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33 results about "Glucosylceramides" patented technology

Cerebrosides which contain as their polar head group a glucose moiety bound in glycosidic linkage to the hydroxyl group of ceramides. Their accumulation in tissue, due to a defect in beta-glucosidase, is the cause of Gaucher's disease.

Pharmaceutical formulations employing short-chain sphingolipids and their use

This invention pertains to pharmaceutical formulations which comprise (i) a drug (e.g., an amphiphilic drug) (e.g., an anthracycline) (e.g., doxorubicin) and (ii) a short-chain sphingolipid (e.g., a short-chain glycosphingolipid or a short-chain sphingomyelin) (e.g., N-octanoyl-glucosylceramide, referred to as C8-GlcCer) (e.g., N-hexanoyl-sphingomyelin, referred to herein as C6-SM), and which provide improved drug delivery and efficacy. The short-chain sphingolipidis selected from compounds of the following formula: wherein: R1 is independently: an O-linked saccharide group; or an O-linked polyhydric alcohol group; or: R1 is independently: an O-linked (optionally N-(C1-4alkyl)-substituted amino)-C1-6alkyl-phosphate group; or an O-linked (polyhydric alcohol-substituted)-C1-6alkyl-phosphate group; R2 is independently C3-9alkyl, and is independently unsubstituted or substituted; R3 is independently C7-19alkyl, and is independently unsubstituted or substituted; R4 is independently —H, —OH, or —O—C1-4alkyl; RN is independently —H or C1-4alkyl; the bond marked with an alpha (α) is independently a single bond or a double bond; if the bond marked with an alpha (α) is a double bond, then R5 is —H; if the bond marked with an alpha (α) is a single bond, then R5 is —H or —OH; the carbon atom marked (*) is independently in an R-configuration or an S-configuration; the carbon atom marked (**) is independently in an R-configuration or an S-configuration; and pharmaceutically acceptable salts, solvates, esters, ethers, chemically protected forms thereof. In one embodiment, the pharmaceutical formulation is a liposomal pharmaceutical formulation prepared using a mixture of lipids comprising, at least, vesicle-forming lipids (e.g., phospholipids) (e.g., phosphatidylcholines) (e.g., fully hydrogenated soy phosphatidylcholine (HSPC)) (e.g., dipalmitoyl-phosphatidylcholine (DPPC)) and said short-chain sphingolipid, and optionally cholesterol and optionally a vesicle-forming lipid which is derivatized with a polymer chain (e.g., a phosphatidylethanolamine (PE) which is derivatized with polyethyleneglycol (PEG)) (e.g., N-(carbonyl-methoxypolyethylene glycol 2000)-1,2-distearoyl-sn-glycero-3-phosphoethanolamine sodium salt (MPEG2000-DSPE). The present invention also pertains to methods for the preparation and use of such formulations.
Owner:NETHERLANDS CANCER INST

Method for preparing D-glucosylceramide by using soy sauce filter residue

The invention relates to a method for preparing D-glucosylceramide by using a soy sauce filter residue, and is characterized in that the method comprises the following steps: activating strains: A, respectively inoculating 100 mL of an activation culture medium with an sphingomonas strain and a yarrowia lipolytica strain; B, carrying out aerobic fermentation culture of the sphingomonas strain activated culture liquid P and the yarrowia lipolytica strain activated culture liquid Q obtained in the step A for 36-72 h, to obtain a composite strain fermentation liquid; C, mixing the composite strain fermentation liquid with the soy sauce filter residue, adding the mixture into a compound fermentation tank, carrying out static culture, and culturing for 48-96 h at the temperature of 25-30 DEG C, to obtain a strain cell-rich filter residue; and carrying out high pressure homogenization for 2 times, to obtain a wall-broken cell homogenate; and D, mixing the wall-broken cell homogenate with an ethanol solution, filtering to obtain a precipitate, and thus obtaining a D-glucosylceramide extract. Through rational use of the soy sauce filter residue, the waste can be turned into treasure, soy sauce industries are facilitated to improve economic benefits, and the resource utilization of the soy sauce filter residue and the development of high-value by-products are greatly improved.
Owner:PROYA COSMETICS

