Patents Assigned to Daiichi Sankyo Company, Limited
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Patent number: 10005725Abstract: 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: GrantFiled: September 8, 2017Date of Patent: June 26, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Masashi Watanabe, Hiroshi Nagasawa, Noritada Sato
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Publication number: 20180170926Abstract: A crystal of a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R1 is a hydrogen atom or a hydroxy group, and R is a 2-(trifluoromethyl)pyrimidin-5-yl group or a 5-(trifluoromethyl)pyrazin-2-yl group.Type: ApplicationFiled: June 10, 2016Publication date: June 21, 2018Applicant: Daiichi Sankyo Company, LimitedInventors: Katsuhiro Kobayashi, Toshio Kaneko
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Publication number: 20180148424Abstract: It is an object of the present invention to provide an excellent method for producing an excellent therapeutic agent. The solution of the present invention is as shown in the following scheme: wherein R1 represents a C1-C6 alkyl group, R2 represents a C1-C6 alkyl group, and R3 represents a C1-C6 alkyl group.Type: ApplicationFiled: April 22, 2016Publication date: May 31, 2018Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Masayuki MURAKAMI, Yuichi AKI, Daisuke FUKATSU, Kenichi KIMURA, Makoto MICHIDA, Koji HAMAOKA
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Publication number: 20180147292Abstract: A method for producing an antibody-drug conjugate composition, comprising: (i) a step of reacting an antibody with a reducing agent in a buffer to reduce interchain disulfides, and (ii) a step of reacting drug linker intermediates with the antibody having thiol groups obtained in the step (i), wherein the reaction temperature in the step (i) is ?10° C. to 10° C., and the average number of bound drugs in the produced antibody-drug conjugate composition is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, in the produced antibody-drug conjugate composition is 50% or more; and an antibody-drug conjugate composition, wherein the content of antibody-drug conjugates wherein the average number of bound drugs is 3.5 to 4.5, and the content of antibody-drug conjugates in which four drug linkers are bound to heavy-light interchain thiols, is 50% or more.Type: ApplicationFiled: June 28, 2016Publication date: May 31, 2018Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shigeru NOGUCHI, Ken SAKURAI, Daisuke OKAJIMA
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Publication number: 20180141960Abstract: 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: ApplicationFiled: January 18, 2018Publication date: May 24, 2018Applicants: Daiichi Sankyo Company, Limited, Sanford Burnham Prebys Medical Discovery InstituteInventors: Shojiro Miyazaki, Yuko Yamamoto, Keisuke Suzuki, Masaharu Inui, Masanori Izumi, Kaori Soma, Anthony Pinkerton, Taeko Shinozaki
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Patent number: 9977846Abstract: A real-time release testing capable of constantly ensuring quality, a method for quality testing of a product using real-time release testing, a method for quality testing of an in-process product and/or an end product by real-time release testing, comprising the step of assessing the quality from design space established with only material attributes as inputs, and a manufacturing parameter-independent method for quality testing of a product using real-time release testing.Type: GrantFiled: July 6, 2012Date of Patent: May 22, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Hiroshi Nakagawa, Makoto Kamada, Jin Maeda
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Publication number: 20180133314Abstract: The present invention provides a pharmaceutical composition or a diagnostic composition targeting human fibroblast growth factor receptor 2 (hFGFR2).Type: ApplicationFiled: April 19, 2016Publication date: May 17, 2018Applicant: Daiichi Sankyo Company, LimitedInventors: Chigusa YOSHIMURA, Reimi KAWAIDA, Kokichi HONDA
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Publication number: 20180118835Abstract: 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: ApplicationFiled: January 29, 2016Publication date: May 3, 2018Applicants: Saitama Medical University, Daiichi Sankyo Company, LimitedInventors: Takenobu Katagiri, Kenji OSAWA, Sho TSUKAMOTO, Shinnosuke TSUJI, Yoshirou KAWAGUCHI, Kensuke NAKAMURA
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Patent number: 9951123Abstract: The purpose of the present invention is to provide a substance having superior antibacterial activity against Pseudomonas aeruginosa, and a pharmaceutical composition for treatment and/or prophylaxis of pseudomonal infections. A pharmaceutical composition is provided, containing an antibody which specifically binds to the LPS O11 antigen of Pseudomonas aeruginosa, and which has superior antibacterial activity.Type: GrantFiled: September 29, 2014Date of Patent: April 24, 2018Assignee: DAIICHI SANKYO COMPANY, LIMITEDInventors: Jun Hasegawa, Kiyoshi Sugihara
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Patent number: 9944660Abstract: The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra-abdominal infections (IAIs) or bacteremia.Type: GrantFiled: December 29, 2016Date of Patent: April 17, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Ajay Soni, Aditi Agarwal, Sangram Shesharao Deshmukh, Kedar Padmakar Purnapatre, Shinji Marumoto
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Patent number: 9938242Abstract: A method for producing a compound (3), which comprises allowing a compound (1) to react with hydrogen gas in an inert solvent, in the presence of a specific chiral ligand and a ruthenium catalyst, or in the presence of an asymmetric transition metal complex catalyst previously generated from the chiral ligand and the ruthenium catalyst.Type: GrantFiled: September 17, 2015Date of Patent: April 10, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Ueda, Kazutoshi Ukai
