Patent classifications
C07F9/2458
Acyclic thiol prodrugs
Disclosed herein are acyclic thiol prodrugs, and pharmaceutical compositions thereof. The prodrugs and pharmaceutical compositions thereof may be used to treat or prevent medical disorders such as, for example cystinosis, cystinuria, cancer neurodegenerative disease, Parkinson's disease, Huntington's disease, malaria, nonalcoholic fatty liver disease, radiation poisoning, arsenic poisoning, radioprotection, Wilson's disease or rheumatoid arthritis.
5-ALA DERIVATIVES AND USE THEREOF
The present invention is directed to new 5-ALA derivatives, particles and formulation thereof, related methods of preparation and methods of use thereof. In particular, the invention relates to compounds of the invention, particles and formulation thereof useful in the treatment of a cancer and/or the diagnosis of a cancer cell such as in photodynamic therapy or photodynamic diagnosis.
HIGH PENETRATION PRODRUG COMPOSITIONS OF MUSTARDS AND MUSTARD-RELATED COMPOUNDS
The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of mustards and mustard-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
IMPROVED PROCESSES FOR THE PREPARATION OF SOFOSBUVIR AND INTERMEDIATES THEREOF
The present disclosure provides procedures and intermediates for the preparation of Sofosbuvir, comprising the step of reacting a compound of formula 2: wherein R.sub.1 and R.sub.2 can independently be hydrogen or halogen, provided that at least one of R.sub.1 and R.sub.2 is a halogen.
##STR00001##
Prodrugs of glutamine analogs
The disclosure provides compounds having formula (I): ##STR00001##
and the pharmaceutically acceptable salts thereof, wherein R.sub.1, R.sub.2, R.sub.2, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
FLAME-RETARDANT VANILLIN-DERIVED SMALL MOLECULES
A flame-retardant vanillin-derived small molecule, a process for forming a flame-retardant polymer, and an article of manufacture comprising a material that contains the flame-retardant vanillin-derived small molecule are disclosed. The flame-retardant vanillin-derived small molecule can be synthesized from vanillin obtained from a bio-based source, and can have at least one phosphoryl or phosphonyl moiety with phenyl, allyl, or thioether substituents. The process for forming the flame-retardant polymer can include reacting a diol vanillin derivative and a flame-retardant phosphorus-based molecule to form the flame-retardant vanillin-derived small molecule, and binding the flame-retardant vanillin-derived small molecule to a polymer. The material in the article of manufacture can be flame-retardant, and contain the flame-retardant vanillin-derived small molecules. Examples of materials that can be in the article of manufacture can include resins, plastics, adhesives, polymers, etc.
Inhibitors of creatine transport and uses thereof
This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer.
UNIVERSAL LINKER REAGENTS FOR DNA SYNTHESIS
Provided herein are methods and compositions for oligonucleotide synthesis utilizing universal linker phosphoramidites. Methods and reagents are described with DNA synthesis using controlled pore glass (CPG) solid supports, and on platinum coated electrodes for electrochemical DNA synthesis. The universal linkers can be used as spacers in single-column PCR primer synthesis to generate 2 strands with free 3-hydroxy termini after cleavage. The methods and compositions utilize a solid support system for synthesis of oligonucleotides, wherein the support has platinum electrodes and a universal linker, optionally wherein the platinum electrode is coated with an amine. The methods and compositions further describe use of universal linker phosphoramidites and the platinum electrode is coated with a monosaccharide, or a disaccharide.
Flame-retardant aconitic acid-derived small molecules
A flame-retardant aconitic acid-derived small molecule, a process for forming a flame-retardant polymer, and an article of manufacture comprising a material that contains a flame-retardant aconitic acid-derived small molecule are disclosed. The flame-retardant aconitic acid-derived small molecule can be synthesized from aconitic acid obtained from a bio-based source, and can have at least one phosphoryl or phosphonyl moiety with phenyl, allyl, or thioether substituents. The process for forming the flame-retardant polymer can include reacting an aconitic acid derivative with a flame-retardant phosphorus-based molecule to form a flame-retardant aconitic acid-derived small molecule, and combining the flame-retardant aconitic acid-derived small molecule with a polymer. The material in the article of manufacture can be a resin, adhesive, polymer, etc.
5-ALA derivatives and use thereof
The present invention is directed to new 5-ALA derivatives, particles and formulation thereof, related methods of preparation and methods of use thereof. In particular, the invention relates to compounds of the invention, particles and formulation thereof useful in the treatment of a cancer and/or the diagnosis of a cancer cell such as in photodynamic therapy or photodynamic diagnosis.