Patent classifications
C07F9/2458
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.
Production of highly fat-soluble phosphoramidite
The purpose of the present invention is to provide a method for purifying and preparing a highly liposoluble phosphoramidite, as well as a capping reaction using the highly liposoluble phosphoramidite compound, and as well as a method for preparing oligonucleotide by a liquid phase process using a pseudo solid phase protecting group said method comprising the capping reaction step. The present invention also provides a method for preparing a compound represented by formula (I) [wherein, R.sup.1, R.sup.2 and R.sup.3 are defined as described in the Detailed Description], which comprises the following steps: (1) reacting an aliphatic alcohol and a trivalent phosphorus compound in organic solvent in the presence of an activator or an organic base; (2) washing the resulting reaction mixture with water in a reparatory funnel; (3) recovering the organic layer after the step (2) and concentrating it (with the proviso that the organic solvent used in the step (1) is a nitrile solvent, the steps (2) to (3) may be omitted); (4) solubilizing the resulting residue obtained in the step (3) in an aliphatic hydrocarbon solvent (with the proviso that the organic solvent used in the step (1) is an aliphatic hydrocarbon solvent, the steps (2) to (3) may be omitted); (5) washing the aliphatic hydrocarbon solution prepared in the step (4) with a nitrile solvent in a separatory funnel; (6) recovering the aliphatic hydrocarbon solution after the step (5) to obtain a solution of a phosphoramidite compound. Also the present invention provides also a solution containing highly liposoluble phosphoramidite compound obtained by the preparation method, a capping reagent comprising the same solution and optionally an additive, a capping reaction using the same capping reagent, as well as a method for preparing (oligo)nucleotide by using the pseudo solid phase protecting group, said method comprising the capping reaction step. ##STR00001##
FUNCTIONALIZED POLYMERS
This document relates to functionalized (e.g., mono- or bi-functional) polymers (e.g., polyethylene glycol and related polymers) as well as methods and materials for making and using such functionalized polymers.
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.
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.
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.
Sorbitol, glucaric acid, and gluconic acid based flame-retardants
A flame-retardant sugar derivative, a process for forming a flame-retardant sugar derivative, and an article of manufacture comprising a flame-retardant sugar derivative are disclosed. The flame-retardant sugar derivative can be synthesized from sorbitol, gluconic acid, or glucaric acid obtained from a bio-based source, and can have at least one phosphoryl or phosphonyl moiety. The process for forming the flame-retardant sugar derivative can include reacting sorbitol, gluconic acid, or glucaric acid and a flame-retardant phosphorus-based molecule to form the flame-retardant sugar derivative.
PREPARATION METHOD OF FLUORINE-SILICON-CONTAINING POLYPHOSPHATE ESTER AND APPLICATION THEREOF
Disclosed are a fluorine-silicon-containing polyphosphate ester and method for preparation thereof, having a chemical structural formula of:
##STR00001##
wherein R .sub.1 is
##STR00002##
R .sub.2 is
##STR00003##
n=10100. The fluorine-silicon-containing polyphosphate ester of the present invention uses silicon phosphorus and fluorine for improving flame retardancy. Phosphorus catalyzes the system to form a phosphorus-rich carbon layer, performing a protective-layer function and thereby preventing further breakdown of the epoxy resin. The silicon-containing epoxy resin forms a silica-containing carbon layer during the process of combustion, strengthening the carbon-layer structure and further improving the protective function of the carbon-layer. The introduction of elemental fluorine improves the thermal stability of the epoxy resin, thereby improving the flame retardancy performance of the system.
Liver Prodrugs of Mitochondrial Proton Ionophores
The present invention provides novel liver-targeted prodrugs of mitochondrial proton ionophores. These compounds have utility in medicine including their use in treatment of diseases such as NASH and NAFLD.
SORBITOL, GLUCARIC ACID, AND GLUCONIC ACID BASED FLAME-RETARDANTS
A flame-retardant sugar derivative, a process for forming a flame-retardant sugar derivative, and an article of manufacture comprising a flame-retardant sugar derivative are disclosed. The flame-retardant sugar derivative can be synthesized from sorbitol, gluconic acid, or glucaric acid obtained from a bio-based source, and can have at least one phosphoryl or phosphonyl moiety. The process for forming the flame-retardant sugar derivative can include reacting sorbitol, gluconic acid, or glucaric acid and a flame-retardant phosphorus-based molecule to form the flame-retardant sugar derivative.