A pharmaceutical product for administration of an antibody-drug conjugate in combination with a bispecific checkpoint 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, preferably an anti-TROP2 or anti-HER2 antibody, via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the bispecific checkpoint inhibitor are administered in combination to a subject:
A pharmaceutical product for administration of an antibody-drug conjugate in combination with a bispecific checkpoint 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, preferably an anti-TROP2 or anti-HER2 antibody, via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the bispecific checkpoint inhibitor are administered in combination 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 39/00 - Medicinal preparations containing antigens or 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
2.
COMBINATION OF ANTI-B7-H3 ANTIBODY-DRUG CONJUGATE AND ANDROGEN RECEPTOR SIGNALING INHIBITOR
In some aspects, a pharmaceutical product comprising an anti-B7-H3 antibody-drug conjugate and an androgen receptor signaling inhibitor for administration in combination is provided.
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 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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 aims to provide a novel compound having SF-1 antagonist activity and a polyfunctional molecule containing a moiety corresponding to the compound, particularly an SF-1 degrader. The present invention relates to a 3-phenylpropylamine derivative compound represented by the formula (1) and the like, and a polyfunctional molecule containing a moiety corresponding to the compound represented by the formula (1) and the like.
The present invention aims to provide a novel compound having SF-1 antagonist activity and a polyfunctional molecule containing a moiety corresponding to the compound, particularly an SF-1 degrader. The present invention relates to a 3-phenylpropylamine derivative compound represented by the formula (1) and the like, and a polyfunctional molecule containing a moiety corresponding to the compound represented by the formula (1) and the like.
C07D 309/04 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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
C07C 69/22 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety
C07D 211/14 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 211/22 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulfur atoms by oxygen atoms
C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ringAlkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
C07D 241/38 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
C07D 307/14 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 401/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 401/14 - 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 three or more hetero rings
C07D 405/12 - 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 chain containing hetero atoms as chain links
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
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.]
The objective of the invention is to provide a novel oligosaccharide, which can be used for producing a biantennary glycan having an α2,6-sialic acid structure at a non-reducing end, a method for production thereof, production intermediates thereof and a method for producing the intermediates, as well as a novel oligosaccharide, which is a biantennary glycan having an α2,6-sialic acid structure at a non-reducing end, a method for producing the oligosaccharide, intermediates thereof, and a method for producing the intermediates. Provided are a novel oligosaccharide represented by Formula A-13 or D-13:
The objective of the invention is to provide a novel oligosaccharide, which can be used for producing a biantennary glycan having an α2,6-sialic acid structure at a non-reducing end, a method for production thereof, production intermediates thereof and a method for producing the intermediates, as well as a novel oligosaccharide, which is a biantennary glycan having an α2,6-sialic acid structure at a non-reducing end, a method for producing the oligosaccharide, intermediates thereof, and a method for producing the intermediates. Provided are a novel oligosaccharide represented by Formula A-13 or D-13:
a method for producing the oligosaccharide represented by Formula A-13 or Formula D-13 shown in, for example, FIG. 1 or FIG. 3, intermediates thereof and a method for producing the intermediates.
A pharmaceutical composition and a therapeutic method wherein an antibody-drug conjugate and an immune checkpoint inhibitor are administered in combination, and 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 the antibody via a thioether bond; and a pharmaceutical composition and a therapeutic method for use in treatment of a disease that can be ameliorated through an antitumor immunity-activating effect wherein the antibody-drug conjugate is included.
A pharmaceutical composition and a therapeutic method wherein an antibody-drug conjugate and an immune checkpoint inhibitor are administered in combination, and 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 the antibody via a thioether bond; and a pharmaceutical composition and a therapeutic method for use in treatment of a disease that can be ameliorated through an antitumor immunity-activating effect wherein the antibody-drug conjugate is included.
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 9/00 - Medicinal preparations characterised by special physical form
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 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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 35/02 - Antineoplastic agents specific for leukemia
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
7.
