40results about How to "Good stability in vitro" patented technology

The invention discloses a 2-(alpha-hydroxy amyl) benzamide derivate as well as a preparation method, a preparation and an application of the deviate. The structural formula of the 2-(alpha-hydroxy amyl) benzamide derivate is shown in the specification, wherein R1 is a link group; and R2 is a functional group containing carboxyl. The preparation method comprises the following steps: performing ring-opening reaction for butylphthalide serving as the raw material to obtain an intermediate product a; and performing condensation reaction for the intermediate product a and a carboxyl-containing compound. The preparation is prepared by adding pharmaceutically acceptable auxiliary materials and can be in a form of powder, a tablet, a capsule, granules, a dropping pill, a honeyed pill, a lyophilized agent or injection. The application includes the application in preparation of medicines for preventing / treating cardio-cerebral ischemia, cardio-cerebral arterial occlusion, parkinson disease and senile dementia. According to the preparation method, opened-loop butylphthalide and ozagrel or clopidogrel and other medicines with platelet aggregation resisting effects are linked through an amido bond so as to be synthesized into a butylphthalide prodrug with a plurality of pharmacologic effects.

The present invention relates to the field of medicinal chemistry, and in particular relates to 18F-labeled ethinyloestradiol and a preparation method and application thereof, a modifying group is introduced into ethinylestradiol, and the ethinylestradiol is labeled by 18F, and the 18F-labeled ethinyloestradiol has good bioactivity, excellent pharmacokinetic properties and good stability in vitro, can be better targeting to breast cancer ER + cells, and can be used as a PET tracer for early diagnosis or therapeutic effect evaluation of high metastatic breast cancer ER + cells. The invention also provides the preparation method of the 18F labeled ethinylestradiol, a labeling group is introduced into the ethinylestradiol as a raw material by Click reaction, and heated for being exchanged with 18F<-> under relatively mild conditions, a labeling step and purification time are simplified, the radiochemical yield of the 18F-labeled ethinyloestradiol is high, and commercial application and clinical promotion of radiolabeled compounds are facilitated.

The invention provides PEGylated benzyltriazolyl pyridazinone compounds of which the molecular formula is Fmppn. The structure of the pyridazinone compounds is disclosed as Formula (1), wherein n is a whole number ranging from 1 to 8; and F is 19F or 18F. The compounds provided by the invention have the characteristics of simple preparation process, low use cost, high radiochemical yield, high radiochemical purity, high stability, favorable biological properties, high target to non-target ratio, high myocardial uptake ratio and the like, and can be applied to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine as a novel fluorine-18 labeled myocardial perfusion developer.

The invention discloses a preparing method with chitose to modify liposome to prepare gene give medicine carrier, which comprises the following steps: building-up film material with phosphatide and cholesterol; adopting counter-current evaporating method or thin film dispersing method; getting liposome solution through probe hypersonic and squeezing film; allocating chitose solution with various molecular weight; hatching the chitose solution and liposome solution; getting the liposome. This invention can used as gene give medicine carrier, which possesses good internal application prospect.

The invention provides a pyridazinone compound containing polyethyleneglycol (PEG) modified benzyl triazolyl. According to the pyridazinone compound, a molecular formula is Fmppn, and a structure is shown as a formula (1), wherein n is an integral number of 1 to 8; and F is 19F or 18F. The pyridazinone compound has the characteristics of simplicity in preparation, low using cost, high radiochemical yield and radiochemical purity, high stability and biological properties, high target-to-nontarget ratio, high myocardial intake value and the like, and is used as a novel fluorine-18 marked myocardial perfusion photographic developer to be applied to the technical fields of radiopharmaceutical chemistry and clinical nuclear medicine.

The invention discloses a PEG (polyethylene glycol) modified recombinant arginine deiminase (ADI) as well as a preparation method and application thereof, belonging to the technical field of biomedical engineering. The stability of ADI-PEG obtained by modifying ADI with PEG in vitro and in mouse plasma is remarkably improved. A pharmacokinetics / pharmacodynamics study shows that compared with free ADI before modification, the half-life period of ADI-PEG in a mouse is prolonged by more than 11 times; the concentration of arginine in the plasma can be reduced and maintained for more than 5 days in the limiting level through single injection of 5U ADI-PEG and can be maintained for 1 day only through injection of unmodified ADI; an H22 liver cancer model mouse is treated for 15 days, and the cancer cell inhibition rate of ADI-PEG (15U) is 95.02% close to 98.34% (the inhibition rate) of a positive control group treated with 5-fluorouracil. PEG modified recombinant arginine deiminase is relatively long in in-vivo half-life period and relatively low in immunogenicity, and serves as an excellent tumor treating or inhibiting drug.

