To provide a method for obtaining a dealkoxyphenylation product with a high yield from a substrate such as a sugar bound to an alkoxyphenyl group through an oxygen atom. A dealkoxyphenylation product can be obtained with a high yield under mild conditions by reacting a substrate that is bound to a phenyl group substituted by C1 to C5 alkoxy at the para- or ortho-position through an oxygen atom with λ3-iodane in a fluorous alcohol and water.
C07H 17/02 - Heterocyclic radicals containing only nitrogen as ring hetero atoms
C07C 45/30 - Preparation of compounds having C=O groups bound only to carbon or hydrogen atomsPreparation of chelates of such compounds by oxidation with halogen containing compounds, e.g. hypohalogenation
C07H 1/00 - Processes for the preparation of sugar derivatives
C07H 15/207 - Cyclohexane rings not substituted by nitrogen atoms, e.g. kasugamycins
2.
DOSAGE REGIMEN OF AN ANTI-CDH6 ANTIBODY-DRUG CONJUGATE
The present disclosure relates to the field of pharmaceutical preparations, dosage regimens, and administration of an antibody-drug conjugate (ADC). More specifically, the ADC is composed of an anti-cadherin-6 (CDH6) antibody connected via a linker to an anticancer agent, such as topoisomerase I inhibitor.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The purpose of the present invention is to provide a new method for producing a compound encoded by an oligonucleotide. Provided according to the present invention is a method for producing a compound encoded by an oligonucleotide, the method including phosphodiester bonding of oligonucleotide chains to each other by chemical ligation under prescribed conditions.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
C40B 50/10 - Liquid phase synthesis, i.e. wherein all library building blocks are in liquid phase or in solution during library creationParticular methods of cleavage from the liquid support involving encoding steps
Provided is an oligonucleotide capable of inducing the editing activity of ADAR in a cell and having excellent stability. The oligonucleotide comprises a first oligonucleotide and a second oligonucleotide linked to the 5'-side of the first oligonucleotide, and is capable of inducing the site-specific editing of target RNA. The first oligonucleotide includes: a target-corresponding nucleotide residue; an oligonucleotide that is located on the 5'-side of the target-corresponding nucleotide residue, is complementary to the target RNA, and is composed of 3 to 6 residues; and an oligonucleotide that is located on the 3'-side of the target-corresponding nucleotide residue, is complementary to the target RNA, and is composed of 10 to 24 residues. At least one of a phosphorus-containing linking group that links a first nucleoside residue to a second nucleoside residue and a phosphorus-containing linking group that links a fourth nucleoside residue to a fifth nucleoside residue is an alkylphosphonic acid residue, an alkyl phosphate residue or a substituted phosphoramide residue, wherein the nucleoside residues are numbered from the target-corresponding nucleotide in 3' direction. The second oligonucleotide has a nucleotide residue in which a nucleotide residue corresponding to the target RNA is deleted at the 3'-end or does not form a complementary pair with the target RNA. The second oligonucleotide is composed of 2 to 10 residues, wherein a nucleotide residue other than a nucleotide residue located at the 3'-end is complementary to the target RNA.
A pharmaceutical product for administration of an anti TROP2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject: Formula (I).
A pharmaceutical product for administration of an anti TROP2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject: Formula (I).
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.
An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.
The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof.
An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.
The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof.
An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.
The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof.
wherein the symbols in the formula are defined below:
R1: e.g., a C1-C6 alkyl group; R2: a C1-C6 alkyl group;
A: e.g., an oxygen atom; and R3: e.g., a C1-C6 alkyl group.
C07D 307/94 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom spiro-condensed with carbocyclic rings or ring systems, e.g. griseofulvins
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibodydrug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
Disclosed are a means capable of stably producing TCR-T cells and CAR-T/CAR-NK cells, and a means for treating diseases such as tumors and autoimmune diseases by applying said means. One aspect of the method for producing TCR/CAR/CAAR-expressing immune cells according to the present invention is a method for producing TCR/CAR/CAAR-expressing immune cells by introducing an exogenous receptor gene into pluripotent blood progenitor cells and then inducing differentiation into immune cells. Another aspect of the method for producing TCR/CAR/CAAR-expressing immune cells according to the present invention is a method for producing TCR/CAR/CAAR-expressing immune cells by inducing differentiation of pluripotent blood progenitor cells into immune cells and then introducing an exogenous receptor gene. As the pluripotent blood progenitor cells, induced leukocyte stem (iLS) cells or T/NK progenitor cells can be preferably used.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention provides, for example, a method for producing mRNA having a high capping rate and a method for improving the capping rate of mRNA. Provided is a method for producing mRNA coding for a target protein, said method comprising the following step: (a) an IVT reaction step for preparing a solution containing at least template DNA designed so as to be capable of transferring mRNA coding for the target protein, a capping reagent, NTP, RNA polymerase, and Mg2+, and transferring, from the template DNA, the mRNA coding for the target protein, where the ratio of molarity of Mg2+to molarity of NTP (molarity of Mg2+/molarity of NTP) is 0.30-0.75.
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Clinical studies and trials of anticancer drugs; providing
information on clinical studies and trials of anticancer
drugs. Providing medical information in the field of anticancer
drugs; providing medical information on the efficacy, side
effects, interactions or administration of anticancer drugs.
Disclosed are compositions and method related to variants of SPINK2 that bind to targets other than an endogenous target of SPINK2. In one embodiment, a peptide is provided that comprises the amino acid sequence SEQ ID NO: 1. In further embodiments, an amino acid sequences encoded by nucleotide positions 4 to 42 and/or nucleotide positions 94 to 189 in the nucleotide sequence of SEQ ID NO: 14 flank the amino terminus and the carboxyl terminus, respectively, of the amino acid sequence. In another embodiment, a peptide is provided that comprises an amino acid sequence derived from the amino acid sequence of SEQ ID NO: 1 in which a conservative substitution, deletion, 10 addition and/or insertion of 1 to 5 (inclusive) amino acids has occurred at amino acids other than the 1st X to the 12th X counting from the amino terminus.
