Hydroboration. 71. Hydroboration of representative heterocyclic olefins with borane-methyl sulfide, 9-borabicyclo[3.3.1]nonane, dicyclohexylborane, and disiamylborane. Synthesis of heterocyclic alcohols
HETEROCYCLIC TRIAZOLE COMPOUNDS AS AGONISTS OF THE APJ RECEPTOR
申请人:AMGEN INC.
公开号:US20170320860A1
公开(公告)日:2017-11-09
Compounds of Formula I and Formula II, pharmaceutically acceptable salts thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures:
where the definitions of the variables are provided herein.
Provided are cyclosporin A analogues that are NTCP inhibitors and useful for treating HBV and/or HDV infection (s), hepatoprotection and amelioration of hypercholesterolemia, diabetes and inhibiting cancer.
Synthesis of 1,2,3-Trisubstituted Pyrrolidines and 2,3-Disubstituted Tetrahydrofurans via Diastereoselective Reductive Cyclization of γ-Chloroimines and γ-Chloroketones
作者:Norbert De Kimpe、Mudiganti Sastry、Sven Mangelinckx、Bart Lucas
DOI:10.1055/s-0031-1289544
日期:2011.12
involves reductive cyclization of gamma-chloroketimines, which were generated in situ from the reaction of 3-substituted 5-chloro-2-pentanones and a primaryamine. Various reduction conditions were explored to induce a diastereoselective reductive cyclization. 2,3-Disubstituted tetrahydrofurans were obtained by the direct reduction of 3-substituted 5-chloro-2-pentanones with sodiumborohydride.
CYCLOSPORIN DERIVATIVES WHEREIN THE MEBMT SIDECHAIN HAS BEEN CYCLIZED
申请人:Allergan, Inc.
公开号:US20160200767A1
公开(公告)日:2016-07-14
The present invention relates to cyclosporin analogs that are potent inhibitors of cyclophilin D and have low immunosuppressive activity; processes for preparing them; pharmaceutical compositions containing them; and methods for using these analogs and compositions containing them for the treatment of medical conditions, including but not limited to ischemic conditions, such as ischemia-reperfusion (I/R) injury, including myocardial FR injury, cerebral I/R injury, and ocular or retinal I/R injury.
This disclosure describes enantiomerically enriched chiral molecular sieves and methods of making and using the same. In some embodiments, the molecular sieves are silicates or germanosilicates of STW topology.