摘要:
A bioerodible polymer - bioactive agent conjugate comprising as part of its polymer backbone a moiety of general formula (I) wherein: A and B, which may be the same or different, represent the remainder of the polymer backbone and are (i) attached to the -O-R(ZD)-O- moiety as shown in formula (I) via a bioerodible moiety, and (ii) each formed from monomeric units that are coupled via a bioerodible moiety; R represents a linear or branched optionally substituted hydrocarbon; Z is a linking group; and D is a releasable bioactive agent.
摘要:
Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
摘要:
Modular dendrimers with cationic groups and lipophilic groups are provided herein. In some aspects, the dendrimers provided herein may be formulated in compositions which contain a nucleic acid and one or more helper excipients. In some aspects, these compositions may also be used to treat diseases or disorders with a therapeutic nucleic acid.
摘要:
The present invention relates to polydixylitol polymer based gene transporter (PdXYP) and a preparation method thereof. Further, the present invention relates to a nucleic acid delivery complex where the nucleic acids for treatment are conjugated to the gene transporter and a pharmaceutical composition for gene therapy including the complex as an active ingredient. In addition, the present invention relates to the gene transporter, gene delivery complex, and gene therapy using the gene transporter and gene delivery complex. It was confirmed that the PdXYP of the present invention has a considerably higher nucleic acid delivery rate than existing gene transporters, has almost no cytotoxicity in the conjugate when conjugated with DNA, also has very high in vivo transfection efficiency, and above all, especially has considerably high transfection efficiency for brain tissues, which has involved difficulty in gene therapy due to the blood brain barrier for a while. Accordingly, the gene transporter of the present invention can not only be used as experimental gene transporters, but can also be broadly used for various tissues in the body based on the nucleic acids for treatment to be conjugated in the field of gene therapy regarding various diseases.
摘要:
A method fits reversing immune suppression or immune exhaustion or for treating a disease associated with immune suppression includes: administering a co position to a subject in need of such treatments wherein the composition contains a CD11b modulator that binds specifically to CD11b on a cell to inhibit PD-L1 expression. The CD11b modulator is an antibody or an antigen-binding portion thereof, or a compound as described.
摘要:
In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.
摘要:
The present invention relates to novel compositions of therapeutic cyclodextrin containing polymeric compounds designed as a carrier for small molecule therapeutics delivery and pharmaceutical compositions thereof. These cyclodextrin-containing polymers improve drug stability and solubility, and reduce toxicity of the small molecule therapeutic when used in vivo. Furthermore, by selecting from a variety of linker groups and targeting ligands the polymers present methods for controlled delivery of the therapeutic agents. The invention also relates to methods of treating subjects with the therapeutic compositions described herein. The invention further relates to methods for conducting pharmaceutical business comprising manufacturing, licensing, or distribution kits containing or relating to the polymeric compounds described herein. The therapeutic agents, e.g. camptothecin, are chemically attached to the cyclodextrin-containing polymer.
摘要:
A method for production of a uniform polymer of high molar mass is provides, the method comprising: (a) polymerizing cyclic imino ether monomer in a first reaction mixture by cationic ring opening polymerization to produce a polymerized first reaction mixture containing (i) polymerized material and (ii) solvent and/or unreacted cyclic imino ether monomer; (b) separating solvent and/or unreacted cyclic imino ether monomer from polymerized material contained in the polymerized first reaction mixture; (c) copolyerizing by cationic ring opening polymerization a second liquid reaction mixture containing cyclic imino ether monomer and solvent by combining the separated unreacted cyclic imino ether monomer and/or the separated solvent with other components. Also disclosed are polyoxazoline polymers comprising at least 50 wt. % of repeating units derived from a 2-substituted 2-oxazoline monomer selected from 2-methyl-2-oxazoline, 2-ethyl-2-oxazoline, 2-n-propyl-2-oxazoline, 2-i-propyl-2-oxazoline and combinations thereof, said polymer having a DP of at least 250 and a very low dispersity.