43 results about "Tumor imaging" patented technology

The invention relates to the technical field of nuclide probes, and discloses a targeted PARP nuclide probe and a preparation method and application thereof, and the targeted PARP nuclide probe comprises a radionuclide labeled compound as shown in formula I; the targeted PARP nuclide probe provided by the invention can be used as a diagnosis and treatment reagent to be applied to tumors with high PARP protein expression in human or animal bodies, and is especially suitable for tumor imaging and radionuclide treatment; animal experiments show that the nuclide probe has a high tumor / muscle uptake ratio and shows good application potential. Formula I.

The invention relates to the technical field of biology, and particularly discloses a tumor imaging biomarker quantitative analysis system based on multi-mode MRI voxel space coupling and application. According to the application, the spatial coupling relationship between blood brain barrier destruction and perfusion in a tumor can be quantitatively reflected through the voxel overlap region proportion of T1CE and CBF signals, the 1p / 19q state can be efficiently predicted, and accurate prediction of IDH mutation and WHO grading (2-3 grade vs.4 grade) is realized in cooperation with clinical factors, so that the application has a wide application prospect. And an efficient and potential noninvasive imaging biomarker is provided for ADG preoperative molecular typing and grading prediction.

This invention discloses an ERβ-targeted hydrogen peroxide-responsive near-infrared fluorescent probe, its preparation method, and its applications, belonging to the field of medical technology. The fluorescent probes of this invention are dicyanomethylene-4H-benzodihydropyran compounds P1 and P2 containing borate ester groups, with the following structural formula. These fluorescent probes use DCM-OH as a backbone, acting as both a fluorophore and an ERβ ligand. The borate ester group is the H2O2 responsive group. The introduction of the borate ester group disrupts the push-pull effect of the DCM-OH fluorophore, preventing fluorescence emission. However, in a high-concentration H2O2 environment, the borate ester group is specifically cleaved by H2O2, subsequently exhibiting strong initiation fluorescence and enabling tumor imaging in vitro and in vivo. This invention brings new opportunities for the diagnosis and research of prostate cancer.

The application belongs to the field of pharmacy, and particularly relates to a whole-process targeting polypeptide molecule with the functions of targeting brain capillary endothelial cells, tumor neovascular endothelial cells, tumor pseudo vascular, tumor cells and tumor stem cells, a stable and optimized polypeptide molecule, and a modified complex and drug delivery system for tumor diagnosis and treatment. The application prepares a whole-process targeting polypeptide WVAP and a WVAP modified drug and high polymer carrier material, and applies the WVAP to the construction of a drug delivery system for tumor imaging and targeted therapy. The results show that the WVAP can cross the blood-brain barrier, target tumor neovascular and cross the blood-tumor barrier, target tumor pseudo vascular, tumor cells and tumor stem cells; and the nano drug delivery system constructed by the WVAP modified high polymer carrier material can effectively deliver the loaded drug to the brain, target tumor tissues, and significantly improve the anti-tumor efficacy.

The invention discloses an enzyme-activated fluorescent molecular precursor as well as a preparation method and application thereof. The enzyme-activated fluorescent molecular precursor has a chemical structure as shown in a formula I which is described in the specification. The invention develops an enzyme-activated fluorescent molecular precursor which can be used for real-time imaging of tumors by targeting exogenous enzyme to the tumors and specifically activating a probe at the tumors; according to the invention, the exogenous enzyme is introduced as an activation trigger, and normal cells do not have the exogenous enzyme, so that the problem of co-expression of the endogenous enzyme in non-tumor tissues can be avoided, background fluorescence signals can be reduced to the greatest extent, and the imaging specificity and accuracy are remarkably improved.

