- CYANO-SUBSTITUTED INDOLE COMPOUNDS AND USES THEREOF AS LSD1 INHIBITORS
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A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for the treatment of lysine (K)-specific demethylase 1A (LSD1) - mediated diseases or disorders: (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein.
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Paragraph 00174
(2017/09/15)
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- Hydroformylation and hydroalkylcarbonylation of 3,4-dihydro[2H]pyran catalysed by Co2(CO)8 under syngas conditions
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In the cobalt-catalysed hydroformylation of 3,4-dihydro[2H]pyran, the influence of different reaction parameters such as time, pressure, triphenylphosphine addition, catalyst and substrate concentration has been investigated. 2-formyl-tetrahydropyran, tetrahydropyran and a hydroalkylcarbonylation product were the main reaction products. The selectivity towards 2-formyl-tetrahydropyran formation is favoured at constant catalyst and substrate concentration. The coordination of the pyran's oxygen to the cobalt atom seems to be an important intermediate for the formation of 2-formyl-tetrahydropyran. Different substrate or catalyst concentrations promote the formation of other reduced products. The addition of triphenylphosphine to the catalyst leads to a less active species, which decreases the yield and promotes the hydroalkylcarbonylation reaction.
- Arias, Jose L.,Sharma, Pankaj,Cabrera, Armando,Beristain, Fernando,Sampere, Rafael,Arizmendi, Cesar
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p. 787 - 792
(2013/10/22)
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- Chiral hetero- and carbocyclic compounds from the asymmetric hydrogenation of cyclic alkenes
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Several types of chiral hetero- and carbocyclic compounds have been synthesized by using the asymmetric hydrogenation of cyclic alkenes. N,P-Ligated iridium catalysts reduced six-membered cyclic alkenes with various substituents and heterofunctionality in good to excellent enantioselectivity, whereas the reduction of five-membered cyclic alkenes was generally less selective, giving modest enantiomeric excesses. The stereoselectivity of the hydrogenation depended more strongly on the substrate structure for the five- rather than the six-membered cyclic alkenes. The major enantiomer formed in the reduction of six-membered alkenes could be predicted from a selectivity model and isomeric alkenes had complementary enantioselectivity, giving opposite optical isomers upon hydrogenation. The utility of the reaction was demonstrated by using it as a key step in the preparation of chiral 1,3-cis-cyclohexane carboxylates. Copyright
- Verendel, J. Johan,Li, Jia-Qi,Quan, Xu,Peters, Byron,Zhou, Taigang,Gautun, Odd R.,Govender, Thavendran,Andersson, Pher G.
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p. 6507 - 6513
(2012/06/29)
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- 1,3,4-oxadiazol-2(3H)-one derivatives, their preparation and their therapeutic application
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1,3,4-Oxadiazol-2(3H)-one derivatives, of formula STR1 in which R1 represents either a hydrogen atom or a linear or branched (C1-4)alkyl group which is substituted with a hydroxyl group, a phenoxy group, a (C1-4)alkoxy group, a (C1-4)alkylthio group, a mercapto group, a (C1-4)alkoxy-(C1-4)alkoxy group, a di(C1-4)alkylamino group or an N-(C1-4)alkyl-N-propynylamino group, or represents a (C3-4)alkynyl group, and R2 either represents a linear or branched (C1-8)alkyl group which is substituted with one or more halogen atoms and/or a hydroxyl group, a 1-imidazolyl group or a 3-tetrahydropyranyl group, or represents a trifluoro(C3-5)alkenyl group, in the form of pure enantiomers or mixtures of enantiomers, including racemic mixtures, as well as the addition salts thereof with pharmaceutically acceptable acids, are useful as inhibitors of monoamine oxidase B.
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