Patents Assigned to Taiho Pharmaceutical Co., LTD
  • Patent number: 10993913
    Abstract: An object of the present invention is to provide an oxaliplatin-encapsulating liposome aqueous dispersion that has excellent long-term storage stability. The present invention provides an aqueous dispersion of liposomes encapsulating oxaliplatin, the oxaliplatin-encapsulating liposome aqueous dispersion containing 2-morpholinoethanesulfonic acid in an external aqueous phase.
    Type: Grant
    Filed: July 3, 2019
    Date of Patent: May 4, 2021
    Assignees: Taiho Pharmaceutical Co., Ltd, University of Tokushima
    Inventors: Yusuke Doi, Tatsuhiro Ishida
  • Patent number: 10981920
    Abstract: The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.
    Type: Grant
    Filed: April 22, 2020
    Date of Patent: April 20, 2021
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita
  • Publication number: 20210107908
    Abstract: The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: March 1, 2019
    Publication date: April 15, 2021
    Applicants: OTSUKA PHARMACEUTICAL CO., LTD., TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Christopher Norbert JOHNSON, Ildiko Maria BUCK, Gianni CHESSARI, James Edward Harvey DAY, Hideto FUJIWARA, Christopher Charles Frederick HAMLETT, Steven Douglas HISCOCK, Rhian Sara HOLVEY, Steven HOWARD, John Walter LIEBESCHUETZ, Nicholas John PALMER, Jeffrey David ST DENIS, David Geoffrey TWIGG, Andrew James WOODHEAD
  • Publication number: 20210101859
    Abstract: This invention relates to a method for producing a high-purity cyclohexenone long-chain alcohol represented by formula I, and produces the compound of formula I by a metal-mediated Barbier reaction. The method of the present invention has advantages in its short scheme, high yield, and high-purity product, and is suitable for industrial scale up.
    Type: Application
    Filed: January 22, 2017
    Publication date: April 8, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Jian ZHANG, Dehui JIANG, Xiaojun SHEN
  • Patent number: 10960004
    Abstract: A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing ?,?,?-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 50 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: March 30, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Kenichiro Yoshida
  • Patent number: 10947233
    Abstract: Provided are crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide which are stable and show excellent oral absorbability. The crystals are Form II crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2?±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.
    Type: Grant
    Filed: November 29, 2019
    Date of Patent: March 16, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Takao Uno
  • Publication number: 20210030755
    Abstract: The object of the present invention is to improve the dissolution and the absorption of (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl-1-pyrrolidinyl)-2-propen-1-one effective as an antitumor agent from a pharmaceutical formulation comprising the same. Provided is a pharmaceutical composition comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl-1H-pyrazolo[3,4-d]pyrimidin-1-yl-1-pyrrolidinyl)-2-propen-1-one in combination with sodium alkyl sulfate having an alkyl group containing 10 to 18 carbon atoms, in particular, with sodium lauryl sulfate.
    Type: Application
    Filed: March 18, 2019
    Publication date: February 4, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kenji KUSUMOTO, Sadahiro MIYAMURA
  • Publication number: 20210030738
    Abstract: The present invention is intended to provide a novel antitumor agent that shows marked antitumor effects with reduced side effects. The present invention relates to an antitumor agent characterized by coadministration of an acyl thiourea compound represented by general formula (I) or a salt thereof, and an immune checkpoint molecule regulator.
    Type: Application
    Filed: September 6, 2018
    Publication date: February 4, 2021
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventor: Tomonori HARUMA
  • Publication number: 20210024530
    Abstract: Provided are a novel pyrimidine compound that inhibits HER2 activity and exhibits brain penetration properties, or a salt thereof, and a pharmaceutical composition comprising the same. A compound represented by the following formula (I), or a salt thereof: wherein R1 represents a C1-C4 alkyl group optionally having a C1-C4 alkoxy group as a substituent, or a C3-C4 cycloalkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-C6 alkyl group optionally having 1 to 5 C1-C4 alkoxy groups or fluorine atoms each as a substituent(s), or a C1-C6 alkoxy group; R3 represents a hydrogen atom, or a C1-C4 alkyl group optionally having 1 to 5 fluorine atoms as a substituent(s); R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 represents a phenyl group optionally having 1 to 3 substituents selected from fluorine atoms and chlorine atoms.
    Type: Application
    Filed: October 8, 2020
    Publication date: January 28, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki NAKAMURA, Takahiro ASAI, Satoru IGUCHI, Kei OGUCHI
  • Patent number: 10894048
    Abstract: The problems to be solved by the present invention are to provide a novel FGFR inhibitor that is potent and highly selective, and to provide an antitumor agent with which side effects such as an elevated blood phosphorus concentration are alleviated while maintaining the antitumor effect of the FGFR inhibitor. The present invention provides an antitumor agent comprising a 3,5-di-substituted benzene alkynyl compound represented by general formula (I) or salt thereof, which is used by administering the 3,5-di-substituted benzene alkynyl compound or salt thereof according to an administration schedule of two or more times/week at an administration interval of at least one day between doses.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: January 19, 2021
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Hiroaki Ochiiwa, Hiroshi Hirai
  • Patent number: 10889555
    Abstract: The present invention provides a novel sulfonamide compound having a ribonucleotide reductase inhibitory activity or a salt thereof, and a pharmaceutical composition containing the same as an active ingredient. A compound represented by Formula (I) [wherein, X1 represents an oxygen atom or the like; X2 represents an oxygen atom; X3 represents —NH—; X4 represents a hydrogen atom or the like; R1 represents —C(R11)(R12)— or the like; R11 and R12 are the same or different and each represents a hydrogen atom or the like; R2 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R3 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R4 represents a hydrogen atom or the like] or a salt thereof.
