Patent classifications
C07C237/08
Hydroxy-substituted amino and ammonium derivatives and their medical use
The present invention relates to hydroxy-substituted amino and ammonium derivatives, in particular the compounds of formula 1 or 2, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder, or a proliferative, neoplastic or dysplastic disease or disorder. ##STR00001##
Hydroxy-substituted amino and ammonium derivatives and their medical use
The present invention relates to hydroxy-substituted amino and ammonium derivatives, in particular the compounds of formula 1 or 2, and their medical use, including their use in the treatment, prevention or amelioration of an inflammatory, autoimmune and/or allergic disorder, or a proliferative, neoplastic or dysplastic disease or disorder. ##STR00001##
LIPID COMPOUND AS WELL AS LIPID VECTOR, NUCLEIC ACID LIPID NANOPARTICLE COMPOSITION, AND PHARMACEUTICAL PREPARATION COMPRISING THE SAME
The present disclosure belongs to the technical field of gene therapy, and specifically relates to a series of lipid compounds as well as lipid vectors, nucleic acid lipid nanoparticle compositions, and pharmaceutical preparations containing the same. The compound having the structure of formula (I) provided by the present disclosure may be used in combination with other lipid compounds to prepare a lipid vector, which exhibits pH responsiveness, has high encapsulation efficiency for nucleic acid drugs, and greatly enhances the in-vivo delivery efficiency of nucleic acid drugs. Moreover, it is possible to select lipid compounds with different structures as lipid vectors to adjust the enrichment of nucleic acid drugs in different organs, thereby having good market application prospect.
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EPOXIDIZED OIL-BASED SURFACTANT AND COMPOSITIONS COMPRISING THE SAME
An epoxidized oil-based surfactant is the reaction product of an epoxidized compound and a primary and/or secondary alkanolamine, wherein the epoxidized compound is chosen from an epoxidized oil, an epoxidized fatty acid, an epoxidized fatty acid ester, and combinations thereof. An herbicidal composition includes glyphosate or a salt thereof and at least one epoxidized oil-based surfactant. The herbicidal composition is used in a method of controlling unwanted vegetation wherein the method includes the step of applying to the unwanted vegetation a herbicidally effective amount of the aforementioned herbicidal composition. The epoxidized oil-based surfactant is prepared using a method that includes reacting the epoxidized compound and the primary and/or secondary alkanolamine. The epoxidized oil-based surfactant is also utilized in a cleaning composition for the cleaning of hard surfaces, wherein the cleaning composition includes the epoxidized oil-based surfactant and an additional component chosen from an additional surfactant and/or a chelating agent.
AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF
Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:
##STR00001##
wherein m, n, p, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.
AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF
Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein:
##STR00001##
wherein m, n, p, R′, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.8, Z, W, Y, and Z are as defined herein.
LIPIDS FOR LIPID NANOPARTICLE DELIVERY OF ACTIVE AGENTS
Compounds are provided having the following structure:
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or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, G.sup.1, G.sup.2, and G.sup.3 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.
CHIRAL MULTIDENTATE LIGAND, AND APPLICATION THEREOF IN ASYMMETRIC HYDROGENATION
Disclosed are a chiral multidentate ligand (I), a preparation, and an application thereof. In this method, compound (M1) is subjected to condensation with compound (M2) followed by amine deprotection in the presence of a deprotection reagent to obtain compound (M4). Compound (1) is subjected to deprotonation by butyl lithium and phosphorization followed by dimethylamino group substitution to produce compound (3). The compound (3) and the compound (M4) are reacted in the presence of triethylamine to produce chiral multidentate ligands.
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CHIRAL MULTIDENTATE LIGAND, AND APPLICATION THEREOF IN ASYMMETRIC HYDROGENATION
Disclosed are a chiral multidentate ligand (I), a preparation, and an application thereof. In this method, compound (M1) is subjected to condensation with compound (M2) followed by amine deprotection in the presence of a deprotection reagent to obtain compound (M4). Compound (1) is subjected to deprotonation by butyl lithium and phosphorization followed by dimethylamino group substitution to produce compound (3). The compound (3) and the compound (M4) are reacted in the presence of triethylamine to produce chiral multidentate ligands.
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AMINO ACID DERIVATIVES AND THEIR USE AS FLAVOR MODIFIERS
The present invention provides derivatives of glutamine of formula (I) and derivatives of arginine of formula (II), and the use of such compounds as flavor modifiers. The invention further provides the use of such derivatives of glutamine and arginine to enhance the salty and umami taste of ingestible compositions as ingestible compositions that include such derivatives of glutamine and arginine and bulking agents.
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