Patents Assigned to Kyorin Pharmaceutical Co. Ltd.
  • Patent number: 9920005
    Abstract: A method for highly efficiently preparing high purity crystals of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]-ethyl]-1,3-propanediol hydrochloride. The method involves dissolving 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which its hydrochloride is highly soluble and a solvent in which its hydrochloride is less soluble, to prepare a solution of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then adding hydrochloric acid to the resulting solution with stirring, to crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]ethyl]-1,3-propanediol.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: March 20, 2018
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hidetaka Komatsu, Hiroya Satoh
  • Publication number: 20180042918
    Abstract: [Problem] The present invention pertains to a safer and more effective respiratory infection treating agent. [Solution] A respiratory infection treating agent containing, as an active ingredient, 7-[(3S,4S)-3-{(cyclopropylamino)methyl}-4-fluoropyrrolidine-1-yl]-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: March 11, 2016
    Publication date: February 15, 2018
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Kota KUME, Hisao YOSHIDA, Hirotaka ANDO, Yuta TANAKA
  • Patent number: 9863955
    Abstract: A method for screening an AMPK activator, wherein inhibition of an interaction between prohibitin and AMPK is used as an index is provided. Besides, an AMPK activator comprising, as an active ingredient, a compound inhibiting an interaction between prohibitin and AMPK, and a prohibitin-AMPK complex are also provided.
    Type: Grant
    Filed: May 16, 2013
    Date of Patent: January 9, 2018
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Tomohiro Ide, Naoki Kobayashi, Yunike Akasaka, Takashi Komine, Koji Murakami
  • Patent number: 9822069
    Abstract: Provided is a compound having a formyl peptide receptor like 1 (FPRL1) agonist effect. The present invention relates to a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof. The present invention also relates to a pharmaceutical composition containing the compound represented by the general formula (I) or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: November 27, 2014
    Date of Patent: November 21, 2017
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Hiroyasu Takahashi, Yoshifumi Saito, Kosuke Tsuda, Mitsuhito Shibasaki, Kohei Ohata
  • Publication number: 20170319571
    Abstract: [Problem] To provide a novel pharmaceutical composition which can suppress delayed, release of the compound represented in general formula (1) or a salt thereof. [Solution] This solid pharmaceutical composition contains the compound represented in general formula (1), or a salt thereof, and a salting-out agent.
    Type: Application
    Filed: October 23, 2015
    Publication date: November 9, 2017
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi UCHIDA, Masataka HANADA, Yoshikazu MIYAZAKI
  • Publication number: 20170246160
    Abstract: [Problem] Provided is a pharmaceutical composition which suppresses gelation of the 7-{(3S,4S)-3-[(cycloproropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride and which suppresses elution delay. [Solution] This solid pharmaceutical composition is obtained by using crystals (B-form crystals) of a hydrate of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride, having peaks at 9.4 and 17.7 degrees (±0.2 degrees for each angle) as 2? diffraction angles in X-ray powder diffraction using CuK? emission.
    Type: Application
    Filed: October 23, 2015
    Publication date: August 31, 2017
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi UCHIDA, Masataka HANADA
  • Patent number: 9687453
    Abstract: [Problem] To provide a novel pharmaceutical composition which contains a medically active component and which can suppress delays in the release of said component due to gelling. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1), or a salt thereof, a cellulosic excipient, and a salting-out agent.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: June 27, 2017
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Uchida, Masataka Hanada, Yoshikazu Miyazaki
  • Patent number: 9603804
    Abstract: [Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: March 28, 2017
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Uchida, Masataka Hanada
  • Publication number: 20170049718
    Abstract: A drug for treatment of patients having tinnitus associated with age-related hearing loss, comprising neramexane or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 27, 2015
    Publication date: February 23, 2017
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Katsumi DOI, Yoshifumi HIRAHARA, Shinji NAGAI, Ai USHIWATA, Ikuyo NIWAYAMA, Koichi WATANABE, Madoka TOMINAGA, Takafumi KUROSE, Shinichi YAMADA, Takehiro SHINOZAKI, Janos CSIKOS, Roman GORTELMEYER
  • Publication number: 20170049717
    Abstract: A drug for treatment of patients having tinnitus associated with sudden hearing loss, comprising neramexane or a pharmaceutically acceptable salt thereof, wherein the morbidity period of the patient having tinnitus associated with sudden hearing loss is 48 months or longer.
    Type: Application
    Filed: April 27, 2015
    Publication date: February 23, 2017
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yoshifumi HIRAHARA, Shinji NAGAI, Ai USHIWATA, Ikuyo NIWAYAMA, Koichi WATANABE, Madoka TOMINAGA, Takafumi KUROSE, Shinichi YAMADA, Takehiro SHINOZAKI, Janos CSIKOS, Roman GORTELMEYER, Barbara ELLERS-LENZ, Michael ALTHAUS, Ulli BANKSTAHL
  • Publication number: 20170015624
    Abstract: A method for highly efficiently preparing high purity crystals of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]-ethyl]-1,3-propanediol hydrochloride. The method involves dissolving 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which its hydrochloride is highly soluble and a solvent in which its hydrochloride is less soluble, to prepare a solution of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then adding hydrochloric acid to the resulting solution with stirring, to crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]ethyl]-1,3-propanediol.
