Patent classifications
C07F9/40
STRUCTURED MOLECULAR VECTORS FOR ANTI-INFLAMMATORY COMPOUNDS AND USES THEREOF
The present invention relates to structured molecular vectors of formula (I), compounds of formula (II) and pharmaceutical compositions comprising such compounds. The invention also relates to such pharmaceutical compositions for use for preventing and/or treating a disease chosen among an inflammatory disease or a disease associated with a cognitive disorder. The invention further relates to such pharmaceutical compositions for use for preventing cognitive decline or restoring cognitive functions altered in brain injuries and/or in traumatic brain injuries and/or in a neuroinflammatory disease, and/or in a neurodegenerative disease.
CHIRAL N-HETEROCYCLIC PHOSPHORODIAMIDIC ACIDS (NHPAS) AND DERIVATIVES AS NOVEL BRONSTED ACID CATALYSTS
Provided herein are diaryl and arylalkyl phosphonates, useful as intermediates in, for example, the synthesis of leukocyte elastase inhibitors, potassium channel modulators, chemiluminescence materials, and flame retardants, and methods for making same. Also provided are N-heterocyclic phosphorodiamidic acids (NHPAs) useful in reactions such as, for example, in the preparation of diaryl and arylalkyl phosphonates. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Prodrugs of prostate specific membrane antigen (PSMA) inhibitor
Methods and compounds are disclosed for treating a disease or condition by inhibiting PSMA (Prostate Specific Membrane Antigen) using prodrugs of 2-PMPA.
Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.
PHOSPHONO PARAFFINS
Aspects described herein generally relate to methods of making a phosphono paraffin comprising forming a reaction mixture by mixing a haloparaffin, a phosphite, and sodium iodide. Methods comprise heating the reaction mixture to form the phosphono paraffin. Aspects described herein further relate to a phosphono paraffin represented by formula (I):
##STR00001##
wherein each instance of R.sup.1 is independently —H or
##STR00002##
wherein each instance of R.sup.2 and R.sup.3 is independently linear or branched C.sub.1-20 alkyl, C.sub.1-20 cycloalkyl, or aryl; the number of instances where R.sup.1 is
##STR00003##
of formula (I) is between about 2 and about 8; and n is an integer between 4 and 22.
METHODS OF SYNTHESIZING A DIFLUOROLACTAM ANALOG
The present invention relates to processes and intermediates for preparing compounds of formula (IA), wherein R.sup.1, R.sup.4, R.sup.5, R.sup.6, and L.sup.1 are as defined herein. Compounds of formula (IA) have been found useful as EP.sub.4 receptor agonists useful in the treatment of glaucoma, osteoporosis, neuropathic pain, and related disorders.
##STR00001##
BIOINSPIRED LIPID DERIVATIVES AND USES THEREOF
The present disclosure relates to compounds, compositions, and methods for delivery of therapeutic, diagnostic, or prophylactic agents (for example, a nucleic acid).
Phosphono paraffins
Aspects described herein generally relate to methods of making a phosphono paraffin comprising forming a reaction mixture by mixing a haloparaffin, a phosphite, and sodium iodide. Methods comprise heating the reaction mixture to form the phosphono paraffin. Aspects described herein further relate to a phosphono paraffin represented by formula (I): ##STR00001##
wherein each instance of R.sup.1 is independently —H or ##STR00002##
wherein each instance of R.sup.2 and R.sup.3 is independently linear or branched C.sub.1-20 alkyl, C.sub.1-20 cycloalkyl, or aryl; the number of instances where R.sup.1 is ##STR00003##
of formula (I) is between about 2 and about 8; and n is an integer between 4 and 22.
Arabitol and xylitol based flame retardants
A flame retardant sugar-derived molecule, a process for forming a flame retardant sugar-derived molecule, and an article of manufacture comprising a flame retardant sugar-derived molecule are disclosed. The flame retardant sugar-derived molecule can be synthesized from arabitol, xylitol, arabic acid, or xylonic 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-derived molecule can include reacting arabitol, xylitol, arabic acid, or xylonic acid and a flame retardant phosphorus-based molecule to form the flame retardant sugar-derived molecule.
Sequestering compositions and materials
The present disclosure relates to a composition that includes a sequestering material capable of binding a target material, where the sequestering material includes a first component that includes at least one of a functional group, a molecule, an oligomer, or a polymer, and the target material includes at least one of an element, a chemical, and/or a compound. In some embodiments of the present disclosure, the element may include at least one element from at least one of Rows 4, 5, 6, and 7 of the Periodic Table and/or an inner transition metal.