Patent classifications
C07F9/24
ACCESS TO CHIRAL BISPHENOL (BPOL) LIGANDS THROUGH DESYMMETRIZING ASYMMETRIC ORTHO-SELECTIVE MONO-HALOGENATION
The subject invention pertains to a method of halogenating phenols, yielding a range of halogenated phenols with enantiomeric ratio of up to 99.5:0.5. In certain embodiments, the subject invention pertains to a method of asymmetric halogenation of bisphenol, yielding a range of chiral bisphenol ligands. The novel chiral bisphenols are potent privileged catalyst cores that can be applied to the preparation of ligands for various catalytic asymmetric reactions. The catalyst library can easily be accessed because late-stage modification of the scaffold can readily be executed through cross-coupling of the halogen handles on the bisphenols.
Method for preparing fluorine-silicon-containing polyphosphate ester and flame retardant epoxy resin
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=10˜100. 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.
Creatine phosphate analog prodrugs, compositions and methods of use thereof
The invention describes membrane permeable creatine phosphate analog prodrugs, pharmaceutical compositions comprising membrane permeable creatine phosphate analog prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine phosphate analog prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine phosphate analog prodrugs or pharmaceutical compositions thereof.
EFFICIENT PHOSPHOROUS STABILISERS BASED ON DIPHENYLAMINE AND HETEROCYCLIC DIPHENYLAMINE DERIVATIVES
The present invention relates to the use of efficient phosphorous substances, in particular based on diphenylamine and heterocyclic diphenylamine derivatives as stabilizers for organic materials, in particular for plastic materials, against oxidative, thermal and/or actinic degradation. Te present invention additionally relates to an organic material that has been correspondingly stabilized as described above. The invention further relates to a method of stabilizing organic materials and to specific stabilizers.
Hydroxyl compounds and compositions for cholesterol management and related uses
The present invention relates to novel hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, pancreatitius, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, metabolic syndrome disorders (e.g., Syndrome X), thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
The invention provides compounds of the formula:
##STR00001## R.sup.1 is OR.sup.11, or NR.sup.5R.sup.5; R.sup.2 is H or F; R.sup.5 is H, C.sub.1-C.sub.6alkyl, OH, C(O)R.sup.6, O(CO)R.sup.6 or O(CO)OR.sup.6; R.sup.5 is H or C.sub.1-C.sub.6alkyl; R.sup.6 is C.sub.1-C.sub.6alkyl or C.sub.3-C.sub.7cycloalkyl; R.sup.13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R.sup.22;
and the other variables are as defined in the claims,
which are of use in the treatment of cancer, and related aspects.
DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER
The invention provides compounds of the formula:
##STR00001## R.sup.1 is OR.sup.11, or NR.sup.5R.sup.5; R.sup.2 is H or F; R.sup.5 is H, C.sub.1-C.sub.6alkyl, OH, C(O)R.sup.6, O(CO)R.sup.6 or O(CO)OR.sup.6; R.sup.5 is H or C.sub.1-C.sub.6alkyl; R.sup.6 is C.sub.1-C.sub.6alkyl or C.sub.3-C.sub.7cycloalkyl; R.sup.13 is H, phenyl, pyridyl, benzyl, indolyl or naphthyl wherein the phenyl, pyridyl, benzyl, indolyl and naphthyl is optionally substituted with 1, 2 or 3 R.sup.22;
and the other variables are as defined in the claims,
which are of use in the treatment of cancer, and related aspects.
METHODS FOR TREATING FILOVIRIDAE VIRUS INFECTIONS
Provided are compounds, methods, and pharmaceutical compositions for treating Filoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula IV:
##STR00001##
The compounds, compositions, and methods provided are particularly useful for the treatment of Marburg virus, Ebola virus and Cueva virus infections.
Process for recovering a mixture comprising a (thio)phosphoric acid derivative
Provided herein is a use of a high-boiling solvent in a mixture comprising a (thio)phosphoric acid derivative and a process including the addition of a high-boiling solvent to a mixture comprising a (thio)phosphoric acid derivative to recover the (thio)phosphoric acid from the mixture by an evaporation process.
Process for recovering a mixture comprising a (thio)phosphoric acid derivative
Provided herein is a use of a high-boiling solvent in a mixture comprising a (thio)phosphoric acid derivative and a process including the addition of a high-boiling solvent to a mixture comprising a (thio)phosphoric acid derivative to recover the (thio)phosphoric acid from the mixture by an evaporation process.