Patent classifications
C07F9/24
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.
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, OH, C.sub.1-C.sub.6 alkyl, OH, C(═O)R.sup.6, O(C═O)R.sup.6 or O(C═O)OR.sup.6; R.sup.5′ is H or C.sub.1-C.sub.6 alkyl; R.sup.6 is C.sub.1-C.sub.6 alkyl or C.sub.3-C.sub.7 cycloalkyl; 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.
Butyrylcholinesterase inhibitors
Butyrylcholinesterase inhibitors, their formulation, and their use primarily in the treatment of neurodegenerative diseases. These inhibitors generally are phosphates, phosphonates, phosphinates, and phosphoramidates. These inhibitors can be incorporated in pharmaceutical compositions and administered to a patient in therapeutically effective amounts to treat neurodegenerative diseases.
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.
ULTRA BRIGHT DIMERIC OR POLYMERIC DYES
Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (II):
##STR00001##
or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.
RADIO-AND CHEMO-PROTECTIVE COMPOUNDS
The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.
RADIO-AND CHEMO-PROTECTIVE COMPOUNDS
The present disclosure relates to prodrugs, double prodrugs, derivatives and analogues of 3-(methylamino)-2-((methylamino)methyl)propane-1-thiol. Their use as radio- and chemo-protectors is also described.
Process for preparation of O,O dimethyl phosphoramidothioate and N-(methoxymethylsulfanylphosphoryl) acetamide
Preparation of O,O-dimethyl phosphoramidothioate and O,O-dimethyl phosphoroamidothioate. A process of making O,O-dimethyl phosphoroamidothioate is described including reacting sulfur with PCl.sub.3 to form PSCl.sub.3, reacting the PSCl.sub.3 formed with methanol to form O-methyl phosphorodichloridothioate, and reacting the O-methyl phosphorodichloridothioate formed with methyl lye to form O,O-dimethyl phosphorochloridothioate in solution in CH.sub.2Cl.sub.2, and reacting the O,O-dimethyl phosphorochloridothioate formed with sodium hydroxide and ammonium hydroxide to form O,O-dimethyl phosphoroamidothioate in solution in CH.sub.2Cl.sub.2. Reacting the O,O-dimethyl phosphoroamidothioate formed with catalytic dimethyl sulfate to form methamidophos and reacting the methamidophos formed with acetic anhydride to form N-(methoxy-methylsulfanylphosphoryl) acetamide is also described. Throughout the process, the O,O-dimethyl phosphorochloridothioate and the O,O-dimethyl phosphoroamidothioate formed are maintained in solution in CH.sub.2Cl.sub.2 at all times.
Ultra bright polymeric dyes with peptide backbones
Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I), including stereoisomers, salts and tautomers thereof, wherein R.sup.1, R.sup.2, R.sup.3, L.sup.1, L.sup.2, L.sup.3, L.sup.4, L.sup.5, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided. ##STR00001##
SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS
Compounds are provided having the structure of Formula (I) or (II) or a pharmaceutically acceptable salt, homolog, hydrate or solvate thereof, wherein R.sup.a, R.sup.d and R.sup.e are as defined herein. Such compounds serve as modulators of the sphingosine-1-phosphate receptor, and have utility for treatment of a malcondition for which activation of this receptor is medically indicated.
##STR00001##