The present invention provides a class of compounds targeting FAK, wherein the structure is represented by the following formula (I), X is an N atom or a Cl-substituted C atom, R1 is -OH, -O-CH2-CH2-OH or -O-CH2-CH2-F, and R2 is methylamino or dimethylamino. The present invention further provides a class of radioactively labeled compounds targeting FAK. According to the present invention, the compounds have excellent in vitro FAK kinase activity inhibition effects, and the radioactive labels have ideal biodistribution in rice bearing S180 tumor. The present invention further provides preparation methods of the compounds and the radioactive labels, and applications in preparation of antitumor drugs. The formula (I) is defined in the specification.

The invention discloses a 99mTc (HYNICNM) (tricine / TPPTS) complex and a preparation method and application thereof. The 99mTc (HYNICNM) (tricine / TPPTS) complex is obtained through two steps of synthesis of a ligand HYNICNM and preparation of a 99mTc (HYNICNM) (tricine / TPPTS) complex. The complex is simple and convenient to prepare and has oxygen deficiency selectivity. Tumor-bearing mice have highuptake and good retention in tumor parts, the tumor / non-target ratio is high, the uptake of non-target organs such as the liver and intestines is obviously reduced, and the 99mTc (HYNICNM) (tricine / TPPTS) complex is a novel tumor hypoxia imaging agent with excellent performance.

The invention relates to euphausia superb symbiotic bacteria, an euphausia superb antioxidant peptide, and a preparation method and application of the euphausia superb antioxidant peptide, belonging to the technical field of microorganisms and biological active peptides. Euphausia superb symbiotic bacteria psychrobacter NL-6 is preserved in China Typical Culture Preservation Center in Wuhan on June 22, 2016, and the preservation number is CCTCCM 2016341. Euphausia superb homogenate is fermented by using the strain to obtain the euphausia superb antioxidant peptide, a hydroxyl radical removal rate of active peptide components, i.e., 1kDa to 5kDa components with highest antioxidant performance reaches 93 percent, the reducing power is 1.32, and an ABTS removal rate is 92.4 percent. The polypeptide is relatively good in stability in vivo and in vitro, better adapts to the requirements of mass production, and relatively good in development and application value as an antioxidant food additive.

The invention belongs to the technical field of nuclear medicine and molecular imaging, and relates to a PET / CT (Positron Emission Tomography / Computed Tomography) in vivo molecular imaging probe 18F-Annexin B1 for apoptosis and a preparation method and application thereof. The PET / CT in vivo molecular imaging probe 18F-Annexin B1 for apoptosis is 18F-marked annexin B1, an 18F-marked prosthetic group and an annexin B1 are coupled under certain conditions, and the 18F-annexin B1 is separated out and purified. The invention also provides the preparation method for the PET / CT in vivo molecular imaging probe 18F-Annexin B1 for apoptosis. The PET / CT in vivo molecular imaging probe 18F-Annexin B1 for apoptosis can be applied in the experiment on the in vitro association capability of the 18F-annexin B1 with apoptotic cells and PET / CT imaging in the disease diagnosis of tumours, the kidney, the liver, the thymus and other related tissues and organs, the evaluation of curative effect and the screening and evaluation of new curatives and new methods.

Therapeutic compounds useful for the treatment of pathogens including bacteria (gram positive and gram negative, mycobacteria), some fungi and viruses. The compounds described herein may include a mixture of therapeutically-effective amounts of a polar amino acid, a CI 1 fatty acid, and an anthraquinone. The invention further provides for the administration of the therapeutic compounds to a patient (e.g., a human) suffering from an infection.