C12N 15/10 - Processes for the isolation, preparation or purification of DNA or RNA
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
C40B 50/00 - Methods of creating libraries, e.g. combinatorial synthesis
This invention provides a novel masked antibody. The masked antibody is a molecule that binds to a target antigen, which comprises a moiety binding to a target antigen, a first peptide recognizing a target antigen-binding site comprised in such moiety, and a second peptide comprising an amino acid sequence cleaved by a protease, wherein, after the second peptide is cleaved by a protease, the molecule has higher binding intensity to the target antigen, compared with that before it is cleaved.
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
It is an object to provide an antibody specifically binding to CD37-positive tumor cells such as malignant B-cell lymphoma, an antibody-drug conjugate comprising the antibody, a pharmaceutical composition having therapeutic effects on a tumor using the antibody, a method for treating a tumor using the aforementioned pharmaceutical composition, a method for producing the antibody, and a method for producing the antibody-drug conjugate, and the like. The present invention provides an anti-CD37 antibody-drug conjugate in which an antibody is conjugated to a drug linker represented by the following formula (wherein A represents a connecting position to the antibody) by a thioether bond, specifically, a humanized anti-CD37 antibody having internalization ability and an antibody-drug conjugate containing the antibody.
It is an object to provide an antibody specifically binding to CD37-positive tumor cells such as malignant B-cell lymphoma, an antibody-drug conjugate comprising the antibody, a pharmaceutical composition having therapeutic effects on a tumor using the antibody, a method for treating a tumor using the aforementioned pharmaceutical composition, a method for producing the antibody, and a method for producing the antibody-drug conjugate, and the like. The present invention provides an anti-CD37 antibody-drug conjugate in which an antibody is conjugated to a drug linker represented by the following formula (wherein A represents a connecting position to the antibody) by a thioether bond, specifically, a humanized anti-CD37 antibody having internalization ability and an antibody-drug conjugate containing the antibody.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A pharmaceutical product for administration of an anti-TROP2 antibody-drug conjugate in combination with a PARP1 selective inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the PARP1 selective inhibitor are administered in combination to a subject: Formula (II)
A pharmaceutical product for administration of an anti-TROP2 antibody-drug conjugate in combination with a PARP1 selective inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the PARP1 selective inhibitor are administered in combination to a subject: Formula (II)
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
22.
PHARMACEUTICAL COMPOSITION HAVING EXCELLENT DISSOLUTION PROPERTIES
The present invention provides a pharmaceutical composition in which valemetostat or a pharmaceutically acceptable salt thereof, particularly valemetostat tosylate, has excellent dissolution properties. It was found that excellent dissolution properties can be achieved by combining valemetostat or a pharmaceutically acceptable salt thereof with one or more of croscarmellose sodium and sodium starch glycolate.
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
The purpose of the present inventio is to provide an antibody-drug conjugate production method including a purification method for efficiently removing a by-product derived from an exatecan compound. Provided is a method for producing an antibody-drug conjugate in which a drug linker represented by the formula shown below (wherein A represents a position at which an antibody is bound) and the antibody is bound to each other through a thioether bond, the method being characterized by including (i) a step for removing a by-product derived from an exatecan compound from a solution containing the antibody-drug conjugate using an activated carbon material.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Clinical studies and trials of anticancer drugs; providing information on clinical studies and trials of anticancer drugs. Providing medical information in the field of anticancer drugs; providing medical information on the efficacy, side effects, interactions or administration of anticancer drugs.
Provided are methods for producing a monoclonal antibody or a binding fragment thereof that binds to domain 3 of human LAG-3 and has one or more of the properties described in (ii) to (v), and the properties described in (i) and (vi) below: (i) having in vitro ADCC activity; (ii) reducing the number of LAG-3 positive cells in vivo in low fucose form; (iii) suppressing experimental autoimmune encephalomyelitis in vivo in low fucose form; (iv) binding to human activated T cells; (v) human LAG-3 binds to human major histocompatibility complex class II molecules in the presence of the antibody or the binding fragment thereof; and (vi) the presence of the antibody or the binding fragment thereof allowing human LAG-3 to exert human T cell suppression function.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 35/12 - Materials from mammalsCompositions comprising non-specified tissues or cellsCompositions comprising non-embryonic stem cellsGenetically modified cells
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
The present invention addresses the problem of providing a solid preparation that contains a high-quality mirogabalin besylate and has excellent storage stability. The solution of the present invention is a pharmaceutical solid preparation that contains mirogabalin besylate and does not substantially contain a reducing sugar.
The present invention pertains to: a pharmaceutical product comprising an (anti-HER3 antibody)-drug conjugate and a RASG12C inhibitor; and/or a treatment method characterized by administering a combination of an (anti-HER3 antibody)-drug conjugate and a RASG12C inhibitor to a subject.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
42.
METHODS OF TREATING CHEMOTHERAPY-RESISTANT CANCER WITH AN ANTIBODY-DRUG CONJUGATE
The present disclosure relates to the field of therapeutic methods for treating a cancer using an ADC. The present disclosure also relates to the field of pharmaceutical products comprising the ADC for treating a cancer. More specifically, the ADC is composed of an anti-cadherin-6 (CDH6) antibody connected via a linker to an anticancer agent, such as topoisomerase I inhibitor, and the cancer may be resistant to chemotherapy.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Crystals of the compound represented by formula (1), a method for the production thereof, and a method for producing an antibody-drug conjugate using the crystals.
