41 results about "Lipid moiety" patented technology

A nanoparticle generally comprising a targeting peptide-lipid conjugate, wherein a targeting peptide moiety of the targeting peptide-lipid conjugate comprises a GRP78 targeting peptide, a polyethylene glycol (PEG)-lipid conjugate, a drug-lipid conjugate comprising a prodrug moiety, wherein the drug-lipid conjugate comprises one or more of a mertansine (DM1) prodrug, a doxorubicin prodrug, and a bortezomib (BTZ) prodrug; and wherein the prodrug is linked to a lipid moiety of the drug-lipid conjugate via a phosphodiester bond or a boron ester bond; cholesterol comprising about 1 mol% to about 10 mol% of the nanoparticle; and distearoylphosphatidylcholine (DSPC).

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Provided herein are a lipopeptide building block comprising a lipid moiety, an amphipathic domain, a hydrophilic polymer block, a protease cleavage site, and lipopeptide constructs, lipopeptide aggregates and immunogenic compositions comprising the same.

Disclosed are compositions comprising a first lipid-conjugated oligonucleotide comprising a first lipid moiety, a first hybridization region, and a first primer region; a second lipid-conjugated oligonucleotide comprising a second hybridization region and a second lipid moiety, wherein the second hybridization region is the reverse complement of the first hybridization region; and a third oligonucleotide comprising a second primer region, a barcode region, and a capture sequence, wherein the second primer region is the reverse complement of the first primer region; compositions comprising a lipid-conjugated DNA oligonucleotide comprising a lipid moiety, a barcode region, and a capture sequence; and composition comprising a first lipid-conjugated DNA oligonucleotide comprising a lipid moiety and a first primer region; and a second DNA oligonucleotide comprising a second primer region, a barcode region, and a capture sequence, wherein the second primer region is the reverse complement of the first primer region. Also disclosed are membranes and cells comprising such compositions and uses of such compositions.

The invention relates to an ionizable cationic lipid mediated lung targeting nucleic acid delivery system and application. Specifically, the present invention provides a lipid nanoparticle, the lipid portion of which comprises an ionizable cationic lipid, a phospholipid, and a polyethylene glycol lipid, in which the ionizable cationic lipid comprises Compound 1, and in which the content of Compound 1 is 80 mol% or more based on the total amount of lipid in the lipid nanoparticle. According to the lipid nanoparticles, the lung targeting efficiency is remarkably improved, and the preparation design process is simplified.

To provide formulated and / or co-formulated liposome compositions containing IDO antagonist prodrugs useful in treatment of cancer and methods thereof.SOLUTION: Formulated and / or co-formulated liposomes comprising IDO prodrugs and methods of making the liposomes are disclosed herein. The IDO prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit that inhibit IDO-1. The IDO prodrugs can be formulated and / or co-formulated into a liposome to provide a method of treating cancer, immunological disorders, and other disease by utilizing a targeted drug delivery vehicle.SELECTED DRAWING: None

The present invention relates to a cationic lipid having one or more biodegradable groups located in the mid- or distal section of a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Formulated and / or co-formulated liposomes, lipid nanoparticle (LNP) and solid-lipid nanoparticles (SLNP) comprising TB Prodrugs and methods of making the LNPs and SLNPs are disclosed herein. The TB prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit that inhibit ALK5. The TB Prodrugs can be formulated and / or co-formulated into a nanocarrier to provide a method of treating cancer, immunological disorders, and other diseases by utilizing a targeted drug delivery vehicle.

The application belongs to the technical field of biological medicine, and provides a ciprofloxacin derivative, a preparation method and application thereof. The ciprofloxacin derivative provided by the application has a structure shown in formula I, a positively charged electrostatic effect sequence (an amino acid part) is connected to a lipid part, then is conjugated with ciprofloxacin through a linker, and a series of amphipathic ciprofloxacin derivatives are formed. The positively charged electrostatic effect sequence can enhance the interaction with a negatively charged bacterial cell membrane through electrostatic action, then the lipid part can be inserted into a phospholipid bilayer of the bacterial cell membrane, leading to the integrity of the bacterial cell membrane being destroyed, the ciprofloxacin derivative entering the cell, and finally leading to the leakage of the bacterial cell content, the breakage of the bacterial chromosome and the death of the bacterial cell. The amphipathic ciprofloxacin derivative of the application simulates the amphipathic structure and membrane destruction mechanism of an antibacterial peptide, so that the ciprofloxacin derivative exhibits a unique advantage of not being prone to drug resistance.