The invention relates to the technical field of nuclear medicine, in particular to a nuclide-labeled PD-1-targeted monoclonal antibody and a preparation method and application thereof. The preparationmethod comprises the steps: mediating a PD-1 monoclonal antibody through N-bromosuccinimide, or coupling the PD-1 monoclonal antibody with a bifunctional chelating agent deferoxamine, and then performing labeling with 124I, 64Cu or 89Zr radionuclide so as to obtain the nuclide-labeled PD-1 monoclonal antibody. The labeled monoclonal antibody has a high labeling rate, high purity, high in-vitro stability, high affinity and specificity to PD-1, high functional activity for PD-1 and a good imaging effect, uptake by PD-1 positive tumors is high, non-specific uptake by livers is low, detection ofliver lesions is facilitated, the whole body background is low, and a good tumor-to-non-tumor ratio is obtained; and the labeled monoclonal antibody can be applied to diagnosis and treatment of PD-1 high-expression tumors, and individualized and precise treatment is achieved through tumor-targeted drugs.

The invention discloses a technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification and a preparation method and application of the technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification, wherein the structural general formula of the technetium-99m labeled FAPI derivative is 99mTc (HYNIC-PGn-FAPI) (Tricine / TPPTS). The < 99m > Tc (HYNIC-PGn-FAP) (trickine / TPPTS) complex is prepared by the following two steps: synthesis of a ligand HYNIC-PGn-FAPI and preparation of the < 99m > Tc (HYNIC-PGn-FAP) (trickine / TPPTS), and the < 99m > Tc (HYNIC-PGn-FAP) (trickine / TPPTS) complex is obtained. The complex is simple and convenient to prepare, high in radiochemical purity and good in stability, has very high uptake and target-to-non-target ratio at the tumor site of a U87MG tumor-bearing mouse, has specific binding with FAP in tumors, and is a novel tumor radiopharmaceutical with clinical application value.

The invention belongs to the technical field of biology and provides a 125I-labeled Caerin polypeptide and an application thereof to preparation of a drug for treating tumors and particularly benign and malignant tumors relevant to HPV infection. The 125I-labeled Caerin polypeptide provided by the invention is prepared by using an optimized direct labeling method, and the preparation method is simple and convenient to operate, high in labeling rate, short in reaction time and good in in-vivo and in-vitro stability. The 125I-labeled polypeptide prepared after a Caerin polypeptide is 125I-labeled has a remarkable effect on inhibiting tumor cells and is capable of remarkably improving the treatment effect of the Caerin polypeptide, reducing the use dosage of the Caerin polypeptide and reducing the preparation cost and chemical toxicity of the drug for treating the tumors and particularly tumors relevant to HPV infection, so that the treatment cost of the tumors is reduced, and the medication safety of the tumors is improved.

The invention discloses a technetium-99m labeled FAPI derivative containing D-proline modification and a preparation method and application of the technetium-99m labeled FAPI derivative containing D-proline modification, wherein the structural general formula of the technetium-99m labeled FAPI derivative is 99mTc (HYNIC-DP-FAPI) (Tricine / TPPTS). The < 99m > Tc (HYNIC-DP-FAPI) (trickine / TPPTS) complex is prepared by the following two steps: synthesis of a ligand HYNIC-DP-FAPI and preparation of the < 99m > Tc (HYNIC-DP-FAPI) (trickine / TPPTS), and the < 99m > Tc (HYNIC-DP-FAPI) (trickine / TPPTS) complex is obtained. The complex is simple and convenient to prepare, high in radiochemical purity and good in stability, has very high uptake and target-to-non-target ratio at the tumor site of a U87MG tumor-bearing mouse, has specific binding with FAP in tumors, and is a novel tumor radiopharmaceutical with clinical application value.

The invention belongs to the technical field of medicinal chemistry and nuclear pharmacy, and discloses an <18>F-labeled EGFR positron imaging agent as well as a preparation method and application thereof. The <18>F-labeled EGFR positron imaging agent has a structure as shown in a formula (II) which is described in the specification. The tracing effect is good, the specificity is relatively good, and high-expression or variant tumors of an epidermal factor receptor (EGFR) can be positively recognized. Meanwhile, the compound is good in in-vitro stability, is mainly metabolized through intestines, galls and kidneys, is quick to remove in vivo, is low in background uptake of background visceral organs and tissues such as muscles, bones, hearts, lungs and livers, and can be used for tumor PET imaging agents, EGFR expression level detection agents and EGFR inhibitor screening agents.

The invention provides an oxygen-carrying bionic nano antidote, and a preparation method and application thereof. The oxygen-carrying bionic nano antidote with an oxygen-carrying function is obtained by wrapping an oxygen-carrying liquid perfluorocarbon compound with an erythrocyte membrane modified by phospholipid derivative oleic acid oxyethyl phosphorylcholine. The obtained bionic nano antidote is good in detoxification effect, toxin-induced hemolysis can be weakened, the hypoxia phenomenon caused by snake bites is relieved, degenerative necrosis of tissue cells is reduced, and wound healing is promoted.