Crystals of the compound represented by formula (1), a method for the production thereof, and a method for producing an antibody-drug conjugate using the crystals.
The present invention relates to an antibody that binds to GARP and is useful as a therapeutic agent for a tumor, and a method for treating a tumor using the aforementioned antibody. It is an object of the present invention to provide an antibody, which inhibits the function of Treg in a tumor and is thereby used as a pharmaceutical product having therapeutic effects, a method for treating a tumor using the aforementioned antibody, and the like. An anti-GARP antibody that binds to GARP and exhibits inhibitory activity to Treg function and exhibits ADCC activity is obtained, and moreover a pharmaceutical composition for use in tumor therapy, comprising the aforementioned antibody, etc. is obtained.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
SPINK2 mutant peptide conjugates are provided that inhibit KLK5. The KLK5 inhibitory peptide conjugates are Fc fusion peptides in which, in certain embodiments, the Fc region of the fusion peptides are the Fc region of human IgG1 or a fragment thereof. The KLK5 inhibitory peptide conjugates include an amino acid sequence of one of SEQ ID NOs: 34, 36, 38, 40, 42, 44, 46, 48, 96, 50, 52, 54, 56, 58, or 60. Pharmaceutical compositions that include the KLK5 inhibitory peptide conjugates useful for treating KLK5-related diseases are also provided.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cardiovascular diseases; pharmaceutical preparations for the treatment of oncological diseases and disorders
47.
COMBINATION OF ANTIBODY-DRUG CONJUGATE AND OTHER MEDICINE
The present invention provides: a pharmaceutical composition characterized in that a specific antibody-drug conjugate and another medicine are administered in combination; and/or a treatment method or the like characterized in that a specific antibody-drug conjugate and another medicine are administered to an individual in combination. A pharmaceutical composition in which an anti-CD37 antibody-drug conjugate and another medicine (one or more medicines selected from the group consisting of molecular targeting agents, medicines related to R-CHOP therapy, medicines related to R-CHP therapy, alkylating agents, and immunomodulators) are administered in combination, the anti-CD37 antibody-drug conjugate being an anti-CD37 antibody-drug conjugate in which a drug linker represented by a formula (in the formula, A indicates the bonding position with the anti-CD37 antibody) and an anti-CD37 antibody are bonded by a thioether bond; and/or a treatment method characterized in that the anti-CD37 antibody-drug conjugate and the other medicine are administered to an individual in combination.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
48.
COMBINATION OF ANTI-B7-H3 ANTIBODY-DRUG CONJUGATE WITH ATR INHIBITOR OR ATM INHIBITOR
In one embodiment, the present invention addresses the problem of providing a pharmaceutical composition and a treatment method characterized in that a specific anti-B7-H3 antibody-drug conjugate and an ATR inhibitor or an ATM inhibitor are combined and administered. In one embodiment, provided are a pharmaceutical composition and a treatment method characterized in that an antibody-drug conjugate, in which a drug linker represented by the formula (where A represents a binding position with an anti-B7-H3 antibody) and an anti-B7-H3 antibody are bound by a thioether bond, and an ATR inhibitor or an ATM inhibitor are combined and administered.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/00 - Drugs for disorders of the urinary system
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
Provided are a therapeutic agent and therapeutic method for cancers having a low sensitivity to existing anticancer agents, comprising an anti-MUC1 antibody-drug conjugate as an active ingredient.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/10 - Drugs for disorders of the urinary system of the bladder
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 35/02 - Antineoplastic agents specific for leukemia
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
The present invention provides endo-β-N-acetylglucosaminidase (Endo-Si) cloning from a strain belonging to Streptococcus iniae and a mutant enzyme thereof, a gene encoding the enzyme, a recombinant plasmid, a transformant obtained by transformation of a cell by the plasmid and use thereof, and a method for producing e.g., a sugar chain remodeled antibody using the enzyme. A polypeptide having an amino acid sequence at amino acid positions 34 to 928 in SEQ ID NO: 2 or an amino acid sequence having the same amino acid sequence except containing one or mutations at more amino acid positions selected from the group consisting of amino acids at position 241 (D241), 190 (T190), 311 (Q311) and 360 (E360), said polypeptide exhibiting a sugar chain hydrolysis activity and/or transglycosylation activity.
C12N 9/24 - Hydrolases (3.) acting on glycosyl compounds (3.2)
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The purpose of the present invention is to provide a method for producing lentinan at a high yield, the obtained lentinan having a high purity and thus showing high complex formation efficiency with a nucleic acid or the like, without using a solvent to be strictly regulated. A method for producing lentinan according to the present invention includes a step for separating and acquiring a floating fraction containing lentinan from a mixture of an aqueous solution (for example, a hot water extract) and an alcohol. Preferably, the method further includes a step (for example, low-temperature alkali treatment) for disrupting the higher-order structure of the lentinan, and a step (for example, alkali hydrolysis) for controlling the molecular weight of lentinan.
