Patent classifications
C08G83/004
MACROMOLECULES
A macromolecule includes i) a dendrimer comprising a core and at least one generation of building units, the outermost generation of building units having surface amino groups wherein at least two different terminal groups are covalently attached to the surface amino groups of the dendrimer, ii) a first terminal group which is a residue of a pharmaceutically active agent comprising a hydroxyl group, and iii) a second terminal group which is a pharmacokinetic modifying agent. The pharmaceutically active agent is cabazitaxel. The first terminal group is covalently attached to the surface amino group of the dendrimer through a diacid linker, the diacid linker comprising an alkyl chain interrupted by one or more oxygen, sulfur or nitrogen atoms, or a pharmaceutically acceptable salt thereof.
A CATION POLYMER CAPABLE OF REMOVING POSITIVE CHARGES THROUGH OXIDATIVE RESPONSE, A PREPARATION METHOD AND APPLICATION
Disclosed are the cation polymers capable of removing their positive charges in oxidative conditions, preparation methods, and applications as gene delivery carriers. The oxidation-responsive unit is the p-(boronic acid or ester)benzylammonium, which upon oxidation eliminates p-hydroxymethlphenol and thus converts in a tertiary amine. Compared with the prior art, different from a common quaternary amination carrier, the synthesized charge reversal type gene delivery carrier for oxidative response of the present invention has a large quantity of positive charges and can well coat a DNA, but the positive charges can be removed under the condition of intracellular oxidation when the charge reversal type gene delivery carrier enters a cell, a charge reverse is triggered, the positive charges turn to negative charges, and the DNA is quickly released for transfection. The carrier is efficient, low in toxicity, and good in application prospect.
Phosphorylated dendrimers as antiinflammatory drugs
Dendrimers with monophosphonic or bisphosphonic terminations for the treatment of inflammatory diseases.
DENDRIMERS FOR GENOMIC ANALYSIS METHODS AND COMPOSITIONS
Provided herein are methods and compositions for nucleic acid processing comprising obtaining a stabilized sample comprising a nucleic acid molecule complexed to at least one nucleic acid binding protein; contacting said stabilized sample to a dendrimer comprising a plurality of nucleic acid binding moieties such that said nucleic acid molecule forms a complex with said plurality of nucleic acid binding moieties; contacting said complex to an endonuclease to cleave said nucleic acid molecule between contact points of said nucleic acid molecule and said plurality of nucleic acid binding moieties creating a plurality of fragments of said nucleic acid molecule each complexed with a nucleic acid binding moiety of said plurality of said nucleic acid binding moieties; isolating said product using an agent that binds to said dendrimer; joining said plurality of fragments to each other to create a concatemer comprising each of said plurality of fragments of said nucleic acid molecule; and isolating said concatemer from said dendrimer.
MACROMOLECULES
A macromolecule includes i) a dendrimer comprising a core and at least one generation of building units, the outermost generation of building units having surface amino groups wherein at least two different terminal groups are covalently attached to the surface amino groups of the dendrimer, ii) a first terminal group which is a residue of a pharmaceutically active agent comprising a hydroxyl group, and iii) a second terminal group which is a pharmacokinetic modifying agent. The pharmaceutically active agent is cabazitaxel. The first terminal group is covalently attached to the surface amino group of the dendrimer through a diacid linker, the diacid linker comprising an alkyl chain interrupted by one or more oxygen, sulfur or nitrogen atoms, or a pharmaceutically acceptable salt thereof.
THERAPEUTIC CONJUGATES
Provided herein is dendrimer-targeting agent conjugate comprising: (a) a dendrimer comprising i) a core unit (C); and ii) building units (BU), wherein the dendrimer has from two to six generations of building units; and wherein the core unit is covalently attached to at least two building units; and the dendrimer further comprising: b) a targeting agent which is covalently linked to the dendrimer by a spacer group; c) one or more first terminal groups attached to an outermost building unit of the dendrimer, wherein the first terminal group comprises a complexation group for complexing a radionuclide; and d) one or more second terminal groups attached to an outermost building unit of the dendrimer, wherein the second terminal group comprises a pharmacokinetic-modifying moiety, or a salt thereof. Also provided are compositions comprising the dendrimer-targeting agent conjugates, and methods of using the dendrimer-targeting agent conjugates and compositions comprising them in therapeutic and imaging applications.
