C07F9/2408

HYDROXYL COMPOUNDS AND COMPOSITIONS FOR CHOLESTEROL MANAGEMENT AND RELATED USES
20210395175 · 2021-12-23 ·

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
20210395530 · 2021-12-23 ·

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.

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##

Reagents based on a tertiary amine backbone to introduce chemical functionality in nucleic acids and sequence-controlled polymers

It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.

PROGRAMMABLE POLYMERIC DRUGS

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): 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.a, L.sup.b, L.sup.1, L.sup.2, L.sup.3, M, m, and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

##STR00001##

PROGRAMMABLE POLYMERIC DRUGS

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L, L.sup.1, L.sup.2, M and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

##STR00001##

Process for Making Levoamphetamine

This is invention is related to processes for synthesis of levoamphetamine derivatives and novel intermediates thereby, and processes for using the same.

Programmable polymeric drugs

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): ##STR00001##
or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, L, L.sup.1, L.sup.2, L.sup.3, M and n are as defined herein. Methods associated with preparation and use of such compounds is also provided.

NITRODIARYLETHENES AS FLUORESCENCE QUENCHERS FOR NUCLEIC ACID PROBES

Fluorescence quenching nitrodiarylethene analogs are useful in oligonucleotide conjugates and probes. These analogs, whose absorption spectra are substantially blue-shifted relatively to emission spectra of common fluorophores (such as fluorescein), do not need to rely on spectral overlap of quencher absorbance and fluorophore's emission for their quenching abilities. The oligonucleotide-quencher conjugates may be used in detection methods for nucleic acid targets.