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 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 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 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 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 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 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 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.