Abstract: To provide a method of detecting abnormal bone metabolism by using a gene strongly expressed in an osteoclast; a method of screening a compound having a therapeutic and/or preventive effect on abnormal bone metabolism; and a pharmaceutical composition for treating and/or preventing abnormal bone metabolism. Provision of a method of detecting abnormal bone metabolism by using the expression of human Siglec-15 gene as an index; a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation; and the like.
Abstract: A pharmaceutical for the prophylaxis or treatment of hypertension or a disease derived from hypertension. The pharmaceutical is characterized by comprising (i) a specific mineralocorticoid receptor antagonist and (ii) one or more components selected from the following components (A) to (C), for administration simultaneously or separately at a time interval: (A) an angiotensin II receptor antagonist, (B) a calcium antagonist, and (C) a diuretic.
Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
Abstract: It is intended to provide a double-stranded polynucleotide that is resistant to RNase and has RNA interference effect, etc. The present invention provides a double-stranded polynucleotide comprising sense and antisense strands comprising polynucleotides comprising a nucleotide unit of DNAs and 2?-O-methyl RNAs alternately combined.
Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I): wherein R1 represents a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R2 and R3 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R4 and R5 are the same or different and each represent a hydrogen atom, an optionally substituted C1-6 alkyl group, or the like, R6 represents a hydrogen atom or the like, each R7 may be the same or different and may each represent an optionally substituted C1-6 alkoxy group or the like, X represents —CH?, —C(—R7)?, or —N?, and m represents 1 to 4, or a pharmacologically acceptable salt thereof.
Type:
Grant
Filed:
April 6, 2017
Date of Patent:
January 30, 2018
Assignees:
Daiichi Sankyo Company, Limited, Sandford Burnham Prebys Medical Discovery Institute
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 (I) 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- or -L1-L2-LP- wherein the antibody is connected to the terminal of L1, the antitumor compound is connected to the terminal of Lc or LP, and any one or two or more of linkers of L1, L2, and LP has a hydrophilic structure.
Abstract: It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway.
Abstract: The present invention relates to a transfected mammalian host cell whose ability to secrete a foreign protein has been enhanced by using a foreign gene expression vector having a promoter derived from a human gene, and a method for producing the foreign protein using the host cell. A method for enhancing the production of a foreign protein to be used in a pharmaceutical protein product in a host cell such as a cultured mammalian cell is provided. A promoter derived from a human gene having a promoter activity higher than that of a cytomegalovirus (CMV) promoter in a host cell such as a cultured mammalian cell is provided.
Abstract: The present invention relates to an antibody which has a therapeutic effect on cancer, an autoimmune disease, or an inflammatory disease. That is, the present invention relates to an antibody which exhibits a cytotoxic activity against death domain-containing receptor-expressing cells through apoptosis. [Object] An object of the invention is to provide a pharmaceutical having a therapeutic effect on cancer. [Means for Resolution] A novel anti-DR5 antibody capable of inducing apoptosis in cells has more potent cytotoxic activity than currently available anti-DR5 antibodies.
Abstract: It is intended to provide a novel pharmaceutical composition that can promote fibrinolysis. The present invention provides a pharmaceutical composition for the promotion of fibrinolysis, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt. The present invention further provides a pharmaceutical composition for the promotion of fibrinolysis, comprising edoxaban or a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt and further comprising a TAFIa inhibitor.
Abstract: The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.
Type:
Application
Filed:
September 8, 2017
Publication date:
December 28, 2017
Applicant:
Daiichi Sankyo Company, Limited
Inventors:
Masashi Watanabe, Hiroshi Nagasawa, Noritada Sato
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:
June 20, 2016
Date of Patent:
December 26, 2017
Assignees:
DAIICHI SANKYO COMPANY, LIMITED, SAPPORO MEDICAL UNIVERSITY
Inventors:
Toshinori Agatsuma, Shu Takahashi, Jun Hasegawa, Daisuke Okajima, Hirofumi Hamada, Miki Yamaguchi
Abstract: Disclosed herein are therapeutic agents and/or preventive agents for pain or therapeutic agents and/or preventive agents for a sodium channel associated disease.
Abstract: An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.
Abstract: Provided are an orally disintegrating tablet that quickly disintegrates when it is placed in the mouth or put into water, provides favorable taste, has a sufficient hardness in general production, transportation and use and is excellent in terms of storage stability, and a process for the production of the same which is excellent in terms of industrial production. An orally disintegrating tablet containing a drug, a crystalline cellulose having a bulk density of 0.23 g/cm3 or less (preferably from 0.10 g/cm3 to 0.23 g/cm3), a sugar alcohol and a pregelatinized starch.
Abstract: An object is to provide a hydromorphone hydrochloride- or oxycodone hydrochloride hydrate-containing sustained-release pharmaceutical composition for oral administration that reliably exhibits its main pharmacological effect and has excellent formulation stability that avoids dose dumping of the principal drug, such as alcohol resistance. The present invention provides a sustained-release pharmaceutical composition comprising (A) hydromorphone hydrochloride or oxycodone hydrochloride hydrate, (B) hydroxypropyl methylcellulose acetate succinate having a median size (D50) of 40 ?m or smaller, (C) hydroxypropyl cellulose, and (D) a saccharide, wherein the content ratio of the component (C) to the component (B) by weight in the composition, (C)/(B), is 11/3 to 3/11.
Abstract: To provide a method of detecting abnormal bone metabolism by using a gene strongly expressed in an osteoclast; a method of screening a compound having a therapeutic and/or preventive effect on abnormal bone metabolism; and a pharmaceutical composition for treating and/or preventing abnormal bone metabolism. Provision of a method of detecting abnormal bone metabolism by using the expression of human Siglec-15 gene as an index; a pharmaceutical composition containing an antibody which specifically recognizes human Siglec-15 and has an activity of inhibiting osteoclast formation; and the like.
Abstract: An object is to provide a solid composition of stabilized pyrrole carboxamide. A means for achieving the object is a solid composition for medical use containing (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide and an appropriate additive.
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: It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.
Type:
Application
Filed:
October 1, 2015
Publication date:
November 2, 2017
Applicants:
Daiichi Sankyo Company, Limited, National Cancer Center