Patent classifications
C07C49/83
POLYSUBSTITUTED BENZENE, PREPARATION METHOD THEREOF, AND METHOD OF USING THE SAME
A polysubstituted benzene compound, preparation method thereof, and method of using the same. The compound has a formula I or I, where X represents carbon, sulfur, or oxygen; R.sup.1 represents a C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; R.sup.2 represents hydrogen, halogen, C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; or an aryl group or a substituted aryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, OC.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; or a heteroaryl group or a substituted heteroaryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, OC.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; the heteroaryl group is a 3-10-membered heteroaryl group including N, S, O, or a combination thereof.
FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF
The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:
##STR00001##
wherein each symbol is as defined in the specification.
FLUORENE COMPOUND AND PHARMACEUTICAL USE THEREOF
The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:
##STR00001##
wherein each symbol is as defined in the specification.
Ketamine flow synthesis
The invention provides a method for synthesizing a compound of formula
##STR00001##
wherein each R independently represents an optionally substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy, acyl, carboxyl, hydroxyl, halogen, amino, nitro, cyano, sulfo or sulfhydryl group, in ortho, meta or para position to the cycloalkylamine moiety; R.sup.1 and R.sup.2 each independently represents a hydrogen atom, a lower alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen group, substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy group; Y represents an oxygen atom, a sulfur atom, a NH group, a NR.sup.4 group or a CH.sub.2 group; R.sup.4 represents a hydrogen atom or an alkyl, aryl or a heteroaryl group; and n and m each independently represents an integer from 1 to 5; or a pharmaceutically acceptable salt thereof; or a precursor thereof; wherein the method comprises one or more of the following steps: (a) reacting a compound of formula (II)
##STR00002##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I) with an oxygenating agent, a first additive and a second additive in a solvent in a fluidic network or in a batch process under thermal and/or photochemical conditions to form a compound of formula (III):
##STR00003##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I), (b) reacting a compound of formula (III) with a nitrogen containing nucleophile in the presence of a third additive and/or a solvent in the fluidic network or in a batch process under thermal conditions to form a compound of formula (IV):
##STR00004##
wherein R, R.sub.1, R.sub.2, R.sub.3, Y, n and m are as defined above in relation to the compound of formula (I); and/or (c) reacting a compound of formula (IV) in a fluidic network or in a batch process, optionally in the presence of a fourth additive, under thermal conditions to form a compound of formula (I); wherein one or more of steps (a), (b) and/or (c) is carried out in a fluidic network that comprises micro- and/or meso-channels having an internal dimension of from 100 m to 2000 m.
Ketamine flow synthesis
The invention provides a method for synthesizing a compound of formula
##STR00001##
wherein each R independently represents an optionally substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy, acyl, carboxyl, hydroxyl, halogen, amino, nitro, cyano, sulfo or sulfhydryl group, in ortho, meta or para position to the cycloalkylamine moiety; R.sup.1 and R.sup.2 each independently represents a hydrogen atom, a lower alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen group, substituted aryl, heteroaryl, alkyl, perfluoroalkyl, cycloalkyl, alkoxy, aryloxy group; Y represents an oxygen atom, a sulfur atom, a NH group, a NR.sup.4 group or a CH.sub.2 group; R.sup.4 represents a hydrogen atom or an alkyl, aryl or a heteroaryl group; and n and m each independently represents an integer from 1 to 5; or a pharmaceutically acceptable salt thereof; or a precursor thereof; wherein the method comprises one or more of the following steps: (a) reacting a compound of formula (II)
##STR00002##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I) with an oxygenating agent, a first additive and a second additive in a solvent in a fluidic network or in a batch process under thermal and/or photochemical conditions to form a compound of formula (III):
##STR00003##
wherein R, R.sup.3, Y, n and m are as defined above in relation to the compound of formula (I), (b) reacting a compound of formula (III) with a nitrogen containing nucleophile in the presence of a third additive and/or a solvent in the fluidic network or in a batch process under thermal conditions to form a compound of formula (IV):
##STR00004##
wherein R, R.sub.1, R.sub.2, R.sub.3, Y, n and m are as defined above in relation to the compound of formula (I); and/or (c) reacting a compound of formula (IV) in a fluidic network or in a batch process, optionally in the presence of a fourth additive, under thermal conditions to form a compound of formula (I); wherein one or more of steps (a), (b) and/or (c) is carried out in a fluidic network that comprises micro- and/or meso-channels having an internal dimension of from 100 m to 2000 m.
FLUORENE POLYFUNCTIONAL PHOTOINITIATOR AND PREPARATION AND USE THEREOF, AND PHOTOSENSITIVE RESIN COMPOSITION CONTAINING FLUORENE PHOTOINITIATOR AND USE THEREOF
This invention discloses a fluorene polyfunctional photoinitiator as represented by general formula (I), a photosensitive resin composition containing the same, the preparation of the same, and uses of the two. This compound has the advantages of simple synthesis, low cost, and good solubility, and has good application effects in photocurable compositions. Compared with conventional small molecule photoinitiators, it is not only excellent in photoinitiation activity, but also has the advantages such as low mobility, low odor, and yellowing resistance. The composition has high photosensitivity and good developability, high resolution, and excellent adaptation to a substrate, and is very suitable for producing a black matrix having high light-shielding property, a high-precision and high quality color filter and a liquid crystal display device, and can also be used in optical spacers and ribs, photoresist, wet film, dry film and so on.
##STR00001##
COMPOUNDS, COMPOSITIONS, AND METHODS FOR USE IN TREATING AUTOPHAGY-ASSOCIATED DISORDERS
The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits.
COMPOSITIONS OF POLYHYDROXYLATED BENZOPHENONES AND METHODS OF TREATMENT OF NEURODEGENERATIVE DISORDERS
The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
COMPOSITIONS OF POLYHYDROXYLATED BENZOPHENONES AND METHODS OF TREATMENT OF NEURODEGENERATIVE DISORDERS
The present invention relates to polyhydroxylated benzophenone compounds useful in the treatment of neurodegenerative, neurological, psychiatric, and cognitive diseases, in particular those associated with a deficiency in HDAC1 deacetylase activity.
PROCESS FOR THE PREPARATION OF ALPH-FUNCTIONALIZED KETONES
The present invention refers to a process for the preparation of an -functionalized ketone, an -functionalized ketone obtained by said process, a photopolymerizable composition comprising the -functionalized ketone and at least one photopolymerizable unsaturated compound, a method of preparing an article, an article obtained by said method, as well as the use of the -functionalized ketone or the photopolymerizable composition as photoinitiator.