Patent classifications
C07D305/14
ISOCYANATES, DERIVATIVES, AND PROCESSES FOR PRODUCING THE SAME
The present invention is directed to processes for producing isocyanates and isocyanate derivatives from epoxide and carbon monoxide reagents. In preferred embodiments, the processes include a step for providing carbonylation of an epoxide reagent with a carbon monoxide reagent to produce a beta-lactone intermediate. In certain preferred embodiments, further carbonylation of a beta-lactone intermediate produces a succinic anhydride intermediate. The processes of the present invention include steps for rearranging beta-lactone intermediates and/or succinic anhydride intermediates to produce isocyanate products and/or isocyanate derivatives. In certain preferred embodiments, the isocyanate products may be copolymerized with polyol oligomers to provide polyurethane products.
ISOCYANATES, DERIVATIVES, AND PROCESSES FOR PRODUCING THE SAME
The present invention is directed to processes for producing isocyanates and isocyanate derivatives from epoxide and carbon monoxide reagents. In preferred embodiments, the processes include a step for providing carbonylation of an epoxide reagent with a carbon monoxide reagent to produce a beta-lactone intermediate. In certain preferred embodiments, further carbonylation of a beta-lactone intermediate produces a succinic anhydride intermediate. The processes of the present invention include steps for rearranging beta-lactone intermediates and/or succinic anhydride intermediates to produce isocyanate products and/or isocyanate derivatives. In certain preferred embodiments, the isocyanate products may be copolymerized with polyol oligomers to provide polyurethane products.
Aromatic compounds and uses thereof
Disclosed herein are substituted indane derivatives useful as HIF-2 inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2 activity are also disclosed.
Aromatic compounds and uses thereof
Disclosed herein are substituted indane derivatives useful as HIF-2 inhibitors. Pharmaceutical compositions comprising said indane derivatives and methods of using said indane derivatives for treating proliferative diseases, such as renal cell carcinoma and von Hippel-Lindau disease, and other conditions associated with HIF-2 activity are also disclosed.
Lipid-linked prodrugs
This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.
Lipid-linked prodrugs
This invention provides lipid-linked prodrugs having structures as set out herein. Uses of such lipid-linked prodrug compounds for treatment of various indications, and methods for making and using lipid-linked prodrugs are also provided.
Method for analyzing related substances of a pharmaceutical composition containing a polymeric carrier
A method for analyzing related substances in a pharmaceutical composition containing an amphiphilic block copolymer comprising a hydrophilic block and a hydrophobic block as a polymeric drug carrier, related substances identified thereby, and a method for evaluating a pharmaceutical composition by using the same are provided. Preferably, the method comprises evaluating a polymeric micelle pharmaceutical composition, which comprises an amphiphilic block copolymer comprising a hydrophilic block (A) and a hydrophobic block (B), and paclitaxel or docetaxel as a poorly water-soluble drug, by using a compound represented by Chemical Formula 1, wherein the hydrophilic block (A) comprises one or more selected from the group consisting of polyethylene glycol or derivatives thereof, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylamide and combinations thereof; and the hydrophobic block (B) is polylactide.
9,10-Alpha,Alpha-OH-Taxane Analogs and Methods for Production Thereof
The present invention relates to a method for the treatment of cancer in a cancer patient. In particular, the invention provides a method for the treatment comprising administering a taxane compound to a cancer patient, wherein the taxane compound is made by a process comprising treating a first compound represented by either Formula G or Formula M:
##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
9,10-Alpha,Alpha-OH-Taxane Analogs and Methods for Production Thereof
The present invention relates to a method for the treatment of cancer in a cancer patient. In particular, the invention provides a method for the treatment comprising administering a taxane compound to a cancer patient, wherein the taxane compound is made by a process comprising treating a first compound represented by either Formula G or Formula M:
##STR00001##
with a second compound of generalized formula R.sub.8R.sub.9C(OCH.sub.3).sub.2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R.sub.1 and R.sub.2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R.sub.7 is an alkyl group, an olefinic group, or an aromatic group; P.sub.1 is a hydroxyl protecting group; P.sub.5 is H or an acid labile protecting group at the 7-O position; R.sub.8 is H, alkyl group, olefinic or aromatic group; and R.sub.9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
SSAO INHIBITORS AND USES THEREOF
Described herein are compounds that are semicarbazide-sensitive amine oxidase (SSAO) inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in treating or preventing a liver disease or condition.