67 results about "Dithiolane" patented technology

The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.

Cosmetic/sunscreen compositions contain a combination of at least one dibenzoylmethane sunscreen compound and a photostabilizing amount of at least one dithiolane compound of formula (I) below:

The thiol modified oligonucleotides have vast number of applications in the field of nucleic acid chemistry. The conjugates generated by mono thiol groups are unstable at higher temperature, in high salt concentration buffers and in presence other thiols. There is strong need to develop a novel thiol modifier probes that can generate multiple thiol groups. Described herein are efficient processes and compounds, dithiolane phosphoramidites derivative and dithiolane succinyl supports. The advantage of our cyclic disulfide thiol modifier is multifold a) each incorporation introduces two thiol groups; b) it can be introduced at any desired site of oligonucleotides; c) The symmetrical branching nature of the spacer in the linker arm of dithiolane allows for clean oligo synthesis, where cleavage of the linker arm and thereby of loss of oligo chain is prevented. We have successfully made 20-mer oligonucleotide containing single dithiolane derivative at 3′, and 21-mer oligonucleotides containing single dithiolane derivative at 5′ or in the middle of the mixed base sequence. HPLC and ESI MS analysis of these oligonucleotides indicated satisfactory purity and correct composition of these oligos, respectively.

The invention discloses a reversibly crosslinked biodegradable polymersome with an asymmetric membrane structure as well as a preparation method and application thereof to nucleic acid medicines. The polymersome and the preparation method have the advantages that a triblock polymer PEG-P(TMC-DTC)-PEI or PEG-P(DLLA-DTC)-PEI is synthesized and is self-assembled and self-crosslinked to obtain the polymersome with the asymmetric membrane structure or the triblock polymer is linked with a targeting molecule and is self-assembled to obtain targeting RCCPs; the inner shell of the polymersome is PEI and is used for compounding and loading nucleic acid through electrostatic interaction; a membrane is reversibly crosslinked biodegradable polyester/polycarbonate with good biocompatibility; dithiolane of a side chain is similar to a human body natural antioxidant lipoic acid; the outer shell of the polymersome takes PEG as the background and can target cancer cells; by studying that the carrier is compounded with functional siRNA and studying the gene silencing effects in vitro and vivo, in vivo blood circulation and bio-distribution, the condition of treating lung cancer in situ bearing mice and toxic and side effects of the polymersome, the polymersome is expected to become a nanosystem platform integrating the advantages of simplicity, stability, multifunction, and the like and is used for carrying out efficient and active targeting delivery on siRNA to tumors in situ.

The invention discloses a preparation method of a crosslinked nanodrug based on an active reaction type one-step method. The preparation method specifically comprises the following step: adding a polymer and a drug with sulfydryl into a solution to be mixed to dialyze to obtain a crosslinked nanodrug, wherein the side chain of the polymer contains a dithiolane structure. The circularly stable nanodrug can be obtained by simple preparation, so that the defects that in the prior art, a chemically bonded nanodrug is complex to prepare and needs a catalyst and the like are overcome. The product prepared by the invention has a stable crosslinking structure and avoids the problem that an existing chemically bonded nanodrug is not crosslinked; and on a B16F10 melanoma-loading model, the nanodrug shows a good curative effect, and the tumor inhibition rate exceeds 90%. The active targeted crosslinked nanodrug has a huge potential application in the field of cancer chemotherapy.

Dithiolane compounds having the structural formula (I):

are useful for reinforcing and/or preserving the natural antioxidant protection of the skin against oxidative stress caused, especially, by UV radiation, e.g., by increasing the level of intracellular glutathione.

The present invention relates to a solid composition comprising a substance that improves the availability of nitric oxide, such as a nitric oxide donor or a biosynthetic nitric oxide precursor thereof or a direct or indirect nitric oxide potentiating agent, wherein arginine is the preferred compound, and combined with dithiolane, wherein the dithiolane and α-lipoic acid are the preferred compound, and this composition can be used to improve sexual function. The composition according to the invention comprises a nitric oxide donor or a precursor thereof in excess, based on the molar amount of the constituents. This composition is also suitable for improving sexual function. In particular, the present invention relates to the use of dithiolane in combination with nitric oxide donors or their precursors as a pharmaceutical treatment for sexual dysfunction.

