924273-15-4Relevant articles and documents
PRODRUGS COMPRISING AN AMINOALKYL GLYCINE LINKER
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, (2016/04/09)
The present invention relates to novel prodrugs of primary or secondary amine- or hydroxyl- comprising biologically active moieties and pharmaceutically acceptable salts thereof, prodrug reagents, pharmaceutical compositions comprising said prodrugs and t
PRODRUGS COMPRISING AN INSULIN LINKER CONJUGATE
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Paragraph 0466-0467; 0469-0470, (2015/11/02)
The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising an insulin linker conjugate D-L, wherein D represents the insulin moiety; and -L is a non-biologically active linker moiety -L1 represented by formula (I), wherein the dashed line indicates the attachment to one of the amino groups of the insulin by forming an amide bond. The invention further relates to pharmaceutical compositions comprising said prodrugs as well as their use as a medicament for treating or preventing diseases or disorders which can be treated by insulin.
Design, synthesis, and biological activity of folate receptor-targeted prodrugs of thiolate histone deacetylase inhibitors
Suzuki, Takayoshi,Hisakawa, Shinya,Itoh, Yukihiro,Suzuki, Nobuaki,Takahashi, Katsumasa,Kawahata, Masatoshi,Yamaguchi, Kentaro,Nakagawa, Hidehiko,Miyata, Naoki
, p. 4208 - 4212 (2008/02/12)
Aiming to develop selective anticancer drugs, we designed and synthesized three disulfides bearing a folic acid moiety as candidate folate receptor (FR)-targeted prodrugs of thiolate histone deacetylase inhibitors. Among them, compound 1 displayed growth-inhibitory activity toward folate receptor-positive MCF-7 breast cancer cells. The activity of 1 was significantly reduced by free folic acid, suggesting that cellular uptake of 1 is mediated by FR.