The invention discloses a technetium-labeled estradiol derivative and a reference compound thereof, and a preparation method, an application and an intermediate thereof. The technetium-labeled estradiol derivative is shown in the formula VII, wherein A is a group -(CH2CH2)x- or -(CH2CH2O)m(CH2CH2)n-; and x, m and n are integral numbers, x is 1-6, m is 1-3, and n is 1-3. The technetium-labeled estradiol derivative has a moderate lipid / water partition coefficient, and can be used for preparing imaging drugs for diagnosing breast cancer. The in-vitro experiment indicates that the technetium-labeled estradiol derivative has favorable affinity with an estrogen receptor, and has favorable in-vitro stability and moderate metabolism speed in phosphate buffer solution (PBS), 1mM histidine solution, 1mM cysteine solution, 1mM diethylene triamine pentacetic acid (DTPA) solution and newborn calf serum. The technetium-labeled estradiol derivative is hopeful to become a radioactive drug which has good targeting property, is suitable for continuing deep research in organisms and is used for diagnostic imaging.

The invention discloses a nuclear medicine and magnetic resonance bimodal development drug precursor (DOTA-SPIONs-PEG-FA). The drug precursor takes superparamagnetic iron oxide nanoparticles as cores and is coated with a biocompatible material and a double functional chelating agent. Folic acid is connected to the superparamagnetic iron oxide nanoparticles through the biocompatible material. The bimodal development drug precursor is labeled by a radioactive metal nuclide, so that a brand-new nuclear medicine and magnetic resonance bimodal development drug (RM-DOTA-SPIONs-PEG-FA) is obtained for the first time. The drug is good in in-vitro stability, has very high initial uptake, a good tumor / blood ratio and a relatively long residence time in tumor if being applied to folate receptor positive tumor detection, moreover, the nanoparticles have obvious active targeting action on tumor, so that the drug precursor can be effectively suitable for MRI development and EPT or SPECT development.

The invention provides a technetium 99m-marked anti-aspergillus monoclonal antibody for detection of aspergillus, and preparation and application thereof. The technetium 99-marked anti-aspergillus monoclonal antibody is characterized by being prepared through coupling of a difunctional coupling agent NHS-MAG3 with a mouse anti-aspergillus monoclonal antibody Mab-WF-AF-1 and <99m>TcO4<->. The prepared technetium 99m-marked anti-aspergillus monoclonal antibody can be used for qualitative and / or quantitative determination of aspergillus spores in the lung.

The invention discloses a nanoscale ultrasonic contrast agent entrapping perfluorocarbon. The prepared nanoscale ultrasonic contrast agent entrapping the low-boiling point perfluorocarbon inside rapidly vaporizes under the action of body temperature and the ultrasonic effect to produce microbubbles; after receiving ultrasonic energy, the microbubbles resonate and scatter ultrasonic signals to achieve the effect of ultrasonic contrast. The ultrasonic contrast agent has a particle size within a nanoscale range, has high penetrating ability, and has better ability of enhancing imaging; moreover,the nanoscale ultrasonic contrast agent is wrapped by multiple layers of phospholipids, so that storage stability is high, in-vivo ultrasonic stability is high, and biological safety is high; a preparation method is simple; the diagnosis and treatment efficiency can be effectively improved; and the nanoscale ultrasonic contrast agent has very high research value and broad application prospects.

A 99mTc-labeled isonitrile-containing glucose derivative having the general formula [99mTc-(CNDG)6]+, preparation method and use thereof is disclosed herein. The derivative is centered on 99mTc+, and the carbon atom of the isonitrile in CNDG coordinates with 99mTc(I) to form a hexacoordinated complex [99mTc-(CNDG)6]+. The [99mTc-(CNDG)6]+ derivative was obtained by the synthesis of the ligand CNDG and the preparation of the lyophilized CNDG kit. The derivative of the present invention this disclosure has good stability, simple preparation, high uptake and good retention at a tumor site, and high tumor / non-target ratio, and it is a novel 99mTc-labeled isonitrile-containing glucose derivative with excellent performance for tumor imaging. The derivative of the present invention this disclosure is advantageous for popularization and application.