The present invention addresses the problem of providing: an antibody that binds to CD25 and has an internalization activity; an antibody-drug conjugate which contains said antibody and has an anti-tumor activity; a medicine which includes said antibody-drug conjugate and has a therapeutic effect on tumors; and a method for treating a tumor using said antibody, said antibody-drug conjugate, or said medicine. Provided is a CD25 antibody or an antigen-binding fragment of the antibody, characterized by (1) not having an IL-2 blocking ability, and (2) having an internalization activity into CD25-expressing cells by binding to CD25. The antibody or antigen-binding fragment of the antibody can be conjugated with a cytotoxically active compound to exhibit ability to remove regulatory T cells and/or ability to promote proliferation of granzyme-positive CD8-positive cells.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C12N 1/15 - Fungi Culture media therefor modified by introduction of foreign genetic material
C12N 1/19 - YeastsCulture media therefor modified by introduction of foreign genetic material
C12N 5/10 - Cells modified by introduction of foreign genetic material, e.g. virus-transformed cells
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
The present invention provides a pharmaceutical composition and a treatment method characterized in that a specific anti-CDH6 antibody-drug conjugate is administered in combination with an HIF-2α inhibitor. Provided are a pharmaceutical composition and a treatment method characterized in that an antibody-drug conjugate in which a drug linker represented by the formula (in the formula, A represents a binding site with an anti-CDH6 antibody or with a functional fragment of the antibody) is bound with an anti-CDH6 antibody or with a functional fragment of the antibody by a thioether bond is administered in combination with an HIF-2α inhibitor.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 13/08 - Drugs for disorders of the urinary system of the prostate
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
The present invention provides a pharmaceutical composition and a therapeutic method characterized in that a specific anti-CDH6 antibody-drug conjugate and a VEGF inhibitor are administered in combination. Provided are a pharmaceutical composition and a therapeutic method characterized in that an antibody-drug conjugate, in which a drug linker shown by the formula (in the formula, A represents the binding site with an anti-CDH6 antibody or a functional fragment of the antibody) and the anti-CDH6 antibody or a functional fragment of the antibody are bonded by a thioether bond, is administered in combination with a VEGF inhibitor.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 7/02 - Linear peptides containing at least one abnormal peptide link
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and/or CLDN9 antibody.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
56.
NOVEL CYCLIC DINUCLEOTIDE DERIVATIVE AND ANTIBODY-DRUG CONJUGATE THEREOF
Desired is development of novel CDN derivatives having STING agonist activity; and a therapeutic agents and/or therapeutic methods using the novel CDN derivatives for diseases associated with STING agonist activity. Further desired is development of a therapeutic agents and/or therapeutic methods capable of delivering the novel CDN derivatives specifically to targeted cells and organs for diseases associated with STING agonist activity. The present invention provides novel CDN derivatives having potent STING agonist activity, and antibody-CDN derivative conjugates including the novel CDN derivatives.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
57.
PEPTIDE FOR TREATING AGE-RELATED MACULAR DEGENERATION
It is intended to provide a novel peptide. The present invention provides a peptide which comprises the amino acid sequence shown in SEQ ID NO: 30 and inhibits protease activity.
C07K 16/38 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against protease inhibitors of peptide structure
C12N 15/85 - Vectors or expression systems specially adapted for eukaryotic hosts for animal cells
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
National University Corporation Kobe University (Japan)
Daiichi Sankyo Company, Limited (Japan)
Inventor
Matozaki, Takashi
Sue, Mayumi
Nakamura, Kensuke
Yoshimura, Chigusa
Abstract
An anti-SIRPα antibody that can be used as a tumor agent and an anti-tumor agent comprising the antibody as an active ingredient. An antibody that binds specifically to human SIRPα to inhibit binding of human SIRPα to CD47.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
59.
GLYCAN, AND METHOD FOR PRODUCING MEDICINE CONTAINING GLYCAN
The present invention addresses the problem of providing: a novel method for pure-chemically producing a biantennary N-glycan with an α2,6-sialic acid structure at each non-reducing end, the method having excellent yield, selectivity, and efficiency; and a method for producing a novel monosaccharide or oligosaccharide, which are useful in the method, and, for instance, intermediates as well as a novel method for producing the glycoprotein or the like by using the method. Provided are: a novel method for pure-chemically producing a biantennary N-glycan with an α2,6-sialic acid structure at each non-reducing end such that for glycosidic linkage, the direct construction of which is difficult using adjacent group involvement, disaccharide blocks are individually constructed and are stereoselectively linked to another sugar block in this synthesis scheme; and a method for producing a novel monosaccharide or oligosaccharide, which are useful in the method, and, for instance, intermediates as well as a novel method for producing the glycoprotein or the like by using the method.
C08B 37/00 - Preparation of polysaccharides not provided for in groups Derivatives thereof
A61K 47/61 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
Provided are lipid particles encapsulating a nucleic acid capable of expressing an E6 antigen and an E7 antigen of human papillomavirus, whereby a vaccine for preventing and/or treating infection with human papillomavirus type 6 and/or type 11 can be provided. The lipid particles comprise a lipid that is a cationic lipid having the general formula (Ia), or a pharmaceutically acceptable salt thereof.
Provided are lipid particles encapsulating a nucleic acid capable of expressing an E6 antigen and an E7 antigen of human papillomavirus, whereby a vaccine for preventing and/or treating infection with human papillomavirus type 6 and/or type 11 can be provided. The lipid particles comprise a lipid that is a cationic lipid having the general formula (Ia), or a pharmaceutically acceptable salt thereof.
Provided are lipid particles encapsulating a nucleic acid capable of expressing an E6 antigen and an E7 antigen of human papillomavirus, whereby a vaccine for preventing and/or treating infection with human papillomavirus type 6 and/or type 11 can be provided. The lipid particles comprise a lipid that is a cationic lipid having the general formula (Ia), or a pharmaceutically acceptable salt thereof.
[In the formula, R1, R2, p, L1 and L2 are as defined in the specification.]
To provide a novel pharmaceutical use of a peptide. A pharmaceutical composition for the treatment or prevention of retinitis pigmentosa, comprising a peptide which comprises the amino acid sequence shown in SEQ ID NO: 30 and inhibits a protease activity.