This invention discloses a water-soluble melanin CEST contrast agent, its preparation method, and its application, relating to the field of magnetic resonance imaging contrast agent technology. This contrast agent, its preparation method, and its application aim to solve the technical problem that existing contrast agents containing paramagnetic metals can damage liver and kidney function. This water-soluble melanin CEST contrast agent comprises the following components by weight: 2-3 parts ammonia, 40 parts ethanol, 100 parts deionized water, and 0.5 parts reaction substrate. The chemical shift corresponding to this contrast agent preparation method is 4.0 ppm, exhibiting good adaptability to acidic environments and suitability for use in the tumor microenvironment. It is polymerized using dopamine hydrochloride or 3,4-dihydroxyphenylalanine, with inexpensive, simple, and readily available raw materials, simple synthesis, and easy large-scale preparation. It achieves tumor imaging without the need for paramagnetic metal ions, avoiding the damage to liver and kidney function caused by heavy metal ions.

An arylboron compound, its preparation method, applications, and pharmaceutical compositions are disclosed for tumor imaging. The compound of formula (I) exhibits high fluorescence quantum efficiency through intramolecular charge transfer. The compound of formula (I) synthesized in this invention can be linked to different antibodies via Q3 at certain concentrations, allowing for precise targeting of corresponding tumors based on the antibody. This type of boron drug formulation can be used in boron neutron capture therapy to kill tumor cells. It exhibits better killing effects; the compound of formula (I) targets tumor cells through antigen-antibody interaction. After the boron-10-containing drug accumulates at the tumor site, neutron radiation triggers a nuclear reaction releasing alpha particles and... 7 Lithium particles kill cells; the range of these two particles is approximately 10 μm. High-energy-density heavy ions disrupt the DNA double helix structure in tumor cells, causing irreparable cell death. Simultaneously, the 10 μm distance avoids damage to normal cells and tissues.

The application discloses a FAPI derivative containing 4-cyano thiazolidine modification and application thereof, relates to the field of drug compounds for diagnosing tumors, and provides a FAPI derivative containing 4-cyano thiazolidine modification, a chemical structural formula of which is shown as formula I. The FAPI derivative has good stability, is simple to prepare, has high radiochemical purity and good biological performance, and can be further used for clinical PET / CT tumor imaging, effectively solving the problems of low tumor uptake rate, short retention time and inability to further delay imaging of F-labeled FAPI probes. 18 The FAPI derivative containing 4-cyano thiazolidine modification can solve the problems of low tumor uptake rate, short retention time and inability to further delay imaging of F-labeled FAPI probes, and make up for the defects of the prior art.

We disclose a composition, comprising a compound, comprising a melanin precursor that spontaneously synthesizes a melanin when in free form in vivo, and a peptide directly covalently bonded to or indirectly linked to the melanin precursor, wherein the direct covalent bond or indirect link of the peptide to the melanin precursor blocks spontaneous synthesis of the melanin in vivo in the absence of protease activity. We also disclose methods of tumor imaging, tumor detection, diagnosis, and treatment, including methods comprising administering, to a patient suffering from a tumor, the composition; and either surgically resecting the tumor or thermally ablating the tumor, wherein the surgical resection is guided at least in part by contrast imparted by, or the thermally ablating targets cells containing, the melanin, wherein the melanin is spontaneously synthesized in the tumor after administering the composition.

The present application relates to the field of biological medicine, and provide a kind of targeting PSMA dimer compound and its derivative and application, the structure general formula of the dimer compound is as shown in formula (I).The dimer compound and its derivative of the present application have very high affinity and targeting to PSMA, after being labeled with suitable radionuclide, can be used as nuclear medicine molecular probe, to realize early diagnosis, staging and treatment of prostate cancer, 68 Ga]diPSMA-1-DOTA showed good tumor uptake in PET imaging of tumor mice.Therefore, this kind of radioactive complex has good clinical application prospect in tumor imaging targeting PSMA (especially PET imaging), and lays an important foundation for the radiotherapy application of [ 177 Lu]diPSMA-1-DOTA and [ 225 Ac]diPSMA-1-DOTA.