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Publication number: 20180094073Abstract: 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: ApplicationFiled: November 22, 2017Publication date: April 5, 2018Applicants: DAIICHI SANKYO COMPANY, LIMITED, SAPPORO MEDICAL UNIVERSITYInventors: Toshinori AGATSUMA, Shu TAKAHASHI, Jun HASEGAWA, Daisuke OKAJIMA, Hirofumi HAMADA, Miki YAMAGUCHI
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Patent number: 9931401Abstract: The present invention provides a combination of an antibody binding to a fibroblast growth factor receptor, and another agent.Type: GrantFiled: October 7, 2014Date of Patent: April 3, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Atsushi Urano, Yasuki Kamai
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Patent number: 9920068Abstract: 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: GrantFiled: July 7, 2016Date of Patent: March 20, 2018Assignees: Daiichi Sankyo Company, Limited, Sanford Burnham Prebys Medical Discovery InstituteInventors: Shojiro Miyazaki, Yuko Yamamoto, Keisuke Suzuki, Masaharu Inui, Masanori Izumi, Kaori Soma, Anthony Pinkerton, Taeko Shinozaki
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Patent number: 9918975Abstract: It is desired to provide a pharmaceutical composition containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, which exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as an agent for preventing and/or treating thrombosis, wherein the pharmaceutical composition exhibits favorable dissolution properties. The present invention provides a method for producing a pharmaceutical composition containing a compound represented by formula (I), comprising the step of mixing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, or a solvate thereof, one or more excipients selected from the group consisting of a sugar alcohol and a water-swelling additive, a disintegrant, and a binder under conditions for keeping the maximum water content of the granules during granulation at 10% or less.Type: GrantFiled: September 19, 2012Date of Patent: March 20, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Makoto Kamada, Gaku Sekiguchi, Motonori Kidokoro
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Patent number: 9918938Abstract: An object of the present invention is to provide a method for producing selectively a powder particle consisting of the ?-form crystal of D-mannitol, using the spray-drying method. It is a method for selective production of powder particles consisting of the ?-form crystal of D-mannitol, wherein a D-mannitol solution containing a water-soluble polymer is spray-dried.Type: GrantFiled: September 29, 2014Date of Patent: March 20, 2018Assignee: Daiichi Sankyo Company, LimitedInventors: Atsutoshi Ito, Shuichi Yada, Mitsuhide Tanimoto, Michiko Kumon
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Patent number: 9920071Abstract: An object of the present invention is to provide a novel method for producing a compound, a salt thereof, or a hydrate of the compound or the salt, which is an FXa inhibitor. The object can be attained by a production method in which a production method via a compound represented by formula (1-1), etc., from a compound represented by the following formula (1-x), etc., is used for a method for producing a compound represented by the following formula (X), etc. [wherein X represents a halogen atom or the like, and R1 represents an optionally substituted phenyl group].Type: GrantFiled: February 13, 2015Date of Patent: March 20, 2018Assignee: Daiichi Sankyo Company, LimitedInventor: Tsuyoshi Ueda
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Publication number: 20180072732Abstract: The present invention relates to a pyrazole derivative of formula (I), a pharmaceutically acceptable salt thereof, a prodrug thereof, a hydrate thereof, stereoisomer thereof or a deuterium form thereof, wherein, n, Y, Ra, R1, R2, R3, R4, R5 and R6 are as defined hereinafter in the specification, a pharmaceutical composition comprising a compound of formula (I) as an active ingredient, methods of production, and methods of use thereof. Particularly, the present invention provides a compound of formula (I) as inhibitors of phosphatidylinositol-3-kinase (PI3K), which can be used for treating or preventing inflammatory, autoimmune, orphan and hyperproliferative disease and disorder.Type: ApplicationFiled: March 29, 2016Publication date: March 15, 2018Applicant: Daiichi Sankyo Company, LimitedInventors: Kirandeep Kaur Samby, Yogesh Baban Surase, Sagar Ramdas Amale, Suresh Kumar Gorla, Priyanka Patel, Ashwani Kumar Verma
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Publication number: 20180073084Abstract: It is intended to develop a therapeutic strategy for specifically targeting cancer cells having the functional suppression of PSS2. The present inventors have found that PSS1 and PSS2 are in a synthetic lethal relationship, and treatment inhibiting PSS1 serves as a promising approach for the treatment of cancer having the functional suppression of PSS2. It has also been revealed that this therapeutic strategy permits efficient treatment based on companion diagnostics because a PSS1 inhibitor can be administered to a subject selected by using the functional suppression of PSS2 as an index.Type: ApplicationFiled: March 15, 2016Publication date: March 15, 2018Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Yohei YOSHIHAMA, Tatsuya INOUE
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Publication number: 20180071403Abstract: 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.Type: ApplicationFiled: November 22, 2017Publication date: March 15, 2018Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Hiroyuki NAITO, Takashi NAKADA, Masao YOSHIDA, Shinji ASHIDA, Takeshi MASUDA, Hideki MIYAZAKI, Yuji KASUYA, Yuki ABE, Yusuke OGITANI