109results about How to "Reduce cardiotoxicity" patented technology

The invention relates to a pH / reduction dual-sensitive multifunctional nano-micelle for tumor chemotherapy and photothermal combined therapy and application of the pH / reduction dual-sensitive multifunctional nano-micelle. The pH / reduction dual-sensitive multifunctional nano-micelle is characterized in that a PCL-acetal-PEG polymer with pH sensitive characteristic, a PCL-ss-PEG-ss-PCL polymer withreduction sensitive characteristic and a phospholipid DSPE-PEG-NH2 with an active group are used as raw materials and are blended to prepare a pH / reduction intelligent responsive polymer nano-micelleas a carrier; a chemotherapeutic drug and a photosensitizer coat a hydrophobic core of the micelle; a casing is made of hydrophilic PEG and has the characteristic of long circulation and space stability; a folic acid targeting group is modified on the surface of the micelle by a covalent bond; the drug loading capacity is 4 to 10 percent, and the mass ratio of the chemotherapeutic drug to the photosensitizer is 0.5 to 2; the particle size is smaller than 200 nm. The pH / reduction dual-sensitive multifunctional nano-micelle disclosed by the invention has the advantages of good dispersity, smallparticle size, better photothermal conversion effect and high drug loading capacity and encapsulation efficiency; the effect of improving tumor suppression by tumor targeted administration, fluorescence imaging of a tumor site, pH / reduction triggered drug release and chemotherapy and photothermal combined therapy can be realized; the pH / reduction dual-sensitive multifunctional nano-micelle has a broad clinical application prospect in combined targeting therapy of tumors.

Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

The invention provides a composition with anti-tumor effect and application thereof. The composition consists of 0.01 to 10 weight parts of pure bufadienolide compound, extract rich in bufadienolide compound, raw toad venom or toad skin and 0.01 to 99.9 weight parts of medicament with anti-arrhythmic effect. The composition with the anti-tumor effect has the advantage that the match among the components is scientific and reasonable; multiple in vitro tumor cytotoxicity and in vivo tumor inhibiting experiments show that the composition provided by the invention has good anti-tumor effect and plays a role in synergy after combination; and cardiotoxic experiments show that the cardiotoxicity of the composition provided by the invention is obviously reduced, and the composition can reduce the cardiotoxicity caused by primary single use of the bufadienolide compound, the toad venom or the toad skin and plays a role in detoxifying. Therefore, the composition is safer and more effective to use, and is expected to develop a new generation anti-cancer medicament.

The invention discloses a xiluomosi liposome freeze dried and making technique, which comprises the following steps: selecting liposome component, buffer, organic solvent, antioxidant and freeze-drying protective as raw material; adopting film diffusion method to make the liposome turbid liquor with xiluomosi through high-pressure or hypersonic dispersing method evenly; drying the liposome to improve the storage stability obviously; dispersing the freeze dried at random proportion in the water evenly without any sediment and impurity; making the packing rate of liposome at 96% with the grain size at 50-250nm; improving the drug effect greatly in comparison with oral agent; lengthening the circulating time in the blood; elevating the biological utility of drug.

The invention discloses an amphipathy block-polymer hydroxyethyl-starch-olylactic-acid copolymer and a preparing method and nanometer medicine loading system thereof. The method includes the steps that 4-dimethylaminopyridine serves as a catalyst, N-N'-dicyclohexylcarbodiimide serves as a dehydrating agent, carboxyl at the tail end of polylactic acid and hydroxyl on hydroxyethyl-starch sugar ring are subjected o an esterification reaction, hydrophobic polylactic acid is coupled on hydrophilic hydroxyethyl starch accordingly, and the amphipathy hydroxyethyl-starch-polylactic-acid block polymer is synthesized. Debydrochlorination adriamycin amycin is loaded to a hydrophobic core with the emulsified solvent evaporation method and the high pressure homogenization technology, evenly-distributed medicine loading polymer nanometer particles with the particle-size of about 140 nm are formed, and are applied in preparing antitumor medicine, the medicine in-vivo cycling time is prolonged, the toxic and side effects of the medicine are reduced, and the good antitumor effect is achieved.

