Patent classifications
C07F9/242
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, pancreatitis, 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.
METHODS AND COMPOSITIONS FOR SYNTHESIS OF TWO-PHOTON CLEAVABLE PHOSPHORAMIDITE MOLECULES FOR OLIGONUCLEOTIDE CONJUGATION
The syntheses of two phosphoramidite building blocks based on BNSF and BNSMB structures are disclosed. Furthermore, some common molecular intermediates have been designed and linked to the central biphenyl core of the two molecules, resulting in a versatile and cost-effective design. These compounds can be effectively introduced to DNA oligonucleotides via the well-established standard cyanoethylphosphoramidite chemistry on the nucleic acid synthesizer. Fragmentation of these BNSF- and BNSMB-functionalized DNA strands is achieved by both one-photon and two-photon photolysis of photoliable bonds of [2-(2-nitrophenyl)propoxy]carbonyl groups on BNSF and BNSMB molecules respectively, resulting in two short pieces of single-stranded DNAs. The versatile design and facile synthesis of these two-photon photocleavage phosphoramidite molecules are beneficial to synthetic chemists and photochemists for the development of new caged compounds which enables to introduce into oligonucleotides as light-triggered carriers via solid-phase synthesis for a wide range of applications in materials science, polymer, chemistry, biology and DNA nanoecthnology.
Trialkyne Linking Agents and Methods of Use
Described are improved linking agents that are useful for facilitating the attachment of targeting groups, pharmacokinetic (PK) enhancers or modifiers, or other delivery agents to oligonucleotides. The described linking agents may exhibit improved reaction yields, stability, and biological activity, particularly when used in connection with oligonucleotide-based compounds, such as RNA interference (RNAi) agents.
Reagents Useful for Synthesizing Rhodamine-Labeled Oligonucleotides
The present disclosure provides reagents that can be used to label synthetic oligonucleotides with rhodamine dyes or dye networks that contain rhodamine dyes.
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.
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.
Reagents useful for synthesizing rhodamine-labeled oligonucleotides
The present disclosure provides reagents that can be used to label synthetic oligonucleotides with rhodamine dyes or dye networks that contain rhodamine dyes.
SUBSTITUTED PHOSPHORAMIDATE COMPOUNDS AND USES THEREOF
The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.
##STR00001##
Phosphorus-containing compound and curing epoxy resin composition containing same
Provided is a novel phosphorus-containing compound represented by general formula (I). The compound has reactivity with a glycidyl group and is therefore capable of providing a curing epoxy resin composition that is expected to achieve flame retardation and reduction of dielectric constant. ##STR00001##
wherein m is a number of 1 to 10; R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are each hydrogen, alkyl, or aryl; R.sup.5 is alkyl, alkanediyl, alkanetriyl, alkanetetrayl, or an aromatic group; X is oxygen or sulfur; Y is oxygen, sulfur, or ═NR′; and R′ is hydrogen, alkyl, or aryl.
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.