Patent classifications
C07H19/056
Camptothecin derivatives and preparation methods and applications thereof
The invention relates to novel camptothecin derivatives and their applications, tumor cell growth inhibitors, ternary complexes, and a method for improving the solubility of the camptothecin derivatives. The camptothecin derivatives are prepared by modifying the substance shown as Formula I with glycosylated triazole at position R.sup.3. In the structure shown as Formula I, R.sup.1 represents H, C.sub.1-10 alkyl, C.sub.1-10 alkyl-D or C.sub.1-10 haloalkyl; R.sup.2 represents H, CH.sub.2N(CH.sub.3).sub.2 or CH.sub.2N(CD.sub.3).sub.2; and R.sup.4 represents ##STR00001##
or H, wherein X represents N, O or S; and L represents polypeptide, C.sub.1-20 linear alkyl or derivatives thereof, C.sub.1-20 linear or branched acyl derivatives, C.sub.2-100 ethylene glycol or derivatives thereof. The camptothecin derivatives have high solubility, the anticancer drugs prepared from them have the advantages of wide anticancer spectrum and high safety, and have in vivo anticancer activity higher than irinotecan hydrochloride.
GALACTOSE-LINKED MULTIMERIC GLYCOMIMETIC INHIBITORS OF E-SELECTINS, GALECTIN-3, AND/OR CXCR4 CHEMOKINE RECEPTORS
Compounds, compositions, and methods for treating and/or preventing at least one disease, disorder, and/or condition N associated with E-selectin, galectin-3, and/or CXCR4 chemokine receptor activity are disclosed herein. For example, multimeric glycomimetic inhibitors of E-selectins, galectin-3, and/or CXCR4 chemokine receptors and their use for treating and/or preventing inflammatory diseases, fibrosis, and cancers are disclosed. Formula (I).
##STR00001##
GALACTOSE-LINKED MULTIMERIC GLYCOMIMETIC INHIBITORS OF E-SELECTINS, GALECTIN-3, AND/OR CXCR4 CHEMOKINE RECEPTORS
Compounds, compositions, and methods for treating and/or preventing at least one disease, disorder, and/or condition N associated with E-selectin, galectin-3, and/or CXCR4 chemokine receptor activity are disclosed herein. For example, multimeric glycomimetic inhibitors of E-selectins, galectin-3, and/or CXCR4 chemokine receptors and their use for treating and/or preventing inflammatory diseases, fibrosis, and cancers are disclosed. Formula (I).
##STR00001##
SELENOGALACTOSIDE COMPOUNDS FOR THE PREVENTION AND TREATMENT OF DISEASES ASSOCIATED WITH GALECTIN AND THE USE THEREOF
Aspects of the invention relate to novel synthetic compounds having a binding affinity with galectin proteins.
SELENOGALACTOSIDE COMPOUNDS FOR THE PREVENTION AND TREATMENT OF DISEASES ASSOCIATED WITH GALECTIN AND THE USE THEREOF
Aspects of the invention relate to novel synthetic compounds having a binding affinity with galectin proteins.
COMPOUNDS FOR THE PREVENTION AND TREATMENT OF DISEASES AND THE USE THEREOF
Aspects of the invention relate to novel synthetic compounds having binding affinity with galectin proteins.
Mannose derivatives for treating bacterial infections
The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: ##STR00001## The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
Mannose derivatives for treating bacterial infections
The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula I: ##STR00001## The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. Finally, the invention provides processes for making compounds of the invention.
MODULATION OF IMMUNE CELLS
Disclosed are immune cell-selective small molecule IMPDH inhibitor compounds and methods of their synthesis and use to treat proliferative disorders.
LARGE SCALE PROCESS
A process for preparing a compound of formula (I)
##STR00001##
wherein the process is suitable for large scale synthesis. The process includes the consecutive steps of a) reacting a compound of formula IX and a catalyst and optionally adding a base in an organic solvent and optional adding a basic fluoride source agent under suitable conditions to obtain a compound of formula X and b) removing the protective groups of the compound X to obtain the compound formula (I).