Patents Assigned to Taiho Pharmaceutical Co., LTD
  • Patent number: 10434103
    Abstract: An object of the present invention is to provide a crystal 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, which is useful as an antitumor agent, the crystal being stable, excellent in oral absorbability, highly chemically pure, and suitable for mass production. The present invention provides a crystal 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 that exhibits an X-ray powder diffraction spectrum containing at least three characteristic peaks at diffraction angles (2?±0.2°) selected from 9.5°, 14.3°, 16.7°, 19.1°, 20.8°, 21.9°, and 25.2°. The present invention also provides a crystal 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 that exhibits an X-ray powder diffraction spectrum containing at least seven characteristic peaks at diffraction angles (2?±0.2°) selected from 13.5°, 17.9°, 19.5°, 20.
    Type: Grant
    Filed: March 31, 2016
    Date of Patent: October 8, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Kosuke Egami
  • Publication number: 20190292190
    Abstract: The invention of the present application provides a compound represented by Formula (I) or a salt thereof, which exhibits an inhibitory activity against at least one kinase selected from the group consisting of Akt kinase, Rsk kinase, and S6K kinase and/or a cell proliferation inhibiting effect and is useful as a prophylactic and/or therapeutic agent for diseases associated with the above-mentioned kinases, particularly cancer.
    Type: Application
    Filed: May 19, 2017
    Publication date: September 26, 2019
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventors: Tetsuya SUGIMOTO, Toshihiro SAKAMOTO, Fuyuki YAMAMOTO, Yu KOBAYAKAWA, Naoki EGASHIRA, Koji ICHIKAWA, Takumitsu MACHIDA
  • Patent number: 10421760
    Abstract: Provided are a novel compound or a salt thereof, and a pharmaceutical composition comprising the same, which selectively and strongly inhibit JAK3, exhibit an excellent activity for suppressing the growth of human peripheral blood monocytes and an excellent oral absorbability, and exhibits an activity of inhibiting IL-2-induced IFN-? production in vivo. A compound represented by formula (I) [wherein X represents —CH?CH—, —NH—, a sulfur atom or an oxygen atom; and n represents an integer of 0 to 2], or a salt thereof.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: September 24, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masayuki Nakamura, Hiroyoshi Yamanaka, Morihiro Mitsuya, Takafumi Harada
  • Patent number: 10383822
    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: August 9, 2013
    Date of Patent: August 20, 2019
    Assignees: TAIHO PHARMACEUTICAL CO., LTD., TOKUSHIMA UNIVERSITY
    Inventors: Yusuke Doi, Tatsuhiro Ishida
  • Patent number: 10370372
    Abstract: To provide a compound having an inhibitory activity for an androgen receptor. A fused pyrimidine compound represented by the following formula (I) or a pharmaceutically acceptable thereof (in the formula, X, Y, Z, R1, and R2 are as defined in the specification).
    Type: Grant
    Filed: November 25, 2016
    Date of Patent: August 6, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Takahiro Asai, Masanori Asai, Yoshio Ogino
  • Publication number: 20190212309
    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: Application
    Filed: July 20, 2018
    Publication date: July 11, 2019
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Daisuke TAKEDA, Akiyo KOJIMA
  • Publication number: 20190195840
    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: Application
    Filed: April 13, 2018
    Publication date: June 27, 2019
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Yoshinori TOKIMITSU
  • Patent number: 10329300
    Abstract: To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 inhibitory effect. The present invention provides a compound of formula (I) wherein X, Y, Z1, Z2, Z3, Z4, W, n, R1, R2, and R3 have meanings as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: March 16, 2018
    Date of Patent: June 25, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yuichi Kawai, Hiroki Irie, Takeshi Sagara, Kazutaka Miyadera
  • Publication number: 20190183897
    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: Application
    Filed: February 13, 2019
    Publication date: June 20, 2019
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiroaki OCHIIWA, Hiroshi HIRAI
  • Patent number: 10323044
    Abstract: An object of the present invention is to provide a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having excellent stability and favorable characteristics in terms of its production and formulation into drugs. The present invention provides a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having characteristic peaks of diffraction angle (2?±0.1°) at 7.7°, 9.5°, 10.3°, 12.3°, 14.5°, 15.6°, 16.3°, 17.8°, 18.3°, 19.3°, 20.9°, 22.8°, 24.2°, 25.7°, 26.8°, 27.7°, 29.0° and 30.1° in a powder X-ray diffraction spectrum.
