490results about "General/multifunctional contrast agents" patented technology

The present invention relates to zwitterionic metal chelators and their use as imaging, diagnostic, chemical processing, and treatment agents. These zwitterionic metal chelators have desirable properties that maximize solubility in aqueous environments, minimize non-specific interactions, and retain the ability to target thus resulting in an improved performance in a variety of medical, agricultural, and chemical processes. In in vivo and medical applications, zwitterionic metal chelators improve the signal-to-background ratio and therapeutic window as compared to other metal chelators while retaining high stability.

The invention discloses a medical developing marker and a manufacturing method thereof, and relates to the field of medical instruments, the medical developing marker comprises a closed tube, the outer wall of the closed tube is provided with a bionic barb structure, the bionic barb structure is distributed in a flexible zigzag convex manner, and the bionic barb structure and the closed tube are integrally formed through an injection molding process; a closed cavity is arranged in the closed tube, four developing strips are symmetrically arranged in the tube wall of the closed cavity, the tube wall of the region where the developing strips are located is etched to form a weak band, and a developing material layer and a sustained-release medicine layer are sequentially deposited at the weak band. The developing material layer and the sustained-release drug and / or marked nano-particle layer are alternately deposited to form a functional composite layer, and the functional composite layer can directionally rupture to release the therapeutic drug under the action of implantation pressure. The marker integrates the functions of precise development, tissue anchoring and drug sustained release, is adaptive to multi-mode imaging such as ultrasonic imaging, X-ray imaging, CT imaging, MRI imaging and PET-CT imaging, and has remarkable clinical value in precise positioning treatment of solid tumors such as breast cancer and liver cancer.

Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I):or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, L, L1, L2, L3, L4, M and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

The invention discloses a multi-metal borate nano-particle as well as a preparation method and application thereof. The preparation method comprises the following steps: in the presence of small molecules with alkyl chains, performing high-temperature thermal decomposition on an organic metal compound or a metal salt compound precursor and organic borate in a solvent, and then centrifuging, modifying, performing ultrafiltration, dialyzing and purifying to obtain the multi-metal borate nanoparticles. The preparation method disclosed by the invention has the characteristics of mildness, high efficiency and strong controllability. The multi-metal borate nanoparticles prepared by the preparation method disclosed by the invention have the advantages of monodisperse size, relatively high magnetic property and good biocompatibility. Therefore, the prepared multi-metal borate nanoparticles not only have multi-modal imaging functions such as magnetic resonance imaging, near-infrared two-region imaging, nuclear medicine imaging and magnetic particle imaging, but also can be used for various treatment means such as magnetocaloric therapy and boron neutron capture therapy; potential advantages are realized in biomedical applications such as magnetic targeting tumor treatment and imaging contrast agents, and high practical values are realized.

The invention discloses nanoparticles for a contrast agent as well as a preparation method and application of the nanoparticles, and relates to the technical field of nano composite materials. According to the nanoparticle for the contrast agent, a shell layer comprises polydopamine and albumin which are connected through a covalent bond, a core structure comprises a complex formed by metal ions and polyphenol, and the metal ions in the core structure and the polydopamine in the shell layer also have a coordination effect. Due to the fact that all the components are tightly connected, the rotation time of the nano-particles is prolonged, the T1 relaxation rate of the nano-particles is greatly increased, meanwhile, due to introduction of polydopamine, release of metal ions in a human body is avoided, the biological safety of the nano-particles is improved, albumin in the nano-particles can further improve the biocompatibility of the particles, and the nano-particles can be used for preparing the nano-particles. Therefore, the nanoparticles provided by the invention also have wide application prospects in the fields of fluorescence imaging and targeted drug delivery.

