[EN] PHOTOCLEAVABLE DRUG CONJUGATES<br/>[FR] CONJUGUÉS DE MÉDICAMENT PHOTOCLIVABLES
申请人:UNIV MISSOURI
公开号:WO2014004278A1
公开(公告)日:2014-01-03
Novel photocleavable drug conjugates for forming drug depots comprise drugs attached to photocleavable groups. In one embodiment, the drug is linked via photocleavable group(s) to a polymer chain to form a photocleavable drug-polymer conjugate that generally forms the depot matrix. In another embodiment, the drug is crosslinked via photocleavable group(s) to themselves to form a photocleavable drug conjugate that generally forms the depot.
Process employing bipyridyls as inks, of the general formula ##STR1## in which R, R' are, for example, alkyl and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are, for example hydrogen or alkyl radicals, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3, and/or R.sup.4 and R.sup.5 or R.sup.5 and R.sup.6 together with the pyridine ring form in isoquinoline or quinoline ring system.
Bifunctional linkers are provided that comprise a photocleavable moiety flanked by two different amine reactive moieties. In some embodiments the photocleavable moiety is a dimethoxynitrobenzyl moiety. In other embodiments the photocleavable moiety is 8-bromo-7-hydroxyquinoline. In other embodiments the photocleavable moiety is nitrodibenzofuran. In other embodiments the photocleavable moiety is 6-bromo-7-hydroxycoumarin-4-ylmethyl. The linkers find use in synthetic methods, including the generation of photocleavable oligonucleotides, e.g. caged morpholinos.
Bifunctional linkers are provided that comprise a photocleavable moiety flanked by two different amine reactive moieties. In some embodiments the photocleavable moiety is a dimethoxynitrobenzyl moiety. In other embodiments the photocleavable moiety is 8-bromo-7-hydroxyquinoline. In other embodiments the photocleavable moiety is nitrodibenzofuran. In other embodiments the photocleavable moiety is 6-bromo-7-hydroxycoumarin-4-ylmethyl. The linkers find use in synthetic methods, including the generation of photocleavable oligonucleotides, e.g. caged morpholinos.
BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF
申请人:Ambit Biosciences Corporation
公开号:US20150065468A1
公开(公告)日:2015-03-05
Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.