    Type: Grant
    Filed: February 26, 2016
    Date of Patent: June 18, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Masaya Hashimoto
  • Patent number: 10300067
    Abstract: A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof
    Type: Grant
    Filed: February 12, 2018
    Date of Patent: May 28, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Shinichi Aoki, Masanori Asai, Takahiro Asai, Hiroyoshi Yamanaka, Suguru Dohi
  • Patent number: 10280174
    Abstract: Provided is a salt having a high selectivity to BTK and is useful as a drug ingredient for a pharmaceutical product. It has been found that fumarate of Compound A is free of a characteristic of channel hydrate and is stable and excellent in absorptive property, compared to Compound A or other salts thereof.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: May 7, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Hiromi Oshiumi
  • Patent number: 10278373
    Abstract: This invention provides an HLA class I-expressing non-human animal that can be prepared efficiently in a simple manner within a short period of time, in which the transgene copy number to be introduced thereinto and the integration site of transgene are regulated, and in which the expression level of the transgene and the site of expression thereof are regulated. The invention also provides a method for preparing such non-human animal. In such HLA class I gene knock-in non-human animal, an artificial chimeric gene encoding an artificial chimeric protein comprising a protein composed of ?2 microglobulin, HLA class I ?1 and ?2 regions, and an MHC class I ?3 region of a non-human animal ligated in such order from the N terminus is expressed under the control of a transcription regulatory region of ?2 microglobulin gene of the non-human animal.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: May 7, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Naomoto Harada, Satoshi Fukaya
  • Patent number: 10259792
    Abstract: The present invention provides a crystal that has preferable oral absorption and can be obtained with particularly preferable reproducibility. Provided is a crystal of (R)—N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: April 16, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Masayoshi Fukuoka
  • Publication number: 20190092776
    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: Application
    Filed: November 29, 2018
    Publication date: March 28, 2019
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Isao MIYAZAKI, Tadashi SHIMAMURA, Masanori KATO, Hidenori FUJITA
  • Patent number: 10233189
    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: September 11, 2017
    Date of Patent: March 19, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita
  • Publication number: 20190046639
    Abstract: Provided is a novel cancer treatment method with less side effects, showing remarkably excellent antitumor effect. An antitumor agent is used for administering a DNA function inhibitor and an immunomodulator in combination.
    Type: Application
    Filed: January 6, 2017
    Publication date: February 14, 2019
    Applicant: TAIHO PHARMACEUTICAL CO., LTD
    Inventor: Norihiko SUZUKI
  • Publication number: 20190015417
    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: Application
    Filed: October 2, 2018
    Publication date: January 17, 2019
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Hiroshi SOOTOME
  • Patent number: 10179788
    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: September 11, 2017
    Date of Patent: January 15, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita
  • Patent number: RE47388
    Abstract: The present invention provides an agent for alleviating side effects caused by use of an anti-tumor agent, which contains 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H-pyrimidi nedione (1) represented by formula (1): or a pharmaceutically acceptable salt thereof. The 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof exhibit an inflammatory-suppressing action in the digestive tract and advantageously alleviate diarrhea and loss of body weight concomitant with administration of a chemical for treating cancer without suppressing the anti-tumor effect. Thus, the compounds of the present invention are of great value as agents for alleviating side effects caused by use of an anti-tumor agent, which enable not only the chemotherapy to be continuedly carried out, but also the body exhaustion to be effectively prevented.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: May 14, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masakazu Fukushima, Noriyuki Yamamoto, Norihiko Suzuki