This application relates to the field of biomedical technology, in particular to miRNA markers related to active tuberculosis and their applications, wherein the miRNA markers related to active tuberculosis include miR-451a, miR-25-3p, miR-425 ‑5p, miR‑1260b, miR‑1273g‑3p, miR‑30e‑5p, miR‑140‑3p, let‑7a‑5p, miR‑1290, miR‑491‑5p, miR‑3615, miR‑15a‑5p One or more of miR-21-3p, miR-424-5p, miR-1268a, miR-1301-3p, miR-345-5p, miR-572, miR-375, miR-151a-5p.

The invention discloses a technetium-labeled estradiol derivative and a reference compound thereof, and a preparation method, an application and an intermediate thereof. The technetium-labeled estradiol derivative is shown in the formula VII, wherein A is a group -(CH2CH2)x- or -(CH2CH2O)m(CH2CH2)n-; and x, m and n are integral numbers, x is 1-6, m is 1-3, and n is 1-3. The technetium-labeled estradiol derivative has a moderate lipid / water partition coefficient, and can be used for preparing imaging drugs for diagnosing breast cancer. The in-vitro experiment indicates that the technetium-labeled estradiol derivative has favorable affinity with an estrogen receptor, and has favorable in-vitro stability and moderate metabolism speed in phosphate buffer solution (PBS), 1mM histidine solution, 1mM cysteine solution, 1mM diethylene triamine pentacetic acid (DTPA) solution and newborn calf serum. The technetium-labeled estradiol derivative is hopeful to become a radioactive drug which has good targeting property, is suitable for continuing deep research in organisms and is used for diagnostic imaging.

The invention provides a liposome modified by lactoferrin, which comprises the following raw materials: lactoferrin, egg yolk lecithin, cholesterol, distearoylphosphatidylethanolamine-polyethylene glycol 2000, distearate Acylphosphatidylethanolamine-N-hydroxysuccinimide-polyethylene glycol 2000 and patchouli alcohol; of which, egg yolk lecithin, cholesterol, distearoylphosphatidylethanolamine-polyethylene glycol 2000, distearyl The ratio of acylphosphatidylethanolamine-N-hydroxysuccinimide-polyethylene glycol 2000 is (29~32):(5~7):(5~7):(0.5~1.5)(w / w) ; Wherein, the patchouli alcohol is encapsulated in liposomes; Wherein, the amino group contained in the lactoferrin is passed with distearoylphosphatidylethanolamine-N-hydroxysuccinimide-polyethylene glycol 2000 N-hydroxysuccinimide in the reaction, thus attached to the liposome surface.

Therapeutic compounds useful for the treatment of pathogens including bacteria (gram positive and gram negative, mycobacteria), some fungi and viruses. The compounds described herein may include a mixture of therapeutically-effective amounts of a polar amino acid, a CI 1 fatty acid, and an anthraquinone. The invention further provides for the administration of the therapeutic compounds to a patient (e.g., a human) suffering from an infection.

The invention provides an oxygen-carrying biomimetic nano antidote and its preparation method and application. The red blood cell membrane modified by the phospholipid derivative oleic acid oxyethylphosphorylcholine is used to wrap the oxygen-carrying liquid perfluorocarbon compound to obtain the oxygen-carrying liquid perfluorocarbon compound. Functional biomimetic nano antidote. The obtained biomimetic nano antidote has good detoxification effect, can weaken the hemolysis induced by the toxin, alleviate the hypoxia phenomenon caused by the snake bite, reduce the degeneration and necrosis of tissue cells and promote wound healing.

The invention belongs to the technical field of biology and provides a 125I-labeled Caerin polypeptide and an application thereof to preparation of a drug for treating tumors and particularly benign and malignant tumors relevant to HPV infection. The 125I-labeled Caerin polypeptide provided by the invention is prepared by using an optimized direct labeling method, and the preparation method is simple and convenient to operate, high in labeling rate, short in reaction time and good in in-vivo and in-vitro stability. The 125I-labeled polypeptide prepared after a Caerin polypeptide is 125I-labeled has a remarkable effect on inhibiting tumor cells and is capable of remarkably improving the treatment effect of the Caerin polypeptide, reducing the use dosage of the Caerin polypeptide and reducing the preparation cost and chemical toxicity of the drug for treating the tumors and particularly tumors relevant to HPV infection, so that the treatment cost of the tumors is reduced, and the medication safety of the tumors is improved.