This invention provides amine-linked C.sup.3-glutarimide Degronimers and Degrons for therapeutic applications as described further herein, and methods of use and compositions thereof as well as methods for their preparation.

The present invention relates to an oral pharmaceutical composition containing pemetrexed as a water-soluble anticancer drug and a method of manufacturing the same, and more particularly to an oral pharmaceutical composition, in which an ion-binding complex of pemetrexed and a bile acid derivative as an oral absorption enhancer is formed, mixed with a pharmaceutical additive, and then provided in the form of a capsule or a tablet through pressing or included in the internal water phase of a w/o/w (water-in-oil-in-water) multiple nanoemulsion, thus increasing the oral bioavailability of pemetrexed as the water-soluble anticancer drug, whereby pemetrexed, which is currently administered only in the form of an injection formulation, can be manufactured into a formulation capable of being orally administered, ultimately alleviating inconvenience and problems with use of injection formulations, improving patient compliance and contributing to a reduction in medical expenses.

The disclosure is generally related to nanoparticles have an oxidized tumor cell lysate encapsulated therein and oligonucleotides on the surface thereof. Methods of making and using the nanoparticles are also provided herein.

Provided is a compound in which a group derived from chondroitin sulfate and a group derived from a steroid are covalently bonded together via a spacer represented by general formula (I). In the formula, m represents an integer of 0 or 1. Here, if m=0, R.sup.1 represents a group selected from the group consisting of electron-donating groups and steric hindrance groups. If m=1, R.sup.1 represents a group selected from the group consisting of a hydrogen atom, electron-donating groups and steric hindrance groups.

—HN—(CH.sub.2).sub.m—CHR.sup.1—CO—  (I)

The present application relates to a lipopeptide for potently inhibiting HIV, a derivative thereof, or a pharmaceutical composition thereof, and use thereof. The lipopeptide is the following a) or b): a) a lipopeptide formed by linking a polypeptide having an antiviral activity to a lipophilic compound linked to the carboxyl-terminus of the polypeptide; or b) a lipopeptide formed by linking a polypeptide having an antiviral activity to a terminal protecting group and a lipophilic compound linked to the carboxyl-terminus of the polypeptide, wherein the terminal protecting group is an amino-terminal protecting group and/or a carboxyl-terminal protecting group, the polypeptide has a sequence of 28 amino acid residues, corresponding to amino acids at positions of 127-154 of the sequence of gp41 from HIV-1 strain HXB2. The anti-HIV activity of the lipopeptide of the present invention is higher than that of T-20 by several thousands of times or even tens of thousands of times, and is also significantly higher than that of the anti-HIV lipopeptides such as C34-Chol, LP-19 and the like.

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.

The invention provides siRNA compositions that specifically downregulates expression of a variant of the PNPLA3 gene and methods of use thereof for treating a chronic liver disease or alcoholic liver disease (ALD).

The present invention relates to the field of biomedicine, and specifically relates to an “LC3 binding portion-lipid droplet binding portion-conjugate” formed by means of covalently linking a structure capable of binding LC3 and a structure capable of binding lipid droplets, and a pharmaceutically acceptable salt, stereoisomer, solvate, polymorph, tautomer, isotope compound, metabolite or prodrug thereof, and the use thereof in the preparation of drugs for preventing or treating lipid metabolism-related diseases.

The present invention provides an antisense nucleic acid medicine that can modulate expression of a target transcriptional product in an ischemic site of a subject. The present invention also provides a composition for modulating expression of a target transcriptional product in an ischemic site of a subject, having a nucleic acid complex formed by annealing together a first nucleic acid strand having an antisense oligonucleotide region with respect to the target transcriptional product, and a lipid-conjugated second nucleic acid strand having a complementary region that is complementary to at least part of the first nucleic acid strand.

The invention relates to a therapeutic combination for use as a medicament, wherein the therapeutic combination comprises: (a) a first pharmaceutical composition comprising a first proteinaceous molecule and at least one saponin covalently bound to said first proteinaceous molecule; and (b) a second pharmaceutical composition comprising a second proteinaceous molecule, comprising an effector moiety, wherein the binding site of the first proteinaceous molecule and the binding site of the second proteinaceous molecule are the same. The invention also relates to the first pharmaceutical composition for use as a medicament. The invention also relates to the first pharmaceutical composition, further comprising the second proteinaceous molecule. The invention also relates to the first pharmaceutical composition, further comprising the second proteinaceous molecule, for use as a medicament. Furthermore, the invention relates to the first pharmaceutical composition, further comprising the second proteinaceous molecule, for use in the treatment or prophylaxis of cancer in a patient in need thereof.