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/62 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
C12Q 1/37 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving peptidase or proteinase
The present invention addresses the problem of providing a compound having an action of suppressing NLRP3 inflammasome activation and useful for prophylaxis and/or therapy of autoinflammatory disease, autoimmune disease and/or inflammatory disease or a pharmaceutically acceptable salt thereof as a medicament. The means for solution of the present invention is a compound of general formula (1) or a pharmaceutically acceptable salt thereof. [The symbols in the formula are defined as follows. A is a carbon atom or the like; R1is a halogen atom or the like; R1' is a hydrogen atom or the like; R1'' is a hydrogen atom or the like; R1''' is a hydrogen atom or the like; R2is a hydrogen atom or the like; R2' is a hydrogen atom or the like; and R3 is a C1-C3 alkyl group or the like.]
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
A61P 9/14 - VasoprotectivesAntihaemorrhoidalsDrugs for varicose therapyCapillary stabilisers
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07D 491/147 - Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
[Problem] To provide a novel LRRC-15 antibody, or antigen-binding fragment thereof, that is capable of being used in an advantageous manner in various therapeutic modalities, particularly an antibody-drug conjugate (ADC). [Solution] Provided is an antibody that specifically binds with a novel epitope in LRRC15.
A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/55 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
The present invention addresses the problem of providing a compound for prophylaxis and/or treatment of central inflammatory diseases, or a pharmacologically acceptable salt thereof. The present invention addresses a compound of a general formula (I) or a pharmacologically acceptable salt thereof as a means to solve the problem. [R1: a C1-C6 alkyl group or the like, R2: a C1-C6 alkyl group or the like, A: a 5-membered aromatic hetero-ring or the like, R3, R3′: a C1-C6 alkyl group or the like]
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 307/94 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom spiro-condensed with carbocyclic rings or ring systems, e.g. griseofulvins
C07D 309/12 - Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers
C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
Provided is a vaccine for preventing and/or treating an infection with an influenza virus. The vaccine comprises lipid particles containing a nucleic acid capable of expressing a haemagglutinin (HA) protein of the influenza virus, wherein a lipid is a cationic lipid having general formula (Ia), or a pharmaceutically acceptable salt thereof.
Provided is a vaccine for preventing and/or treating an infection with an influenza virus. The vaccine comprises lipid particles containing a nucleic acid capable of expressing a haemagglutinin (HA) protein of the influenza virus, wherein a lipid is a cationic lipid having general formula (Ia), or a pharmaceutically acceptable salt thereof.
Provided is a vaccine for preventing and/or treating an infection with an influenza virus. The vaccine comprises lipid particles containing a nucleic acid capable of expressing a haemagglutinin (HA) protein of the influenza virus, wherein a lipid is a cationic lipid having general formula (Ia), or a pharmaceutically acceptable salt thereof.
[In the formula, R1, R2, p, L1 and L2 are as defined in the specification.]
NATIONAL INSTITUTES OF BIOMEDICAL INNOVATION, HEALTH AND NUTRITION (Japan)
UNIVERSITY OF THE RYUKYUS (Japan)
DAIICHI SANKYO COMPANY, LIMITED (Japan)
Inventor
Ishii, Ken
Fukushima, Takuya
Tanaka, Yuetsu
Takeshita, Fumihiko
Koizumi, Makoto
Niwa, Takako
Nogusa, Shoko
Jonai, Nao
Onodera, Yoshikuni
Abstract
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
or a pharmaceutically acceptable salt thereof,
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
or a pharmaceutically acceptable salt thereof,
wherein
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
or a pharmaceutically acceptable salt thereof,
wherein
R1 and R2 each independently represent a C1-C3 alkyl group;
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
or a pharmaceutically acceptable salt thereof,
wherein
R1 and R2 each independently represent a C1-C3 alkyl group;
L1 represents a C17-C19 alkenyl group optionally having one or more C2-C4 alkanoyloxy groups;
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
or a pharmaceutically acceptable salt thereof,
wherein
R1 and R2 each independently represent a C1-C3 alkyl group;
L1 represents a C17-C19 alkenyl group optionally having one or more C2-C4 alkanoyloxy groups;
L2 represents a C10-C19 alkyl group optionally having one or more C2-C4 alkanoyloxy groups, or a C10-C19 alkenyl group optionally having one or more C2-C4 alkanoyloxy groups; and
Provided is a vaccine for preventing and/or treating infection with human T-cell leukemia virus type 1 (HTLV-1).
A lipid particle encapsulating a nucleic acid expressing a gp46 antigen or a Tax antigen of human T-cell leukemia virus type 1 (HTLV-1), wherein the lipid comprises a cationic lipid represented by general formula (Ia):
or a pharmaceutically acceptable salt thereof,
wherein
R1 and R2 each independently represent a C1-C3 alkyl group;
L1 represents a C17-C19 alkenyl group optionally having one or more C2-C4 alkanoyloxy groups;
L2 represents a C10-C19 alkyl group optionally having one or more C2-C4 alkanoyloxy groups, or a C10-C19 alkenyl group optionally having one or more C2-C4 alkanoyloxy groups; and
p is 3 or 4.