The invention provides a whole-process targeting polypeptide, a drug compound thereof, a drug delivery system and application of the whole-process targeting polypeptide. The whole-process targeting polypeptide comprises pHA and VAP which are covalently connected through a bridging structure; the VAP is LVAP, a reverse sequence polypeptide of the LVAP, DVAP or SVAP; wherein the amino acid sequence of the LVAP is as shown in SEQ ID NO: 1; the SVAP is a D-configuration polypeptide of the LVAP; the DVAP is a D-configuration polypeptide of the LVAP inverted sequence polypeptide; the bridging structure is amino-monoethylene glycol-carboxylic acid or a derivative thereof. The whole-process targeting polypeptide not only can cross a blood-brain barrier, target tumor neovascularization, cross a blood-tumor barrier, target tumor mimicry vessels, tumor cells and stem cells thereof, but also has better tumor cell affinity, anti-tumor treatment and in-vivo safety effects. Meanwhile, the drug compound or the drug delivery system has a synergistic effect after being combined with a chemotherapeutic drug, and the anti-tumor drug effect can be remarkably improved.

Described herein are compositions, systems, and methods for targeted and controlled drug release. In some embodiments, the compositions, systems, and methods may comprise magnetoelectric silica nanoparticles for targeted and controlled release of chemotherapeutic drugs for cancer treatment. In some embodiments, an external magnetic field may be used to release one or more drugs from the magnetoelectric silica nanoparticles. The disclosed compositions, systems, and methods may improve drug targeting and reduce systemic drug toxicity.

The invention discloses a multi-active targeting tumor nano-drug with a multimode imaging function and an immune activation effect and a preparation method thereof, and belongs to the technical field of nano-drugs. The preparation method comprises the following steps: coupling inorganic metal-based nano particles / nano drugs with a multimode imaging function or / and targeting active organic biomolecules with specific functions and specific therapeutic drugs through a silane cross-linking agent or a combination of the silane cross-linking agent and a carbodiimide condensing agent; the active targeting type organic-inorganic composite nano-drug aggregate with a multi-mode imaging function and an immune activation effect is prepared. Wherein the inorganic component is a metal-based heterostructure nanoparticle with a multimode imaging function, and the organic component is a bioactive molecule or / and a specific therapeutic drug. The obtained nano-drug aggregate is stable in system, uniform and controllable in size and good in biocompatibility, and has specific targeting, such as specific targeting liver cancer cells.

The invention relates to a gadolinium-doped carbon dot complex based on liver cancer cell membrane coating and a preparation method of the gadolinium-doped carbon dot complex. The gadolinium-doped carbon dot complex is prepared on the basis of gadolinium-doped carbon dots Gd-CDs which are prepared from indocyanine green, citric acid, polyethylene glycol and gadolinic acid through a one-step microwave thermal method and have fluorescence-magnetic resonance bimodal imaging capacity. The Gd-CDs complex Gd-CDs coated HCM is placed in a cell membrane suspension extracted from human hepatoma carcinoma cells HepG2, and the Gd-CDs complex Gd-CDs coated HCM which is uniform in particle size and has the capacity of photothermal and immunotherapy of hepatocellular carcinoma is obtained through extrusion construction of a liposome extruder. The Gd-CDs (at) HCM complex constructed by the invention not only has good bimodal imaging ability, but also has a specific inhibition effect on liver tumor cells, can be applied to preparation of drugs for inhibiting the growth of the liver tumor cells, and realizes a good treatment effect on liver cancer at a nanometer level.

The invention discloses a radionuclide-labeled collagen hybrid peptide probe as well as a preparation method and application thereof. The chemical structural general formula of the radionuclide-labeled collagen hybrid peptide probe is (metal nuclide-chelating agent)-Linker-CHP, wherein the metal nuclide is selected from any one of Al18F, 64Cu, 67Cu, 67Ga, 68Ga, 99mTc, 89Zr, 111In, 177Lu, 186Re and 225Ac, and the metal nuclide is selected from any one of Al18F, 64Cu, 67Cu, 67Ga, 68Ga, 99mTc, 89Zr, 111In, the chelating agent is selected from any one of NODAGA, NOTA2 and DOTA; linker is a connecting joint, and CHP is a collagen hybrid peptide with a polypeptide sequence of (GfO) n or (GPO) n. The probe not only has the characteristic of radiochemical marking stability, but also has the excellent biological distribution characteristics of high uptake in target organs such as tumors and low uptake in non-target organs such as liver and kidney, and has a good clinical application prospect.