EZH1/2 DUAL INHIBITOR-CONTAINING PHARMACEUTICAL COMPOSITION TO BE USED AS A COMBINATION DRUG
An object of the present invention is to provide a combination drug having an EZH1/2 dual inhibitor in combination with another medical agent and exerting an excellent anticancer effect. Provided is a combination drug having an EZH1/2 dual inhibitor in combination with another medical agent and exerting an excellent anticancer effect.
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
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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 31/475 - QuinolinesIsoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
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 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
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
A61K 31/7068 - 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
Provided is a vaccine for preventing and/or treating infection and symptom onset resulting from SFTSV. These lipid particles encapsulate a nucleic acid capable of expressing Gn, Gc, or NP of SFTSV, wherein the lipid includes an amphiphilic lipid, a sterol, a PEG lipid, and a cationic lipid.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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
The purpose of the present invention is to provide: a substance that is useful for allogeneic technologies relating to organ transplantation and cell therapy and that has an activity of binding to an inhibitory receptor on the surface of NK cells and suppressing the cytotoxic activity of NK cells; and a method for producing the same Provided are: a substance that has an activity of binding to an inhibitory receptor on the surface of NK cells and suppressing the cytotoxic activity of NK cells; and a cell in which the substance is expressed on the cell surface.
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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 aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
wherein each symbol is as described in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. In addition, the present invention also relates to a medicament containing the aforementioned compound, for the prophylaxis and/or treatment of diseases involving oxidative stress selected from the group consisting of chronic kidney disease, non-alcoholic steatohepatitis, chronic obstructive pulmonary disease, radiation skid: disorder, radiation mucosal disorder, cardiac failure, pulmonary arterial hypertension, Parkinson's disease, Friedreich's ataxia, multiple sclerosis, age-related macular degeneration, retinitis pigmentosa and glaucoma.
A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
C07D 417/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 419/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 419/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three 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
36 - Financial, insurance and real estate services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
(1) 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
(2) Advisory and consultancy services for patients in the field of patient access to medical treatment services; providing healthcare information to patients, patient advocates and health care professionals in the field of oncology disease information; providing information for patients and health care professionals in the field of oncology via a website; providing information for patients and healthcare professionals in the field of oncology and hematology; providing information to patients in the field of adverse event management; drug usage and information on side effects
Provided is a promoter having high foreign gene expression-enhancing activity in host cells such as cultured mammalian cells. An approach for using the promoter to enhance the production of a foreign protein to be used as a protein-based pharmaceutical product is the provision of a polynucleotide that is a Chinese hamster-derived gene promoter, the polynucleotide comprising a nucleotide sequence that is selected from SEQ ID NO: 1, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 10, SEQ ID NO: 11, SEQ ID NO: 12, SEQ ID NO: 13 and SEQ ID NO: 14, or has 85% or higher sequence identity to each of the sequences, or a partial sequence of the nucleotide sequence.
An antibody that can be used as an anti-tumor agent and an anti-tumor agent comprises a molecule containing such an antibody. Such an antibody or a binding fragment thereof comprises: a heavy chain CDRH1 consisting of SEQ ID NO: 54, a heavy chain CDRH2 consisting of SEQ ID NO: 55, a heavy chain CDRH3 consisting of SEQ ID NO: 56, a light chain CDRL1 consisting of SEQ ID NO: 57 or a light chain CDRL1 consisting of an amino acid sequence derived from SEQ ID NO: 57 in which amino acid 7 is W and/or amino acid 8 is K, a light chain CDRL2 consisting of SEQ ID NO: 58, and a light chain CDRL3 consisting of SEQ ID NO: 59 or a light chain CDRL3 consisting of an amino acid sequence derived from SEQ ID NO: 59 in which amino acid 2 is A or S.
