47results about How to "High target/non-target ratio" patented technology

The invention discloses an Evans blue complex as well as a preparation method and application thereof. The Evans blue complex structurally contains macrocylic polymine chelation groups NOTA. A marker complex is obtained after marking by using radionuclides (Fluorine-18, copper-64, gallium-68 and the like). The marker complex is prepared by using a wet process or a lyophilisation method. The invention further relates an application of the complex as a developer in organs or tissues of human or animals, and especially a blood pool developer. The Evans blue complex has the advantages of low cost and higher target-to-nontarget ratio, and is simple to prepare.

The invention provides an RGD polypeptide coordination complex of a radioactive nuclide label. According to the structure of the coordination complex, the radioactive nuclide is selected from 64Cu, 68Ga, 111In, 62Cu, 67Cu, 67Ga, 86Y, 89Zr or 18F; the ligand is a ligand compound containing an RGD structure, which is shown in a formula (I). The coordination complex has stronger ligand stability and high target / non-target ratio, and the appetency of the ligand with integrin AlphavBeta3 is stronger. The invention further provides a preparation method of the coordination complex, and an application of the coordination complex in preparing tumor developers.

The invention discloses a radioactive iodine marked protein binding ligand and application thereof. A structural formula of the radioactive iodine marked protein binding ligand is shown in a followingimage, wherein the I is radioactive iodine nuclide, the R is OH or derived from PEG, folic acid, RGD, octreotide, epidermal growth factor, protein, nucleic acid or polysaccharide. The radioactive iodine marked protein binding ligand disclosed by the invention has the advantages of simple marking method, low cost and good stability. Animal live test results show that the albumin binding ligand hashigher uptake and longer-time retention in blood and further has a higher target / non-target specific value. When the radioactive iodine marked protein binding ligand is modified to a target group orother functional groups, pharmacokinetic characters of compound can be obviously improved, a blood half-life period of the compound is prolonged, and the compound is suitable for being utilized as a blood pool, lymph and tumor diagnosing and treating reagent.

The invention discloses a trans-oligonucleotide probe contrast-medium to mark superparamagnetism iron oxide, which consists of carrier constituted by gluglucosan enveloped by ferroferric oxide nanometer particle with superparamagnetism and trans-oligonucleotide segment of c-erbB2 cancer gene, wherein the trans-oligonucleotide connects the gluglucosan in the carrier at covalent bond. The invention also relates to a making method of the contrast-medium. The invention uses trans-gene technique of molecular biological domain into imaging diagnosis to combine the superiority and specificity of two advanced techniques, which increases the ratio of target / non-target of probe to the maximum degree to scan the size, position and anatomical relationship of adjacent structures of tumour through magnetic resonance, in order to build new imaging method of early-stage tumor diagnosis of specificity on the gene level. The invention can be applied to do early-stage imaging diagnosis for malignant tumour, epoophoron cancer, uterine neck cancer, esophagus cancer and cervical scale cancer.

The invention provides a multifunctional imaging probe. The multifunctional imaging probe is a radionuclide labelled peptide complex and takes a peptide compound which has the structure as shown in the formula (I) defined in the description and has the tumor targeting fluorescence imaging function, wherein X is a NOTA radical group or-CH2-, R is targeting peptide BBN with the structure as shown in the formula (II) defined in the description or targeting peptide RM26 with the structure as shown in the formula (III). The multifunctional imaging probe can be used for positron emission computer tomography (PET) and optical imaging simultaneously. The invention further provides a preparation method of the functional probe and application in preparation of a human or animal organ or tissue imaging agent, precise positioning on the tumor boundary can be achieved through application, and the advantages of real-time performance, high precision, high specificity, high sensitivity and high resolution are brought to preoperative and intraoperative imaging navigation.

