Abstract: A novel anti-HER2 antibody-pyrrolobenzodiazepine (PBD) derivative conjugate, a medicine having therapeutic effect against tumor with the antibody-drug conjugate, and a method for treating a tumor by using the antibody-drug conjugate or medicine.
Abstract: To provide an antitumor drug having excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. Provided is an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER3 antibody via a linker having a structure represented by the formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(?O)— or -L1-L2-LP- (the anti-HER3 antibody is connected to the terminal of L1, the antitumor compound is connected to the carbonyl group of —(CH2)n2-C(?O)— moiety or the C terminal of LP, with the nitrogen atom of the amino group at position 1 as a connecting position).
Type:
Application
Filed:
February 10, 2022
Publication date:
June 2, 2022
Applicants:
DAIICHI SANKYO COMPANY, LIMITED, DAIICHI SANKYO EUROPE GMBH
Abstract: A novel antibody-pyrrolobenzodiazepine (PBD) derivative conjugate, a medicine having therapeutic effect against tumor with the antibody-drug conjugate, and a method for treating a tumor by using the antibody-drug conjugate or medicine.
Abstract: A pharmaceutical composition for treatment of cancer or a method for treating cancer, wherein an antibody-pyrrolobenzodiazepine derivative conjugate and a PARP inhibitor are administered in combination.
Abstract: An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: wherein R1 and R2 are the same or different, and represent a C1-C6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.
Abstract: 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.
Abstract: A method for producing a compound represented by formula (C) wherein R1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C).
Abstract: The present invention provides a medicament comprising a compound represented by general formula (1) which has Axl inhibitory activity, and an EGFR tyrosine kinase inhibitor in combination, and a method for treating cancer using this combination. The present invention provides an excellent medicament and method for treating cancer which is highly effective for inhibiting resistance to an EGFR tyrosine kinase inhibitor in cancer treatment, and causes less adverse reactions such as weight loss.
Abstract: 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, addition and/or insertion of 1 to 5 (inclusive) amino acids has occurred at amino acids other than the 1st Xaa to the 12th Xaa counting from the amino terminus.
Abstract: The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and/or CLDN9 antibody.
Abstract: This application provides: an antibody which specifically binds to an ALK2 protein and has an activity of inhibiting BMP signal transduction mediated by ALK2; a method for producing the antibody; and a pharmaceutical composition comprising the antibody, for treating and/or preventing ectopic ossification and/or bone dysplasia, anemia, or diffuse intrinsic pontine glioma (DIPG).
Type:
Grant
Filed:
August 19, 2019
Date of Patent:
April 26, 2022
Assignees:
Saitama Medical University, Daiichi Sankyo Company, Limited
Abstract: The present invention provides a pharmaceutical composition containing an inhibitor selected from the group consisting of an EZH1 inhibitor, an EZH2 inhibitor and an EZH1/2 dual inhibitor as an active ingredient, for use in treating HTLV-1-associated myelopathy. The present invention provides a pharmaceutical composition for use in treating HTLV-1-associated myelopathy, containing a 1,3-benzodioxole derivative or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 18, 2018
Date of Patent:
April 26, 2022
Assignees:
DAIICHI SANKYO COMPANY, LIMITED, ST. MARIANNA UNIVERSITY SCHOOL OF MEDICINE
Abstract: A method of producing a tablet in which an uncoated tablet is coated by a coating agent, the method including: a coating process of coating uncoated tablets with a coating agent by spray coating the coating agent onto tablets that are churned and tumbled inside a container, and drying the tablets inside the container by supplying drying air into the container and exhausting air from the container, wherein spray coating conditions, including air supply temperature, air supply rate, and spray speed, are controlled according to the weight of the coating agent with which the uncoated tablets are coated, such that the humidity of air exhausted during spray coating is within a range of from 14% RH to 30% RH.
Type:
Grant
Filed:
August 13, 2018
Date of Patent:
April 19, 2022
Assignees:
FUJIFILM Business Innovation Corn., Daiichi Sankyo Company, Limited
Abstract: To provide an antitumor drug having excellent therapeutic effect, which is excellent in terms of antitumor effect and safety. Provided is an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER3 antibody via a linker having a structure represented by the formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2-C(?O)— or -L1-L2-LP- (the anti-HER3 antibody is connected to the terminal of L1, the antitumor compound is connected to the carbonyl group of —(CH2)n2-C(?O)— moiety or the C terminal of LP, with the nitrogen atom of the amino group at position 1 as a connecting position).
Type:
Grant
Filed:
January 31, 2019
Date of Patent:
April 12, 2022
Assignees:
DAIICHI SANKYO COMPANY, LIMITED, DAIICHI SANKYO EUROPE GMBH
Abstract: An object of the present invention is to provide a novel anti-CD147 antibody exhibiting potent antitumor efficacy and having excellent safety. Another object of the present invention is to provide a pharmaceutical product comprising such an antibody. Another object of the present invention is to provide a method for treating tumors using the antibody or the pharmaceutical product, for example. The present invention provides a CD147-specific antibody that activates CD147 and exhibits high antitumor efficacy. The present invention provides the anti-CD147 antibody that exhibits high antitumor efficacy independent of effector functions. The present invention provides a pharmaceutical composition comprising such an anti-CD147 antibody. The present invention provides a method for treating tumors using such an anti-CD147 antibody and/or pharmaceutical composition.
Abstract: A novel peptide which comprises an amino acid sequence represented by SEQ ID NO: 23, and specifically inhibits the protease activity of a target molecule.
Abstract: SPINK2 mutant peptide conjugates are provided that inhibit KLK5. The KLK5 inhibitory peptide conjugates are Fc fusion peptides in which, in certain embodiments, the Fc region of the fusion peptides are the Fc region of human IgG1 or a fragment thereof. The KLK5 inhibitory peptide conjugates include an amino acid sequence of one of SEQ ID NOs: 34, 36, 38, 40, 42, 44, 46, 48, 96, 50, 52, 54, 56, 58, or 60. Pharmaceutical compositions that include the KLK5 inhibitory peptide conjugates useful for treating KLK5-related diseases are also provided.
Abstract: To provide a method for purifying an antibody to a sufficient degree of purity for therapeutic use in humans by removing impurities contained in a solution efficiently while reducing production cost and the purification period in the purification of the antibody. It was found that an antibody can be reliably purified to a high degree of purity by an activated carbon material, regardless of the amounts or species of impurities co-present, and that high viral clearance can be attained reliably. Based on the finding, a treatment with an activated carbon material could be used in place of AEX chromatography achieving viral clearance in a step of purifying a therapeutic antibody using CHO cells. As a result, an antibody can be simply and effectively purified to a sufficient degree of purity for therapeutic use in humans compared to a conventional purification method, while reducing production cost.
Abstract: 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.
Abstract: The present invention provides a compound having excellent histone acetyl transferase inhibitory activity against EP300 and/or CREBBP, or a pharmacologically acceptable salt thereof. The compound is represented by the following formula (1) or a pharmacologically acceptable salt thereof: wherein ring Q1, ring Q2, R1, R2, R3 and R4 respectively have the same meanings as defined in the specification.