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39results about How to "Increase the maximum tolerated dose" patented technology

Specific target polypeptide self-assembled nano-carrier, drug-carrying nanoparticle and preparation method

The invention relates to the technical field of biology and in particular relates to a specific target polypeptide self-assembled nanoparticle. The nanoparticle is prepared from a hydrophobic anti-tumor drug with a therapeutic dosage and an amphipathic polypeptide which covers the periphery of the hydrophobic anti-tumor drug through a self-assembling manner, wherein the amphipathic polypeptide is a target peptide which can be used for specifically targeting a epidermal growth factor receptor of a tumor cell; a terminal N of the target peptide is coupled with a hydrophobic functional molecule. After the nanoparticle targets the tumor cell, the target peptide is exposed; the nanoparticle targets the tumor cell and enters the tumor cell through receptor-mediated endocytosis, and the drug is released to inhibit DNA (Deoxyribonucleic Acid) synthesis and repairing; the nanoparticle has dual killing effects on the tumor cells and the growth of the tumor cell is inhibited. The amphipathic polypeptide does not generate a covalent bond in a self-assembling process and no reverse reaction is caused; the specific target polypeptide self-assembled nanoparticle is used for treating tumors and has the advantages of no toxin and good biocompatibility.
Owner:THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA

Active targeting type amphipathic polypeptide nano-drug carrier and preparation and application thereof

The invention provides an active targeting type amphipathic polypeptide nano-drug carrier and preparation and application thereof, and belongs to the technical field of biological medicines. According to an amphipathic polypeptide, an alkyl chain serves as the hydrophobic end, a polypeptide chain with active targeting functional and side chain modification fluorescent functional molecules serves as the hydrophilic end, and an anti-tumor drug is wrapped in a hydrophobic cavity of a micelle formed by self-assembling the amphipathic polypeptide. The nano-carrier can actively target tumor cells and enter the tumor cells through receptor-mediated endocytosis, the amphipathic polypeptide and phospholipid molecules have strong interaction, and the phagocytosis of a nano-drug by tumor cells is promoted. In the process, tracing can be conducted through fluorescent imaging of fluorescent functional molecules modified on the polypeptide chain, and the tumor imaging aim is realized. Finally, the anti-tumor drug is slowly released to kill tumor cells and restrain the growth of tumors. The amphipathic polypeptide nano-carrier is free of toxin, high in biocompatibility and remarkable in anti-tumor efficiency, and the tumor diagnosis and treatment can be integrated.
Owner:HUAZHONG UNIV OF SCI & TECH

Medical use of 7-hydroxy-butylphthalide

The invention belongs to the technical field of pharmaceutical chemistry and particularly relates to medical use of 7-hydroxy-butylphthalide in preparation of drugs for preventing and / or treating cardiac and cerebral vascular diseases.
Owner:NCPC NEW DRUG RES & DEV

Panax notoginseng saponin composition and preparation method and application thereof

The invention provides a panax notoginseng saponin composition and a preparation method and application thereof.The composition is prepared from, by weight, 30-50% of ginsenoside Rg1, 25-40% of ginsenoside Rb1, 7-16% of notoginsenoside R1, 2.7-8% of ginsenoside Re, 0.5-7.0% of ginsenoside Rd, 0.5-2% of ginsenoside Rf, 0.3-2.0% of ginsenoside Rh2, 1-3% of ginsenoside Rc, 0.3-2.5% of ginsenoside Rb3 and 0.5-2.5% of ginsenoside Rg3, wherein ginsenoside Rg1, ginsenoside Rb1 and notoginsenoside R1 account for 70-95% of the total weight of the active components, and the sum of the contents of ginsenoside Rb1 and notoginsenoside R1 is not smaller than 8 times of the content of ginsenoside Rd.Compared with commercially available Xueshuantong injections and Xueshuantong preparations, the panax notoginseng saponin composition has a more obvious arterial and venous thrombosis resistant effect, low toxicity and high safety.
Owner:HARBIN ZHENBAO PHARMA

Compositions for the treatment of metabolic disorders

InactiveUS20080096915A1Reduce impactLess-pronounced potassium-lowering effectBiocideSenses disorderPrevention complicationsDisease cause
Preferred embodiments of the present invention are related to novel therapeutic drugs and drug combinations, and associated methods, for treating and / or preventing complications or otherwise treating disease in patients with hypertension, diabetes, metabolic syndrome, obesity and / or other metabolic disorders.
Owner:GILEAD SCI INC

