Patents Assigned to Otsuka Pharmaceutical Co., Ltd.
  • Publication number: 20210113582
    Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.
    Type: Application
    Filed: December 23, 2020
    Publication date: April 22, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Shinsuke Nakagawa, Kai Suzuki, Tadashi Mukai
  • Publication number: 20210113556
    Abstract: The present invention provides a heterocyclic compound represented by the general formula (1): The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Application
    Filed: December 22, 2020
    Publication date: April 22, 2021
    Applicant: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi YAMASHITA, Nobuaki ITO, Shin MIYAMURA, Kunio OSHIMA, Jun MATSUBARA, Hideaki KURODA, Haruka TAKAHASHI, Satoshi SHIMIZU, Tatsuyoshi TANAKA
  • Publication number: 20210115030
    Abstract: An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases.
    Type: Application
    Filed: August 4, 2020
    Publication date: April 22, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Tetsuya SATO, Takuya MINOWA, Yusuke HOSHIKA, Hidekazu TOYOFUKU, Tatsuya YAMAGUCHI, Masahiro SOTA, Shuuji KAWANO, Takayuki NAKAMURA, Ryohei ETO, Takuma IKEBUCHI, Kei MORIYAMA, Nobuaki ITO
  • Patent number: 10980803
    Abstract: The disclosed embodiments relate to methods of initiating aripiprazole treatment in a patient who is a CYP2D6 poor metabolizer or a CYP3A4 poor metabolizer, or both.
    Type: Grant
    Filed: December 11, 2019
    Date of Patent: April 20, 2021
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventor: Arash Raoufinia
  • 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: 20210101889
    Abstract: This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.
    Type: Application
    Filed: April 20, 2018
    Publication date: April 8, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Michael READER, Nicola Elizabeth WILSHER, Mark Henry SAUNDERS, Paul Anthony BAGULEY, Colin Thomas LINDLEY, Robert Craig MELLING, Bozena Ewa ADAMCZYK, Mirka SCARATI
  • Patent number: 10966983
    Abstract: The present invention provides an externally applied composition capable of enhancing a stimulatory effect of an essential oil on IGF-1 secretion, the composition including (A) essential oil; and (B) at least one member selected from the group consisting of purine substances and salts thereof. Further, the present invention provides an externally applied composition capable of increasing the stratum corneum water content of the skin and maintaining transepidermal water loss at an appropriate level.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: April 6, 2021
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Akihiro Aoki, Kosaburo Wakamatsu, Shigeo Shinohara, Osamu Takasu
  • Patent number: 10969390
    Abstract: A method for evaluating an efficacy of a chemoradiotherapy against squamous cell carcinoma comprises the following steps (a) to (c): (a) detecting an expression level of at least one gene selected from a SIM2 gene and genes co-expressed with the SIM2 gene in a squamous cell carcinoma specimen isolated from a subject; (b) comparing the expression level detected in the step (a) with a reference expression level of the corresponding gene; and (c) determining that an efficacy of a chemoradiotherapy against squamous cell carcinoma in the subject is high if the expression level in the subject is higher than the reference expression level as a result of the comparison in the step (b).
    Type: Grant
    Filed: September 24, 2015
    Date of Patent: April 6, 2021
    Assignees: NATIONAL CANCER CENTER, KYOTO UNIVERSITY, OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroki Sasaki, Kazuhiko Aoyagi, Manabu Muto, Hiroo Takahashi
  • Publication number: 20210085794
    Abstract: An object of the present invention is to provide a storage-stable injectable preparation comprising a composition comprising a poorly soluble drug as an active ingredient and a dispersion medium. Another object of the present invention is to provide a compact, lightweight prefilled syringe by filling a syringe with the injectable preparation. The present invention provides an injectable preparation comprising a composition comprising a poorly soluble drug, a dispersion medium, and a specific suspending agent, the composition having a viscosity of 40 pascal-seconds or more in at least one point in the shear rate range of 0.01 to 0.02 s?1 and having a viscosity of 0.2 pascal-seconds or less in at least one point in the shear rate range of 900 to 1,000 s?1, as measured.
    Type: Application
    Filed: December 1, 2020
    Publication date: March 25, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Daiki KANEKO, Takakuni MATSUDA, Yusuke HOSHIKA
  • Publication number: 20210078976
    Abstract: The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin V1a and V2 antagonisms, and medical uses thereof. In the formula, R1 is optionally substituted C1-6 alkyl, etc.; L is —C(?O)—NH—, etc.; Ring A1 is a hydrocarbon ring, etc.; Ring A2 is a hydrocarbon ring, etc.; and each of Rings A1 and A2 may have at least one substituent.
    Type: Application
    Filed: November 24, 2020
    Publication date: March 18, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Keizo KAN, Masatoshi TAKUWA, Hirotaka TANAKA, Hideto FUJIWARA, Hokuto YAMABE, Satoshi MATSUDA, Kazuhiro OHDACHI, Taiki HANARI, Yasuhiro MENJO, Tatsuya URUSHIMA, Shigekazu FUJITA
  • Publication number: 20210069207
    Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.
