Patents Assigned to Kyorin Pharmaceutical Co. Ltd.
  • Method for producing 3-substituted-4-fluoropyrrolidine derivative
    Patent number: 8501965
    Abstract: An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.
    Type: Grant
    Filed: May 30, 2011
    Date of Patent: August 6, 2013
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Masashi Suzuki, Muneki Nagao
  • Spirocyclic aminoquinolones as GSK-3 inhibitors
    Patent number: 8476261
    Abstract: Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases. In Formula (I): X1 is O or NR8; A is bond or substituted or unsubstituted C1-C2 alkylene, wherein the substituents when present are selected from one to four Q2 groups; where Q2 is alkyl or haloalkyl; p is 0 or 1; and q is an integer of 0 to 2.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: July 2, 2013
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Oana Cociorva, Yasumichi Fukuda, Yasushi Kohno, Bei Li, Kyoko Okada, Ayako Nakamura, Masahiro Nomura, Shigeki Seto, Anna Katrin Szardenings, Kazuhiro Yumoto
  • Process for production of bicyclo[2.2.2]octylamine derivative
    Patent number: 8476470
    Abstract: The present invention herein provides a process for production of a bicyclo[2.2.2]octylamine derivative which may be used as an intermediate for preparation of medical and pharmaceutical products. The process is quite efficient and can produce the derivative in a large-scale while using mild reaction conditions. The process for producing a bicyclo[2.2.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: July 2, 2013
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Tomohiro Akeboshi, Yusuke Iriyama, Hirotaka Kawanami
  • Therapeutic agent or prophylactic agent for inflammatory bowel disease comprising amino alcohol derivative as active ingredient
    Patent number: 8476305
    Abstract: A novel therapeutic agent or prophylactic agent for an inflammatory bowel disease is provided. An amino alcohol derivative represented by the general formula (1): which is a sphingosine-1-phosphate receptor agonist or a pharmaceutically acceptable salt or hydrate thereof are a therapeutic agent or prophylactic agent for an inflammatory bowel disease comprises.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: July 2, 2013
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Naoya Yamamuro, Koichi Nakamaru, Tokutarou Yasue
  • PROPHYLACTIC OR THERAPEUTIC AGENT FOR NON-ALCOHOLIC STEATOHEPATITIS
    Publication number: 20130143913
    Abstract: An object of the present invention is to provide an agent for prevention or treatment of a fatty liver disease, preferably NAFLD, more preferably NASH. The present invention provides an agent for prevention or treatment of a fatty liver disease containing ibudilast as an active agent.
    Type: Application
    Filed: August 11, 2011
    Publication date: June 6, 2013
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Toshiyuki Matsui, Tomohiro Ide, Masaki Tsunoda, Tomomi Ogata, Minoru Ito
  • Phosphodiesterase 10A inhibitor
    Patent number: 8404710
    Abstract: A phosphodiesterase 10A inhibitor serving as an effective prophylactic or therapeutic agent for Parkinson's disease, Huntington's disease, Alzheimer's disease, and schizophrenia. The PDE10A inhibitor contains as an active ingredient a pyrazolo[1,5-a]pyridine derivative represented by the following general formula: wherein R1 and R2 are each independently a hydrogen atom or a lower alkyl group having 1 to 4 carbons; and R3 is a hydrogen atom, a lower alkyl group having 1 to 4 carbons, or a lower alkoxyl group having 1 to 3 carbons.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 26, 2013
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Michiaki Nagasawa, Simon John Mackenzie
  • Cyanoaminoquinolones and tetrazoloaminoquinolones as GSK-3 inhibitors
    Patent number: 8389514
    Abstract: Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: March 5, 2013
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Bei Li, Anna Katrin Szardenings
  • Oral sustained-release tablet
    Patent number: 8343544
    Abstract: (Object) An oral sustained-release tablet is provided, which does not cause initial rapid increases in the bloodlevels of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) and can maintain constant the blood levels. (Solving means) An oral sustained-release tablet comprises a pharmaceutical composition and a gel-forming material, the pharmaceutical composition containing KRP-197 as an active ingredient.
    Type: Grant
    Filed: August 12, 2010
    Date of Patent: January 1, 2013
    Assignees: Kyorin Pharmaceutical Co., Ltd., Ono Pharmaceutical Co., Ltd.