    Type: Grant
    Filed: January 24, 2020
    Date of Patent: January 12, 2021
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Seiji Miyahara, Hiroyuki Ueno, Shoki Hara, Yoshio Ogino
  • Publication number: 20200405697
    Abstract: The present invention provides a method of enhancing an antitumor effect by a compound strongly inhibiting ribonucleotide reductase (RNR) or a salt thereof. A combination formulation involving combined administration of a sulfonamide compound represented by Formula (I) [In the formula, X1 represents an oxygen atom or the like; X2 represents an oxygen atom; X3 represents —NH—; X4 represents a hydrogen atom or the like; R1 represents —C(R11) (R12)— or the like; R11 and R12 are the same or different and each represents a hydrogen atom or the like; R2 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R3 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R4 represents a hydrogen atom or the like] or a salt thereof, having RNR inhibitory activity, and other antitumor agent(s).
    Type: Application
    Filed: November 28, 2018
    Publication date: December 31, 2020
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Ueno, Takuya Hoshino
  • Publication number: 20200399235
    Abstract: The present invention provides a novel sulfonamide compound having a ribonucleotide reductase inhibitory activity or a salt thereof, and a pharmaceutical composition containing the same as an active ingredient. A compound represented by Formula (I) [wherein, X1 represents an oxygen atom or the like; X2 represents an oxygen atom; X3 represents —NH—; X4 represents a hydrogen atom or the like; R1 represents —C(R11)(R12)— or the like; R11 and R12 are the same or different and each represents a hydrogen atom or the like; R2 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R3 represents an optionally substituted C6-C14 aromatic hydrocarbon group or the like; R4 represents a hydrogen atom or the like] or a salt thereof.
    Type: Application
    Filed: August 24, 2020
    Publication date: December 24, 2020
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Seiji Miyahara, Hiroyuki Ueno, Shoki Hara, Yoshio Ogino
  • Patent number: 10866219
    Abstract: This invention provides a method that is capable of detecting a trifluridine-related substance and a tipiracil-related substance contained in a sample containing trifluridine or a salt thereof and tipiracil or a salt thereof using the same procedure. The method is for detecting a trifluridine-related substance or a tipiracil-related substance or both, the method comprising the step of subjecting a sample containing trifluridine or a salt thereof and tipiracil or a salt thereof to high-performance liquid chromatography using a mobile phase composed of an organic phase and an aqueous phase.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: December 15, 2020
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Yoshinori Tokimitsu
  • Patent number: 10849886
    Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: December 1, 2020
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromi Muraoka, Akira Kanoh
  • Publication number: 20200361883
    Abstract: The present disclosure relates to novel crystalline forms of sulfonamide compounds, pharmaceutical compositions containing the crystalline form compounds and methods of preparing and using the same.
    Type: Application
    Filed: November 28, 2018
    Publication date: November 19, 2020
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Nakamura, Jing Teng, Nathan Gignac
  • Patent number: 10835536
    Abstract: The problem to be solved by the present invention is to provide an anticancer agent for treating tumors resistant to other antitumor agents that inhibit FGFR, and a method for treating such tumors. The present invention provides an antitumor agent for administration to a tumor patient resistant to an FGFR inhibitor, the antitumor agent comprising a 3,5-disubstituted benzene alkynyl compound represented by Formula (I) below or a salt thereof. The present invention also provides a therapeutic method using the anticancer agent.
    Type: Grant
    Filed: October 2, 2018
    Date of Patent: November 17, 2020
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Hiroshi Sootome
  • Patent number: 10816517
    Abstract: The present invention provides a novel method that is capable of detecting a trifluridine-related substance from a sample containing trifluridine or a salt thereof by high-performance liquid chromatography comprising two steps that are performed under gradient conditions. More specifically, the method is for detecting a trifluridine-related substance, the method comprising the step of subjecting a sample containing trifluridine or a salt thereof to high-performance liquid chromatography using a mobile phase composed of an organic phase and an aqueous phase, wherein the step of high-performance liquid chromatography comprises steps 1 and 2 that satisfy the following requirements: Step 1: the percentage of the organic phase in the entire mobile phase is 1 to 14% by volume; and Step 2: after step 1, elution is performed by applying a gradient of increasing the percentage of the organic phase in the entire mobile phase.
    Type: Grant
    Filed: July 20, 2018
    Date of Patent: October 27, 2020
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Daisuke Takeda, Akiyo Kojima
  • Patent number: 10809237
    Abstract: The present invention provides a novel method that is capable of detecting a trifluridine-related substance from a sample containing trifluridine or a salt thereof by high-performance liquid chromatography comprising two steps that are performed under gradient conditions. More specifically, the method is for detecting a trifluridine-related substance, the method comprising the step of subjecting a sample containing trifluridine or a salt thereof to high-performance liquid chromatography using a mobile phase composed of an organic phase and an aqueous phase, wherein the step of high-performance liquid chromatography comprises steps 1 and 2 that satisfy the following requirements: Step 1: the percentage of the organic phase in the entire mobile phase is 1 to 14% by volume; and Step 2: after step 1, elution is performed by applying a gradient of increasing the percentage of the organic phase in the entire mobile phase.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: October 20, 2020
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Daisuke Takeda, Akiyo Kojima
  • Patent number: 10807986
    Abstract: The problem to be solved by the present invention is to provide a novel compound having RET inhibitory activity. The present invention also provides a pharmaceutical preparation that is useful for the prevention and/or treatment of RET-related diseases, particularly cancer, based on RET inhibitory activity. The present invention provides a compound represented by Formula (I): wherein A, R2, and X are as defined in the specification; or a salt thereof.
    Type: Grant
    Filed: November 1, 2018
    Date of Patent: October 20, 2020
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita, Satoru Iguchi