The invention discloses a vesicle nano-drug loaded with a chloroquine compound as well as a preparation method and application of the vesicle nano-drug. The vesicle nano-drug loaded with the chloroquine compound is prepared by taking a polymer and a chloroquine compound as raw materials, wherein the polymer comprises a hydrophilic chain segment and a hydrophobic chain segment; a side chain of the hydrophobic chain segment is dithiolane containing a disulfide bond. According to the vesicle nano-drug loaded with the chloroquine compound disclosed by the invention, a safe and efficient macrophage-targeted nano-drug is researched and developed for treating rheumatoid arthritis; polymer vesicles are designed for efficiently loading, carrying out targeted delivery and controlling to release drug hydroxychloroquine or chloroquine, so that the enrichment of the drug in cytoplasm is improved; M1M is re-polarized to M2M, so that secretion of proinflammatory cytokines is reduced and secretion of anti-inflammatory cytokines is increased; and the drug can be used for inhibiting DC activation and also can be used for removing ROS and enriching in inflammatory joints. In-vitro and in-vivo experiment results prove that the vesicle nano-drug loaded with the chloroquine compound can be used for carrying out targeted treatment on the rheumatoid arthritis.

The invention provides a benzoxazole linked triphenylimidazole polymer. The polymer is prepared by the following preparation steps: firstly, performing thioacetal protection on terephthalaldehyde, performing a benzoin condensation reaction, performing oxidation to obtain 4,4-di(1,3-dithiolane)bibenzoyl, performing imidazole ring formation, and performing deprotection to obtain 2,4,5-tris(4-formylphenyl)-1H-imidazole; and performing a reaction on the 2,4,5-tris(4-formylphenyl)-1H-imidazole and 1,7-diamine-6H,12H-5,11-dimethylbenzo[1,5]diaza-1,8-diol to obtain the benzoxazole linked triphenylimidazole polymer. The polymer provided by the invention is a solid adsorbent which is easy to prepare, and has low costs and a good adsorption effect, and the gas adsorption capacity is enhanced by enlargement of the specific surface area of the polymer.

The invention relates to 1,3-dithiolane derivatives, synthesis, a nano structure, an activity, and an application thereof as a lead dispelling agent. The invention discloses 16 1,3-dithiolane derivatives represented by the formula Ia-p, wherein in the formula the R1 represents 4-chlorophenyl, 4-methoxylphenyl, phenyl, 4-isopropylphenyl, 2,6-dimethoxylphenyl, 3,5-dimethoxylphenyl, or 2,4,6-trimethoxylphenyl, and the R2 represents CO2CH3 or CH2OH; and also discloses preparation, a nano structure, and a lead removing activity of the derivatives. So the 1,3-dithiolane derivatives are advantageously used as a lead dispelling agent in clinic.

Compositions of the invention comprise 1,2-dithiolane, dithiol and related compounds useful as therapeutic agents for the treatment and prevention of diseases and conditions associated with aberrant EGFR activity.

This invention is related to nucleic acid chemistry and describes novel 1,2-dithiolane functionalized nucleoside phosphoramidites (1, Chart 1) and corresponding solid supports (2, Chart 1). In addition to these derivatives, 1,2-dithiolane moiety can also be functionalized to at the various positions of the nucleobase and sugar part as shown in Schemes 1 to 8. The nucleosides of our invention carry a primary hydroxyl for DMTr (4,4′-dimethoxytrityl) function for chain elongation. Furthermore, the phosphoramidite function is attached at the 3′-hydroxyl of the nucleoside. This allows oligonucleotide chain extension under standard DNA and RNA synthesis chemistry conditions and techniques, thus leading to high quality oligonucleotides. These derivatives are useful for introduction of reactive thiol groups either at 3′- or 5′-end of the oligonucleotides on the solid supports such as gold, silver and quantum dots.