Abstract: 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.
Type:
Grant
Filed:
January 24, 2019
Date of Patent:
May 18, 2021
Assignees:
DAIICHI SANKYO COMPANY, LIMITED, SAPPORO MEDICAL UNIVERSITY
Inventors:
Toshinori Agatsuma, Shu Takahashi, Jun Hasegawa, Daisuke Okajima, Hirofumi Hamada, Miki Yamaguchi
Abstract: The present invention provides a conjugate comprising a hANP peptide bonded via a polyethylene glycol linker to a glycan attached to Asn297 of a Fc-containing molecule (N297 glycan), or a pharmaceutically acceptable salt thereof, a medicament comprising the same as an active ingredient, a method for producing the same, etc.
Abstract: The present invention provides an EndoS mutant enzyme having an amino acid sequence of EndoS D233Q and further having a particular additional mutation and exhibiting a reduced hydrolysis activity, in comparison with the activity of EndoS D233Q, to an N-linked sugar chain (N297-linked sugar chain) linked to Asn at position 297 in IgG and a gene encoding the same.
Abstract: A pharmaceutical composition comprising (i) an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents a connecting position to an antibody) is conjugated to the antibody via a thioether bond, (ii) a histidine buffer, (iii) sucrose or trehalose, and (iv) a surfactant; and a method of lyophilizing the pharmaceutical composition.
Abstract: The present invention relates to the medical use of antibodies against the FGF receptor 4 (FGFR4) combined with Sorafenib, in particular for the prevention or treatment of hyperproliferative diseases associated with FGFR expression, overexpression or hyperactivity.
Type:
Grant
Filed:
February 9, 2017
Date of Patent:
May 4, 2021
Assignees:
Daiichi Sankyo Europe GmbH, Daiichi Sankyo Company Limited
Abstract: As an antitumor drug 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 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.
Abstract: 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.
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: Provided are compositions comprising Compound I having the following structure: or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
Abstract: An object of the present invention is to provide a vector capable of oligodendrocyte-specifically suppressing expression of the PLP1 gene for treating PMD caused by abnormality of the PLP1 gene, and a promoter and miRNA therefor, and a pharmaceutical composition comprising the vector. The oligodendrocyte-specific promoter of the present invention comprises a nucleic acid having a sequence identity of at least 90% to a nucleotide sequence set forth in SEQ ID NO: 1. The miRNA of the present invention specific to the PLP1 gene comprises a pair of nucleotide sequences consisting of a specific antisense sequence and sense sequence.
Type:
Application
Filed:
February 6, 2019
Publication date:
March 25, 2021
Applicants:
NATIONAL CENTER OF NEUROLOGY AND PSYCHIATRY, NIPPON MEDICAL SCHOOL FOUNDATION, DAIICHI SANKYO COMPANY, LIMITED
Abstract: The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1, 3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R1, R2, R3, R4, R5, R6, and V in the formula (I) are each as defined in the present specification).
Abstract: The present invention provides a modified atrial natriuretic peptide that exhibits prolonged duration in blood and maintains cGMP elevating activity. The present invention provides a modified peptide in which at least one sugar substance is linked directly through a glycosidic bond or via a linker structure to at least one hANP peptide, or a pharmaceutically acceptable salt thereof, a medicament comprising the modified peptide or the salt thereof as an active ingredient, etc.
Abstract: It is an object of the present invention to provide a new compound capable of efficiently inducing differentiation from pluripotent stem cells into insulin-producing cells. The object of the present invention is achieved by a compound represented by formula (I): wherein R1, R2, R3, n and A have the same meanings as defined in the description, respectively, or a salt thereof.
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. Provided is a pharmaceutical composition containing, as an active ingredient, a compound represented by formula (I) or a pharmacologically acceptable salt thereof. In the formula (I), R1 and R2 are the same or different, and represent a C1-C6 alkyl group, a halogeno C1-C6 alkyl group or a C3-C6 cycloalkyl group; n represents 0, 1 or 2; each X represents a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a halogen atom or the like; and Y represents a hydrogen atom, a C1-C6 alkoxy group, a C3-C6 cycloalkoxy group or a halogeno C1-C6 alkoxy group.
Abstract: The object of the present invention is to improve the post-transplantation engraftment rate of cardiomyocytes that have been purified to such an extent that they are free from non-cardiomyocytes and any components derived from other species. To solve this problem, the present inventors studied the possibility of constructing cell masses from the purified cardiomyocytes. As a result, they revealed that the stated problem could be solved by providing a method of preparing cell masses of cardiomyocytes derived from pluripotent stem cells, characterized in that cell masses of aggregated cells containing cardiomyocytes that had been differentiated and induced from pluripotent stem cells were dispersed to single cells to thereby obtain purified cardiomyocytes, which were then cultured in a culture medium under serum-free conditions so that they were reaggregated.
Type:
Grant
Filed:
July 14, 2015
Date of Patent:
February 16, 2021
Assignees:
DAIICHI SANKYO COMPANY, LIMITED, HEARTSEED INC.
Abstract: The present invention directs to provide a novel compound for treating and/or preventing pain, having excellent skin permeation and reduced skin irritation.
Abstract: The present invention provides a modified atrial natriuretic peptide that exhibits prolonged duration in blood and maintains cGMP elevating activity. The present invention provides a modified peptide in which at least one sugar substance is linked directly through a glycosidic bond or via a linker structure to at least one hANP peptide, or a pharmaceutically acceptable salt thereof, a medicament comprising the modified peptide or the salt thereof as an active ingredient, etc.
Abstract: The present invention provides a pharmaceutical composition comprising an antibody which binds specifically to human TLR7 or monkey TLR7 and does not bind to mouse TLR7 or rat TLR7, and has an activity of inhibiting a function of human TLR7 or monkey TLR7, and the like.
Type:
Application
Filed:
October 13, 2020
Publication date:
February 11, 2021
Applicants:
Daiichi Sankyo Company, Limited, The University of Tokyo
Abstract: It is an object of the present invention to provide an antibody specifically binding to GPR20-positive tumor cells such as GIST, a pharmaceutical product comprising the antibody and having therapeutic effects on a tumor, a method for treating a tumor using the aforementioned pharmaceutical product, and the like. It is another object of the present invention to provide an anti-GPR20 antibody having internalization activity, an antibody-drug conjugate containing the antibody, and the like.