[EN] COMPOUNDS FOR THE TREATMENT OF AMYLOID-ASSOCIATED DISEASES<br/>[FR] COMPOSÉS POUR LE TRAITEMENT DE MALADIES ASSOCIÉES À LA SUBSTANCE AMYLOÏDE
申请人:REMYND NV
公开号:WO2016083490A1
公开(公告)日:2016-06-02
This invention provides novel compounds of formulae (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein the substituents are as defined in the specification. The present invention also relates to the novel compounds for use as a medicine, more in particular for the prevention or treatment of amyloid-related diseases, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, disorders characterized by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such amyloid-related diseases. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.
Deoxygenative hydroboration of primary, secondary, and tertiary amides: Catalyst‐free synthesis of various substituted amines
作者:Jaeeun Yi、Hyun Tae Kim、Ashok Kumar Jaladi、Duk Keun An
DOI:10.1002/bkcs.12438
日期:2022.1
less reactive functional groups under catalyst-free conditions is an interesting aspect and requires a typical protocol. Herein, we report the synthesis of various primary, secondary, and tertiary amines through hydroboration of amides using pinacolborane under catalyst-free and solvent-freeconditions. The deoxygenative hydroboration of primary and secondary amides proceeded with excellent conversions
Catalytic Hydrogenation of Amides to Amines under Mild Conditions
作者:Mario Stein、Bernhard Breit
DOI:10.1002/anie.201207803
日期:2013.2.18
Under (not so much) pressure: A general method for the hydrogenation of tertiary and secondary amides to amines with excellent selectivity using a bimetallic Pd–Re catalyst has been developed. The reaction proceeds under low pressure and comparatively low temperature. This method provides organic chemists with a simple and reliable tool for the synthesis of amines.
First example of direct reductive amination of aldehydes with primary and secondary amines catalyzed by water-soluble transition metal catalysts
作者:André Robichaud、Abdelaziz Nait Ajjou
DOI:10.1016/j.tetlet.2006.03.153
日期:2006.5
selective direct reductive amination of aldehydes with primary and secondaryamines in water using gaseous hydrogen and water-soluble catalysts is developed. The catalytic system formed in situ from Pd(PhCN)2Cl2 and 2,2′-biquinoline-4,4′-dicarboxylic acid dipotassium salt (BQC), allows full conversion of aldehydes and the formation of desired alkylated amines with excellent yields and selectivities
A compound selected from 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-sulfanyl)-acetyl]-12-epi-mutilins, or 14-O-[((Alkyl-, cycloalkyl-, heterocycloalkyl-, heteoroaryl-, or aryl)-oxy)-acetyl]-12-epi-mutilins, wherein 12-epi-mutilin is characterized in that the mutilin ring at position 12 is substituted by two substituents, the first substituent at position 12 of the mutilin ring is a methyl group which methyl group has the inverse stereochemistry compared with the stereochemistry of the methyl group at position 12 of the naturally occurring pleuromutilin ring, the second substituent at position 12 of the mutilin ring is a hydrocarbon group comprising at least one nitrogen atom and all other substituents of the mutilin ring having the same stereochemistry compared with the stereochemistry of the substituents at the corresponding positions in the naturally occurring pleuromutilin ring; optionally in the form of a salt and/or solvate, wherein the naturally occurring pleuromutilin is of formula
processes for the preparation of such compounds and their use as pharmaceuticals.