38 results about "Evans Blue" patented technology

A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt. Definitions of R1-R13 and L1-L4 are provided in the disclosure, and R14 is a group capable of binding to prostate-specific membrane antigen (PSMA).

The invention relates to a combined technology for marking an organic blue dye of a sentinel lymph node and fluorescence imaging. The fluorescence given out by the organic blue dye is displayed by a fluorescence imaging device by the illumination of excitation light of the fluorescence imaging device with a wavelength not less than 570nm; wherein, the organic blue dye is one from methylene blue, Evans blue, isosulfan blue and patent blue or a compound thereof. The combined technology has the advantages of: overcoming the defect of needing to cut a larger opening on a skin for finding out a blue stain lymph node when using an organic dye to dye and position in the normal method for carrying out location of the sentinel lymph node of a tumor in clinical practice, and the sentinel lymph node can be located without an operation, thus reducing the pain of a patient. The combined technology has non-radioactivity, is convenient, fast and accurate and is a method which has excellent clinical application value.

The invention provides a truncated Evans blue modified fibroblast activating protein inhibitor compound, which is formed by connecting truncated Evans blue, a fibroblast activating protein inhibitor and a nuclide chelating group together by linking groups L1, L2, L3, L4 and X. The structure of the truncated Evans blue modified fibroblast activating protein inhibitor compound is as shown in formula (I), r1 is a fibroblast activating protein inhibitor; l1 is lysine, glutamic acid or a derivative structure thereof; l2 is-(CH2) n-, where n is an integer from 0 to 30, where each CH2 may be substituted individually with-O-,-NH (CO)-or-(CO)-NH-; l3 is-(CH2) m-, where m is an integer from 0 to 30, where each CH2 may be replaced individually with-O-, or-(CO)-; l4 is-(CH2) p-, where p is an integer from 0 to 30, where each CH2 may be substituted individually with-O-,-NH (CO)-or-(CO)-NH-; x is selected from N, C, O, S or R2 is a nuclide chelating group. The invention further provides a radioactive marker based on the structure of the compound, and the compound and the radioactive marker have remarkably prolonged blood circulation half-life period and enhanced tumor uptake enrichment and retention time, and are suitable for nuclide treatment and imaging of FAP protein high-expression tumors.

The invention provides a therapeutic prodrug compound targeting fibroblast activating protein. The structure of the therapeutic prodrug compound is shown as a formula (I). The invention also provides a therapeutic drug targeting the fibroblast activating protein, the therapeutic drug is a complex obtained by taking the compound as shown in the formula (I) as a ligand and labeling with therapeutic nuclide, and the structure of the therapeutic drug is shown in the formula (II). The invention also provides a preparation method of the prodrug compound and the therapeutic drug, and an application of the prodrug compound and the therapeutic drug in preparation of the therapeutic drug for FAP protein high-expression tumors. According to the therapeutic drug targeting the fibroblast activation protein, the circulating half-life period of the fibroblast activation protein inhibitor modified by truncated Evans blue can be remarkably prolonged, and tumor uptake enrichment and retention time can be prolonged.

A compound of Formula (I) or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt wherein the definitions of R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a group capable of binding to prostate-specific membrane antigen (PSMA).

The invention provides an experimental method of lycium barbarum polysaccharide in inhibition of glioma growth by regulating a blood brain barrier and belongs to the field of traditional Chinese medicine. The experimental method comprises the following steps: taking a male SD rat, feeding for 3-4 weeks with lycium barbarum polysaccharide solution; then constructing a rat glioma model; molding, continuing feeding with the lycium barbarum polysaccharide solution, and detecting, namely firstly detecting survival time, survival rate and median survival time of rats in each group; secondly taking brain tissues of the rats in each group, observing and measuring tumor size; thirdly judging permeability change of the blood brain barrier by carrying out femoral vein Evans blue solution on the rats in each group, taking the same amount of brain tissues and detecting Evans blue content; fourthly observing ultrastructure change of the blood brain barrier by virtue of an electron microscope; fifthly carrying out cardiac apex injection on the rats in each group with paraformaldehyde solution, taking the brain tissues, slicing and then carrying out an immunohistochemical test; and sixthly directly cutting off heads of the rats in each group, taking brains, extracting RNA and proteins and carrying out RT-PCR and Western blotting experiments. The experimental method provided by the invention provides a new treatment approach for treatment of multiple blood brain barrier diseases.

The present invention is directed to a compound of Formula I or Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula I Formula II The compounds of Formula I may be covalently bonded to a therapeutic compound or fragment thereof to provide a compound of Formula II and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

The present invention is directed to a compound of Formula I or Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

The invention provides a save and non-invasive alternative to the traditional modified Evans blue dye test for dysphagia in intubated patients. The method employs direct application of dye to the tongue, in combination with a tracheal tube that provides suction in the subglottal region above the cuff. By keeping the cuff inflated, the aspiration of food and liquid, as used in the traditional test, is avoided entirely.

The present invention provides a nanovesicle drug, containing camptothecin (EB-CPT) and paclitaxel coupled with Evans blue; the inside of the nanovesicle has a cavity, and its wall structure is determined by the EB-CPT CPT physically wraps the paclitaxel; the nanovesicle drug is spherical, the diameter of any cross-section is not greater than 150nm, and the size ratio of any two dimensions in the three-dimensional dimension is not greater than 2:1, and the thickness of the capsule wall is between 2 and 1. 20nm; The EB-CPT structure is shown in the following formula (I), wherein, R1 is camptothecin or its derivative group from the structure shown in formula (II) or formula (III); R2 is -CH 2 ‑, or one of ‑O‑; X is S or ‑CH 2 One of ‑; n1, n2 are the number of repeating units, which are all integers of 0‑10. The nanovesicle drug of the present invention has the advantage of being more suitable for clinical application, and simultaneously has high drug loading capacity and drug loading rate. The present invention also provides a preparation method of the nanovesicle drug and its application in the preparation of cancer treatment drugs.