The invention relates to the technical field of nuclide probes, and discloses a COX-2 targeting nuclide probe as well as a preparation method and application thereof, and the COX-2 targeting nuclide probe comprises a radionuclide labeled compound as shown in a formula I; the targeting COX-2 nuclide probe provided by the invention can be used as a diagnosis and treatment reagent to be applied to tumors with high COX-2 protein expression in human or animal bodies, and is especially suitable for tumor imaging and radionuclide treatment; animal experiments show that the nuclide probe has a high tumor / muscle uptake ratio and shows good application potential. Formula I.

The invention discloses a nuclide-labeled compound targeting PSMA-TATE double targets as well as a preparation method and application of the nuclide-labeled compound. The nuclide-labeled compound is DOTA-PSMA-TATE labeled by < 68 > Ga or < 177 > Lu. The < 68 > Ga and < 177 > Lu labeled PSMA-TATE targeted double-target tumor developer provided by the invention is stable in property and good in imaging effect, and has high affinity and specificity to PSMA and TATE, and further preclinical animal experiment research proves that < 68 > Ga-DOTA-PSMA-TATE is expected to become a broad-spectrum tumor developer with a good application prospect, and < 177 > Lu-DOTA-PSMA-TATE is expected to become a treatment means.

The application relates to the field of organic chemistry and high polymer chemistry, in particular to a functionalized double-block copolymer and a preparation method and application thereof. The application provides a functionalized double-block copolymer, and a chemical structural formula of the functionalized double-block copolymer is shown as formula I. The functionalized double-block copolymer or polymer particle provided by the application can be widely applied in the fields of tumor imaging and tumor treatment, and has not only good safety, realizes faster and adjustable (by changing the number of pipe groups) degradation and removal of the polymer under an acidic condition, but also has excellent specific high-quality imaging effects at a target site, has characteristics of high signal-to-noise ratio, clear boundary, long half-life and the like, solves the problem of real-time intraoperative navigation of the fluorescence imaging technology, and thus has good industrialization prospects.

The present application relates to a kind of tyrosine derivatives and its preparation method, preparation raw materials and application.The above-mentioned tyrosine derivative has the following structural formula:Experimental demonstration, the above-mentioned tyrosine derivative is introduced by deuterium in traditional 18 F-tyrosine, which can improve the imaging target ratio and enhance the sensitivity of tumor imaging when used for the preparation of imaging agents.

The invention discloses a charge-assisted targeting cyclodextrin carrier molecule as well as a preparation method and application thereof, the cyclodextrin carrier molecule integrates cyclodextrin, an M2pep ligand and a pH response group through chemical connection to obtain a biologically safe carrier with a clear structure and simple components. The carrier molecule is used for loading a drug and constructing nanoparticles, and cyclodextrin is responsible for loading a fluorescent dye or a nuclear drug; the M2pep ligand provides an active targeting function for the tumor; on one hand, the pH response group adjusts the surface charge of the nano-particles to enable the nano-particles to be negatively charged and prolong the blood circulation time of the medicine, and on the other hand, the nano-particles respond to an acidic tumor microenvironment and are switched into positive charges to enhance the tumor targeting of the nano-particles. In addition, the nano-particles also have the characteristics of quickly developing tumors, retaining in the tumors for a long time and quickly removing in normal organs, so that the technical problems of low tumor drug delivery efficiency and more non-target organ accumulation in the prior art are solved.

The application discloses a kind of high specificity tumor imaging fluorescent probe, preparation method and application thereof, belong to fluorescent probe technical field, the structural formula of the fluorescent probe is as shown in formula III, formula IV: compared with the specificity fluorescent probe that currently exists, high specificity tumor imaging fluorescent probe III and IV will tumor growth attack system and tumor defense system combination, without introducing bulky targeting group in molecule, also do not need to obtain specific site by a large number of screening, with better performance-price ratio.Compared with the fluorescent probe I and II without being improved, high specificity tumor imaging fluorescent probe can effectively realize the distinction of normal cells and tumor cells at cell level.

