[EN] Anticancer Drugs and Methods of Making and Using Same<br/>[FR] MÉDICAMENTS ANTICANCÉREUX ET LEURS PROCÉDÉS DE FABRICATION ET D'UTILISATION
申请人:UNIV YALE
公开号:WO2019023621A1
公开(公告)日:2019-01-31
The present invention provides drug modifications for improving biodistribution and/or specificity of an anticancer drug. In certain embodiments, the compound of the invention comprises a drug, a linker and a core acid. The core acid can be varied to tune the properties of the compound within the body such that the compound more selectively distributes to tumors and is, or becomes active in the cytosol.
A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L
D
-D, the protein based recognition-molecule being connected to the polymeric carrier by L
P
. Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. L
D
and L
P
are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
ANTICANCER DRUGS AND METHODS OF MAKING AND USING SAME
申请人:YALE UNIVERSITY
公开号:US20210085796A1
公开(公告)日:2021-03-25
The present invention provides drug modifications for improving biodistribution and/or specificity of an anticancer drug. In certain embodiments, the compound of the invention comprises a drug, a linker and a core acid. The core acid can be varied to tune the properties of the compound within the body such that the compound more selectively distributes to tumors and is, or becomes active in the cytosol.
A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric scaffold having one or more -LD-D, the PBRM being connected to the polymeric scaffold by Lp, wherein the polymeric scaffold comprises a linear, branched or cyclic polymer having four or more -OH groups. Each occurrence of D is independently a therapeutic agent having a molecular weight < 5 kDa. LD and Lp are linkers connecting the therapeutic agent and PBRM to the polymeric scaffold respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
[EN] ANTICANCER DRUGS AND METHODS OF MAKING AND USING SAME<br/>[FR] MÉDICAMENTS ANTICANCÉREUX ET LEURS PROCÉDÉS DE PRODUCTION ET D'UTILISATION
申请人:UNIV YALE
公开号:WO2020154672A1
公开(公告)日:2020-07-30
The present invention provides drug modifications for improving biodistribution and/or specificity of an anticancer drug. In certain embodiments, the compound of the invention comprises a drug, a linker and a core acid. The core acid can be varied to tune the properties of the compound within the body such that the compound more selectively distributes to tumors and is, or becomes active in the cytosol.