The invention provides a polypeptide compound with a HER2 targeting function. The polypeptide compound with the HER2 targeting function is formed by connecting a HER2 affinity with a bifunctional chelating agent through a polypeptide sequence; the polypeptide sequence is Met-Val-Lys; the general structural formula of the polypeptide compound is shown in formula (I) as shown in specification, wherein R is a HER2 affinity molecule and X is a bifunctional chelator group. The invention also provides a radiolabelled complex targeting HER2 by taking the polypeptide compound as a ligand. The radiolabeled complex provided by the invention can be used as a radioactive diagnostic probe for evaluating the HER2 receptor of breast cancer, and the probe can reduce the concentration of the kidney under the condition of keeping the uptake of the tumor unchanged, so that the target-to-non-target ratio of the tumor is improved, and the radiation dose to the kidney is reduced. The invention also provides a preparation method of the polypeptide compound and the radiolabelled complex, and application of the polypeptide compound and the radiolabelled complex in preparation of a HER2 positive breast cancer radioactive diagnosis and treatment probe for humans or animals.

The invention discloses a targeted probe for nuclide labeling and a preparation method and an application of the targeted probe. A general structural formula of a complex is as shown in the specification, wherein R' is a nuclide chelating group; R is a targeted group; Dn is a molecular skeleton which is formed by repeated michael addition reaction and amidation reaction employing propargylamine as an initial reactant, the peripheral group is amino, n represents different algebras, and the numerical value of n is an integer greater than or equal to 0; and m is equal to 2n. A polymer in the targeted probe for nuclide labeling is beneficial to improvement of the specific activity; a high-quality developing result can be obtained by instrument scanning; the targeted probe can play a role in effectively monitoring tumors or inflammatory diseases; meanwhile, carrying of relatively many nuclides on a molecule is facilitated by the formed polymer; the nuclide concentration of focus location is improved; and the targeted probe plays a relatively good treatment role.

The invention discloses a prostate-specific membrane antigen inhibitor, a radionuclide labeled substance thereof, a preparation method and application, and belongs to the technical field of biological medicines. The chemical structure of the prostate-specific membrane antigen inhibitor is shown as a formula I, the chemical structure of the radionuclide labeled substance is shown as a formula II, and the prostate-specific membrane antigen inhibitor is used for preparing prostate cancer diagnostic reagents / drugs or / and therapeutic drugs. The compound is novel in structure and stable in physicochemical property, and can be used for preparing drugs for diagnosis and treatment of prostate cancer and be applied to the fields of diagnosis, staging, curative effect evaluation and treatment of prostate cancer.

The invention relates to an 18 / 19F-ester nitroimidazole compound, preparation method thereof and application as a hypoxic tissue developing agent. The invention provides F-ester nitroimidazole compounds as shown in a general formula, wherein an 18F-ester nitroimidazole compound is a radioactive compound. According to an S180 tumor-bearing mice experiment, the 18F-ester nitroimidazole compound has the characteristics of good tumor targeted intake and low liver background level, and is a potential positron emission tomography (PET) hypoxic tissue developing agent.

The invention discloses a novel bone seeking complex. The complex comprises a nuclide <99m>Tc and a ligand, wherein the ligand is a diphosphate derivative containing NO-donors and has a general formula represented by the following formula, wherein R1 is an aliphatic hydrocarbon, an aromatic ring or a nitrogen-containing heterocyclic ring containing 1 to 2 NO-donors; X is a group of -H, -OH, -NH2 and the like; Y is oxygen, sulfur or amino; and n is an integer between 2 and 9. The invention also discloses a preparation method for the complex and application of the complex as a bone imaging agent. Compared with the current bone imaging agent <99m>Tc-MDP widely used in the clinic at home and abroad, the bone imaging agent has high bone tissue initial stage uptake, long stay time and low non-target tissue uptake, particularly low liver uptake, and is expected to become a novel bone imaging agent with better performance.