The present invention relates to labeled compounds suitable for positron emission tomography (PET) imaging and / or fluorescence imaging such as near-infrared fluorescence imaging (NIRF). The invention further relates to the use of these compounds for carrying out PET scans. imaging calcium sensing receptor (CSR)-positive organs. excising parathyroid tissue. protecting parathyroid tissue during thyroid surgery, and treating disorder(s) of a CSR-positive tissue in a subject.

Keto-amide based FAP-targeted ligands, conjugate comprising same, pharmaceutical compositions comprising same, and methods of use for imaging and treatment.

The invention discloses a polyethylene glycol modified gold and manganese dioxide nano particle and a preparation method and application thereof, and belongs to the technical field of biological medicine, the polyethylene glycol modified gold and manganese dioxide nano particle (GMCN and PEG) has good biocompatibility under neutral physiological conditions, can relieve tumor hypoxia and increase generation of active oxygen in acidic TME, and has a good anti-tumor effect. The radiotherapy sensitivity is improved; and immune cell death is induced. Meanwhile, a cGAS-STING signal channel can be activated, dendritic cell maturation, macrophage M1 polarization and T cell infiltration are promoted, and the immunosuppression state in TME is counteracted. In addition, the GMCN-coated PEG also has an MR-CT bimodal imaging enhancement function, and integration of diagnosis and treatment is realized. The nano sensitizer disclosed by the invention has huge potential in the aspects of improving the radiotherapy curative effect, remodeling the tumor microenvironment, promoting the anti-tumor immunity, enhancing the biomedical imaging and the like.

A mesoporous silica nanoparticle (“MSN”); a bioactive agent loaded into the MSN and an enteric coating encapsulating the surface of the MSN for oral administration or combination with more than one other pharmaceutical composition each having distinct bioactive agents.

The tumor stroma, which accounts for a large portion of the tumor mass, is an attractive target for the delivery of diagnostic and therapeutic compounds. Here, we focus specifically on a subpopulation of stromal cells known as cancer-associated fibroblasts, which are present in over 90% of epithelial cancers, including pancreatic, colon, and breast cancers. Cancer-associated fibroblasts are characterized by high expression of FAPs, which are undetectable in adult normal tissues but are associated with poor prognosis in cancer patients. The present invention provides small molecule radiopharmaceuticals and imaging agents based on FAP-specific inhibitors.

This disclosure relates to polyethylene glycol (PEG)-functionalized nanoparticles comprising a functional agent, and preparation methods, properties and applications thereof. The nanoparticle represented by PEG-L-G / P, comprising a type of hydrophilic PEG, a hydrophobic functional agent G, which are covalently linked by L: a linker or a chemical bond, and a type of hydrophobic polymer P. The G and P form the hydrophobic core, while the PEG constitutes the hydrophilic outer layer of the nanoparticle in an aqueous medium. The functional agent comprises one or more functional compounds including a therapeutic drug, an imaging diagnostic agent, a photoelectric responsive diagnostic agent, an immune-stimulating agent, or a combination thereof. The nanoparticles comprising such functional agent can offer various applications in multiple biomedical fields.

Low-molecular weight gadolinium (Gd)-based MR contrast agents for PSMA-specific T1-weighted MR imaging are disclosed. The (Gd)-based MR contrast agents exhibit high binding affinity for PSMA and exhibit specific T1 contrast enhancement at PSMA+ cells. The PSMA-targeted Gd-based MR contrast agents can be used for PSMA-targeted imaging in vivo. 86Y-labeled PSMA-binding ureas also are provided, wherein the PSMA-binding ureas also are suitable for use with other radiotherapeutics.

The invention belongs to the technical field of biochemistry, and relates to a fluorescence / photoacoustic bimodal probe responding to Cu (I) and a preparation method and application thereof. The fluorescence / photoacoustic bimodal probe responding to Cu (I) has high selectivity and sensitivity, has efficient tumor targeting ability, can be used for dynamic tracing of Cu (I) in tumor, can dynamically image Cu (I) in tumor by combining with a three-dimensional photoacoustic / living body fluorescence imaging technology and the probe HCyCu1, provides a new detection means for detection of Cu (I), and has wide application prospects. And a potential tool is provided for tumor diagnosis. According to the preparation method of the bimodal probe, the adopted raw materials are easy to obtain, the reaction conditions are mild and easy to control, the reaction cost is saved, and the yield of a target product is guaranteed. The structural formula of the probe is as follows: # imgabs0 #.

