Patent classifications
C07D307/58
Purified forms of rofecoxib, methods of manufacture and use
The subject matter disclosed herein relates to rofecoxib, also known as TRM-201 or RXB-201, its method of manufacture, and use. In certain aspects, the highly pure or substantially pure rofecoxib as provided herein has a favorable purity profile and is the active ingredient in a pharmaceutical composition that is administered to treat or prevent a number of conditions, including pain associated with a condition caused by a bleeding disorder.
Use of functionalized alpha-angelica lactones
The present invention is directed to the use as a reactive component in the curing of compositions based on epoxy resins of a functionalized α-angelica lactone (XOMAL) having the general formula: ##STR00001##
wherein: R.sup.a is a C.sub.1-C.sub.30 alkyl, C.sub.3-C.sub.30 cycloalkyl, C.sub.6-C.sub.18 aryl or C.sub.2-C.sub.12 alkenyl group.
Use of functionalized alpha-angelica lactones
The present invention is directed to the use as a reactive component in the curing of compositions based on epoxy resins of a functionalized α-angelica lactone (XOMAL) having the general formula: ##STR00001##
wherein: R.sup.a is a C.sub.1-C.sub.30 alkyl, C.sub.3-C.sub.30 cycloalkyl, C.sub.6-C.sub.18 aryl or C.sub.2-C.sub.12 alkenyl group.
Synthesis of alkynones via carbonylative Sonogashira coupling reactions catalyzed by Pd(II)-N-Heterocyclic carbene-pyridine complexes
This disclosure relates to N-substituted Pd(II)-N-heterocyclic carbene-pyridine complexes, methods of preparing the complexes, and methods of using the complexes in Sonogashira coupling reactions.
Synthesis of alkynones via carbonylative Sonogashira coupling reactions catalyzed by Pd(II)-N-Heterocyclic carbene-pyridine complexes
This disclosure relates to N-substituted Pd(II)-N-heterocyclic carbene-pyridine complexes, methods of preparing the complexes, and methods of using the complexes in Sonogashira coupling reactions.
NOVEL P62 LIGAND COMPOUND, AND COMPOSITION CONTAINING SAME FOR PREVENTING, AMELIORATING, OR TREATING PROTEINOPATHIES
Novel p62 ligand compounds, or a stereoisomer, a solvate, a hydrate, or a prodrug thereof are disclosed. The novel compounds, stereoisomer, solvate, hydrate, or prodrug activates selective autophagy in cells to selectively remove proteins, organelles, and coagulations in the body, and thus can be advantageously used as a pharmaceutical composition for preventing, ameliorating, or treating various proteinopathies. Compositions such as pharmaceutical composition or food compositions containing the novel p62 ligand compounds, stereoisomer, solvate, hydrate, or prodrug thereof as well as uses thereof are disclosed.
NOVEL P62 LIGAND COMPOUND, AND COMPOSITION CONTAINING SAME FOR PREVENTING, AMELIORATING, OR TREATING PROTEINOPATHIES
Novel p62 ligand compounds, or a stereoisomer, a solvate, a hydrate, or a prodrug thereof are disclosed. The novel compounds, stereoisomer, solvate, hydrate, or prodrug activates selective autophagy in cells to selectively remove proteins, organelles, and coagulations in the body, and thus can be advantageously used as a pharmaceutical composition for preventing, ameliorating, or treating various proteinopathies. Compositions such as pharmaceutical composition or food compositions containing the novel p62 ligand compounds, stereoisomer, solvate, hydrate, or prodrug thereof as well as uses thereof are disclosed.
PURIFIED FORMS OF ROFECOXIB, METHODS OF MANUFACTURE AND USE
The subject matter disclosed herein relates to rofecoxib, also known as TRM-201 or RXB-201, its method of manufacture, and use. In certain aspects, the highly pure or substantially pure rofecoxib as provided herein has a favorable purity profile and is the active ingredient in a pharmaceutical composition that is administered to treat or prevent a number of conditions, including pain associated with a condition caused by a bleeding disorder.
CYCLIC PANTETHEINE DERIVATIVES AND USES THEREOF
The present disclosure relates to compounds of Formula (P) or (II′-0): (Formulae (I′), (II′-0)), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.
##STR00001##
Method for directly constructing highly optically active tetrasubstituted allenic acid compounds
The present invention discloses a method for directly constructing highly optically active tetrasubstituted allenic acid compounds, i.e., a one-step process for directly constructing highly optically active axially chiral tetrasubstituted allenic acid compounds by using tertiary propargyl alcohol, carbon monoxide and water as reactants in an organic solvent in the presence of palladium catalyst, chiral diphosphine ligand, monophosphine ligand and organic phosphoric acid. The method of the present invention has the following advantages: operations are simple, raw materials and reagents are readily available, the reaction conditions are mild, the substrate has high universality, the functional group has good compatibility, and the reaction has high enantioselectivity (90%˜>99% ee). The highly optically active allenic acid compounds obtained by the present invention can be used as an important intermediate to construct γ-butyrolactone compounds containing tetrasubstituted chiral quaternary carbon centers, tetrasubstituted allenic alcohol and other compounds.