The invention provides a dimeric amido benzimidazole compound. The structure of the dimeric amido benzimidazole compound is shown as a formula (I), wherein R0 is an integer of n from 0 to 5. The invention also provides a compound with anti-tumor activity and a radionuclide labeled compound targeted by interferon stimulating protein, wherein the compound is based on the dimeric amido benzimidazole compound. The dimeric amido benzimidazole compound has high affinity and high specificity to interferon stimulating protein, the compound with anti-tumor activity has the characteristic of activating an STING pathway in vitro, and the radionuclide labeled compound has the advantages that target uptake and non-target uptake are obviously compared, and the lipid solubility can be changed by introducing nuclides with different properties so that the application scene is greatly widened, and the compound can be combined with treatment nuclides for tumor treatment, and even can be used for immunotherapy.

The invention provides novel 18F labeled substituted benzimidazole compounds, which are characterized in that: one end of each compound contains an 18F substituted alkoxy structure, and the other end contains a 6-carboxyl / H benzimidazole structure; a substituent group R1, located on the site 2 of benzimidazole matrix, is hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, benzyl, 2-methylthio ethyl and phenyl; a substituent group R2, located on the site 4 of benzimidazole matrix, is hydrogen, methyl and ethyl; and the structure of the compound is shown in formula A, wherein n is between 1 and 5, R2 is H, Me and Et, X is COOH and H. Experiments show that the compounds have high bioactivity such as fast serum removal, high serum stability and relatively low intake in tissues or organs such as liver and relatively high enrichment and slow removal rate in tumor cells, and therefore the compounds have relatively high tumor / background value and are favorable for PET tumor imaging. Meanwhile, the labeled precursor of the compounds is easy to synthesize and the labeling rate is extremely high; and such advantages indicate that the compounds have the tremendous potential to become PET tumor imaging agents.

The invention discloses a two-dimensional palladium-based probe with radioiodine labeling and a preparation method and application of the probe. The probe comprises a two-dimensional palladium-based nanomaterial, a PEG linking molecule, a targeting group R and radioiodine, a thiol group is arranged at one end of the PEG linking molecule, a modifiable group is arranged at the other end of the PEG linking molecule, one end of the PEG linking molecule is linked to the two-dimensional palladium-based nanomaterial through the above thiol group, the other end is linked to the targeting group R through the modifiable group, and radioiodine is directly labelled on the two-dimensional palladium-based nanomaterial. According to the present invention, a plurality of radioiodine can be carried on a unit of nanocarrier based on the strong binding force between the two-dimensional palladium-based nanomaterial and halogen ions, the probe has the characteristics of strong labeling ability, short labeling time, high labeling yield and no need of subsequent purification before application, and is more conducive to commercial application and clinical promotion of markers.

The invention discloses a prostate specific membrane antigen inhibitor, a metal marker, a preparation method and application thereof, and belongs to the technical field of biological medicines. The structure of the prostate specific membrane antigen inhibitor is shown as a formula I, the structure of the metal marker is shown as a formula II, and the prostate specific membrane antigen inhibitor isused for preparing a prostate cancer diagnosis reagent / drug or / and a treatment drug. The compound is novel in structure and stable in physicochemical property, and can be applied to the fields of diagnosis, staging, curative effect evaluation and treatment of prostate cancer in preparation of prostate cancer diagnosis and treatment medicines.

The invention discloses 18F-E[c(RGDyk)2], a medicine box used for automatic production thereof, and a preparation method and use of the medicine box, relates to a polyethylene terephthalate (PET) developer and a preparation method and use thereof and relates to the technical field of radiative medicines and nuclear medicines. The medicine box contains a raw material reagent A and a raw material reagent B. A bottle A contains E[c(RGDyk)2]-NO2; and A bottle B contains acetonitrile solution of crown ether K222 / K2CO3. The 18F-E[c(RGDyk)2] prepared by the medicine box has high absorbing performance and excellent retaining performance in model mouse tumor, and has a very high target / non target ratio, excellent pharmacokinetic characteristic and high biological performance, and can completely meet the requirements of PET developer of tumour integrin alphavbeta3 receptor.