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 39/00 - Medicinal preparations containing antigens or 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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
JAPAN AS REPRESENTED BY DIRECTOR GENERAL OF NATIONAL INSTITUTE OF INFECTIOUS DISEASES (Japan)
Inventor
Onishi Yoshiyuki
Watashi Koichi
Akazawa Daisuke
Abstract
One problem to be addressed by the present invention is to provide a drug which is capable of suppressing the proliferation of SARS-CoV-2 with high efficiency. Another problem to be addressed by the present invention is to provide a drug which exhibits an inhibitory effect on a wide range of coronaviruses and thereby can immediately respond to the pandemic of unknown SARS-CoV-2 mutants and new types of coronaviruses which could happen in the future. Provided is an oligonucleotide or a pharmaceutically acceptable salt thereof, wherein: the oligonucleotide comprises an oligonucleotide that is composed of 17-30 nucleotides and comprises a nucleotide sequence and is complementary to a region lying between a nucleotide located at position-13520 to a nucleotide located at position-13550 in SARS-CoV-2 RNA genome comprising the nucleotide sequence represented by SEQ ID NO: 1; and the oligonucleotide is a mixmer and is capable of inhibiting the viral proliferation of coronaviruses, wherein the 5'-end and/or the 3'-end of the oligonucleotide may be chemically modified. Also provided is a drug comprising the oligonucleotide or a pharmaceutically acceptable salt thereof.
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
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
The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
wherein each symbol is as described in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. In addition, the present invention also relates to a medicament containing the aforementioned compound, for the prophylaxis and/or treatment of diseases involving oxidative stress selected from the group consisting of chronic kidney disease, non-alcoholic steatohepatitis, chronic obstructive pulmonary disease, radiation skin disorder, radiation mucosal disorder, cardiac failure, pulmonary arterial hypertension, Parkinson's disease, Friedreich's ataxia, multiple sclerosis, age-related macular degeneration, retinitis pigmentosa and glaucoma.
A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
C07C 317/34 - SulfonesSulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
Provided are a pharmaceutical composition, treatment method, and anti-SIRPα antibody excellent in antitumor effect and safety aspects. A pharmaceutical composition and treatment method, wherein any one antibody-drug conjugate selected from the group consisting of Sacituzumab govitecan, Polatuzumab vedotin, and Trastuzumab emtansine, and an anti-SIRPα antibody are administered in combination, and an anti-SIRPα antibody to be administered in combination with an antibody-drug conjugate.
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 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 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
21.
COMBINATION OF ANTI-CDH6 ANTIBODY–DRUG CONJUGATE WITH OTHER AGENT
[Problem] To provide a novel drug combination treatment for diseases, particularly cancer. [Solution] The present invention provides a combination administration of an anti-CDH6 antibody–drug conjugate with another agent, such as an immune checkpoint inhibitor.
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 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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 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 31/7068 - 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic 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
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
[Problem] To provide a novel drug combination therapy for diseases, in particular, cancer. [Solution] Provided is a combination administration of an anti-EGFR antibody-drug conjugate with another agent such as an immune checkpoint inhibitor.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/7084 - Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
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
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
It is intended to provide an antitumor drug having an excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. There is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-TROP2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(═O)— wherein the anti-TROP2 antibody is connected to the terminal of L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2-C(═O)— moiety with the nitrogen atom of the amino group at position 1 as a connecting position.
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 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 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
[Problem] To provide a novel drug combination treatment for diseases, particularly cancer. [Solution] The present invention provides a combination administration of anti-HER2 antibody-drug conjugates with other agents, such as immune checkpoint inhibitors.
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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 31/7068 - 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic 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
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
05 - Pharmaceutical, veterinary and sanitary products
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical preparations and substances; medicines for
human purposes. Providing medical information in the field of pharmaceutical
preparations; providing medical information on the efficacy,
side effects, interactions or administration of
pharmaceutical preparations.