    Inventors: Ryouichi Hoshino, Katashi Nakashima, Kazuo Kazama
  • Method for treating an inflammatory bowel disease using 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol or a salt thereof
    Patent number: 8318811
    Abstract: A novel therapeutic and prophylactic agent for inflammatory bowel diseases and a method for treating inflammatory bowel diseases is provided. The agent comprises a 2-amino-1,3-propanediol derivative (e.g., 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl-1,3-propanediol hydrochloride) represented by the chemical formula (1) or a pharmaceutically acceptable salt or hydrate thereof: The agent is useful in the treatment or prevention of Crohn's disease, Crohn's disease in large intestine, intestinal Behcet's disease, ulcerative colitis, bleeding rectal ulcer and pouchitis.
    Type: Grant
    Filed: February 5, 2007
    Date of Patent: November 27, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Ryotaro Kojima, Koichi Nakamaru, Tokutarou Yasue
  • MALEIC ACID SALT AND CRYSTAL THEREOF
    Publication number: 20120245346
    Abstract: Disclosed is a benz[d][1,3]oxazine derivative having excellent stability when used as an active ingredient for a medicinal agent, and also having excellent solubility and crystallinity. Specifically disclosed is 2-[2-((S)-3-dimethylaminopyrrolidin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-benz[d][1,3]oxazin-4-one maleate.
    Type: Application
    Filed: September 27, 2010
    Publication date: September 27, 2012
    Applicant: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Takeshi Tsubuki, Tetsuya Sagawa, Keiko Funada, Ichiro Araya
  • Amino alcohol derivative and immunosuppresive agent having same as an active ingredient
    Patent number: 8273748
    Abstract: An amino alcohol derivative useful as an excellent immunosuppressive agent is provided. As a result of intensive research to create a highly safe compound which has an excellent immunosuppressive activity, it was discovered that an amino alcohol derivative represented by the general formula (1), has excellent immunosuppressive activity.
    Type: Grant
    Filed: August 7, 2007
    Date of Patent: September 25, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoshi Fujii, Tatsuhiro Saito, Kazuhiko Kuriyama, Tokutarou Yasue
  • TREATMENT OF INFLUENZA
    Publication number: 20120232128
    Abstract: The present invention provides a double-stranded RNA which inhibits replication of influenza B viruses by RNA interference, in which the double-stranded RNA comprises an RNA having 19 to 25 nucleotides homologous with a part of an mRNA transcribed from a genomic RNA of the influenza B viruses and an antisense RNA thereof.
    Type: Application
    Filed: May 11, 2012
    Publication date: September 13, 2012
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Misako NAKAZAWA, Shin-etsu Kadowaki, Yoshiji Fujita, Masato Miyake, Takanori Ueda, Tomohiro Yoshikawa
  • Amino phosphate derivative and S1P receptor modulator having same as an active ingredient
    Patent number: 8232319
    Abstract: To provide an amino phosphate derivative having an excellent sphingosine-1-phosphate (S1P) receptor modulatory action. As a result of continued intensive research to create a highly safe compound which has an S1P receptor modulatory action, is has been discovered that an amino phosphate derivative represented by the following general formula (1), has a strong S1P receptor modulatory action.
    Type: Grant
    Filed: August 7, 2007
    Date of Patent: July 31, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoshi Fujii, Tatsuhiro Saito
  • Mutilin derivative having heterocyclic aromatic ring carboxylic acid structure in substituent at 14-position
    Patent number: 8222407
    Abstract: To provide a novel mutilin derivative having a substitution at the 14-position, which is a novel mutilin analogue exhibiting a potent and broad antimicrobial action against Gram-positive bacteria and Gram-negative bacteria including various drug-resistant bacteria, and which is expected to be useful as an agent for treating infectious diseases. A mutilin derivative represented by the following general formula (1): or a pharmaceutically acceptable addition salt thereof.