The invention provides a antisense short nucleotide of c-erbB2 cancer gene whose sequence is: SEQ ID NO 1. The antisense short nucleotide is combined with epidermal growth factor by Poly-L-Lysine, injecting the vinculum into tumour cell of body, EGFR receptor and c-erbB2 both belong to epidermal growth factor receptor family with distributed conformity and consanguinity in organisation, so increasing ratio of target / nontarget, raising diagnostic sensibility and treatment effect of antisense gene for excess expressed cancer of c-erbB2 cancer gene.

The present invention relates to one kind of 99mTc marked amino acid-glucose derivative complex, which has kernel of [99mTcO]3+ and ligand as shown below is L7 or L8. The complex has relatively high tumor ingestion, long detention time of the marker in tumor, and high targeting / non-targeting ratio.

The invention provides an RGD polypeptide coordination complex of a radioactive nuclide label. According to the structure of the coordination complex, the radioactive nuclide is selected from 64Cu, 68Ga, 111In, 62Cu, 67Cu, 67Ga, 86Y, 89Zr or 18F; the ligand is a ligand compound containing an RGD structure, which is shown in a formula (I). The coordination complex has stronger ligand stability and high target / non-target ratio, and the appetency of the ligand with integrin AlphavBeta3 is stronger. The invention further provides a preparation method of the coordination complex, and an application of the coordination complex in preparing tumor developers.

The invention relates to a kind of dimercaptosuccinate complex marked by technetium- 99m, the preparation method and its application. It is characterized in that it takes 99mTc(V), 99mTcN(22) and 99mTc(I)(CO)3 as central nuclear, the dimercaptosuccinate ligand is represented by DMSR / DMSR2, the R is alkyl or cyclohexyl with carbon number from 1 to 5. Said complex is prepared with wet or freeze- dried method, and is used as imaging agent for tumor. The advantages includes simple preparation, low price and high target / non target ratio.

The invention relates to an 18 / 19F-ester nitroimidazole compound, preparation method thereof and application as a hypoxic tissue developing agent. The invention provides F-ester nitroimidazole compounds as shown in a general formula, wherein an 18F-ester nitroimidazole compound is a radioactive compound. According to an S180 tumor-bearing mice experiment, the 18F-ester nitroimidazole compound has the characteristics of good tumor targeted intake and low liver background level, and is a potential positron emission tomography (PET) hypoxic tissue developing agent.

The invention discloses a VISTA targeted probe and a preparation method and application thereof, and relates to the field of medical chemistry, and a targeted compound is formed by connecting a VISTA inhibitor molecule and a nuclide labeling group in a specific chemical form. The invention also provides a radionuclide labeled diagnosis and treatment probe based on the targeting compound, and the diagnosis and treatment probe is prepared according to a wet method or a freeze-drying method. The invention also relates to application of the probe as a diagnosis and treatment reagent in human or animal tumors or immune diseases, and the probe has the advantages of simple preparation, good stability, high focus uptake and the like, and is suitable for clinical popularization.

The invention relates to a kind of dimercaptosuccinate complex marked by technetium- 99m, the preparation method and its application. It is characterized in that it takes <99m>Tc(V), <99m>TcN(22) and <99m>Tc(I)(CO)3 as central nuclear, the dimercaptosuccinate ligand is represented by DMSR / DMSR2, the R is alkyl or cyclohexyl with carbon number from 1 to 5. Said complex is prepared with wet or freeze- dried method, and is used as imaging agent for tumor. The advantages includes simple preparation, low price and high target / non target ratio.

The invention discloses a <18>F-labeled-8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene (S14161) and a preparation method thereof. The preparation method has the following advantages: preparation raw materials are cheap and are easy to obtain, the synthesis process is simple, reaction conditions are mild, and the radiochemical synthesis time is short; the above product is simple and convenient to purify and separate, the radiochemical purity of the product exceeds 98%, the radiochemical yield of the product is high, the uncorrected yield reaches up to 92%, and the radioactivity of the product is high; and the product is useful in the inspection and diagnosis of tumors and the radiation therapy of the tumors. The structural formula of the <18>F-labeled-8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene is shown in the description.

