Patents Assigned to Taiho Pharmaceutical Co., LTD
  • Publication number: 20220184082
    Abstract: The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with pembrolizumab to a cancer patient with resistance to immune checkpoint inhibitors.
    Type: Application
    Filed: February 28, 2020
    Publication date: June 16, 2022
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhiko YONEKURA, Hiroshi HIRAI, Kazuaki MATSUOKA
  • Publication number: 20220160719
    Abstract: The present invention provides a novel compound inhibiting EGFR or a salt of the compound. According to one embodiment of the present invention, provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: February 14, 2020
    Publication date: May 26, 2022
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Fuyuki YAMAMOTO, Takashi MIZUTANI, Hidefumi KASUGA, Hirokazu FUCHIDA, Shoki HARA, Yu KOBAYAKAWA, Yoshio OGINO
  • Publication number: 20220125793
    Abstract: The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with an immune checkpoint inhibitor, except for pembrolizumab, to a cancer patient with resistance to immune checkpoint inhibitors.
    Type: Application
    Filed: February 28, 2020
    Publication date: April 28, 2022
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhiko YONEKURA, Hiroshi HIRAI, Kazuaki MATSUOKA
  • Patent number: 11292800
    Abstract: The present invention provides a compound represented by Formula (I) or a salt thereof; an LSD1 inhibitor that contains the compound or a salt thereof as an active ingredient; a pharmaceutical composition that contains the compound or a salt thereof; and an antitumor agent that contains the compound or a salt thereof as an active ingredient.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: April 5, 2022
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Satoshi Yamashita, Takahiro Ogawa
  • Publication number: 20220047572
    Abstract: Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.
    Type: Application
    Filed: October 29, 2021
    Publication date: February 17, 2022
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Akio FUJIOKA
  • Patent number: 11236096
    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: February 1, 2022
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita
  • Publication number: 20220023300
    Abstract: Provided is a novel treatment method for cancer tumors to which endocrine therapy is to be applied, using an FGFR inhibitor (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a pharmaceutically acceptable salt thereof. Further provided are a pharmaceutical composition comprising the above compound or a pharmaceutically acceptable salt thereof for use in treatment and/or prevention of tumors to which endocrine therapy is to be applied, the pharmaceutical composition being used in combination with endocrine therapy, as well as its related compound, use, method, and combination.
    Type: Application
    Filed: November 25, 2019
    Publication date: January 27, 2022
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi HIRAI, Akihiro MIURA, Hiroshi SOOTOME
  • Publication number: 20220016090
    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: Application
    Filed: September 30, 2021
    Publication date: January 20, 2022
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromi MURAOKA, Akira KANOH
  • Publication number: 20210401745
    Abstract: This invention provides a water-in-oil (w/o) emulsion formulation that stably contains 3 types of peptides having 4 linked CTL epitopes. This invention also provides a method for efficiently preparing the w/o emulsion formulation containing 3 types of peptides having 4 linked CTL epitopes. This invention provides a w/o emulsion formulation that stably contains 3 types of peptides having 4 linked CTL epitopes and a method for efficiently preparing such w/o emulsion formulation. In addition, this invention provides an improved method and an apparatus to prepare such emulsion formulation.
    Type: Application
    Filed: November 1, 2019
    Publication date: December 30, 2021
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventor: Yusuke DOI
  • Publication number: 20210387990
    Abstract: A method for producing a compound represented by formula (A-1) or a salt thereof, the method comprising reacting (S)-3-((3,5-dimethoxyphenyl)ethynyl)-1-(pyrrolidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine or a salt thereof with a compound represented by formula (I-1-A). Formula (I-1-A) and formula (A-1) are as described in the specification.
    Type: Application
    Filed: November 8, 2019
    Publication date: December 16, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Masashi KONDO
  • Publication number: 20210388002
    Abstract: A compounds represented by any one of the following formulas (1) to (5) or a salt thereof, or a combination thereof: (1) 1,3-bis((S)-3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)propan-1-one; (2) 1-((S)-3-(4-((3-((S)-3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-3-oxopropyl)amino)-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one; (3) (S)-3-((1-(1-acryloylpyrrolidin-3-yl)-6-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)propanoic acid; (4) (S)-3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidine-1-carbaldehyde; (5) (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-3-hydroxypropan-1-one.
    Type: Application
    Filed: November 8, 2019
    Publication date: December 16, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yuji KANAMOTO, Reina OTA, Masaya HASHIMOTO, Kohei KANDA
  • Patent number: 11191759
    Abstract: Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.