This disclosure relates to polyethylene glycol (PEG) -functionalized nanoparticles comprising a functional agent, and preparation methods, properties and applications thereof. The nanoparticle represented by PEG-L-G / P, comprising a type of hydrophilic PEG, a hydrophobic functional agent G, which are covalently linked by L: a linker or a chemical bond, and a type of hydrophobic polymer P. The G and P form the hydrophobic core, while the PEG constitutes the hydrophilic outer layer of the nanoparticle in an aqueous medium. The functional agent comprises one or more functional compounds including a therapeutic drug, an imaging diagnostic agent, a photoelectric responsive diagnostic agent, an immune-stimulating agent, or a combination thereof. The nanoparticles comprising such functional agent can offer various applications in multiple biomedical fields.

The invention discloses preparation and application of an ovarian cancer cell membrane bionic nano sound-sensitive agent, and belongs to the field of pharmacy. The technical problem to be solved by the invention is to provide the preparation method of the ovarian cancer cell membrane bionic nano sound-sensitive agent. The method is based on the homologous targeting property and immune escape property of an ovarian cancer cell membrane to ovarian tumor cells, the SKOV-3 source ovarian cancer cell membrane (CCM) is innovatively coated on the surfaces of mesoporous silica-titanium nanoparticles (MSTN) encapsulated by manganese dioxide (BSA-MnO2), and a water-soluble sound-sensitive agent azoic compound 2, 2 ', 2', 2 '-tetramethyldisiloxane is added into the mesoporous silica-titanium nanoparticles (MSTN) to prepare the SKOV-3 source ovarian cancer cell membrane. And encapsulating 2, 2 '-azobis [2-(2-imidazoline-2-yl) propane] dihydrochloride (AIPH) into mesopores of the MSTN to prepare the ovarian cancer cell membrane bionic nano sound-sensitive agent. The ovarian cancer cell membrane bionic nano sound-sensitive agent prepared by the invention is high in biocompatibility, strong in targeting specificity and good in stability, and can effectively escape from immune system recognition and elimination. On the basis, the ovarian cancer cell membrane bionic nano sound-sensitive agent can effectively realize targeted ultrasound and magnetic resonance (MRI) bimodal imaging of the sound-sensitive agent to ovarian cancer cells, effectively realize fixed-point and quantitative release of drugs, achieve adjustable diagnosis and treatment of ovarian cancer, and is expected to provide a new thought for clinical early diagnosis and precise treatment of ovarian cancer.

Disclosed herein are peptide urea derivatives, pharmaceutical compositions thereof and uses thereof. The derivatives are represented by formula I, in which R is a group containing a radioactive metal ion or an optically imageable group. The derivatives can be used for preoperative imaging diagnosis and grading of PSMA-positive prostate cancer, and can also be used for the treatment of various types and stages of prostate cancer, realizing the integration of diagnosis and treatment, and are expected to be widely used. JPEG2025505467000166.jpg32157

The invention described herein pertains to the diagnosis, imaging, and / or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and / or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

The invention discloses an iron-based metal nano diagnosis and treatment agent as well as a preparation method and application thereof. The iron-based metal nano diagnosis and treatment agent comprises an iron-based metal nano material and a diagnosis and treatment agent loaded with therapeutic nuclide 177Lu and / or a micromolecular chemotherapeutic drug F16. The iron-based metal nano diagnosis and treatment agent contains an iron element, can be used for MRI imaging and can induce tumor ferroptosis at the same time, radionuclide 177Lu can emit gamma rays for SPECT imaging and can emit beta rays for tumor internal radiotherapy, tumor mitochondria targeting small molecule medicine F16 has the fluorescence characteristic and can be used for tumor real-time fluorescence imaging, and the application range is wide. Meanwhile, a mitochondrial targeting tumor killing effect is achieved. Therefore, the iron-based metal nano diagnosis and treatment agent disclosed by the invention can realize comprehensive collaborative treatment of intratumor radiotherapy, targeted chemotherapy and ferroptosis under the guidance of MRI (Magnetic Resonance Imaging), SPECT (Single Photon Emission Computed Tomography) and multi-mode imaging of fluorescence imaging, and improves the precise diagnosis and treatment of tumors.

