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 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 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 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 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 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.