Pharmaceutical composition and preparation method thereof

The invention provides a pharmaceutical composition. The pharmaceutical composition comprises the following components: ginsenoside Rb1, ginsenoside Rg1, notoginsenoside R1, ginsenoside Rd, ginsenoside Re, ginsenoside Rf, ginsenoside Rc, ginsenoside Rh1, ginsenoside Rb2 and ginsenoside Rg3. The invention further provides a preparation method of the pharmaceutical composition. The pharmaceutical composition disclosed by the invention has clear components, stable quality, good controllability, acute toxicity, undue toxicity and hemolysis in comparison with panax notoginseng saponins in the prior art. Test results indicate that the pharmaceutical composition disclosed by the invention has high safety and wide clinical application prospect.
Owner:KPC PHARM INC

Preparation of stabilizing brain for curing apoplexy and migraine and producing method

A Chinese medicine for treating apoplexy and hemicrania is prepared from Chuan-xiong rhizome, Chinese angelica root, ginseng safflower and borneol. Its preparing process is also disclosed. Its advantages are low dosage and high curative effect.
Owner:安徽雷允上药业有限公司

Active targeting type amphiphilic polypeptide composite nano-micelle prodrug as well as preparation and application thereof

The invention discloses an active targeting type amphiphilic polypeptide composite nano-micelle prodrug as well as preparation and application thereof, and belongs to the technical field of biological medicines. The composite nano-micelle prodrug is obtained by co-assembling a first polypeptide with negative charges and a second polypeptide with positive charges through electrostatic interaction and hydrophilic and hydrophobic effects; the first polypeptide is Lys-AAm-Gly-Arg-Gly-Asp-Ser, wherein AA is aspartic acid or glutamic acid, and m is 1, 2, 3 or 4; the second polypeptide is Cys-BBn, wherein BB is lysine, arginine or histidine, and n is 1, 2, 3 or 4; amino at a N end of the first polypeptide is connected with a hydrophobic alkyl chain, and amino at a lysine side chain of the first polypeptide is connected with a fluorescent molecule; cysteine in the second polypeptide is covalently linked with an anti-tumor drug through sulfydryl. The nano-composite micelle can be actively targeted to tumor cells, and is disassembled after responding to a tumor slightly acidic environment to form a small-size micelle with a size of 20-30 nm, so that deep delivery of the polypeptide anti-tumor prodrug at a tumor part is facilitated.
Owner:HUAZHONG UNIV OF SCI & TECH

Method of Treating a Tumor and Biodistribution of a Drug Delivered by Worm-Like Filomicelles

Provided are filomicelle nanocarrier systems for the controlled transport and bioselective delivery of encapsulatable, cytotoxic active agents contained therein, particularly anticancer agents. Further provided are methods for controlling destabilization of the filomicelle membrane and the resulting hydrolysis-triggered, controlled release of the active agent(s) encapsulated therein by controlling the blend ratio (mol %) of hydrolysable PEO-block copolymer of the hydrophilic component(s) and of the more hydrophobic PEO-block copolymer component(s), wherein bioselective release of the encapsulated cytotoxic agents is distributed intracellularly, and wherein lowered dosage of the drug was delivered to the non-tumor organs. Thus, the filomicelle system offers enhanced tumor-selective biodistribution of a drug, and a reduced toxicity of the encapsulated drug to other organs.
Owner:THE TRUSTEES OF THE UNIV OF PENNSYLVANIA

Tetravalent platinum naphthalimide complex, preparation method and application thereof

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a tetravalent platinum naphthalimide complex, a preparation method and application thereof. The tetravalent platinum naphthalimide complex has good anti-tumor activity, which is better than that of cis-platinum and oxaliplatin, and the tetravalent platinum naphthalimide complex has better stability than bivalent platinum like cis-platinum, carboplatin and oxaliplatin. According to the invention, the naphthalimide modified tetravalent platinum has good targeting performance on tumor cells, high selectivity on tumor cells is improved, and different from a classic divalent platinum drug, the complex provided by the invention regulates and controls subcellular organelles and cell nucleus functionsto reverse drug resistance by targeting a tumor high polyamine microenvironment, and relieves immunosuppression of T cells around tumors at the same time. The complex provided by the invention also solves the problems of poor solubility, tedious clinical compatibility, poor patient immunity in clinical application of chemotherapeutic drugs and the like of previous bivalent platinum antitumor drugs, and has good fat solubility and water solubility.
Owner:HENAN UNIVERSITY