N-(5-((aryl or heteroaryl)methyloxy)pentyl)-substituted iminosugars as inhibitors of glucosylceramide synthase

ActiveUS10189784B2Organic chemistryMetabolism disorderFabry diseaseGm1 ganglioside
Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. These compounds display an increased inhibitory potency towards GCS, and / or an increased inhibitory potency towards GBA2, and / or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration. Therefore, compounds of the present invention are effective in the treatment of diseases which are associated with an irregular level of cytosolic or lysosomal glucosylceramide and / or higher glycosphingolipids, such as a lysosomal storage disorder, such as Gaucher disease, Fabry disease, Tay-Sachs disease, Sandhoff disease, GM1 gangliosidosis, Sialidosis, Niemann Pick disease type C and AMRF, or a symptom of one of the diseases collectively classed as metabolic syndrome, such as obesity, insulin resistance, hyperlipidemia, hypercholesterolemia, polycystic kidney disease, type II diabetes and chronic inflammation, or a neurodenegerative disorder, such as Parkinson disease or Lewy-body dementia.
Owner:LEIDEN UNIVERSITY +1

N-(5-((aryl or heteroaryl)methyloxy)pentyl)-substituted iminosugars as inhibitors of glucosylceramide synthase

ActiveUS20170226058A1Organic chemistryMetabolism disorderFabry diseaseGm1 ganglioside
Deoxynojirimycin and deoxygalactonojirimycin derivatives according to the present invention are N-alkylated D-galacto, D-gluco- or L-ido-deoxynojirimycin with a linear methyloxypentyl group bearing various sidegroups and a non-fused bicyclic aromatic group (“X”) on the methyloxy-carbon. These compounds display an increased inhibitory potency towards GCS, and/or an increased inhibitory potency towards GBA2, and/or a decreased inhibitory potency towards GBA1, relative to known deoxynojirimycin derivatives of the same (D-gluco, L-ido or D-galacto) configuration. Therefore, compounds of the present invention are effective in the treatment of diseases which are associated with an irregular level of cytosolic or lysosomal glucosylceramide and/or higher glycosphingolipids, such as a lysosomal storage disorder, such as Gaucher disease, Fabry disease, Tay-Sachs disease, Sandhoff disease, GM1 gangliosidosis, Sialidosis, Niemann Pick disease type C and AMRF, or a symptom of one of the diseases collectively classed as metabolic syndrome, such as obesity, insulin resistance, hyperlipidemia, hypercholesterolemia, polycystic kidney disease, type II diabetes and chronic inflammation, or a neurodenegerative disorder, such as Parkinson disease or Lewy-body dementia.
Owner:LEIDEN UNIVERSITY +1

A kind of method utilizing soy sauce filter residue to prepare d-glucosylceramide

The invention relates to a method for preparing D-glucosylceramide by using a soy sauce filter residue, and is characterized in that the method comprises the following steps: activating strains: A, respectively inoculating 100 mL of an activation culture medium with an sphingomonas strain and a yarrowia lipolytica strain; B, carrying out aerobic fermentation culture of the sphingomonas strain activated culture liquid P and the yarrowia lipolytica strain activated culture liquid Q obtained in the step A for 36-72 h, to obtain a composite strain fermentation liquid; C, mixing the composite strain fermentation liquid with the soy sauce filter residue, adding the mixture into a compound fermentation tank, carrying out static culture, and culturing for 48-96 h at the temperature of 25-30 DEG C, to obtain a strain cell-rich filter residue; and carrying out high pressure homogenization for 2 times, to obtain a wall-broken cell homogenate; and D, mixing the wall-broken cell homogenate with an ethanol solution, filtering to obtain a precipitate, and thus obtaining a D-glucosylceramide extract. Through rational use of the soy sauce filter residue, the waste can be turned into treasure, soy sauce industries are facilitated to improve economic benefits, and the resource utilization of the soy sauce filter residue and the development of high-value by-products are greatly improved.
Owner:PROYA COSMETICS
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