Patents Assigned to Taiho Pharmaceutical Co., LTD
  • 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: 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: 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: 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: 10174040
    Abstract: A pyrrolopyrimidine compound or a salt thereof and compositions, NAE inhibitors and anti-tumor agents containing the pyrrolopyrimidine compound or a salt thereof.
    Type: Grant
    Filed: February 7, 2018
    Date of Patent: January 8, 2019
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Takashi Mizutani, Chihoko Yoshimura, Hitomi Kondo, Makoto Kitade, Shuichi Ohkubo
  • Publication number: 20180369224
    Abstract: A piperidine compound represented by a general formula (I) or a salt thereof: wherein, R1 represents a carboxyl group, —C(?O)NR5R6, or an oxadiazolyl group optionally having a C1-C6 alkyl group or a trifluoromethyl group as a substituent; R2 represents a halogen atom or a C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 same or different group(s) selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, and a trifluoromethyl group as a substituent; R4 represents a hydrogen atom or a C1-C6 alkyl group; and R5 and R6 are the same or different and each represent a hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, or R5 and R6 optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group together with a nitrogen atom to which R5 and R6 are bound, are provided.
    Type: Application
    Filed: August 31, 2018
    Publication date: December 27, 2018
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Tetsuya SUGIMOTO, Hidekazu TAKAHASHI, Morihiro MITSUYA, Norio MASUKO, Hiroshi SOOTOME
  • Patent number: 10155768
    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: September 19, 2017
    Date of Patent: December 18, 2018
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Isao Miyazaki, Tadashi Shimamura, Masanori Kato, Hidenori Fujita, Satoru Iguchi
  • Publication number: 20180354960
    Abstract: A compound or a salt thereof represented by Formula (I). An LSD1 inhibitor containing the compound or a salt thereof as an active ingredient. A pharmaceutical composition containing the compound or salt thereof. An antitumor agent containing the compound or a salt thereof as an active ingredient.
    Type: Application
    Filed: November 25, 2016
    Publication date: December 13, 2018
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Satoshi YAMASHITA, Takahiro OGAWA, Hideya KOMATANI
  • Patent number: 10143688
    Abstract: An object of the present invention is to provide a salt compound of 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide, which is useful as an antitumor agent, and crystal of the salt. The salt and the crystal are excellent in terms of solubility, stability, and peroral absorbability and can be mass-produced. The present invention relates to: a mesylic acid salt of 4-(2-fluoro-4-(3-(2-phenylacetyl)thioureido)phenoxy)-7-methoxy-N-methylquinoline-6-carboxamide; and the mesylic acid salt including a crystal which gives an X-ray powder diffraction spectrum having characteristic peaks at specific diffraction angles.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: December 4, 2018
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Ayako Sato
  • Publication number: 20180338976
    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: Application
    Filed: August 3, 2018
    Publication date: November 29, 2018
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Kenichiro YOSHIDA
  • Patent number: 10138223
    Abstract: An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4 (1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2?±0.1°) in powder X-ray diffraction.
    Type: Grant
    Filed: November 16, 2016
    Date of Patent: November 27, 2018
    Assignee: TAIHO PHARMACEUTICALS CO., LTD.
    Inventors: Hideki Kazuno, Tomonobu Mutsumi
  • Patent number: 10137183
    Abstract: This invention provides a cancer antigen peptide that can be administered to a wide range of cancer patients in the form of a peptide vaccine for cancer without the need for HLA typing and regardless of the HLA types of patients. Such peptide having 4 linked CTL epitopes is obtained by linking 4 CTL epitope peptides selected from among CTL epitope peptides derived from tumor antigen molecules that are reported to have the capacity for CTL induction via linkers.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: November 27, 2018
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Satoshi Fukaya, Toshihiro Osada, Hiroshi Wada
  • 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