Patent classifications
C07C235/10
Use of ruthenium complexes for preparing amides, polypeptides and cyclic dipeptides
A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.
Polyamine transport inhibitors as novel therapeutics
Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.
Polyamine transport inhibitors as novel therapeutics
Novel polyamine transport inhibitors have been synthesized and demonstrated to block the uptake of native polyamines into human cancer cells. A combination therapy of the transport inhibitor and DFMO (a drug which blocks polyamine biosynthesis) provided synergistic activity against a metastatic human colon cancer cell line. The strategy uses polyamine depletion and polyamine metabolism to generate reactive oxygen species within cells as a novel way to treat cancers. This approach may be implemented for widespread use in the treatment of diseases which rely upon polyamine transport activity for proliferation.
Three-dimensional cage-like hyperbranched monomer, and preparation method and application thereof
The invention discloses a three-dimensional cage-like hyperbranched monomer and preparation method and application thereof. The three-dimensional cage-like hyperbranched monomer has the structural formula I: ##STR00001## ##STR00002##
wherein in the structural formula I: X is any one of —O, —S, —NH; y is any integer from 2 to 8; R is —H or —CH.sub.3. The beneficial effect of the technical scheme proposed in the present invention is: by introducing easily polymerizable olefin groups, the carboxyl group and amide group are combined in the three-dimensional cage-like hyperbranched monomer to make the water solubility good, and it can be copolymerized with many other monomers to obtain the three-dimensional cage-like hyperbranched polymer; when used as an additive for wellbore working fluids, due to the hyperbranched structure of the polymer, it has good salt and temperature resistance, and also has viscosity increasing, filtration loss, and flocculation properties; meanwhile, the synthesis method is simple and the cost is low.
RHEOLOGICAL ADDITIVE BASED ON OPTIONALLY BIOSOURCED 1,5-PENTAMETHYLENEDIAMINE
The present invention relates to a rheology additive, according to which A) said additive consists of: a) at least one symmetrical fatty diamide of formula (I): (AGH)—CONH—(PMDA)-NHCO-(AGH) (I) with: (AGH): hydroxylated fatty acid residue R1CO2H, without —CO2H group, with R1 of C18 to C20 comprising a hydroxyl group, —NHCO— or —CONH—: amide group, —(PMDA): residue without amine groups of 1,5-pentamethylenediamine; or alternatively according to which: B) said additive comprises: a) at least one symmetrical fatty diamide as defined above according to formula (I) and, in addition, b) at least one other symmetrical fatty diamide of formula (II): (AGH)—CONH—(R)—NHCO-(AGH) (II) with (AGH), —NHCO— and —CONH— having the same definition as that above in said formula (I), and (R) being the residue without amine groups of a diamine, other than (PMDA), chosen from a cycloaliphatic, aliphatic or aromatic diamine.
RHEOLOGICAL ADDITIVE BASED ON OPTIONALLY BIOSOURCED 1,5-PENTAMETHYLENEDIAMINE
The present invention relates to a rheology additive, according to which A) said additive consists of: a) at least one symmetrical fatty diamide of formula (I): (AGH)—CONH—(PMDA)-NHCO-(AGH) (I) with: (AGH): hydroxylated fatty acid residue R1CO2H, without —CO2H group, with R1 of C18 to C20 comprising a hydroxyl group, —NHCO— or —CONH—: amide group, —(PMDA): residue without amine groups of 1,5-pentamethylenediamine; or alternatively according to which: B) said additive comprises: a) at least one symmetrical fatty diamide as defined above according to formula (I) and, in addition, b) at least one other symmetrical fatty diamide of formula (II): (AGH)—CONH—(R)—NHCO-(AGH) (II) with (AGH), —NHCO— and —CONH— having the same definition as that above in said formula (I), and (R) being the residue without amine groups of a diamine, other than (PMDA), chosen from a cycloaliphatic, aliphatic or aromatic diamine.
LIPIDS AND LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS
Compounds are provided having the following structure:
##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, L.sup.1, L.sup.2, G.sup.1, G.sup.2, G.sup.3, a, b, c and d are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
LIPIDS AND LIPID NANOPARTICLE FORMULATIONS FOR DELIVERY OF NUCLEIC ACIDS
Compounds are provided having the following structure:
##STR00001##
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1a, R.sup.1b, R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, L.sup.1, L.sup.2, G.sup.1, G.sup.2, G.sup.3, a, b, c and d are as defined herein. Use of the compounds as a component of lipid nanoparticle formulations for delivery of a therapeutic agent, compositions comprising the compounds and methods for their use and preparation are also provided.
CARBON DOTS, METHODS OF MANUFACTURE THEREOF, AND USES THEREOF IN THE PRODUCTION OF BIOFUEL
The present disclosure relates to carbon dots, uses thereof and methods of manufacture thereof. For example, such carbon dots can be used in the production of biofuels such as biodiesel. For example, these carbon dots can be used as catalysts in transesterification reactions. For example, these carbon dots can be glycine-citric acid carbon dots, amine-passivated carbon dots, or combinations thereof.
Amide compounds, pharmaceutical compositions thereof, and methods of using the same
Amide compounds are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds as well as methods of treating neurodegenerative diseases that involve administering the compounds or pharmaceutical compositions to a subject.