Acid-addition salt of Prasugrel, preparation method and application

The invention discloses an acid-addition salt of Prasugrel, a preparation method and an application. The preparation method comprises the following steps: respectively adding Prasugrel and hydroxyl substituted benzenesulfonic acid in an organic solvent, stirring and dissolving to obtain a settled solution, reacting under certain temperature, concentrating, standing, precipitating crystals, and filtrating to obtain the acid-addition salt of Prasugrel. Compared with Prasugrel, the acid-addition salt of Prasugrel provided by the invention has good stability, the preparation method is simple and easy to be carried out, a single crystal with high purity and a crystal form suitable for drug use can be obtained, the product quality is good, and the yield is high.
Owner:SICHUAN HAISCO PHARMA CO LTD

Reduction-responding polyethylene glycol-polycarbonate targeting maytansine prodrug micelle and preparation method and application thereof

The invention discloses reduction-responding polyethylene glycol-polycarbonate targeting maytansine prodrug micelle and a preparation method and application thereof. The reduction-responding polyethylene glycol-polycarbonate maytansine prodrug micelle is made by the self-assembly of amphiphilic polyethylene glycol-polycarbonate maytansine prodrug polymer and amphiphilic polyethylene glycol-polycarbonate maytansine prodrug micelle with targeting molecules bonded at its tail end, in a buffer solution; the micelle is 30-150 nanometers in particle size and 2-60% by weight in maytansine loading capacity. The reduction-responding polyethylene glycol-polycarbonate targeting maytansine prodrug micelle provided herein has good targeting property, amphiphilicity and biodegradability and may be prepared into nano drugs, it is possible to significantly improve drug water-solubility, enhance drug stability during cycling, improve pharmacokinetic behavior of the drugs and improve bioavailability of the drugs; the micelle is applicable to the preparation of targeting drugs for treating malignant tumors, such as melanoma.
Owner:SUZHOU UNIV

A kind of notoginseng total saponins composition and its preparation method and application

The invention provides a panax notoginseng total saponin composition and a preparation method and application thereof. The Panax notoginseng saponin composition provided by the invention contains 30-50% of ginsenoside Rg1, 25-40% of ginsenoside Rb, 7-16% of notoginsenoside R1, 2.7-8% of ginsenoside Re, Saponin Rd 0.5-7.0%, ginsenoside Rf 0.5-2%, ginsenoside Rh2 0.3-2.0, ginsenoside Rc 1-3, ginsenoside Rb3 0.3-2.5 and ginsenoside Rg 30.5-2.5%; Ginsenoside Rb1 and Panax notoginsenoside R1 account for 70-95% of the total weight of the active ingredients, and the sum of the content of ginsenoside Rb1 and notoginsenoside R1 is not less than 8 times the content of ginsenoside Rd. Compared with the commercially available Xueshuantong and Xuesaitong preparations, the Panax notoginseng saponin composition provided by the invention has more obvious anti-arteriovenous thrombosis effect and low toxicity and safety.
Owner:HARBIN ZHENBAO PHARMA

Propionamide derivative and application for schizophrenia

The invention belongs to the field of medicines, and particularly relates to a propionamide derivative and application thereof in schizophrenia. The propionamide derivative is CY150112-9, and tests show that the in-vitro affinity of the propionamide derivative is similar to that of CY150112. The CY150112-9 has high affinity with 5-HT2A and D2 receptors, the affinity with 5-HT2A is higher than thatof D2 receptors, it is speculated that the CY150112-9 has a certain effect on negative symptoms while positive symptoms are improved, and the CY150112-9 has a low extrapyramidal side reaction. CY150112-9 also has certain affinity to D3 and 5-HT7, and it is speculated that CY150112-9 may have the effect of improving cognition clinically. And the maximum tolerance of CY150112-9 is higher than 112.
Owner:NHWA PHARMA CORPORATION

Cabazitaxel-oligo/polylactic acid conjugated prodrug, preparation, preparation method and application thereof