05 - Pharmaceutical, veterinary and sanitary products
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical preparations and substances; medicines for
human purposes. Providing medical information in the field of pharmaceutical
preparations; providing medical information on the efficacy,
side effects, interactions or administration of
pharmaceutical preparations.
38.
METHOD FOR PRODUCING PROTEIN USING ENVIRONMENTALLY RESPONSIVE PEPTIDE
The present invention addresses the problem of providing a new method for producing a protein. The problem is solved by a method for producing a molecule 1 comprising an [a] part, a [b] part, a [c] part, and optionally an [e] part. The method includes a step of bringing a starting sample containing one or more molecules 1 and one or more other molecules into contact with a carrier and separating the molecules 1 from other molecules, the number of the [c] parts contained in the other molecule being greater than the number of the [c] parts contained in the molecule 1 by one or more. The [a] part is a part 1 that binds to a target antigen; the [b] part is a first peptide that recognizes a target antigen binding site 1 contained in the [a] part; the [c] part is a second peptide comprising an amino acid sequence containing an amino acid side chain in which the charge changes from no charge to positive charge in response to the pH changing from a neutral condition to an acidic condition; and [e] part is an Fc region of the antibody.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
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
It is an object of the present invention to provide an antibody binding to CDH6 and having internalization activity, an antibody-drug conjugate of the antibody and a drug having antitumor activity, a pharmaceutical product comprising the antibody-drug conjugate and having therapeutic effects on a tumor, a method for treating a tumor using the antibody, the antibody-drug conjugate or the pharmaceutical product, and the like. The present invention provides an anti-CDH6 antibody having internalization activity, an antibody-drug conjugate of the antibody and a drug having antitumor activity, a pharmaceutical product comprising the antibody or the antibody-drug conjugate, and a method for treating a tumor.
A61K 9/00 - Medicinal preparations characterised by special physical form
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 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
The present invention provides a cyclic peptide represented by formula (I)
The present invention provides a cyclic peptide represented by formula (I)
The present invention provides a cyclic peptide represented by formula (I)
[wherein A is selected from the ring-forming groups A1 to A5; Xaa1 is a residue of an aromatic amino acid; Xaa2 is a residue of an aromatic amino acid, a basic amino acid, or an aliphatic amino acid; Xaa3 and Xaa8 each have a structure independently selected from a residue of an amino acid represented by formula (III) or (III′) in which thiol groups of Xaa3 and Xaa8 form a bond; Xaa4 is a residue of a neutral amino acid; Xaa5 is a residue of a basic amino acid; Xaa6 is a residue of a neutral amino acid or an acidic amino acid; Xaa7 is a residue of an aromatic amino acid; Xaa9 is a residue of an aromatic amino acid, an aliphatic amino acid, or a basic amino acid; Xaa10 is a residue of an aromatic amino acid; and Xaa11 is a residue of an aliphatic amino acid], or a pharmaceutically acceptable salt thereof.
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 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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
C07K 7/54 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
C07K 7/64 - Cyclic peptides containing only normal peptide links
The present invention pertains to novel antibody drug conjugates (ADC) comprising anti-MUC1 antibody. In particular, said ADC showed significant anti-tumor efficacy.
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 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 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
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
[Problem] To establish a method for producing an Fc-containing molecule having a homogeneous glycan structure with high purity with the smallest possible amount of a glycan donor molecule used, the method allowing free selection of an enzyme to be used from a wide range of options regardless of residual hydrolysis activity or the identity of the enzyme, and the like. [Solution] A novel method for producing an Fc-containing molecule having a desired N297-linked glycan, characterized by combining Steps 1 and 2 that are described in detail in the present specification, and the like are provided.
The present invention relates to crystals of (1'S,6'R)-7-chloro-2',4-dimethoxy-6'-methyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-3H-spiro[1]benzofuran-2,1'-cyclohexa[2]ene]-3,4'-dione (compound 6).
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 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
55.