The invention provides a series of cyanine or cyanine-like multifunctional probe molecules which are derivatives with a near-infrared cyanine dye molecular skeleton, and the skeleton is modified with any one or a combination of more than two of a protein affinity agent structure, a targeting group or a functional group; the near-infrared cyanine dye molecule is a near-infrared indole cyanine dye molecule or a near-infrared naphthopyrrole cyanine or flavonoid dye molecule; the structure of the protein affinity agent is from a 4 (p-iodophenyl) butyric acid derivative, Evans blue or a derivative thereof; the targeting group is a structure containing any one pharmaceutically acceptable targeting peptide; the functional group comes from any nuclide chelating agent or a functional drug molecule with a modification site. The multifunctional probe molecule provided by the invention can realize clear near-infrared first-region and second-region lymphatic imaging and angiography, and has good biological safety and adjustable circulation metabolism time at the same time. The invention also provides a method for preparing the multifunctional probe molecule and application of the multifunctional probe molecule in multi-mode diagnosis and treatment.

The invention provides a nano material suitable for multi-mode diagnostic imaging and targeted photodynamic (PDT) and photo-thermal (PTT) cancer therapy, and belongs to the field of nano biomedicine. According to the invention, an upconversion material (NaYF4: Yb / Er / Gd) and a photo-thermal material (Bi2Se3) are taken as a core, mesoporous silica is taken as a shell, and a photosensitizer (Ce6) and lipid / PEG and acidity-triggered membrane (ATRAM) peptide coated on the surface of the shell are loaded. The PDT and PTT synergistic anticancer effect achieved through near-infrared laser induction is achieved, magnetic resonance imaging, thermal imaging and fluorescence imaging of tumors can be achieved, and the requirement for diagnosis and treatment integration is met. In addition, the in-vivo lifetime of the nano-carrier is effectively prolonged through lipid / PEG, and aggregation and premature degradation of the nano-carrier are prevented; and the pH-mediated acidity-triggered membrane peptide is utilized to improve the uptake of cancer cells to the nano-carrier, so that the effect of the nano-carrier and the cancer cells is enhanced.

The present invention provides a glutathione-activated co-assembled nanoprobe and a preparation method and application thereof, belonging to the technical fields of chemical synthesis, biological analysis and detection, tumor imaging and treatment. In the present invention, amphiphilic small molecule probes 1-Zn-PPA and 1-NLG are constructed, and the probes 1-Zn-PPA and 1-NLG can be co-assembled in a solution to form co-assembled nanoprobes 1-NPs. The nanoprobes 1-NPs can accumulate at the tumor site under the tumor EPR effect and the targeting action of cRGD on the probe surface, and disassemble under the action of GSH present in the tumor reducing environment to release Gd-containing hydrophilic small molecule 2-Gd, light / sound-sensitive drug Zn-PPA-SH and immune adjuvant drug NLG919. The nanoprobes 1-NPs can realize combined sonodynamic therapy / photodynamic therapy / immunotherapy of living tumors. The nanoprobes 1-NPs have good applications in fluorescence imaging, magnetic resonance imaging, and the preparation of tumor treatment drugs and tumor-killing devices.

The present invention relates to a particulate structure comprising: a / biodegradable polymer particles; b / gold nanoparticles whose surfaces are coated with a macrocyclic chelating agent that complexes at least one target ion and / or radionuclide for medical imaging; and c / a polycation that has a positive charge over a pH range of 5 to 11, wherein the gold nanoparticles b / are encapsulated in the polymer particles a / and / or adsorbed to the surface of the polymer particles a / . The present invention also relates to a method for producing the particulate structure. The present invention further relates to the use of the particulate structure for radiotherapy or chemotherapy in cancer treatment.