    Type: Grant
    Filed: May 23, 2008
    Date of Patent: July 17, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasumichi Fukuda, Masanori Takadoi, Yoshikazu Asahina, Taro Sato, Haruaki Kurasaki, Hiroyuki Ebisu, Masaya Takei, Hideyuki Fukuda
  • Method for preparing sustained release tablet
    Patent number: 8202456
    Abstract: Herein provided is a method for easily preparing a sustained release tablet which contains an orally administrable medicinal component, while maintaining the uniformity of the content of the medicinal component. The method comprises mixing (1) a granulated product A obtained by granulating an excipient and an enteric coating agent while spraying thereon with a solution or a suspension containing an orally administrable medicinal component, with (2) a composition B containing a hydrogel-forming substance; and then compressing the resulting mixture into a tablet.
    Type: Grant
    Filed: November 12, 2007
    Date of Patent: June 19, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Katashi Nakashima, Kazuo Kazama
  • Treatment of influenza
    Patent number: 8198256
    Abstract: The present invention provides a double-stranded RNA which inhibits replication of influenza B viruses by RNA interference, in which the double-stranded RNA comprises an RNA having 19 to 25 nucleotides homologous with a part of an mRNA transcribed from a genomic RNA of the influenza B viruses and an antisense RNA thereof.
    Type: Grant
    Filed: July 2, 2008
    Date of Patent: June 12, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Misako Nakazawa, Shin-etsu Kadowaki, Yoshiji Fujita, Masato Miyake, Takanori Ueda, Tomohiro Yoshikawa
  • Glucokinase activator
    Patent number: 8173649
    Abstract: A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; 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-C6 alkyl group, a C1-C6 alkoxy group, a C1-C6 alkylsulfanyl group, a C1-C6 alkylsulfinyl group or a C1-C6 alkylsulfonyl group; and A is a substituted or unsubstituted heteroaryl group), or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: May 8, 2012
    Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma Limited
    Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Ayako Nakamura, Kenji Fujita, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
  • TABLET HAVING HOLLOW STRUCTURE
    Publication number: 20120100212
    Abstract: A water floatable tablet, which is either: (a) a tablet comprising at least one filler selected from the group consisting of a sugar alcohol, a sugar, a cellulose derivative, and a starch and a component which exhibits a hydrophobic effect, wherein the tablet has a hollow cavity in a center section; or (b) a tablet obtained by a process including: (1) forming a crust comprising at least one filler selected from the group consisting of a sugar alcohol, a sugar, a cellulose derivative, and a starch on an outer surface of a core comprising a sublimation solid, to obtain a dry coated tablet having the core positioned at a center section; (2) heating the dry coated tablet, to obtain a tablet having a hollow cavity; and (3) contacting the tablet having a hollow cavity with a component which exhibits a hydrophobic effect.
    Type: Application
    Filed: July 5, 2010
    Publication date: April 26, 2012
    Applicant: KYORIN PHARMACEUTICAL, CO., LTD.
    Inventors: Mamoru Fukuda, Akinori Goto
  • Method for producing aminoacetylpyrrolidinecarbonitrile derivative
    Patent number: 8143427
    Abstract: It is to provide a method for efficiently producing an aminoacetylpyrrolidinecarbonitrile derivative which is useful as a DPP-IV inhibitor. It is a method for producing an aminoacetylpyrrolidinecarbonitrile derivative represented by the formula (2): (in the formula, A and R1 are as defined in the following), comprising allowing an acid to act on an aminoacetylpyrrolidinecarboxamide derivative represented by the formula (1): (in the formula, A represents CH2, CHF or CF2; and R1 represents a secondary amino group which may be substituted), and then allowing a dehydrating agent to act thereon.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: March 27, 2012
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuo Orita, Takayuki Gotoh
  • MATRIX-TYPE SUSTAINED RELEASE PREPARATION CONTAINING BASIC ADDITIVE
    Publication number: 20120029032
    Abstract: Disclosed is a matrix-type sustained release preparation containing a basic drug unstable against an acid as an active pharmaceutical ingredient, wherein the decomposition of the basic drug unstable against the acid can be prevented and therefore the pH-dependent release can be reduced. A hardly water-soluble basic normal salt is added to a matrix-type sustained release preparation containing a basic drug that is unstable against an acid.
    Type: Application
    Filed: March 26, 2010
    Publication date: February 2, 2012
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Mamoru Fukuda, Mayuko Takahashi, Takahiro Goto