01 - Chemical and biological materials for industrial, scientific and agricultural use
03 - Cosmetics and toiletries; cleaning, bleaching, polishing and abrasive preparations
Goods & Services
Chemicals for industrial purposes, adhesives for industrial purposes not for stationery or household purposes, plant growth regulating preparations, fertilizers, ceramic glazings in the nature of a dry chemical preparation for use in the manufacture of ceramics, higher fatty acids for use as a food additive; chemicals, namely, actinium, americium, antimony, ytterbium, yttrium, uranium, erbium, gadolinium, gallium, californium, curium, samarium, dysprosium, silicon, mercury, scandium, strontium, cesium, cerium, selenium, bismuth, thallium, thulium, technetium, terbium, tellurium, thorium, neodymium, neptunium, berkelium, barium, fermium, praseodymium, francium, plutonium, protactinium, promethium, holmium, europium, radium, lanthanum, lithium, rubidium and rhenium; non-metallic minerals, namely, sulfur, foundry sand, kaolin, talc, rock salt, diatomaceous earth, acid clay, barites, saltpeter, natural graphite, dolomite, cryolite, bentonite, bauxite, fluorite, magnesite, alunite and rock phosphate; photographic supplies, namely blueprint paper, photographic paper, photographic sensitizers, photographic dry plates, photographic developers, flash powder, photographic fixers and unexposed photographic films; reagent paper other than for medical purposes; artificial sweeteners; flour and start for industrial purposes; unprocessed plastics in primary form; paper pulp for manufacturing purposes and wood pulp for manufacturing. Cosmetics and toiletries; soaps and detergents; body cream soaps; facial cleansing preparations; essences for skin whitening; baby oils; moisturizing milk (cosmetics); moisturizing creams; creamy makeup foundations; skin whitening creams; skin lotions; skin lightening creams; cosmetic products for skin care; skin cosmetics; non-medicated skin care preparations; toilet water; cleansing creams; make-up removal preparations; skin washing products (cosmetics); shampoos; hair conditioners; essential oils; makeup powders; beauty masks for the face; moisturizing skin masks; lipsticks; bath oils; toothpastes; toothpaste; mint essence (essential oil); Perfumes; fragrances; incense; hand creams; mouthwashes, not for medical purposes; non-medicated oral mouthwashes for pets; breath freshening preparations, not for medical purposes; mouthwash preparations, other than for medical purposes; body cleansing creams; products for cleaning body skin (cosmetics); skin cleansing creams; products to clean the skin (cosmetics).
36 - Financial, insurance and real estate services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Providing financial assistance to patients in the nature of payment assistance for medications and pharmaceuticals, as well as providing financial assistance to others in respect of health insurance approval and coverage for medications and pharmaceuticals, and consultancy and information services relating thereto; insurance services, namely, assisting healthcare professionals with insurance verifications and prior authorizations in the nature of health insurance eligibility review, verification of coverage for pharmaceuticals, and consultancy and information services relating thereto Providing medical information in the field of pharmaceutical preparations; providing medical information on the efficacy, side effects, interactions or administration of pharmaceutical preparations
The problem addressed by the present invention is to provide a novel compound that acts as an agonist on orexin 2 receptors and can be used in the treatment of diseases associated with the orexin 2 receptors, especially narcolepsy. Provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof. (Here, in formula (I), R1, R2, R3, R4, R5, R6, and Z are each as defined in the specification.)
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61P 25/00 - Drugs for disorders of the nervous system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 413/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
71.
COMBINATION OF ANTI-GARP ANTIBODY AND IMMUNOMODULATOR
Provided is a pharmaceutical composition for use in the treatment or prevention of cancer, etc. The present invention provides a pharmaceutical composition or a method for treating cancer, wherein an anti-GARP antibody and an immunomodulator are administered in combination.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A pharmaceutical product for administration of an antibody-drug conjugate in combination with a DNA methyltransferase (DNMT) inhibitor is provided. The antibody-drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an antibody, in particular an anti-TR0P2 antibody, via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the DNMT inhibitor are administered in combination to a subject: Formula (I)
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
To provide a stable bispecific molecule.
To provide a stable bispecific molecule.
A Fab that specifically binds to CD3, the Fab comprising the following CDRH1 to 3 and CDRL1 to 3:
CDRH1 consisting of the amino acid sequence represented by SEQ ID NO: 32;
CDRH2 consisting of the amino acid sequence represented by SEQ ID NO: 33;
CDRH3 consisting of the amino acid sequence represented by SEQ ID NO: 34;
CDRL1 consisting of the amino acid sequence represented by SEQ ID NO: 35;
CDRL2 consisting of the amino acid sequence represented by SEQ ID NO: 36; and
CDRL3 consisting of the amino acid sequence represented by SEQ ID NO: 37.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
It is an object to provide an antibody specifically binding to CD37-positive tumor cells such as malignant B-cell lymphoma, an antibody-drug conjugate comprising the antibody, a pharmaceutical composition having therapeutic effects on a tumor using the antibody, a method for treating a tumor using the aforementioned pharmaceutical composition, a method for producing the antibody, and a method for producing the antibody-drug conjugate, and the like. The present invention provides an anti-CD37 antibody-drug conjugate in which an antibody is conjugated to a drug linker represented by the following formula (wherein A represents a connecting position to the antibody) by a thioether bond, specifically, a humanized anti-CD37 antibody having internalization ability and an antibody-drug conjugate containing the antibody.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present invention provides a chimeric polypeptide receptor in which an extracellular region comprising an antigenic region capable of being bound by an anti-human nicotinic acetylcholine receptor α1 subunit (nAChRα1) antibody, a transmembrane region, and an intracellular domain comprising an intracellular signaling domain are arranged in the presented order from the N-terminus towards the C-terminus, wherein an amino acid sequence of the antigenic region comprises the amino acid sequence as set forth in SEQ ID NO: 2 or an amino acid sequence derived from the amino acid sequence as set forth in SEQ ID NO: 2 by the substitution, deletion, insertion, and/or addition of one or several amino acids, a polynucleotide encoding the chimeric polypeptide receptor polypeptide, a cell expressing the chimeric polypeptide receptor, etc., which are useful in the treatment of myasthenia gravis.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61P 21/04 - Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof.
The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof.
3: e.g., a C1-C6 alkyl group.