This invention relates to the field of molecular probe technology, and more particularly to a near-infrared fluorescent probe, its preparation method, and its applications. The near-infrared fluorescent probe provided by this invention has the structure shown in Formula I. Through click chemical bridging, it enables convenient enrichment and identification of covalently targeted proteins, thereby simultaneously achieving high-sensitivity tumor imaging and in-depth proteomics analysis. The near-infrared fluorescent probe provided by this invention not only retains and optimizes the high-contrast tumor imaging capabilities of IR-780, but also serves as a highly efficient chemical proteomics tool, systematically revealing its target map and binding mechanism. Ultimately, it forms a platform technology integrating bright pan-tumor labeling and functional proteomics analysis, providing a solution to overcome tumor heterogeneity and advance the rational design of probes.

The invention is suitable for the technical field of medical instrument auxiliary equipment, provides a tumor ablation preoperative simulation system and device, and relates to a multi-module integration system for soft tissue ablation preoperative planning, scheme simulation and doctor-patient communication. In the embodiment provided by the invention, for a target patient needing ablation treatment, tumor imaging data (such as CT and MRI) of the patient are acquired, a digital model of a tumor and peripheral tissues is reconstructed through three-dimensional modeling software, a preliminary ablation scheme is adjusted to obtain a personalized ablation scheme of the user, and a solid mold is manufactured; based on the personalized ablation scheme, simulated ablation is conducted through a human body bionic material, ablation parameters are adjusted in the ablation process according to the real-time electric field distribution state and the actual ablation range, and therefore the personalized ablation scheme is further optimized; according to the final ablation scheme of the patient, the high-light-transmittance medical glass three-dimensional mold is manufactured, and visual support is provided for doctor-patient communication. According to the system and the device, the risk that important tissues are damaged due to ablation range deviation is effectively reduced, the distribution state of ablation energy is truly fed back through a human body bionic material, and the problem that the scheme optimization efficiency is low due to the fact that the feedback time of a waiting result of a traditional simulation ablation scheme is long is solved.

The invention relates to the field of synthesis of organic fluorescent dyes, and discloses a conjugate of indocyanine green and cholesterol as well as synthesis and application of the conjugate. The conjugate is formed by connecting an indocyanine green derivative and a cholesterol derivative through an amido bond; the indocyanine green derivative is ICG-R-COOH; iCG is indocyanine green, R is-(CH2) nH. [I-], n is an integer of 1-6, or R is-(CH2) mSO3-, and m is 3 or 4; and the cholesterol derivative is cholesterole-NH2, beta-sitosterole-NH2, stigmasterole-NH2 or ergosterole-NH2. The invention also discloses a preparation method of the cholesterol derivative. The lipidosome constructed by the conjugate is high in stability, good in dispersity and strong in NIR-II fluorescence, the blood vessel and tumor imaging contrast ratio and definition under a 1300 nm near-infrared imaging window are superior to those of lipidosome constructed by commercial ICG, more excellent diagnosis and treatment performance is shown, and wide application prospects are achieved.

The present application relates to the technical field of tumor fluorescence contrast agent, and specifically provides a kind of indocyanine green and multi-arm polyethylene glycol conjugate or its pharmaceutically acceptable salt and preparation method and purposes thereof, the conjugate has the structural formula shown in formula (I), the binding capacity of the conjugate with serum protein is significantly reduced, and the tumor targeting is significantly improved, accumulates and lingers in tumor tissue, to realize targeted treatment or high-resolution imaging, to realize more accurate tumor localization and diagnosis, with very high application value, and open up new method for tumor imaging and treatment development.