COMBINATION OF MULTISPECIFIC MOLECULE AND IMMUNE CHECKPOINT INHIBITOR
Provided is a novel combination of medicaments for the treatment of a cancer. The present invention provides a pharmaceutical composition for the treatment and/or prevention of a cancer, comprising a multispecific antibody or antigen-binding fragment thereof [i], the pharmaceutical composition being used in combination with compound [ii] which is an immune checkpoint inhibitor or a chemotherapeutic.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
Provided is novel siRNA having an RNA interfering action and/or a gene expression suppressing action on mRNA encoding TfR2, or the like. An oligonucleotide or a pharmaceutically acceptable salt thereof, or the like, has a knockdown action on mRNA of transferrin receptor 2, and consists of an antisense strand region containing a target-matching sequence substantially complementary to a target sequence in mRNA encoding TfR2, and a sense strand region containing a nucleotide sequence substantially complementary to the target-matching sequence of the antisense strand region.
A pharmaceutical product for administration of an antibody-drug conjugate in combination with a blood brain barrier-penetrant PARP1 selective 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 anti-HER2 or anti-TROP2 antibody via a thioether bond. The antibody-drug conjugate is in particular trastuzumab deruxtecan (DS-8201) or datopotamab deruxtecan (DS-1062). The PARP1 selective inhibitor is in particular AZD 9574. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the blood brain barrier-penetrant PARP1 selective inhibitor are administered in combination 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
There is provided an oligonucleotide or a pharmaceutically acceptable salt thereof with a novel chemical modification pattern, which has a RNA interfering action and/or a gene expression suppressing action. A sense strand region has a specific modification pattern with a 3′-modified nucleoside, and an antisense strand region has, in a specific region, a modification pattern in which DNA, RNA, 2′-O,4′-C-bridging-modified nucleosides, 2′-MOE RNA or the like are appropriately combined.
05 - Pharmaceutical, veterinary and sanitary products
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseases Providing medical information in the field of pharmaceutical preparations; providing medical information on the efficacy, side effects, interactions or administration of pharmaceutical preparations
05 - Pharmaceutical, veterinary and sanitary products
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Pharmaceutical preparations and substances for use in oncology; pharmaceutical preparations for the treatment of cardiovascular diseas Providing medical information in the field of pharmaceutical preparations; providing medical information on the efficacy, side effects, interactions or administration of pharmaceutical preparations.
62.
COMPOSITION FOR NUCLEOTIDE SEQUENCE EDITING, AND NUCLEOTIDE SEQUENCE EDITING METHOD USING SAME
Provided are a composition and others, the composition containing a first single-stranded polynucleotide and a third single-stranded polynucleotide, wherein: the first single-stranded polynucleotide has a length of 50-200 nucleotides; the nucleotide sequence for the first single-stranded polynucleotide has 80% or higher sequence identity with the nucleotide sequence for a portion of an editing target strand in a target region present in double-stranded DNA in a cell, and includes at least one mutation for editing purpose selected from the group consisting of deletion, substitution and insertion of one nucleotide or a plurality of nucleotides compared with the nucleotide sequence for the editing target strand; the third single-stranded polynucleotide has a length of 15-200 nucleotides; the nucleotide sequence for the third single-stranded polynucleotide has 90% or higher sequence identity with a nucleotide sequence that is included in the editing target strand and is located closer to the 5'-terminus or the 3'-terminus than a position corresponding to the position of the mutation for editing purpose in the first single-stranded polynucleotide; and, in the editing target strand, the nucleotide sequence having the sequence identity with the first single-stranded polynucleotide and the nucleotide sequence having the sequence identity with the third single-stranded polynucleotide overlap with each other, or are located adjacent to each other, or are separated from each other with 1 to 9 nucleotides interposed therebetween.