C07D 307/94 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom spiro-condensed with carbocyclic rings or ring systems, e.g. griseofulvins
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/10 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 413/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
81.
NOVEL METHOD FOR PRODUCING ANTIBODY-IMMUNOSTIMULATOR CONJUGATE
The purpose of the present invention is to provide a novel stereoselective method for preparing a cyclic dinucleotide derivative and a production intermediate therefor, which can be used for an antibody-immunostimulant conjugate. Also provided is a method for producing a cyclic dinucleotide-linker and an antibody-immunostimulant conjugate while using the above production method. Further provided is a method for preparing a cyclic dinucleotide derivative, the method including the step of subjecting a compound (I) and a compound (IV) to stereoselective condensation using an optically active phosphitylating agent (Rc-II) or (Sc-II).
C07H 19/213 - Purine radicals with the saccharide radical being esterified by phosphoric or polyphosphoric acids containing cyclic phosphate
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
82.
METHOD FOR AVOIDING IMMUNE REJECTION USING AGONIST FOR INHIBITORY KIR
The purpose of the present invention is to provide: a substance which has an activity of binding to an inhibitory KIR to inhibit the cytotoxic activity of an NK cell and is useful for allogeneic technologies associated with organ transplantation and cell therapy; and a method for producing the substance. Provided are: a substance which has an activity of binding to an inhibitory KIR to inhibit the cytotoxic activity of an NK cell; and a cell which has the substance expressed on a cell surface thereof.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
A61K 35/22 - UrineUrinary tract, e.g. kidney or bladderIntraglomerular mesangial cellsRenal mesenchymal cellsAdrenal gland
A61K 35/28 - Bone marrowHaematopoietic stem cellsMesenchymal stem cells of any origin, e.g. adipose-derived stem cells
An object of the present invention is to provide a medicine that can simply treat and/or prevent a retinal degenerative disease associated with photoreceptor degeneration, including retinitis pigmentosa. The solution is to provide an agent for treating and/or preventing a retinal degenerative disease associated with photoreceptor degeneration, containing a compound having a retinoic acid receptor agonistic activity (for example, tamibarotene, tamibarotene methyl ester, tamibarotene ethyl ester, tazarotene, tazarotenic acid, adapalene, palovarotene, retinol, isotretinoin, alitretinoin, etretinate, acitretin or bexarotene) or a salt thereof.
A61K 31/196 - Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
A01K 67/0275 - Genetically modified vertebrates, e.g. transgenic
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
The present invention addresses the problem of providing a capsule particle manufacturing method. Provided is a method for manufacturing capsule particles by using a Taylor reactor.
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
TRI-INSTITUTIONAL THERAPEUTICS DISCOVERY INSTITUTE (USA)
DAIICHI SANKYO COMPANY, LIMITED (Japan)
Inventor
Poirier, John T.
Rudin, Charles
Lewis, Jason
Khan, Abdul
Andrew, David
Chen, Xinlei
Lorenz, Ivo
Matsunaga, Hironori
Abstract
The present invention provides a novel anti-DLL3 antibody-pyrrolodiazepine derivative and a novel anti-DLL3 anti-body-pyrrolodiazepine derivative conjugate using the same.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
86.
METHOD FOR PRODUCING COMPOUND HAVING TWO-BRANCHED N-ACETYL-D-GALACTOSAMINE STRUCTURE
The present invention addresses the problem of providing: a novel method for producing a N-acetyl-D-galactosamine ligand-oligonucleotide conjugate, particularly a novel method for producing a N-acetyl-D-galactosamine unit; and a novel intermediate. Studies have been made about the selective deprotection of a benzyl group using a palladium catalyst in a novel method for producing a N-acetyl-D-galactosamine unit. As a result, a novel production method that can achieve high quality and high yield and is industrially advantageous and a novel intermediate are discovered, which leads to the accomplishment of the invention.
C07H 15/12 - Acyclic radicals, not substituted by cyclic structures attached to a nitrogen atom of a saccharide radical
C07C 271/22 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
C07H 1/00 - Processes for the preparation of sugar derivatives
TRI-INSTITUTIONAL THERAPEUTICS DISCOVERY INSTITUTE (USA)
DAIICHI SANKYO COMPANY, LIMITED (Japan)
Inventor
Poirier, John T.
Rudin, Charles
Lewis, Jason
Khan, Abdul
Andrew, David
Chen, Xinlei
Lorenz, Ivo
Matsunaga, Hironori
Abstract
It is an object of the present invention to provide an antibody-drug conjugate of an antibody binding to DLL3 and a drug having antitumor activity, a pharmaceutical composition comprising the antibody-drug conjugate and having therapeutic effects on a tumor, a method for treating a tumor using the antibody-drug conjugate or the pharmaceutical composition, and the like. The present invention provides an antibody-drug conjugate of an antibody binding to DLL3 and a drug having antitumor activity, a pharmaceutical composition comprising the antibody or the antibody-drug conjugate, and a method for treating a tumor.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
88.
IMIDAZOPYRIDINE DERIVATIVES WITH BICYCLIC STRUCTURE
PUBLIC UNIVERSITY CORPORATION YOKOHAMA CITY UNIVERSITY (Japan)
DAIICHI SANKYO COMPANY, LIMITED (Japan)
Inventor
Namiki Hideki
Takeda Yasuyuki
Yoshikawa Kenji
Akiu Mayuko
Kawamoto Yoshito
Motoyama Keisuke
Yoshioka Shun
Minakawa Kosuke
Kadoshima Kumiko
Yoshihama Yohei
Tsunematsu Hiroki
Ono Shigeo
Yamashita Akio
Abstract
The present invention addresses the problem of providing a novel compound having an SMG1 inhibitory activity and an anticancer effect, or a pharmaceutically acceptable salt thereof etc. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof. (Here, in formula (1), R1, R2, R3, R4, X, Y, and Z are each as defined in the specification.)
