247 results about "Phosphatidylethanolamine" patented technology

Disclosed is the surprising discovery that aminophospholipids, such as phosphatidylserine and phosphatidylethanolamine, are specific, accessible and stable markers of the luminal surface of tumor blood vessels. The present invention thus provides aminophospholipid-targeted diagnostic and therapeutic constructs for use in tumor intervention. Antibody-therapeutic agent conjugates and constructs that bind to aminophospholipids are particularly provided, as are methods of specifically delivering therapeutic agents, including toxins and coagulants, to the stably-expressed aminophospholipids of tumor blood vessels, thereby inducing thrombosis, necrosis and tumor regression.

Mixtures of natural phosphatidylcholine species, natural lysophosphatidylcholine species, phosphatidylserine species, phosphatidylethanolamine species, 1-hydroxy-2-acyl-phosphatidylcholine species, 1-hydroxy-2-acyl-phosphatidylserine molecular species, 1-hydroxy-2-acyl-phosphatidylethanolamine molecular species, 1-O-alkyl-2-hydroxy phosphatidylcholine species, 1-O-alkyl-2-docosaheaxnoyl phosphatidylcholine species 1-O-alkyl-2-docosahexaenoyl phosphatidylserine species, and 1-O-alkyl-2-docosahexaenoyl phosphatidylethanolamine species, Methods using the above disclosed mixtures in mammals to treat various conditions.

The invention discloses a reductively-responsive paclitaxel prodrug. The reductively-responsive paclitaxel prodrug is synthesized from paclitaxel (PTX) and dithiodicarboxylic acid in a mol ratio of 2: 1 through covalent combination via an ester bond, and the molecular structure of the synthesized paclitaxel prodrug is PTX-SS-PTX. A PTX prodrug nano-micelle carrier is mainly composed of PTX-SS-PTX and distearoyl-phosphatidylethanolamine-polyethylene glycol (DSPE-PEG). According to the PTX-SS-PTX prodrug in the invention, a disulfide bond can rotate freely; and on the condition that the paclitaxel prodrug and a paclitaxel prodrug nano-micelle drug delivery system provided by the invent are stimulated by a high-concentration glutathione reductive environment in tumor cells, the disulfide bond breaks, and a parent drug is released. The reductively-responsive paclitaxel prodrug can obviously improve the drug loading capacity and encapsulation efficiency of PTX and improves stability of a PTX nanometer drug delivery system.

Disclosed herein are polar lipid mixtures, comprising glycerophospholipids such as phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidylserine (PS) and phosphatidyl-inositol (PI), and sphingolipids such as sphyngomyelin (SM). Most importantly, the ratio of phospholipids in said mixture is comparable to that of HMF, and is represented by SM>PC>PE>PS>PI or SM=PC>PE>PS>PI. Processes for the preparation of said mixtures and uses thereof are also described herein.

A lipid preparation including a glycerophospholipid or salt, conjugate and derivatives thereof, particularly phosphatidylserine (PS), phosphatidylcholine (PC), phosphatidylethanolamine (PE), phosphatidyl-inositol (PI), phosphatidylglycerol (PG) and phosphatidic acid (PA), and poly-unsaturated fatty acid (PUFA) acyl groups, particularly long-chain poly-unsaturated fatty acid (LC-PUFA) acyl groups such as omega-3 and / or omega-6 acyl groups, wherein said PUFA is covalently bound to said glycerophospholipid. The preparation possesses an improved bioactivity, and is useful in the treatment of various cognitive and mental conditions and disorders and for maintenance of normal functions of brain-related systems and processes.

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.

A lipid preparation including a glycerophospholipid or salt, conjugate and derivatives thereof, particularly phosphatidylserine (PS), phosphatidyicholine (PC), phosphatidylethanolamine (PE), phosphatidyl-inositol (PI), phosphatidylglycerol (PG) and phosphatidic acid (PA), and poly-unsaturated fatty acid (PUFA) acyl groups, particularly long-chain poly-unsaturated fatty acid (LC-PUFA) acyl groups such as omega-3 and / or omega-6 acyl groups, wherein said PUFA is covalently bound to said glycerophospholipid. The preparation possesses an improved bioactivity, and is useful in the treatment of various cognitive and mental conditions and disorders and for maintenance of normal functions of brain-related systems and processes.

Disclosed are the surprising discoveries that aminophospholipids, such as phosphatidylserine and phosphatidylethanolamine, are stable and specific markers accessible on the luminal surface of tumor blood vessels, and that the administration of an anti-aminophospholipid antibody alone is sufficient to induce thrombosis, tumor necrosis and tumor regression in vivo. This invention therefore provides anti-aminophospholipid antibody-based methods and compositions for use in the specific destruction of tumor blood vessels and in the treatment of solid tumors. Although various antibody conjugates and combinations are thus provided, the use of naked, or unconjugated, anti-phosphatidylserine antibodies is a particularly important aspect of the invention, due to simplicity and effectiveness of the approach.

The invention provides a cellulose derivative having a repeating unit of the formula below, a composition including the cellulose derivative and a phospholipid, a method for production thereof, and an adhesion barrier including the cellulose derivative or the composition.In the formula, R1, R2, and R3 are —H, —CH2—COOH, —CH2—COOX, or —CH2CO-phosphatidylethanolamine, and X is an alkali metal or an alkali earth metal. The degree of substitution of —CH2—COOH and —CH2—COOX is 0.3 to 2.0 in total, and the degree of substitution of —CH2CO-phosphatidylethanolamine is 0.001 to 0.05.

The invention provides a polyethylene glycol-modified phospholipid derivative taking a 4-substituted anilino-quinazoline group as a targeting ligand and a preparation method thereof. The method comprises the following steps of: performing condensation with para-methylbenzene sulfonyl chloride, substitution with phthalimide potassium salt and hydrolysis with a hydrazine hydrate by taking polyethylene glycol (PEG) as a starting raw material to obtain diamine PEG; and reacting with targeting ligands, i.e., N-(3-chlorin-4-fluorin)-6-(3-chloropropyl)-7-methoxylquinazoline-4-amine and distearoylphosphatidylethanolamine (DSPE) to respectively obtain 4-anilino-quinazoline group-PEG-DSPE. A liposome preparation of the 4-anilino-quinazoline group-PEG-DSPE can be used for realizing target administration of tumor cells and reducing the toxic and side effects of a tumor medicament; and the pharmacodynamic structure of gefitinib can give play to dual medicament effects together with other liposome-coated antitumor medicaments, so that the tumor treatment effect is enhanced greatly.