The present invention provides a polypeptide compound having high affinity for GLP-1 receptors, the molecular structure thereof being as shown in the following formula (I), wherein R represents Evans blue or a derivative group thereof. The polypeptide compound of the present invention has the advantages of stable structure, simple preparation, significant therapeutic effect, long-term drug efficacy, convenient storage, etc. The present invention further provides a preparation method for the polypeptide compound and use thereof in preparing a medicament for diagnosing, preventing or treating GLP-1 / GLP-1 receptor pathway-related diseases.

A process of evaluating blood-brain barrier permeability of a stroke rat by using fluorescent substance is disclosed. This process uses an Evans blue dye having spontaneous fluorescence properties, in combination with the use of a new non-invasive in vivo imaging system (IVIS), to obtain fluorescent signals so as to assess the change in the blood-brain barrier permeability of rodents after a cerebral artery stroke model surgery. In operation, an Evans blue dye is injected into a stroke rat of middle cerebral artery occlusion model. A non-invasive in vivo imaging system is used to detect the fluorescence distribution of the whole brain, and obtain images combined by the fluorescence images and optical images for the whole brain tissue. Thereby, the change in the blood-brain barrier permeability of the stroke rat can be completely realized.

The invention relates to the technical field of medicines, in particular to a novel application of alpha-asarone in preparation of a medicine for treating or preventing cerebral infarction hemorrhage transformation, and particularly relates to a novel application of alpha-asarone in preparation of a medicine for treating or preventing cerebral infarction hemorrhage transformation caused by thrombolytic therapy. The alpha-asarone can inhibit the current of the voltage-gated sodium ion channel, and can selectively act on the inactivated sodium ion channel and prolong the reactivation time of the sodium ion channel. Accordingly, it is found that alpha-asarone can significantly improve the neurological function score of a cerebral infarction hemorrhage transformation model rat, reduce the cerebral infarction volume, relieve encephaledema and improve blood-brain barrier permeability (reduce the content of Evans blue in brain tissue), and therefore nerve injury caused by cerebral infarction hemorrhage transformation is relieved. The clinical use of alpha-asarone is expected to be helpful for improving the prognosis of a cerebral apoplexy patient and prolonging the thrombolysis treatment time window of the cerebral apoplexy patient; the nerve injury of cerebral apoplexy patients is relieved, the death rate is reduced, and the life quality is improved.

The invention discloses the application of vitamin K3 in the preparation of anti-allergic drugs. Vitamin K3 has a clear therapeutic effect on improving anaphylactoid symptoms. By comparing the degranulation of KU812 cells, the degree of swelling of the toe, and the degree of Evans blue exudation of the toe , Serum histamine release evaluation test drug group, normal saline control group and normal control group, to evaluate the therapeutic effect of drugs on allergic diseases, to determine that vitamin K3 can be used in the preparation of anti-allergic drugs. Vitamin K3 can effectively alleviate the symptoms of local and systemic anaphylaxis in mice; reduce mast cell degranulation and significantly improve the symptoms caused by anaphylaxis.

The invention discloses application of Licochalcone A in preparation of an antiallergic drug. A to-be-detected drug group, a normal saline control group and a normal control group are evaluated by comparing a mastocyte degranulation degree, a mouse toe swelling degree, a toe Evans blue exudation degree and a body temperature lowering degree, so that the treatment effect of the drug for allergic diseases is evaluated; a result determines that the Licochalcone A can be used for preparing the antiallergic drug. The Licochalcone A can effectively relieve local and systemic anaphylactic reaction symptoms of mice. Mastocyte degranulation is reduced, and symptoms caused by allergy are remarkably eliminated.

A process of evaluating blood-brain barrier permeability of a stroke rat by using fluorescent substance is disclosed. This process uses an Evans blue dye having spontaneous fluorescence properties, in combination with the use of a new non-invasive in vivo imaging system (IVIS), to obtain fluorescent signals so as to assess the change in the blood-brain barrier permeability of rodents after a cerebral artery stroke model surgery. In operation, an Evans blue dye is injected into a stroke rat of middle cerebral artery occlusion model. A non-invasive in vivo imaging system is used to detect the fluorescence distribution of the whole brain, and obtain images combined by the fluorescence images and optical images for the whole brain tissue. Thereby, the change in the blood-brain barrier permeability of the stroke rat can be completely realized.

The present invention provides a polypeptide drug prodrug, which is a prodrug formed by monomethylauristat or maytansine and Evans blue, and its structural formula is as formula (I); wherein, R 1 for or ‑CH 2 One of ‑; R 2 It is one of the new structures of monomethyl auristatin or metan, a polypeptide drug; m and n are the number of repeating units, and both are integers of 0-4. The polypeptide drug prodrugs of the present invention have excellent tumor cell uptake both in vivo and in vitro, and some prodrugs also show significant cancer cell inhibitory effect. The present invention also provides the preparation method of the prodrug and the application of the prodrug in the preparation of cancer treatment drugs.

The present invention is directed to a compound of Formula III or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula III wherein the definitions of R1-R12 and L1-L4 are provided in the disclosure, wherein R13 is a chelating group comprising 177Lu, and wherein R14 is a peptide. The compounds of Formula I may be covalently bonded to a peptide via a linker to provide a compound of Formula III and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.

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.