Thiourea-containing dendrimer and thiourea-containing hyperbranched polymer as well as preparation methods thereof and applications thereof
The present invention discloses thiourea-containing dendrimers and thiourea-containing hyperbranched polymers, and respectively a preparation method for the thiourea-containing dendrimer and a preparation method for the thiourea-containing hyperbranched polymer, and a thiourea-containing dendrimer and a thiourea-containing hyperbranched polymer having increased water solubility prepared by using the thiourea-containing dendrimer and the thiourea-containing hyperbranched polymer as raw materials. Finally, disclosed are applications of the thiourea-containing dendrimers and the thiourea-containing hyperbranched polymers in the preparation of antitumor and antimicrobial drugs. The thiourea-containing dendrimer and the thiourea-containing hyperbranched polymer have a significant growth inhibitive effect on solid tumors and low toxicity to normal tissues, and thus can be used for preparing drugs for treating malignant tumors. The thiourea-containing dendrimer and the thiourea-containing hyperbranched polymer also have a good antimicrobial effect on various bacterial strains and thus can be used for preparing antiviral or antibacterial drugs.
FUCAN-DENDRIMER BASED COMPOUNDS AND COMPLEXES
Compositions, systems, methods, etc., related to fucan-dendrimer complexes wherein a fucan molecule is linked or otherwise attached to a dendrimer. For example, the current compositions can comprise fucan covalently linked, conjugated, attached, tagged, adducted, bound, etc., to a dendrimer. These fucan-dendrimer complexes include fucan-hyperbranched polyglycerol, fucan-hyperbranched poly(glycerol ester), fucan-hyperbranched poly(1,3-diether), fucan-poly(3-ethyl-3-(hydroxymethyl)oxetane), fucan-hyperbranched polyesters, fucan-hyperbranched polyethylene, fucan-hyperbranched polystyrene, fucan-hyperbranched poly(urea-urethanes), fucan-hyperbranched polyethyleneimine, fucan-hyperbranched poly(amido amine)s, fucan-hyperbranched polyphosphates, fucan-hyperbranched polypeptides, fucan-hyperbranched polysaccharides, fucan-hyperbranched polyacrylates and fucan-hyperbranched beta-cyclodextrin. These fucan-dendrimer complexes may be used in medically and/or pharmaceutically effective compositions, for a plurality of applications, including the treatment of fibrous adhesions. In some embodiments, the fucan is fucoidan.
Transdermal Drug Delivery Using Amphiphilic Dendron-Coil Micelles
The invention generally relates to the field of drug delivery. In particular, the invention relates to amphiphilic dendron-coils, micelles thereof and their use for the transdermal delivery of drugs.
Dendritic polymer heavy metal precipitant with double functions of chelation and self-flocculation and its application
Dendritic polymer heavy metal precipitant with double functions of chelation and self-flocculation and its application is provided. The heavy metal precipitant is dithiocarbamates end group polyamidoamine dendritic polymer prepared by reaction of carbon bisulfide and polyamidoamine dendritic polymer with a generation at a range of 1-3 (denoted as PAMAM-(NH2).sub.8G, wherein G is generation number). Due to the special three dimensional spatial structure, appropriate molecular weight, high density of the end chelating group dithiocarbamates, the dithiocarbamates end group polyamidoamine dendritic polymer of the present invention not only has strong chelating performance with the heavy metal iron, the sediment floc formed has a large volume, a fast sedimentation velocity and easy separation. The present invention has high efficiency performance in chelating and flocculating heavy metals.