The application discloses a kind of 18 The application discloses a risk prediction method for myocardial physiological uptake of F-FDG PET / CT tumor imaging, candidate clinical data of malignant tumor patients who have undergone examination are collected, independent risk factors for myocardial physiological uptake are determined by using single factor and multi-factor logistic regression analysis, and a logistic regression prediction model and multiple machine learning prediction models are established. The ROC curve analysis is used to select the pending prediction model with the largest AUC value. Furthermore, the application evaluates whether the pending prediction model is the best prediction model through calibration curve analysis and decision curve analysis. The best prediction model can be used to predict whether a new patient has the risk of myocardial physiological uptake before the examination, which has the advantages of fast prediction speed, high accuracy and reliability.

The present invention relates to the field of molecular imaging, and more particularly, to a molecular probe targeting GPC3. The present invention sets forth a molecular probe targeting GPC3. The molecular probe is a compound having the following sequence, or a pharmaceutically acceptable salt or ester thereof: (GPC3 antibodies, comprising antibody fragments of GPC3 antibodies, or single domain antibodies thereof)m-Rn, wherein R is selected from a group consisting of a linking group, a chelating agent, a radionuclide, another targeting polypeptide or monoclonal antibody, a monoclonal antibody fragment, a single domain antibody, and a small molecule inhibitor, wherein n represents the number of R, n = 0-4, and m is not 0. The probe has good stability in vitro, clear imaging in tumors, and good specificity.

The invention provides a radioactive metal chelate as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The radioactive metal chelate contains a dye derivative capable of being efficiently chelated with radioactive metal, and is obtained by coupling a deferoxamine chelating group through a chemical bond by taking a heptamethyl carbon cyanine dye as a parent nucleus; the structure can be rapidly and efficiently coordinated with radioactive metal, so that the radioactive metal chelate which is high in labeling rate and keeps relatively good radiochemical stability in a protein-containing environment is obtained, the radioactive metal chelate is used for long-term tumor PET imaging, and the remarkable effect that the probe can realize long-term and high-contrast tumor imaging is realized; continuous visual monitoring and delayed diagnosis of malignant tumors can be realized, and a new technical path is provided for long-acting molecular imaging.

The invention discloses a water-soluble tetrasulfonic aza boron fluoride dipyrrole near-infrared fluorescent dye as well as a preparation method and application thereof. The fluorescent dye has the following structure: R is selected from-(CH2) nSO3-, and n is an integer greater than or equal to 2 and less than or equal to 6. The water solubility is remarkably improved through tetrasulfonic acid group modification, the fluorescent probe shows high fluorescent brightness in a water solution, the maximum emission wavelength is about 725 nm, the fluorescent probe is located in a biological tissue optical window, and high-contrast imaging of deep tissue is facilitated. Compared with clinical indocyanine green (ICG), the water solubility, the fluorescence quantum yield and the light stability are remarkably improved, the molar extinction coefficient is high, and the photobleaching rate is low; the synthesis route is simple, the repeatability is good, the product is easy to purify, and the biocompatibility is good. The dye is applicable to real-time navigation, tumor imaging and blood vessel visualization in fluorescence-guided surgery, and shows excellent clinical application potential and industrialization prospect.

This invention provides a c-MET-targeting nuclide probe, its preparation method, and its applications, relating to the field of nuclide probe technology. The c-MET-targeting nuclide probe comprises a compound of formula I labeled with a radionuclide. The c-MET-targeting nuclide probe of this invention can be used as a diagnostic and therapeutic agent in human or animal lesions with high c-MET protein expression, particularly as a tumor imaging agent and a radionuclide therapeutic drug.

The application discloses a polypeptide positive probe targeting PD-L1 and a preparation method and application thereof, and provides a polypeptide compound, which is obtained by combining different connecting groups and metal ion chelating agent NOTA on the basis of the structure of a PD-L1 polypeptide CLP002. The polypeptide compound is combined with a nuclide to obtain two PD-L1-targeting polypeptide molecular probes. The two polypeptide probes have high molar activity and good in-vivo and in-vitro stability, can be quickly distributed to the whole body in a model animal, are partially taken up in a PD-L1 positive tumor, are quickly removed from the body, can obtain a PET image with a high target / non-target ratio, and can monitor the expression level and change of PD-L1 in a tumor in real time, dynamically and non-invasively at a molecular level. Therefore, the polypeptide probes have a clinical application prospect in a PD-L1-targeting imaging agent and a tumor imaging drug.