The invention discloses a cabazitaxel oligo / polylactic acid coupled prodrug and a preparation method thereof. The preparation method is characterized in that cabazitaxel and oligo / polylactic acid undergo an esterification reaction under the action of a condensing agent and a catalyst to obtain the cabazitaxel oligo / polylactic acid coupled prodrug. The invention also discloses a cabazitaxel-oligo / polylactic acid coupled prodrug preparation, and a preparation method and an application thereof. The oligo / polylactic acid is covalently coupled with cabazitaxel, so the in vivo release rate of cabazitaxel is can be regulated, the precipitation of cabazitaxel, caused by strong release, is prevented, the in vivo cycle period of the cabazitaxel is prolonged, and the maximum tolerable dose is increased. The oligo / polylactic acid is approved for use by the US FDA and has an excellent application prospect. The cabazitaxel oligo / polylactic acid prodrug and an amphiphilic polymer PEG5k-PLA8k are assembled to form nanoparticles, and the nanoparticles have a passive targeting effect, and are easily retained in the tumor site by the EPR effect in order to greatly reduce the toxic and side effects ofthe drug on normal tissues.
Owner:ZHEJIANG UNIV

A kind of tetravalent platinum polyamine complex, its preparation method and application

The invention belongs to the technical field of pharmaceutical chemistry, in particular to tetravalent platinum polyamine complexes, a preparation method and application thereof. The aim of the invention is to provide a tetravalent platinum antitumor drug modified by a polyamine with high stability and high targeting and the preparation method thereof so as to overcome shortcomings existing in theprior art. The synthesized compounds have good antitumor activity, the anti-tumor activity is better than that of cisplatin and oxaliplatin, and the stability is better than that of bivalent platinumsuch as cisplatin, carboplatin, oxaliplatin and the like. The cancer cell targeting of the polyamine modified tetravalent platinum is relatively good, and the high selectivity of cancer cells is improved. The compounds solve the existing problems that divalent platinum antitumor drugs have poor solubility and complicated clinical compatibility, and the compounds have relatively good liposolubility and water solubility.
Owner:HENAN UNIVERSITY

Reduction-responsive targeted polyethylene glycol-polycarbonate maytansinoid prodrug micelles, its preparation method and application

The invention discloses a reduction-responsive targeted polyethylene glycol-polycarbonate maytansine prodrug micelle, a preparation method and application thereof. The amphiphilic polyethylene glycol-polycarbonate maytansinoid prodrug polymer composed of amphiphilic polyethylene glycol-polycarbonate maytansinoid prodrug polymer and the terminal-bonded targeting molecule were automatically activated in buffer. Targeted polyethylene glycol-polycarbonate maytansine prodrug micelles with reduction response were assembled; the particle size of the micelles was 30-150 nanometers, and the drug-loading capacity of maytansine was 2-60 wt .%. The reduction-responsive targeted polycarbonate maytansinoid prodrug micelles provided by the present invention have targeting properties, amphiphilicity and biodegradability, and nano-medicines can be prepared therefrom, which can significantly improve the water-solubility of drugs and enhance drug Stability in circulation process, improvement of drug pharmacokinetic behavior and improvement of drug bioavailability; it can be applied in the preparation of malignant tumors such as targeted therapy drugs for melanoma.
Owner:SUZHOU UNIV

Tetravalent platinum glycosyl complex for tumor treatment and preparation method thereof

The invention provides a quadrivalent-platinum glycosyl complex for treating tumors and a preparation method thereof. The synthesized compound has good anti-tumor activity better than that of cisplatin and oxaliplatin, and has better stability than that of bivalent platinums such as cisplatin, carboplatin and oxaliplatin. In addition, since the quadrivalent platinum with galactosylated modification has better targeting for tumor cells, the high selectivity to the tumor cells is improved. Furthermore, the compound provided by the invention has the advantages that the problems of poor solubility and more troublesome clinical compatibility of the original bivalent-platinum anti-tumor medicine are solved, and both fat solubility and water solubility are better. The quadrivalent-platinum glycosyl derivative not only can improve the in-vivo availability and enhance the curative effect, but also can reduce the toxic and side effects of the original bivalent-platinum medicine on the kidney and the like.
Owner:NANKAI UNIV

Application of Tilorone in prevention/treatment of African swine fever virus infection

The invention relates to the technical field of medicines, in particular to application of Tilorone to prevention / treatment of African swine fever virus infection. The invention relates to application of telolone and salt forms, hydrates, solvates and isotope substitutes thereof in preparation of drugs for preventing or treating African swine fever viruses. The invention has the following advantages: (1) the bioavailability is high, and the half-life period is long; and (2) the maximum tolerance dose is high, the selectivity coefficient is high, and the safety is high. And (3) the activity of preventing / resisting African swine fever virus infection is strong. And (4) the drug delivery modes are multiple, and the application range is wide. And (5) the composition can be combined for use and has a good effect of preventing / treating African swine fever virus infection.
Owner:HARBIN VETERINARY RES INST CHINESE ACADEMY OF AGRI SCI +1