    Type: Application
    Filed: September 30, 2016
    Publication date: January 19, 2017
    Applicant: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Hidetaka KOMATSU, Hiroya SATOH
  • Patent number: 9493410
    Abstract: A method for highly efficiently preparing high purity crystals of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]-ethyl]-1,3-propanediol hydrochloride. The method involves dissolving 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol in a mixed solvent comprising a solvent in which its hydrochloride is highly soluble and a solvent in which its hydrochloride is less soluble, to prepare a solution of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol; and then adding hydrochloric acid to the resulting solution with stirring, to crystallize the hydrochloride of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chloro-phenyl]ethyl]-1,3-propanediol.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: November 15, 2016
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hidetaka Komatsu, Hiroya Satoh
  • Patent number: 9452977
    Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: September 27, 2016
    Assignees: KYORIN PHARMACEUTICAL CO., LTD., TEIJIN PHARMA LIMITED
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
  • Patent number: 9382250
    Abstract: The present invention relates to a method for producing a complex crystal composed of two or more different compounds, comprising crystallizing the two or more different compounds under a condition at which menthol is heat melted, and a method for screening a complex crystal. In accordance with the method for producing a complex crystal of the present invention, a complex crystal capable of being used as a drug material can be produced rapidly, simply and efficiently. In addition, in accordance with the method for screening a complex crystal of the present invention, a stable complex crystal can be searched, which is industrially useful.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: July 5, 2016
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Akinori Goto, Mamoru Fukuda
  • Patent number: 9328089
    Abstract: Disclosed is a technique for improving the water solubility and storage stability of 7-{(3S,4S)-3-[(cyclopropylamino)methyl]-4-fluoropyrrolidine-1-yl}-6-fluoro-1-(2-fluoroethyl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (compound (1)) that is safe and not only has a strong antibacterial action but also is effective for resistant bacteria for which conventional antibacterial agent are less effective. Crystals of the hydrochloride salt of the compound (1), crystals of the hydrochloride salt hydrate of the compound (1), and crystals of the methanesulfonate salt of the compound (1) are provided. In these crystals, decomposition due to influences of light is suppressed as compared to that in crystals of the compound (1) in free, and their storage stability is high. These crystals have higher solubility in water than the crystals of the compound (1) in free.
    Type: Grant
    Filed: June 17, 2015
    Date of Patent: May 3, 2016
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Ichiro Araya, Akinori Goto, Wataru Minagawa, Keiko Funada, Muneki Nagao
  • Patent number: 9315453
    Abstract: [Problem] For example, 4-(3-benzyloxyphenylthio)-2-chloro-1-(3-nitropropyl)benzene (compound 1) is used as an intermediate for producing a 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride which has excellent immunosuppressive activity. This compound 1 is traditionally obtained only as an oil and thus handling and refining were difficult. [Solution] A crystal of the compound 1 is obtained. A method of crystallizing the same is also established. Furthermore, a simple refining method is also found which comprises stirring in suspension the crystal in a solvent. Since the compound 1 can be obtained as a crystal, it is easier to handle and long term storage is possible.
    Type: Grant
    Filed: April 17, 2013
    Date of Patent: April 19, 2016
    Assignee: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Takeshi Tsubuki, Hiroya Sato
  • Publication number: 20160074330
    Abstract: [Problem] To provide a novel pharmaceutical composition which contains a medically active component and which can suppress delays in the release of said component due to gelling. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1), or a salt thereof, a cellulosic excipient, and a salting-out agent.
    Type: Application
    Filed: April 24, 2014
    Publication date: March 17, 2016
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi UCHIDA, Masataka HANADA, Yoshikazu MIYAZAKI
  • Publication number: 20160067185
    Abstract: [Problem] To provide a solid pharmaceutical composition which contains a compound represented by general formula (1) or a salt thereof and suppresses decomposition of said compound or salt thereof, and a production method of said solid pharmaceutical composition. [Solution] This solid pharmaceutical composition contains a compound represented by general formula (1) or a salt thereof, a cellulosic excipient, and an acidic substance of pH 4.0 or less.
    Type: Application
    Filed: April 24, 2014
    Publication date: March 10, 2016
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi UCHIDA, Masataka HANADA
  • Patent number: 9216163
    Abstract: A novel angiogenesis inhibitor, and a method for inhibiting angiogenesis are provided. Also provided are a prophylactic or therapeutic agent for a disease accompanied by angiogenesis, and a method for preventing or treating a disease accompanied by angiogenesis. The angiogenesis inhibitor contains L-carbocisteine or a pharmaceutically acceptable salt thereof as an active ingredient.
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: December 22, 2015
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Keizo Sato, Tomohiro Shinya, Shiori Nakayama
  • Patent number: 9164075
    Abstract: [Problem] To provide a novel isotope-labeled compound that can be used as a trapping agent and that is useful for picking out drug-candidate compounds that produce reactive metabolites. [Solution] Provided is a glutathione alkylester isotopologue represented by general formula (1). In formula (1), R1 represents a linear or branched alkoxy group in which at least one of carbon, oxygen, and hydrogen atoms contained therein is isotope-labeled and which has 1 to 8 carbon atoms or a cycloalkoxy group in which at least one of carbon, oxygen, and hydrogen atoms contained therein is isotope-labeled and which has 3 to 8 carbon atoms.
    Type: Grant
    Filed: May 21, 2012
    Date of Patent: October 20, 2015
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventor: Toshikazu Yamaoka