Synthesis and dopaminergic activity of 3-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans: characterization of an auxiliary binding region in the D1 receptor
摘要:
The synthesis and dopaminergic activity of a series of C3 and nitrogen-substituted 1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-1H-2-benzopyrans (isochromans) is described. The synthesis of the compounds was stereospecific for the 1,3 cis isomer, and the enantioselective synthesis of both enantiomers of one of the analogoues (20) was achieved. It was determined that all of the dopaminergic activity resides in the [1R,3S] isomer. Generally, substitution at the C3 position provided compounds with very high potency (< 10 nm EC50) and selectivity for the D1 receptor, with a wide range of intrinsic activities (60-160%). Analogues containing C3 substituents including aryl, arylalkyl, and cyclic and acyclic alkyl groups showed a marked enhancement of dopaminergic activity compared to the unsubstituted compound. As a class, the drugs were orally active in the rat rotation model with a very long duration of action.
High glass transition temperature polycarbonates derived from adamantane epoxides
申请人:PROMERUS, LLC
公开号:US10626216B2
公开(公告)日:2020-04-21
Embodiments in accordance with the present invention relate generally to polycarbonate polymers having repeat units derived from adamantane epoxide monomers and methods of using such polymers and compositions containing them. The compositions thus formed are useful in a variety of optoelectronic device fabrications.
HIGH GLASS TRANSITION TEMPERATURE PHOTOIMAGEABLE POLYCARBONATE POLYMERS WITH PENDENT POLYCYCLIC FUNCTIONAL GROUPS
申请人:PROMERUS, LLC
公开号:US20150353679A1
公开(公告)日:2015-12-10
Embodiments in accordance with the present invention relate generally to polycarbonate polymers having repeat units derived from polycyclic-epoxide monomers and methods of using such polymers and compositions containing them, and more specifically to polymers and compositions of polycarbonates that encompass repeat units derived from norbornane and tetracyclododecane, and methods of using such compositions.
HIGH GLASS TRANSITION TEMPERATURE POLYCARBONATES DERIVED FROM ADAMANTANE EPOXIDES
申请人:Promerus, LLC
公开号:US20190127522A1
公开(公告)日:2019-05-02
Embodiments in accordance with the present invention relate generally to polycarbonate polymers having repeat units derived from adamantane epoxide monomers and methods of using such polymers and compositions containing them. The compositions thus formed are useful in a variety of optoelectronic device fabrications.
US9527957B2
申请人:——
公开号:US9527957B2
公开(公告)日:2016-12-27
[EN] HIGH GLASS TRANSITION TEMPERATURE PHOTOIMAGEABLE POLYCARBONATE POLYMERS WITH PENDENT POLYCYCLIC FUNCTIONAL GROUPS<br/>[FR] POLYMÈRES DE POLYCARBONATES PHOTOIMAGEABLES AYANT UNE TEMPÉRATURE DE TRANSITION VITREUSE ÉLEVÉE PORTANT DES GROUPES FONCTIONNELS POLYCYCLIQUES LATÉRAUX
申请人:PROMERUS LLC
公开号:WO2014134373A1
公开(公告)日:2014-09-04
Embodiments in accordance with the present invention relate generally to polycarbonate polymers having repeat units derived from polycyclic-epoxide monomers of formula (I) and methods of using such polymers and compositions containing them, and more specifically to polymers and compositions of polycarbonates that encompass repeat units derived from norbomane and tetracyclododecane, and methods of using such compositions.