This invention provides a masked antibody having performance superior to that of conventional masked antibodies. The masked antibody is a target-antigen-binding molecule comprising a moiety [a], a moiety [b], and a moiety [c]: i.e., a moiety [a]: a moiety binding to a target antigen; a moiety [b]: a first peptide recognizing a target antigen-binding site in the moiety [a]; and a moiety [c]: a second peptide consisting of an amino acid sequence comprising amino acids that are converted from an uncharged state to a positively charged state in response to a pH change from neutral to acidic conditions at a pH 7.5 or lower.
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
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
66.
COMBINATION OF ANTIBODY-DRUG CONJUGATE AND RASG12C INHIBITOR
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with a RASG12C inhibitor is provided. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the RASG12C inhibitor are administered in combination to a subject.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
Provided are: a novel photosensitive substance; an antibody-photosensitive substance conjugate obtained by binding the photosensitive substance and an antibody via a linker; and an antitumor agent containing the antibody-photosensitive substance conjugate. [Solution] An antibody-photosensitive substance conjugate is represented by formula (1). (In formula (1), Ab represents an antibody or an antigen-binding fragment of the antibody, L represents a linker that links Ab and P, Ab is directly bound to L through the amino acid residue or indirectly bound to L through the glycan chain, P represents a monovalent group derived from a photosensitive substance and connected to L, and x represents a number in the range of 1 to 10.)
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 31/409 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having four such rings, e.g. porphine derivatives, bilirubin, biliverdine
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 35/02 - Antineoplastic agents specific for leukemia
C07D 487/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups in which the condensed system contains four or more hetero rings
In one aspect, the effect of cancer treatment or prevention in using a pharmaceutical composition containing an anti-CD147 antibody or an antigen-binding fragment thereof is further enhanced. In one aspect, when a combination of a pharmaceutical composition containing an anti-CD147 antibody or an antigen-binding fragment thereof with another antitumor agent is used in a subject in need thereof, the effect of cancer treatment or prevention is further enhanced.
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
A61K 31/7068 - 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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
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
A pharmaceutical product for administration of an antibody-drug conjugate in combination with an anti-PD- l /TIM-3 bispecific binding protein 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-TROP2 antibody or an anti-HER2 antibody, via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the anti- PD-l/TIM-3 bispecific binding protein are administered in combination 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
Provided is a composition for cytotoxic T cell depletion, comprising an anti-LAG-3 antibody or a binding fragment thereof having the properties described in (i) to (iii) below: (1) having in vitro ADCC activity; (ii) reducing, in a low fucose form, the number of LAG-3 positive cells in vivo; and (iii) binding to activated human T cells. Also provided are methods for depleting cytotoxic T cells using the disclosed anti-LAG-3 antibody or binding fragment 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 39/00 - Medicinal preparations containing antigens or antibodies
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
Provided are novel antibody-pyrrolodiazepine derivatives and novel antibody-pyrrolodiazepine derivative conjugates, as well as methods of using the same, and a novel CLDN6 and/or CLDN9 antibody. The disclosed compounds are of the class of alkyl benzene sulfonyl ureas, useful as oral anti-diabetics, and include substituted benzo[e]pyrrolo[1,2-α][1,4]diazepine.
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
74.
METHOD FOR PRODUCING N-PYRIDYLSULFONAMIDE COMPOUND, PYRIDINE COMPOUND, AND CRYSTAL OF N-PYRIDYLSULFONAMIDE COMPOUND
Disclosed is a production method that involves synthesizing an N-pyridylsulfonamide compound (III) by means of a coupling reaction between a pyridine compound (I) and a sulfonamide compound (II).
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61P 43/00 - Drugs for specific purposes, not provided for in groups
The purpose of the present invention is to provide a novel compound having SF-1 antagonist activity, and a polyfunctional molecule comprising a moiety corresponding to this compound, particularly an SF-1 degrader. The present invention relates to a 3-phenylpropylamine derivative compound represented by formula (1), etc., and a polyfunctional molecule comprising a moiety corresponding to the compound represented by formula (1), etc.