The present invention relates to a gene construct characterized by encoding a fusion protein of flgM and Strep-tag through the linkage of an anti-sigma factor flgM gene and a gene encoding Strep-tag, enabling the expression of Strep-tag on the surface of an anti-cancer strain that can target tumor sites and stimulate immune activity, and to an anti-cancer adjuvant and tumor imaging agent that, when transformed by this construct, exhibits anti-cancer activity itself and can be effectively utilized in the diagnosis and treatment of tumor cells together with anti-cancer substances or contrast agents labeled with substances specifically interacting with Strep-tag.

This invention discloses nucleic acid aptamer-functionalized ultrasmall luminescent gold nanoparticles, their preparation method, and applications. The method involves: reacting an aqueous solution of chloroauric acid with an aqueous solution of glutathione ligand at room temperature until the reaction color becomes colorless; then adding a thioylated nucleic acid aptamer; followed by the addition of an aqueous solution of sodium borohydride; reacting until the solution turns brown; stopping the reaction; ultrafiltration; and finally, precipitating the nucleic acid aptamer-functionalized gold nanoparticles using an ethanol solution containing magnesium chloride and sodium chloride to remove free thioylated nucleic acid aptamers from the supernatant; redissolving the precipitate with buffer and water; and storing the concentrated precipitate at 4°C to obtain the nucleic acid aptamer-functionalized gold nanoparticle material. The product of this invention exhibits good biocompatibility, low toxicity, low fluorescence background interference, high detection sensitivity, and good selectivity. It is simple to operate for cell and tumor imaging research and can achieve non-invasive, high-resolution, and low-signal-to-background early diagnosis of in vivo tumors.

The invention discloses a near-infrared two-region fluorescent dye, which takes squaric acid dye as a framework, takes 4-methylene phenylboronic acid ester as a substituent group, and can form a stable J-aggregate without carrier coating. The synthesis method comprises the following steps: carrying out nucleophilic addition reaction on diethyl squarate and malononitrile under the catalytic action of weak base triethylamine to obtain a first intermediate product; carrying out electrophilic substitution reaction on the 4-methylquinoline and the 4-bromomethylphenylboronic acid pinacol ester to obtain a second intermediate product; and carrying out nucleophilic addition reaction on the two intermediate products to obtain the near-infrared two-region fluorescent dye. Compared with the traditional fluorescent dye with J-aggregation property, the J-aggregate constructed by the fluorescent dye disclosed by the invention has the remarkable advantage of long absorption / emission wavelength, the maximum emission peak red shift reaches about 1345 nm, the stable J-aggregate can be formed without carrier coating, and the J-aggregate has good biological safety and can be used for preparing the fluorescent dye with the J-aggregation property. The fluorescent probe can be applied to in-vivo angiography, tumor imaging, surgical navigation and the like through fluorescence imaging.

The application provides a kind of contrast agent based on Gd-DOTBA skeleton and its preparation method and application, belongs to the technical field of contrast agent.The contrast agent based on Gd-DOTBA skeleton is glucose small molecule gadolinium complex Gd-DOTBA-Glc and thiol-maleimide coupled Gd-DOTBA-Mal-Cys and Gd-DOTBA-Mal-GSH.The contrast agent prepared by the application has high longitudinal relaxivity and excellent stability, and can sensitively evaluate renal dysfunction with half dose, has tumor imaging ability, establishes a four-valent, plug-and-play platform for advanced molecular MRI probe development, and perfectly solves the contradiction that high sensitivity and high safety are difficult to achieve in the prior art.