Formulated and / or co-formulated liposomes comprising IDO prodrugs and methods of making the liposomes are disclosed herein. The IDO prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit that inhibit IDO-1. The IDO prodrugs can be formulated and / or co-formulated into a liposome to provide a method of treating cancer, immunological disorders, and other disease by utilizing a targeted drug delivery vehicle.

The problem to be solved by the present invention is to provide cationic lipids for oligonucleotide delivery which can provide a high drug: lipid ratio, which protect the nucleic acid from degradation and clearance in serum, which are suitable for systemic delivery, which can result in intracellular delivery of the nucleic acid, and which are well tolerated, provide an adequate therapeutic index, and treatment of patients with an effective dose of the nucleic acid is not associated with significant toxicity and / or risk to the patient.SOLUTION: The present invention relates to cationic lipids having one or more biodegradable groups located in the lipid portion (e.g., hydrophobic chain) of the cationic lipid. These cationic lipids can be incorporated into lipid particles for the delivery of active agents such as nucleic acids. The present invention also relates to a lipid particle comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the invention and optionally a sterol. The lipid particles may further comprise a therapeutic agent, such as a nucleic acid.SELECTED DRAWING: None

An in vitro method of detecting one or more endotoxins of one or more pathogens in a sample, comprising the steps of a. coating a lipid binding protein on a substrate or capturing a lipid binding protein on a capture molecule immobilized on a substrate, b. contacting the lipid binding protein, thus coated or captured, with the sample, c. detecting whether an endotoxin binds to the lipid binding protein, wherein the one or more endotoxins comprise a lipid A moiety and O- polysaccharide moiety, wherein the lipid binding protein is capable of binding the lipid A moiety of an endotoxin, and characterized in that the lipid binding protein is a mammalian protein and preferably is a murine or human protein.

The invention belongs to the technical field of biological medicines, and provides a ciprofloxacin derivative as well as a preparation method and application thereof. The ciprofloxacin derivative provided by the invention has a structure as shown in a formula I, an electrostatic effect sequence (amino acid part) with positive charges is connected to a lipid part, and then a series of amphiphilic ciprofloxacin derivatives are formed through conjugation of Linker and ciprofloxacin. The electrostatic effect sequence with positive charges can enhance the interaction with a bacterial cell membrane with negative charges through electrostatic interaction, then the lipid part can be inserted into a phospholipid bilayer of the bacterial cell membrane, so that the integrity of the bacterial cell membrane is damaged, the ciprofloxacin derivative enters the cell, and the ciprofloxacin derivative is degraded. Finally, bacterial cell content leakage, bacterial chromosome breakage and bacterial cell death are caused. According to the amphiphilic ciprofloxacin derivative disclosed by the invention, the amphiphilic structure and the membrane destruction mechanism of the antibacterial peptide are simulated, so that the ciprofloxacin derivative shows the unique advantage that the drug resistance is not easy to generate. # imgabs0 #

The present invention relates to a lipopeptide building block consisting of (i) a peptide moiety comprising a coiled coil peptide chain segment, wherein said coiled coil peptide chain segment comprises 3 to 8 repeat units, and wherein said repeat unit consists of the sequence IEKKIE-X0 (SEQ ID NO:58), wherein X0 represents an amino acid; and (ii) a lipid moiety comprising the formula LM-Iwherein R1 and R2 are independently C11-15 alkyl, wherein R3 is hydrogen or —C(O)C11-15 alkyl wherein said lipid moiety is linked to said peptide moiety, wherein the wavy line in formula LM-I indicates the linkage site to said peptide moiety, as well as conjugates comprising said lipopeptide building blocks to which antigens are coupled, bundles of such conjugates, synthetic virus-like particles (SVLPs) comprising at least one bundle of conjugates and pharmaceutical compositions comprising the same.

The present disclosure provides a Lipid-Phosphocholine-Carboxylic Acid Agent being a compound comprising one or more groups, wherein each group is independently selected from Lipid Moiety (LM), Phosphocholine Moiety (PCM), Carboxylic Acid Moiety, Amide Moiety, and Attachment Moiety (AM), and wherein each group is covalently attached, directly or indirectly, to a multivalent linker (i.e., Composition Linker Moiety (CLM)), or pharmaceutically acceptable salts thereof, and related conjugates. The present disclosure also relates to uses of the Lipid-Phosphocholine-Carboxylic Acid Agents and conjugates, e.g., in delivering nucleic acid and / or treating or preventing diseases.

