MASKED CARBOXYLATE NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE
申请人:Jandeleit Bernd
公开号:US20090069419A1
公开(公告)日:2009-03-12
Masked carboxylate neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
COMPLEX PANTOIC ACID ESTER NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE
申请人:Jandeleit Bernd
公开号:US20090076147A1
公开(公告)日:2009-03-19
Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
SIMPLE PANTOIC ACID ESTER NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE
申请人:Jandeleit Bernd
公开号:US20090082440A1
公开(公告)日:2009-03-26
Pantoic acid ester neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs exhibiting enhanced oral bioavailability and methods of using acamprosate prodrugs to treat neurodegenerative disorders, psychotic disorders, mood disorders, anxiety disorders, somatoform disorders, movement disorders, substance abuse disorders, binge eating disorder, cortical spreading depression related disorders, tinnitus, sleeping disorders, multiple sclerosis, and pain are disclosed.
Synthesis of Enantiomerically Pure Eight- and Nine-Membered Lactones by Copper(I) Chloride/2,2’-Bipyridine-Catalyzed Cyclization
作者:Frank O.H. Pirrung、Henk Hiemstra、W. Nico Speckamp、Bernard Kaptein、Hans E. Schoemaker
DOI:10.1055/s-1995-4429
日期:1995.4
The stereocontrolled formation of eight- and nine-membered lactones by Cu(I)Cl/2,2’-bipyridine-catalyzed atom transfer cyclization of enantiomerically pure oxygen-substituted Ï-alkenyl di- and trichloroacetates is described. The lactones are formed exclusively via the endo-cyclization mode and generally show a characteristic cis-relationship between the C-5 and C-6 substituents due to a highly stereoselective ring closure and chlorine transfer.