Patent classifications
A61K41/0095
Conjugates Comprising An Anti-EGFR1 Antibody
The present invention relates to a conjugate comprising an anti-EGFR1 antibody or an EGFR binding fragment thereof and at least one dextran derivative, wherein the dextran derivative comprises at least one D-glucopyranosyl unit, wherein at least one carbon selected from carbon 2, 3 or 4 of the at least one D-glucopyranosyl unit is substituted by a substituent of the formula O(CH.sub.2).sub.SBi2Hii.sup.2 wherein n is in the range of 3 to 10; and the dextran derivative is bound to the anti-EGFR antibody or an EGFR1 binding fragment thereof via a bond formed by a reaction between at least one aldehyde group formed by oxidative cleavage of a D-glucopyranosyl unit of the dextran derivative and an amino group of the anti-EGFR1 antibody or an EGFR1 binding fragment thereof.
Proton induced boron capture therapy
The present disclosure provides methods of treating a biological tissue using a proton beam. A method includes the steps of: irradiating a proton beam to a biological tissue containing a reactant. The reactant includes a composite. The composite reacts with at least one proton from the proton beam and releases at least one particle or rays. The particle or rays reacts with the biological tissue. Another method includes the steps of: providing a reactant, the reactant comprising a composite; introducing the reactant into a biological tissue, the reactant being distributed in the biological tissue; and irradiating the biological tissue with the proton beam. The composite reacts with at least one proton from the proton beam to release at least one particle or rays, and the particle or the rays reacts with the biological tissue.
COMPOUNDS AND METHODS FOR THE DETECTION OF TRPV-6 CANCERS AND DRUG DELIVERY
Compounds containing TRPV6-binding peptides and their use in the detection and diagnosis of cancer are described. Also described are methods for detecting and staging cancer that use the compounds of the invention. Compounds containing TRPV6-binding peptides are useful for the delivery of diagnostic and therapeutic agents to cells or tumors that express TRPV6.
NEUTRON CAPTURE THERAPY SYSTEM AND THERAPY PLANNING SYSTEM FOR NEUTRON CAPTURE THERAPY
A neutron capture therapy system includes a therapy table on which an irradiation target is placed, a neutron beam irradiation unit which irradiates the irradiation target placed on the therapy table with a neutron beam, a position measurement unit which measures a position of the irradiation target placed on the therapy table, and a radiation dose distribution output unit which outputs a radiation dose distribution of a neutron beam used for irradiating the irradiation target, based on an amount of positional misalignment of the position of the irradiation target measured by the position measurement unit.
Conjugates comprising an anti-EGFR1 antibody
The present invention relates to a conjugate comprising an anti-EGFR1 antibody or an EGFR binding fragment thereof and at least one dextran derivative, wherein the dextran derivative comprises at least one D-glucopyranosyl unit, wherein at least one carbon selected from carbon 2, 3 or 4 of the at least one D-glucopyranosyl unit is substituted by a substituent of the formula O(CH.sub.2).sub.nSB.sub.12H.sub.11.sup.2 wherein n is in the range of 3 to 10; and the dextran derivative is bound to the anti-EGFR antibody or an EGFR1 binding fragment thereof via a bond formed by a reaction between at least one aldehyde group formed by oxidative cleavage of a D-glucopyranosyl unit of the dextran derivative and an amino group of the anti-EGFR1 antibody or an EGFR1 binding fragment thereof.
BORON-CONTAINING COMPOUND
To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent BH; R.sup.1 represents (CH.sub.2)n-X.sup.1R.sup.3 (n represents an integer of 0 to 6; X.sup.1 represents O, S, NH, SS, OCO, NHCO or SCO, or does not exist; R.sup.3 represents C.sub.6-C.sub.20 alkyl, hydroxy C.sub.6-C.sub.20 alkyl, amino C.sub.6-C.sub.20 alkyl, azido C.sub.6-C.sub.20 alkyl, hydroxycarbonyl C.sub.6-C.sub.20 alkyl, or the like), or a group having a repeating sequence of (CH.sub.2).sub.2O 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and R.sup.2 is (CH.sub.2)m-X.sup.2R.sup.4 (m represents an integer from 0 to 8; X.sup.2 represents O, S, NH, SS, OCO, NHCO or SCO, or does not exist; and R.sup.4 represents a tumor recognition moiety), or does not exist
are prepared and used.
##STR00001##
Compound for specifically binding to amyloid β-protein
Provided is a compound for specifically binding to amyloid -protein. The compound has thereon a nuclide with a large thermal neutron capture cross section and the compound is capable of specifically binding to the amyloid -protein. The property of the compound allows it to be used in conjunction with a neutron capture therapy device to eliminate amyloid -protein. Similarly, when the compound is labelled with radioactive element .sup.11C, the compound can also be used in conjunction with PET/CT for determining the part of the brain where amyloid -protein is deposited, for diagnosing Alzheimer's disease. Also disclosed is a preparation process for the compound. The beneficial effect of the present disclosure is to make the therapy and diagnosis of Alzheimer's disease more targeted by providing the compound for specifically binding to amyloid -protein.
BORONO-PHENYLALANINE DERIVATIVE
Provided are new compounds that can have the property of being specifically taken up into cancer cells. In the present invention, novel 4-borono-phenylalanine derivatives, borono-phenylalanine derivatives having a heterocyclic skeleton, borono-phenylalanine derivatives having a fused ring structure, or pharmaceutically acceptable salts thereof are prepared. These compounds have the property of being taken up specifically by LAT1 and thus easily taken up specifically by cancer cells in the evaluation of LAT1 and LAT2 selective uptake, and can be conveniently used for neutron capture therapy and the like. A typical example is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.
##STR00001##
COMPOUND FOR SPECIFICALLY BINDING TO AMYLOID B-PROTEIN
Provided is a compound for specifically binding to amyloid -protein. The compound has thereon a nuclide with a large thermal neutron capture cross section and the compound is capable of specifically binding to the amyloid -protein. The property of the compound allows it to be used in conjunction with a neutron capture therapy device to eliminate amyloid -protein. Similarly, when the compound is labelled with radioactive element .sup.11C, the compound can also be used in conjunction with PET/CT for determining the part of the brain where amyloid -protein is deposited, for diagnosing Alzheimer's disease. Also disclosed is a preparation process for the compound. The beneficial effect of the present disclosure is to make the therapy and diagnosis of Alzheimer's disease more targeted by providing the compound for specifically binding to amyloid -protein.
BORON NEUTRON CAPTURE THERAPY SYSTEM AND USE OF α-AMINO ACID-LIKE BORON TRIFLUORIDE COMPOUND IN PREPARATION OF MEDICAMENT FOR TUMOR THERAPY
The present disclosure discloses a boron neutron capture therapy system comprising: a boron neutron capture therapy device and an -amino acid-like boron trifluoride compound having a structure shown as formula (I) below:
##STR00001##
Wherein: R is selected from hydrogen, methyl, isopropyl, 1-methylpropyl, 2-methylpropyl, hydroxymethyl, 1-hydroxyethyl, benzyl or hydroxybenzyl; M is H or metal atom. The energy generated from the action of the neutron beam generated by the boron neutron capture therapy device on the -amino acid-like boron trifluoride compound destroys tumor cell DNA. In another aspect, the present disclosure discloses a use of an -amino acid-like boron trifluoride compound in the preparation of a medicament for tumor therapy.