The invention belongs to the technical field of medicines, relates to a paclitaxel medicinal composition and a preparation method thereof, and in particular relates to an injection paclitaxel nanocrystal preparation and a preparation method thereof as well as application of the preparation for preparing anti-tumor medicines. The paclitaxel nanocrystal belongs to a nano preparation, is small in grain diameter and good in stability, and cannot be easily separated, so that the dissolubility of paclitaxel is remarkably improved, and in-vivo studies prove that the paclitaxel nanocrystal has certain targeting performance, and can be used in anti-tumor treatment.

A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I):wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):

Provided are fragments of human p97 (melanotransferrin) polypeptides having blood-brain barrier (BBB) transport activity, including variants and combinations thereof, conjugates comprising said p97 fragments, and related methods of use thereof, for instance, to facilitate delivery of therapeutic or diagnostic agents across the BBB.

The invention relates to a tumor-targeted sound and light power medicine-carrying nanometer nano-micelle, and a preparation method and a purpose thereof. The medicine-carrying nanometer nano-micelle is structurally characterized in that porphyrins compounds and anthracyclines chemotherapeutic medicine form a nanometer composition through a pi-pi conjugation effect; and amphiphilic block copolymers with PEO (polyoxyethylene) or PEG (polyethylene glycol) hydrophilic segments cover nanometer compounds through the hydrophobic effect to form a hydrophilic case. The medicine-carrying nanometer nano-micelle is in a regular spherical form, and has the advantages of uniform distribution, stable property and high medicine carrying capacity; the medicine can be conveyed to the tumor focus in the targeted way and can be effectively enriched in the tumor tissue; under the ultrasound (illumination) condition, the treatment effect of the anthracyclines chemotherapeutic medicine on the tumor can be obviously enhanced; and the tumor drug resistance can be effectively reversed. Wide clinic application prospects can be realized in an aspect of combined tumor treatment by a sound (light) power therapy method and chemotherapy.

The invention provides therapeutically effective compounds for the prevention and treatment of cancer and pharmaceutical compositions containing these compounds as well as methods of using and administering these compounds. The invention also includes methods of activating a prodrug of these therapeutically effective compounds by the administration of a peptide-directed targeting construct that delivers a prodrug-activating enzyme to a target activation site.

A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I): wherein R1 and R2 represent hydrogen atom, or the like; R3 represents an alkyl group containing 1 to 6 carbon atoms, or the like; R4 and R5 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R4 and R5 do not simultaneously represent hydrogen atom; or the substituents R4 and R5 together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R4 and R5 to form a spirocyclic structure with the pyrrolidine ring; R6 and R7 independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R8 represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X1 represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):

Anaphylactic diseases comprising urticaria, papilla, subacute dermatitis, eczema, and the like, are skin diseases which seriously puzzle the human beings. In the invention, antihistamine, zinc salt and weak acid are prepared into a topical compound preparation, which not only reduces the untoward effect of drugs, avoids the first pass effect of the liver when feeding the drugs by mouth, avoids the blood concentration peak valley phenomenon caused by oral feeding, but also can improve the curative effect and is convenient for clinic application. Simultaneously pharmacological tests show that the topical compound preparation obtains excellent drug synergism to the anaphylactic skin diseases and has excellent effects on curing the anaphylactic diseases.

The invention belongs to the field of medicine, which relates to Deferiprone and a novel medicated purpose of a Deferiprone preparation, in particular to Deferiprone (1,2- dimethyl-3-hydroxide radical-4-pyridine, Deferiprone) and the application of the Deferiprone preparation in the prevention and curing of Anthracycline medicine heart toxicity. The invention researches the preventing and curing function of the Deferiprone to bandicoot heart toxicity caused by Adriamycin from the cell level, the tissue level and the whole level and prepares biodegradable type Deferiprone implant, Deferiprone troche, capsule, oral liquor and injection that can release medicine continuously. An experimental result proves that the Deferiprone and the Deferiprone preparation can not only improves the cardiac muscle shrinkage functions and protects the myocardial cell organ structure, but also complexes free iron ions directly, reduces the heart toxicity and other side and toxic effects caused by the Anthracycline medicine obviously and the mortality rate caused by the Anthracycline medicine.