Cabazitaxel-oligo/polylactic acid coupled prodrug, preparation thereof, preparation method and application of preparation

The invention discloses a cabazitaxel oligo / polylactic acid coupled prodrug and a preparation method thereof. The preparation method is characterized in that cabazitaxel and oligo / polylactic acid undergo an esterification reaction under the action of a condensing agent and a catalyst to obtain the cabazitaxel oligo / polylactic acid coupled prodrug. The invention also discloses a cabazitaxel-oligo / polylactic acid coupled prodrug preparation, and a preparation method and an application thereof. The oligo / polylactic acid is covalently coupled with cabazitaxel, so the in vivo release rate of cabazitaxel is can be regulated, the precipitation of cabazitaxel, caused by strong release, is prevented, the in vivo cycle period of the cabazitaxel is prolonged, and the maximum tolerable dose is increased. The oligo / polylactic acid is approved for use by the US FDA and has an excellent application prospect. The cabazitaxel oligo / polylactic acid prodrug and an amphiphilic polymer PEG5k-PLA8k are assembled to form nanoparticles, and the nanoparticles have a passive targeting effect, and are easily retained in the tumor site by the EPR effect in order to greatly reduce the toxic and side effects ofthe drug on normal tissues.
Owner:ZHEJIANG UNIV

Specific targeting polypeptide self-assembled nanocarrier, drug-loaded nanoparticle and preparation method

The present invention relates to the field of biotechnology, in particular to a specific targeting polypeptide self-assembled nanoparticle, the nanoparticle comprises a therapeutic amount of a hydrophobic antitumor drug, and two self-assembly methods wrapped around the hydrophobic antitumor drug. An affinity polypeptide, the amphiphilic polypeptide is a targeting peptide that can specifically target tumor cell epidermal growth factor receptor, and the N-terminus of the targeting peptide is coupled with a hydrophobic functional molecule. After targeting tumor cells, the nanoparticles expose targeting peptides, target tumor cells, enter tumor cells through receptor-mediated endocytosis, release drugs, inhibit DNA synthesis and repair, and perform double killing on tumor cells , inhibit tumor growth. The amphiphilic polypeptide does not generate covalent bonds and has no reverse reaction during the self-assembly process, and has the advantages of non-toxicity and good biocompatibility for tumor treatment.
Owner:THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA

Targeted delivery to beta cells

The disclosure includes zinc prodrugs for targeted delivery of therapeutic, diagnostic or imaging agents to β-cells and methods of use therefor. The disclosure also includes targeted delivery of small molecules to β-cells that stabilize and activate CRISPR effector proteins comprising at least one destabilization domain, to enable CRISPR-based genome editing and transcriptional activation or repression in β-cells.
Owner:THE BROAD INST INC +1

An active targeting amphiphilic polypeptide nano drug carrier and its preparation and application

ActiveCN110237035BHigh physiological stabilityHigh cell phagocytosis efficiencyEmulsion deliveryMacromolecular non-active ingredientsSide chainPhospholipid
The invention provides an active targeting type amphipathic polypeptide nano-drug carrier and preparation and application thereof, and belongs to the technical field of biological medicines. According to an amphipathic polypeptide, an alkyl chain serves as the hydrophobic end, a polypeptide chain with active targeting functional and side chain modification fluorescent functional molecules serves as the hydrophilic end, and an anti-tumor drug is wrapped in a hydrophobic cavity of a micelle formed by self-assembling the amphipathic polypeptide. The nano-carrier can actively target tumor cells and enter the tumor cells through receptor-mediated endocytosis, the amphipathic polypeptide and phospholipid molecules have strong interaction, and the phagocytosis of a nano-drug by tumor cells is promoted. In the process, tracing can be conducted through fluorescent imaging of fluorescent functional molecules modified on the polypeptide chain, and the tumor imaging aim is realized. Finally, the anti-tumor drug is slowly released to kill tumor cells and restrain the growth of tumors. The amphipathic polypeptide nano-carrier is free of toxin, high in biocompatibility and remarkable in anti-tumor efficiency, and the tumor diagnosis and treatment can be integrated.
Owner:HUAZHONG UNIV OF SCI & TECH
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