Patent classifications
C07H15/26
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.
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.
Novel Sugar Derivatives and Uses Thereof to Prepare Novel Senolytic Agents
Provided herein are novel sugar derivatives which are intermediates for preparing senolytic agents that selectively kill senescent cells associated with numerous pathologies and diseases, including age-related pathologies and diseases.
Novel Sugar Derivatives and Uses Thereof to Prepare Novel Senolytic Agents
Provided herein are novel sugar derivatives which are intermediates for preparing senolytic agents that selectively kill senescent cells associated with numerous pathologies and diseases, including age-related pathologies and diseases.
COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS
The present invention encompasses compounds and methods for treating and preventing bacterial infections specifically urinary tract infections and those caused by bacteria containing type 1 pili and FimH. The present invention also encompasses compounds and methods for treating inflammatory bowel disease specifically Crohn's Disease.
COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS
The present invention encompasses compounds and methods for treating and preventing bacterial infections specifically urinary tract infections and those caused by bacteria containing type 1 pili and FimH. The present invention also encompasses compounds and methods for treating inflammatory bowel disease specifically Crohn's Disease.
CAMPTOTHECIN CONJUGATES
Antibody conjugates with camptothecin compounds are described, with methods of use and preparations.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
##STR00001##
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
##STR00001##
Compounds, Compositions, and Methods for Coloring Edible Materials
The present invention provides compounds isolated from avocado seeds for use as a natural colorant in edible materials. The compounds of the invention are useful for coloring edible materials red, orange, or yellow. The invention also provides compositions and methods for coloring edible materials to a desired color such as red, orange, or yellow.