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/5395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines having two or more nitrogen atoms in the same ring, e.g. oxadiazines
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 35/02 - Antineoplastic agents specific for leukemia
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
C07D 513/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains four or more hetero rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
Provided is an oligonucleotide which may induce an editing activity of ADRC in cell and has excellent stability in a living body. The oligonucleotide includes a first oligonucleotide identifying a target RNA and a second oligonucleotide linked to the 5′-side of the first oligonucleotide. The first oligonucleotide consists of a target-corresponding nucleotide residue, an oligonucleotide of 10 to 24 residues at the 3′-side, and an oligonucleotide of 3 to 6 residues at the 5′-side. The second oligonucleotide has no nucleotide residue corresponding to a nucleotide residue of the target RNA or has a nucleotide residue which does not form a complementary pair at the 3′-end thereof and the number of residue is 3 to 6. The residue at the 3′-side of the target-corresponding nucleotide residue is a 2′-deoxynucleotide residue, and the third nucleotide residue counted in the 3′-direction from the target-corresponding nucleotide in the oligonucleotide at the 3′-side of the target-corresponding nucleotide residue is a 2′-deoxy-2′-fluoronucleotide residue.
A method for producing a compound represented by formula (C) wherein R1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C).
A method for producing a compound represented by formula (C) wherein R1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C).
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
C07C 233/15 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
C07C 233/33 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
C07C 233/54 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07K 5/103 - Tetrapeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
The present invention is directed to methods of identifying and treating a human subject harboring a tumor or other disease comprising assessing HRG gene expression at a protein level in the human subject and administering a treatment comprising an anti-HER3 antibody to the human subject whose HRG gene expression at a protein level is assessed as high. The present invention is also directed to methods of identifying a human subject harboring a tumor or other disease comprising assessing HRG gene expression at a protein level in the human subject and withholding a treatment comprising an anti-HER3 antibody to the human subject whose HRG gene expression at a protein level is assessed as low. The invention is also directed to methods of performing an ELISA, including sequential steps of contacting a solid surface with a plurality of solutions each comprising in turn a capture antibody, a blocking agent, a sample suspected of containing an analyte, a detection antibody and an enzyme conjugate, in which the solid surface is subjected to a wash process after each sequential step.
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/40 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against enzymes
G01N 33/569 - ImmunoassayBiospecific binding assayMaterials therefor for microorganisms, e.g. protozoa, bacteria, viruses
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/48 - Ergoline derivatives, e.g. lysergic acid, ergotamine
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
96.
NOVEL OLIGOSACCHARIDE, PRODUCTION INTERMEDIATE FOR NOVEL OLIGOSACCHARIDE, PRODUCTION METHOD FOR NOVEL OLIGOSACCHARIDE, AND PRODUCTION METHOD FOR PRODUCTION INTERMEDIATE FOR NOVEL OLIGOSACCHARIDE
[Problem] The present invention addresses the problem of providing a novel oligosaccharide that is a two-branched glycan that has an α2,6-sialic acid structure at the non-reducing end, a production method for the oligosaccharide, an intermediate for the oligosaccharide, and a production method for the intermediate. [Solution] Provided are a novel oligosaccharide represented by formula A-22, a production method for the oligosaccharide as shown in fig. 1, an intermediate for the oligosaccharide, and a production method for the intermediate.
[Problem] It is desired to develop a molecule that maintains antitumor activity and offers excellent safety. It is also desired to develop an antibody-drug conjugate that can be administered systemically and delivers a STING agonist specifically to target cells or an organ (for example, a tumor site), and a therapeutic agent and/or therapeutic method that uses the antibody-drug conjugate and is for diseases related to STING agonist activity, for example, diseases (for example, cancers) to which immunostimulation therapy can be applied. [Solution] Provided are: an antibody-drug conjugate in which a CDN derivative characterized by having a fused tricyclic substituent is joined via a linker with a specific antibody including a mutant Fc region, or with a functional fragment of the antibody; and an antibody including a mutant Fc region.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/7064 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
A61K 31/708 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Clinical studies and trials of anticancer drugs; providing
information on clinical studies and trials of anticancer
drugs. Providing medical information in the field of anticancer
drugs; providing medical information on the efficacy, side
effects, interactions or administration of anticancer drugs.
The present invention is directed to methods of identifying and treating a human subject harboring a tumor or other disease comprising assessing HRG gene expression at an mRNA level in the human subject and administering a treatment comprising an anti-HER3 antibody to the human subject whose HRG gene expression at an mRNA level is assessed as high. The present invention is also directed to methods of identifying a human subject harboring a tumor or other disease comprising assessing HRG gene expression at an mRNA level in the human subject and withholding a treatment comprising an anti-HER3 antibody to the human subject whose HRG gene expression at an mRNA level is assessed as low.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
100.
NOVEL METHOD FOR PRODUCING ANTIBODY-DRUG CONJUGATE HAVING ANTINEOPLASTIC EFFECT
The purpose of the present invention is to provide: a novel stereoselective method for producing a cyclic dinucleotide derivative that can be used for an antibody-immunostimulator conjugate; and a production intermediate thereof. Another purpose is to provide a method for producing a cyclic dinucleotide-linker and antibody-immunostimulator conjugate, in which said production method is used. Provided is a method that makes it possible to produce, in large amounts and with high yield, a cyclic dinucleotide derivative having a desired steric configuration, by using an optically active phosphitylation agent twice, during coupling and cyclization.
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
A61K 31/7076 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
