role in determining the stereochemistry of hydrogenation.