    Type: Application
    Filed: November 16, 2020
    Publication date: March 11, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Shinsuke Nakagawa, Kai Suzuki, Tadashi Mukai
  • Publication number: 20210053925
    Abstract: An improved process for preparing 2-chloro-4-nitroimidazole derivatives which are useful intermediates in the preparation of an anti-tuberculosis drug is provided. The process may comprise the step of chlorinating nitroimidazoles with a chlorinating agent and an activating agent to give 2-chloro-4-nitroimidazole derivatives.
    Type: Application
    Filed: January 29, 2018
    Publication date: February 25, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Petr NOVAK, Petr ZAHRADNIK, Jiri TAUCHMAN, Jan KOCI, Antonin STURC
  • Publication number: 20210052575
    Abstract: Provided is a superior, novel hetrocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: June 9, 2020
    Publication date: February 25, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi YAMASHITA, Yohji SAKURAI, Motoyuki MIYAMOTO, Yuichi NAKAMURA, Hideaki KURODA, Takuya MINOWA
  • Patent number: 10925813
    Abstract: The present invention provides a sunscreen composition comprising two or more oil-soluble ultraviolet absorbers and composite silicone particles having an average particle diameter of 10 ?m or less.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: February 23, 2021
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Masahiko Tanaka, Miyoko Ogihara, Junko Kako
  • Publication number: 20210032207
    Abstract: The present invention provides a compound represented by the formula (T) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: October 19, 2020
    Publication date: February 4, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Patent number: 10905694
    Abstract: The subject invention provides a novel pharmaceutical solid preparation that has superior disintegration properties and excellent solubility, leading to sufficient absorbability of active ingredients through the gastrointestinal tract. The pharmaceutical solid preparation of the present invention comprises: (a) 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H-benzoazepine and/or salt thereof; (b) hydroxypropylcellulose containing a hydroxypropoxyl group in an amount of 50% or greater; and (c) at least one member selected from the group consisting of carmellose, sodium carboxy methyl starch, crospovidone, and low substituted hydroxypropylcellulose with an average particle diameter of 30 to 70 ?m, and a 90% cumulative particle diameter of 100 to 200 ?m.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: February 2, 2021
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Shinsuke Nakagawa, Kai Suzuki, Tadashi Mukai
  • Publication number: 20210023078
    Abstract: This invention relates to a tablet containing, as an active ingredient, 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, that has excellent disintegration ability, storage stability and photostability. The tablet of the present invention comprising an uncoated tablet containing 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof as an active ingredient, excipients such as lactose, corn starch, and microcrystalline cellulose; disintegrants such as low-substituted hydroxypropylcellulose, croscarmellose sodium, and sodium carboxymethyl starch; binders such as hydroxypropylcellulose; lubricants such as stearate; and further comprising a coating layer containing hypromellose; talc; titanium oxide; colorant; and the like, the coating layer being applied to the surface of the uncoated tablet.
    Type: Application
    Filed: October 1, 2020
    Publication date: January 28, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventor: Yoshiharu INOUE
  • Publication number: 20210017134
    Abstract: The present invention provides a novel compound having an excellent antitumor effect, stability and metabolic stability. The compound of the present invention is represented by the following general formula (1) wherein R1 represents a halogen atom, an aryl group, an aryloxy group or a lower alkyl group optionally substituted with one or more halogen atoms; R2 represents a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; and; m represents an integer of 1 to 3; provided that when m represents 2 or 3, R1s are the same or different.
    Type: Application
    Filed: September 30, 2020
    Publication date: January 21, 2021
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Takashi NAKAGAWA, Makoto SAKAMOTO, Kazuya YAMAGUCHI, Yuki TERAUCHI, Masamichi SHIRAKURA, Yasuo HARADA, Yutaka KOJIMA, Takumi SUMIDA
  • Patent number: 10889570
    Abstract: The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin V1a and V2 antagonisms, and medical uses thereof. In the formula, R1 is optionally substituted C1-6 alkyl, etc.; L is —C(?O)—NH—, etc.; Ring A1 is a hydrocarbon ring, etc.; Ring A2 is a hydrocarbon ring, etc.; and each of Rings A1 and A2 may have at least one substituent.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: January 12, 2021
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Keizo Kan, Masatoshi Takuwa, Hirotaka Tanaka, Hideto Fujiwara, Hokuto Yamabe, Satoshi Matsuda, Kazuhiro Ohdachi, Taiki Hanari, Yasuhiro Menjo, Tatsuya Urushima, Shigekazu Fujita
  • Publication number: 20200407326
    Abstract: The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.
    Type: Application
    Filed: September 6, 2018
    Publication date: December 31, 2020
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Yuya NAKAI, Masashi HAYASHI, Wataru MITSUHASHI