168144-41-0Relevant articles and documents
VLA-4 INHIBITORY DRUG
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, (2008/12/08)
There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally. A compound represented by the following formula (I): wherein R1 represents a hydrogen atom or a C1-8 alkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, orabenzyloxygroupwhichmaybe substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group whichmaybe substituted; R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and A1 represents a nitrogen atom or C-R3d (wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group), or a salt thereof, or a VLA-4 inhibitory drug comprising the compound or the salt as an active ingredient.
Synthesis of substituted 5-aminomethyl tetrahydro-isoquinolines and dihydro-isoindoles
Fray, M. Jonathan,Allen, Paul,Bradley, Paul R.,Challenger, Clare E.,Closier, Michael,Evans, Tim J.,Lewis, Mark L.,Mathias, John P.,Nichols, Carly L.,Po-Ba, Yvonne M.,Snow, Hayley,Stefaniak, Mark H.,Vuong, Hannah V.
, p. 6869 - 6875 (2007/10/03)
The synthesis of ten substituted aminomethylene tetrahydro-isoquinolines is described, proceeding in eight steps from 5-hydroxyisoquinoline via reductive amination of N-Boc tetrahydro-isoquinoline 5-carboxaldehyde. Likewise, reductive amination was used to prepare four substituted dihydro-isoindoles from the corresponding aldehyde. The dihydro-isoindole ring system was conveniently accessed via a 2+2+2 cycloaddition reaction.
A Comvenient Synthesis of 3-Alkoxyazetidines
Kimpe, Norbert De,Smaele, Dirk De
, p. 5465 - 5478 (2007/10/02)
N-(Alkylidene or arylidene)-2-substituted-2-propenylamines were regiospecifically functionalized into novel N-(alkylidene or arylidene)-2-alkoxy-3-bromo-2-substituted-propylamines, which were proven to be excellent sources for 3-alkoxyazetidines through s