A 13-deoxy anthracycline and a taxane can be administered to a patient simultaneously, separately, sequentially, or consecutively to produce a therapeutic anticancer effect with reduced toxicity and side effect profile, compared to the administration of equieffective amounts of either compound alone. A composition or preparation of a 13-deoxy anthracyclines and a taxane for producing a potent anticancer therapeutic effect is also provided.

The present invention relates to methods of reducing cardiotoxicity and / or improving survival from treatment with anthracycline agents comprising administering a therapeutically effective amount of a composition comprising a vasopressin antagonist compound or a pharmaceutically acceptable salt thereof as an active ingredient, administered simultaneously or prior to the anthracycline administration.

The invention relates to astragalus polyose calcium phosphate nano taxol complex injection and a preparation method and the application thereof. 100 mL of injection comprises the following components: 0.01 to 1 g of astragalus polyose calcium phosphate nano to particles, 1.0 to 50 mg of taxol, 0 to 5.0 g of osmotic pressure regulator and appropriate amount of water. The pH value of the injection is 6.0 to 7.5. The preparation method comprises the following steps: blending the taxol with absolute ethyl alcohol to form taxol-absolute ethyl alcohol solution; blending the astragalus polyose with ultrapure water to form astragalus polyose solution; performing stirring and ultrasonic processing to the solution, rejecting the supernatant fluid after separation, and after depositing, drying and sterilizing, obtaining astragalus polyose calcium phosphate nano taxol complex granules used for injection, then adding the osmotic pressure regulator into the water for injection, and mixing with the astragalus polyose calcium phosphate nano taxol complex granules; after ultrasonic processing, astragalus polyose calcium phosphate nano taxol complex injection is formed. The complex injection can be used for the treatment or auxiliary treatment of tumor.

The invention provides pH-sensitive doxorubicin hydrochloride loaded silver nano-cluster hydrogel. A preparation method of the silver nano-cluster hydrogel comprises the following steps: (1), an AgNO3 solution is prepared, placed in a microwave reactor, stirred and heated, a cysteine solution is added dropwise, and a silver nano-cluster dispersing agent is prepared through reaction; (2), a citric acid solution is added to the silver nano-cluster dispersing agent, the mixture is placed on a small shaking table and subjected to ultraviolet irradiation, an NaHCO3 solution is added to regulate pH after the solution is transparent, high-speed centrifugation is performed, doxorubicin hydrochloride powder is added, the mixture is placed in a high-pressure reactor, nitrogen is introduced, the pressure and the temperature in the reactor are adjusted, red and clear jelly, namely, the pH-sensitive doxorubicin hydrochloride loaded silver nano-cluster hydrogel, is obtained through reaction. The silver nano-cluster hydrogel is taken as a carrier to coat doxorubicin hydrochloride and is injected to a tumor position through orthotopic injection, the pH of the tumor position is responded, so that slow drug release is realized, the tumor inhibition rate is increased, and cardiac toxicity is reduced.

This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.

Methods are provided for using doxorubicin active agents in which reduced host toxicity is observed. Aspects of the methods including administering to a subject an effective amount of a doxorubicin active agent in conjunction with a doxorubicin toxicity-reducing adjuvant, e.g., a nitrone compound, or a nitrone compound in combination with a bisdioxopiperazine compound. Also provided are compositions for use in practicing the subject methods. The methods and compositions find use in a variety of different applications, including in the treatment of a variety of different disease conditions.