Disclosed herein are formulated and / or co-formulated lipid nanoparticles (LNPs) and solid lipid nanoparticles (SLNPs) comprising TB prodrugs and methods of making the LNPs and the SLNPs. TB prodrug compositions comprising a drug moiety, a lipid moiety, and a linking unit, inhibit ALK5. The TB prodrugs can be formulated and / or co-formulated into liposomes or solid lipid nanoparticles to provide methods of treating cancer, immune disorders, and other diseases by taking advantage of targeted drug delivery vehicles.

The present disclosure provides a Lipid-Phosphocholine-Carboxylic Acid Agent being a compound comprising one or more groups, wherein each group is independently selected from Lipid Moiety (LM), Phosphocholine Moiety (PCM), Carboxylic Acid Moiety, Amide Moiety, and Attachment Moiety (AM), and wherein each group is covalently attached, directly or indirectly, to a multivalent linker (i.e., Composition Linker Moiety (CLM)), or pharmaceutically acceptable salts thereof, and related conjugates. The present disclosure also relates to uses of the Lipid-Phosphocholine-Carboxylic Acid Agents and conjugates, e.g., in delivering nucleic acid and / or treating or preventing diseases.

To provide formulated and / or co-formulated liposomal compositions containing TFG β antagonist prodrugs useful in the treatment of cancer, and methods thereof.SOLUTION: Disclosed herein are formulated and / or co-formulated liposomes (LNPs) and solid lipid nanoparticles (SLNPs) comprising TB prodrugs, and methods of making said LNPs and SLNPs. TB pro-drug compositions comprise a drug moiety, a lipidic moiety, and a linking unit, and inhibit ALK5. TB prodrugs can be formulated and / or co-formulated into liposomes or solid lipid nanoparticles to provide a method of treating cancer, immunological disorders, and other diseases by utilizing a targeted drug delivery vehicle.SELECTED DRAWING: None

Formulated and / or co-formulated liposomes comprising TLR prodrugs and / or TLR Lipid Moieties and methods of making the liposomes are disclosed herein. The TLR prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit that inhibit Toll-Like Receptor (e.g., TLR1 / 2, TLR4, and / or TLR7). The TLR prodrugs can be formulated and / or co-formulated into a liposome to provide a method of treating cancer, immunological disorders, and other disease by utilizing a targeted drug delivery vehicle.

Disclosed herein are formulated and / or co-formulated liposomes, lipid nanoparticles (LNPs), and solid lipid nanoparticles (SLNPs) comprising a TB prodrug, as well as methods of making the LNPs and the SLNPs. The TB prodrug composition includes a drug moiety, a lipid moiety, and a linking unit that inhibits ALK5. The TB prodrugs may be formulated and / or co-formulated into nanocarriers to provide methods of treating cancer, immune disorders, and other diseases by utilizing targeted drug delivery vehicles.

The present invention relates to a cationic lipid having one or more biodegradable groups located in the mid- or distal section of a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Disclosed is an oligonucleotide delivery agent comprising at least one lipid moiety directly or indirectly coupled to a single-stranded oligonucleotide, the lipid moiety comprising at least one linear alkyl or linear alkenyl group, which oligonucleotide delivery agent can be delivered to various subjects, such as muscles, heart, liver, and the like, and has enhanced efficiency, and therefore, expression regulation of the target gene is improved. Also disclosed are pharmaceutical compositions comprising the oligonucleotide delivery agent and methods of using the pharmaceutical compositions to modulate expression of a target gene.

The invention relates to a process for the preparation of a composition comprising an oligosaccharide or a polysaccharide encapsulated in lipid nanoparticles, the process comprising the following steps: preparing a first solution of a lipid portion comprising a phospholipid, a neutral lipid, and a lipid sterol; preparing a second solution comprising a poly- or oligosaccharide; preparing a third solution containing a buffer; mixing the first and second solutions using a microfluidic system to obtain lipid nanoparticles encapsulating the oligosaccharide or the polysaccharide; combining the third solution with the first and second solutions. The invention also relates to a composition comprising lipid nanoparticles obtainable by the above-defined process, said composition comprising a lipid portion comprising a phospholipid, a neutral lipid compound in which a lipid chain is bound to a glycol group, and a lipid sterol; a buffer; and an oligosaccharide or polysaccharide.