    Type: Grant
    Filed: June 2, 2020
    Date of Patent: December 7, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Akio Fujioka
  • Publication number: 20210369739
    Abstract: Combination therapy of cancer using a c-Met selective inhibitor, an acylthiourea compound or a pharmaceutically acceptable salt thereof, and showing an excellent antitumor effect with less side effects is provided. An antitumor agent contains a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: characterized by being used in combination with abiraterone or a derivative thereof.
    Type: Application
    Filed: September 18, 2019
    Publication date: December 2, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Yuko ISHIBASHI
  • Patent number: 11166943
    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: May 19, 2020
    Date of Patent: November 9, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromi Muraoka, Akira Kanoh
  • Publication number: 20210332056
    Abstract: An object of the invention is to provide a crystal of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide which is excellent in stability and preferable from the viewpoint of manufacturing and formulation. The present invention provides a crystal having an X-ray powder diffraction spectrum having characteristic peaks at diffraction angles (2?±0.2°) of 6.0°, 7.7°, 8.9°, 10.6°, 12.1°, 13.1°, 14.0°, 14.7°, 15.5°, 15.8°, 16.8°, 17.7°, 18.1°, 18.4°, 19.4°, 23.4°, 24.1°, 24.7°, 25.1° and 25.7°.
    Type: Application
    Filed: August 28, 2019
    Publication date: October 28, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Tadashi SHIMAMURA, Hiromi OSHIUMI
  • Publication number: 20210308056
    Abstract: An object of the present invention is to provide a pharmaceutical composition which has excellent stability, disintegratability, and absorbability, is easily prepared, and contains 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof and a cyclodextrin derivative. The present invention relates to a pharmaceutical composition containing 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof and hydroxypropyl-Bi-cyclodextrin.
    Type: Application
    Filed: June 15, 2021
    Publication date: October 7, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Shinji OKADA
  • Patent number: 11110062
    Abstract: An object of the present invention is to provide a pharmaceutical composition which has excellent stability, disintegratability, and absorbability, is easily prepared, and contains 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof and a cyclodextrin derivative. The present invention relates to a pharmaceutical composition containing 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide or a pharmaceutically acceptable salt thereof and hydroxypropyl-?-cyclodextrin.
    Type: Grant
    Filed: February 14, 2018
    Date of Patent: September 7, 2021
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Shinji Okada
  • Publication number: 20210252000
    Abstract: Provided is an anti-tumor agent for the treatment of a HER2-positive tumor that is tolerant to other anti-tumor agents or an intractable HER2-positive tumor. More specifically provided is a therapeutic agent for a HER2-positive tumor that is tolerant to other anti-tumor agents or an intractable HER2-positive tumor, which contains a pyrazolo[3,4-d]pyrimidine compound or a salt thereof as an active ingredient.
    Type: Application
    Filed: August 28, 2019
    Publication date: August 19, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiroki IRIE, Yayoi FUJIOKA
  • Publication number: 20210236613
    Abstract: Provided is a novel cancer treatment method that exhibits a significantly excellent antitumor effect and causes less adverse reactions. The present invention provides an antitumor agent wherein a peptide having 4 linked epitopes and an immune checkpoint modulator are administered in combination. An antitumor effect in humans can be evaluated by providing a cell coexpressing an epitope peptide of a human tumor antigen derived from SART2 and human HLA-A24.
    Type: Application
    Filed: June 28, 2019
    Publication date: August 5, 2021
    Applicant: Taiho Pharmaceutical Co., Ltd.
    Inventor: Yuki TANAKA
  • Publication number: 20210236475
    Abstract: Provided is an effective method for using an orally administrable compound having an excellent Aurora A selective inhibitory effect, and a microtubule-targeting drug in combination. The present invention provides a method for treatment of malignant tumor by a combination of 1-(2,3-dichlorobenzoyl)-4-[5-fluoro-6-(5-methyl-1H-pyrazol-3-ylamino)pyridin-2-yl]methyl-4-piperidinecarboxylic acid (compound I) or a salt thereof and a microtubule-targeting drug, wherein the following administration schedule thereof is performed: one cycle involves 7 days; the microtubule-targeting drug is administered once; and the compound I or the salt thereof is administered for 3 consecutive days with cessation of the drug for remaining 4 days.
    Type: Application
    Filed: May 28, 2019
    Publication date: August 5, 2021
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Hiroshi HIRAI