C07D 211/46 - Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/438 - 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 being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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 31/4545 - 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 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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 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
A61P 5/42 - Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
A61P 5/46 - Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 309/04 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 309/06 - Radicals substituted by oxygen atoms
C07D 401/14 - 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 three or more hetero rings
C07D 405/12 - 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 chain containing hetero atoms as chain links
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 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
76.
ANTISENSE OLIGONUCLEOTIDE AND COMPOSITION FOR PREVENTION OR TREATMENT OF GLYCOGEN STORAGE DISEASE TYPE IA
NATIONAL CENTER FOR CHILD HEALTH AND DEVELOPMENT (Japan)
HIROSHIMA UNIVERSITY (Japan)
DAIICHI SANKYO COMPANY, LIMITED (Japan)
Inventor
Tajima, Go
Okada, Satoshi
Tsumura, Miyuki
Abstract
The present invention provides a novel antisense oligonucleotide and a composition for preventing or treating glycogen storage disease type Ia. The present invention provides an antisense oligonucleotide which hybridizes with a pre-mRNA sequence derived from a region including at least one of a base at position 42911000, a base at position 42911004, and a base at position 42911005 in a base sequence of human chromosome 17 of GRCh38/hg38 and has activity to inhibit aberrant splicing of pre-mRNA of c.648G>T variant G6PC.
The present invention provides, for example, a new siRNA that has a gene expression suppression effect and/or an RNA interference effect on an mRNA encoding PLN. Provided is: an oligonucleotide having a knockdown effect on a PLN mRNA, the oligonucleotide comprising an antisense strand region including a target corresponding sequence complementary to a target sequence in an mRNA encoding PLN, and a sense strand region including a nucleotide sequence complementary to the target corresponding sequence of the antisense strand region; or a pharmaceutically acceptable salt of the oligonucleotide.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
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
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
78.
SIRNA CAPABLE OF SUPPRESSING EXPRESSION OF α-SYNUCLEIN
The purpose of the present invention is, for example, to provide novel siRNA that has a gene expression suppressing effect and/or an RNA interference effect with respect to mRNA encoding SNCA. Provided are an oligonucleotide having a knockdown effect on SNCA mRNA, the oligonucleotide comprising an antisense strand region containing a target corresponding sequence complementary to a target sequence in mRNA encoding SNCA, and a sense strand region containing a nucleotide sequence complementary to the target corresponding sequence in the antisense strand region, or a pharmaceutically acceptable salt of the oligonucleotide etc.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 31/711 - Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61K 31/7115 - Nucleic acids or oligonucleotides having modified bases, i.e. other than adenine, guanine, cytosine, uracil or thymine
A61K 31/712 - Nucleic acids or oligonucleotides having modified sugars, i.e. other than ribose or 2'-deoxyribose
A61P 25/00 - Drugs for disorders of the nervous 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
The present invention aims to provide a medicament capable of treating and/or preventing diseases associated with oxidative stress by inhibiting the protein-protein interaction between Keap1 and Nrf2 and activating Nrf2. The present invention relates to a compound represented by the following formula (1):
wherein each symbol is as described in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. In addition, the present invention also relates to a medicament containing the aforementioned compound, for the prophylaxis and/or treatment of diseases involving oxidative stress selected from the group consisting of chronic kidney disease, non-alcoholic steatohepatitis, chronic obstructive pulmonary disease, radiation skin disorder, radiation mucosal disorder, cardiac failure, pulmonary arterial hypertension, Parkinson's disease, Friedreich's ataxia, multiple sclerosis, age-related macular degeneration, retinitis pigmentosa and glaucoma.
C07D 409/06 - 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 only aliphatic carbon atoms
A61K 31/4353 - 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
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/554 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
C07D 417/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 419/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 419/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms containing three 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
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
81.
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
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 personalized healthcare and medical information in the nature of the efficacy, side effects, interactions and administration of pharmaceutical preparations
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