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

The present application relates to ionizable cationic lipid-mediated pulmonary targeting nucleic acid delivery system and application. Specifically, the present application provides a kind of lipid nanoparticles, the lipid part of the lipid nanoparticles includes ionizable cationic lipid, phospholipid and polyethylene glycol lipid, wherein ionizable cationic lipid includes compound 1, and wherein the content of compound 1 is 80 mol% or more based on the total amount of lipid in the lipid nanoparticle. The lipid nanoparticle significantly improves the lung targeting efficiency and simplifies the formulation design process.

A nanoparticle generally comprising a targeting peptide-lipid conjugate, wherein a targeting peptide moiety of the targeting peptide-lipid conjugate comprises a GRP78 targeting peptide, a polyethylene glycol (PEG)-lipid conjugate, a drug-lipid conjugate comprising a prodrug moiety, wherein the drug-lipid conjugate comprises one or more of a mertansine (DM1) prodrug, a doxorubicin prodrug, and a bortezomib (BTZ) prodrug; and wherein the prodrug is linked to a lipid moiety of the drug-lipid conjugate via a phosphodiester bond or a boron ester bond; cholesterol comprising about 1 mol% to about 10 mol% of the nanoparticle; and distearoylphosphatidylcholine (DSPC).

The present invention relates to a lipopeptide building block, the lipid building block consisting of: (i) a peptide portion, the peptide portion comprising a coiled-coil peptide segment, wherein the coiled-coil peptide segment comprises 3 to 8 repeating units, and wherein the repeating units consist of the sequence IEKKIE-X0 (SEQ ID NO: 58), wherein X0 represents an amino acid, and wherein preferably the repeating units consist of a sequence selected from IEKKIEG (SEQ ID NO: 59), IEKKIEA (SEQ ID NO: 12) or IEKKIES (SEQ ID NO: 13), and wherein further preferably the repeating units consist of the sequence IEKKIES (SEQ ID NO: 13); (ii) a lipid portion, the lipid portion comprising or preferably consisting of formula LM-I, wherein R 1 and R 2 Independently C 11‑15 Alkyl, wherein preferably R 1 and R 2 Independently C 11 H 23 ,‑C 13 H 27 or ‑C 15 H 31 , and wherein further preferably R 1 and R 2 C 15 H 31 ; and where R 3 is hydrogen or ‑C(O)C 11‑15 alkyl, and wherein preferably R 3 H or ‑C(O)C 15 H 31 and wherein the lipid portion is linked to the peptide portion, wherein the wavy line in formula LM-I indicates the site of attachment to the peptide portion, and wherein preferably the lipid portion is linked to the N-terminus of the peptide portion, and the present invention relates to conjugates comprising the lipopeptide building block to which an antigen is coupled, bundles of such conjugates, synthetic virus-like particles (SVLPs) comprising a bundle of at least one conjugate, and pharmaceutical compositions comprising the conjugates. The present invention further relates to the conjugates, bundles of conjugates, the SVLPs and the pharmaceutical compositions for use as medicaments, as vaccines and in methods for preventing or treating diseases preferably selected from infectious diseases, allergies and cancer and generally for effectively inducing an antigen-specific immune response. #imgabs0#

Formulated and / or co-formulated liposomes comprising IDO prodrugs and methods of making the liposomes are disclosed herein. The IDO prodrug compositions comprise a drug moiety, a lipid moiety, and linkage unit that inhibit IDO-1. The IDO prodrugs can be formulated and / or co-formulated into a liposome to provide a method of treating cancer, immunological disorders, and other disease by utilizing a targeted drug delivery vehicle.

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

[Problem] To provide a novel composition which contains a lipid peptide and a sucrose ester that comprises a contamination suppressing effect and a penetration enhancing effect. [Solution] This composition contains: a lipid peptide-type compound in which a peptide moiety formed by the repetition of at least two or more identical or different amino acids is bonded to a lipid moiety that is composed of an aliphatic group having 10-24 carbon atoms; a sucrose ester; a 1,2-alkanediol; a fatty acid; and water.