The invention belongs to the field of chemical synthesis, and in particular relates to a tilmicosin inclusion complex chitosan temperature-sensitive gel and a preparation method thereof. The preparation method comprises the following steps: dissolving chitosan in 0.1mol / L hydrochloric acid by weighing and fully stirring until Dissolve the sodium glycerophosphate in deionized water, add the sodium glycerophosphate solution dropwise into the chitosan solution, adjust the pH value of the mixed solution, and stir the resulting mixed solution at 4°C to obtain the chitosan thermosensitive gel, which is called Take a tilmicosin inclusion compound in a conical flask, add an appropriate amount of chitosan thermosensitive gel into the conical flask, and stir evenly with a magnetic stirrer at room temperature to obtain a tilmicosin inclusion complex thermosensitive gel. The invention has the advantages of low toxicity, high bioavailability and low injection irritation.

The invention provides an application of a dihydromyricetin composition in preparation of medicines for inhibiting adriamycin cardiotoxicity. The composition is composed of dihydromyricetin and adriamycin; as shown by in vivo and in vitro experimental studies, the dihydromyricetin can inhibit cell apoptosis activated by the adriamycin and dependent to mitochondrial membrane potential so as to reduce lethality caused by adriamycin cardiotoxicity, and the composition provided by the invention has excellent protection effect on cardiotoxicity induced by adriamycin. The composition provided by the invention can be used for preventing and alleviating the cardiotoxicity educed by adriamycin and has clinical practicability.

The present invention relates to a series of phosphoryl-containing steroidal compounds, a preparation method and an application thereof, in particular to the compounds as a formula I, an isomer, pharmaceutically acceptable salts or chemically protected forms thereof, the preparation method thereof, and the application of the compounds in preparation of a medicine for treating cancer-related diseases. The compounds of the present invention have the good activity for inhibiting malignant tumors such as melanoma and prostate cancer.

The invention discloses a histone deacetylase subtype inhibitor, namely a thioacetyl arylamine compound and application thereof. Pharmacological experiments show that the compound has a selective inhibition effect on HDAC6 enzyme, shows high anti-proliferative activity on various tumor cells, and is low in toxicity to normal cells and low in potential cardiotoxicity. Moreover, the compound has a protective effect on nerve cells, is ideal in pharmacokinetic characteristics, and has relatively high blood-brain barrier dredging characteristics. The compound disclosed by the invention has a deep development prospect as a high-efficiency low-toxicity anti-tumor or neurodegenerative disease therapeutic agent. The structural general formula of the histone deacetylase subtype inhibitor, namely thethioacetyl arylamine compound is as shown in the specification.

The invention discloses an application of chiral chloroquine, hydroxychloroquine or pharmaceutically acceptable salts of the chiral chloroquine and hydroxychloroquine in preparation of drugs used forpreventing and / or treating coronavirus pneumonia by using a coronavirus key drug target 3CL hydrolase (Mpro) as an action target. The chiral chloroquine and hydroxychloroquine have high bonding strength with the Mpro causing inflammation of the lung and the like; the activity of the Mpro can be significantly inhibited; and the chiral chloroquine and hydroxychloroquine are indicated to have the effect of preventing and treating pneumonia caused by coronaviruses and be able to be used as anti-pneumonia drugs. Through evaluation on the inhibitory activity of an hERG potassium ion channel, the concentration at which the chloroquine, hydroxychloroquine and enantiomers of the chloroquine and hydroxychloroquine are likely to generate cardiotoxicity to the hERG potassium ion channel is provided. The chiral chloroquine and hydroxychloroquine are prepared through chiral high-performance liquid chromatography and chiral synthesis; S-configuration chloroquine, hydroxychloroquine or salts of the chloroquine and hydroxychloroquine can be selected as a drug independently, or form a pharmaceutical composition for treating diseases caused by the coronaviruses; and due to higher activity and low cardiotoxicity of the chloroquine, hydroxychloroquine or salts of the chloroquine and hydroxychloroquine, the administration dosage range is greatly widened.

This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.