The invention discloses a prostate-specific membrane antigen inhibitor, a metal marker thereof, a preparation method and an application, and belongs to the technical field of biomedicine. The structure of the prostate specific membrane antigen inhibitor of the present invention is shown in formula I, and the structure of its metal label is shown in formula II, which is used in the preparation of prostate cancer diagnostic reagents / medicines, or / and therapeutic drugs. The compound of the invention has novel structure and stable physical and chemical properties, and can be used in the fields of diagnosis, staging, curative effect evaluation and treatment of prostate cancer in the preparation of drugs for diagnosis and treatment of prostate cancer.

The present invention discloses a radiolabeled T140 polypeptide compound, and a preparing method and an application thereof. The structure of the T140 polypeptide compound labeled by radionuclide <18>F contains a radionuclide and a polypeptide (Ac-TC14012) targeting a CXCR4 receptor. According to different radiolabeling methods, the compound is grouped into two classes: a compound 1 and a compound 2. The present invention also relates to the application of the compound as an imaging agent in organs or organizations of human or animals, especially as a tumor imaging agent, and the compound has the advantages of high tumor uptake, low non-specificity uptake and higher target / non-target ratio.

The invention discloses 18F-E[c(RGDyk)2], a medicine box used for automatic production thereof, and a preparation method and use of the medicine box, relates to a polyethylene terephthalate (PET) developer and a preparation method and use thereof and relates to the technical field of radiative medicines and nuclear medicines. The medicine box contains a raw material reagent A and a raw material reagent B. A bottle A contains E[c(RGDyk)2]-NO2; and A bottle B contains acetonitrile solution of crown ether K222 / K2CO3. The 18F-E[c(RGDyk)2] prepared by the medicine box has high absorbing performance and excellent retaining performance in model mouse tumor, and has a very high target / non target ratio, excellent pharmacokinetic characteristic and high biological performance, and can completely meet the requirements of PET developer of tumour integrin alphavbeta3 receptor.

The invention discloses a trans-oligonucleotide probe contrast-medium to mark superparamagnetism iron oxide, which consists of carrier constituted by gluglucosan enveloped by ferroferric oxide nanometer particle with superparamagnetism and trans-oligonucleotide segment of c-erbB2 cancer gene, wherein the trans-oligonucleotide connects the gluglucosan in the carrier at covalent bond. The invention also relates to a making method of the contrast-medium. The invention uses trans-gene technique of molecular biological domain into imaging diagnosis to combine the superiority and specificity of two advanced techniques, which increases the ratio of target / non-target of probe to the maximum degree to scan the size, position and anatomical relationship of adjacent structures of tumour through magnetic resonance, in order to build new imaging method of early-stage tumor diagnosis of specificity on the gene level. The invention can be applied to do early-stage imaging diagnosis for malignant tumour, epoophoron cancer, uterine neck cancer, esophagus cancer and cervical scale cancer.

The invention discloses a novel bone seeking complex. The complex comprises a nuclide <99m>Tc and a ligand. The ligand is a diphosphate derivative containing NO-donors and has a general formula represented by the following formula, wherein R1 is an aliphatic hydrocarbon, an aromatic ring or a nitrogen-containing heterocyclic ring containing 1 to 2 NO-donors; X is a group of -H, -OH, -NH2 and the like; Y is oxygen, sulfur or amino; and n is an integer between 2 and 9. The invention also discloses a preparation method for the complex and application of the complex as a bone imaging agent. Compared with the current bone imaging agent <99m>Tc-MDP widely used in the clinic at home and abroad, the bone imaging agent has high bone tissue initial stage uptake, long stay time and low non-target tissue uptake, particularly low liver uptake, and is expected to become a novel bone imaging agent with better performance.