Patents Assigned to Nippon Chemiphar Co., Ltd.
  • ACTIVATING AGENT FOR PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA
    Publication number: 20130217734
    Abstract: A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR?. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.
    Type: Application
    Filed: February 12, 2013
    Publication date: August 22, 2013
    Applicant: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Nobutaka Mochiduki, Rie Takahashi, Masatoshi Ushioda, Tomio Yamakawa, Seiichiro Masui
  • P2X4 RECEPTOR ANTAGONIST
    Publication number: 20130184459
    Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is C1-8 alkoxy, hydroxyl, cyano, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene ring or the like.
    Type: Application
    Filed: July 27, 2011
    Publication date: July 18, 2013
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Masatoshi Ushioda, Shogo Sakuma, Toshiyasu Imai, Kazuhide Inoue
  • P 2 X 4 RECEPTOR ANTAGONIST
    Publication number: 20130178625
    Abstract: A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl having 1-3 halogens, C1-8 hydroxyalkyl, halogen, hydroxyl, nitro, cyano, amino, C1-8 alkylamino, benzenesulfonylamino optionally having a substituent, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene, tetrahydronaphthalene, or indan ring.
    Type: Application
    Filed: July 27, 2011
    Publication date: July 11, 2013
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Masatoshi Ushioda, Shogo Sakuma, Atsushi Tendo, Toshiyasu Imai, Kazuhide Inoue
  • P2X4 RECEPTOR ANTAGONIST
    Publication number: 20130172550
    Abstract: A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X4 receptor antagonist: wherein each of R21 and R22 is hydrogen, a C1-8 alkyl group or the like; R23 is hydrogen, a C1-8 alkyl group or the like; each of R24 and R25 is hydrogen, a C1-8 alkyl group or the like; R26 is hydrogen, a C1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.
    Type: Application
    Filed: July 13, 2011
    Publication date: July 4, 2013
    Applicant: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Masahiko Arai, Kunio Kobayashi, Yoshikazu Watanabe, Toshiyasu Imai, Kazuhide Inoue
  • Diazepinedione derivative
    Patent number: 8470814
    Abstract: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
    Type: Grant
    Filed: February 15, 2010
    Date of Patent: June 25, 2013
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Shogo Sakuma, Toshihiro Takahashi, Masatoshi Ushioda, Toshiyasu Imai, Kazuhide Inoue
  • G-PROTEIN-CONJUGATED RECEPTOR HAVING ALTERED LIGAND AFFINITY, AND USE THEREOF
    Publication number: 20130149715
    Abstract: A modified G-protein-coupled receptor (GPCR), having modified ligand affinity is provided by binding a G-protein-coupled receptor to a polypeptide consisting of an amino acid sequence of SEQ ID NO: 1. Furthermore, agonists for or antagonists against the modified GPCR are screened using a transformant in which the modified GPCR has been expressed. This makes it possible to provide a technique for analyzing the function of many putative GPCRs whose entities have not been clarified.
    Type: Application
    Filed: April 12, 2012
    Publication date: June 13, 2013
    Applicants: Nippon Chemiphar Co., Ltd., Pharmacome LLC
    Inventor: Ikunobu Muramatsu
  • Activating agent for peroxisome proliferator activated receptor ?
    Patent number: 8404726
    Abstract: A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR?. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: March 26, 2013
    Assignee: Nippon Chemiphar Co. Ltd.
    Inventors: Shogo Sakuma, Nobutaka Mochiduki, Rie Takahashi, Masatoshi Ushioda, Tomio Yamakawa, Seiichiro Masui
  • Agent for overcoming resistance to anti-cancer agent
    Patent number: 8314085
    Abstract: An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.
    Type: Grant
    Filed: June 27, 2011
    Date of Patent: November 20, 2012
    Assignee: Nippon Chemiphar Co., Ltd.
    Inventors: Masuharu Hirano, Tomio Yamakawa, Toshihisa Ishikawa, Hikaru Saito
  • PHARMACEUTICAL CONTAINING PPAR-DELTA AGONIST
    Publication number: 20120270910
    Abstract: Provision of an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, and a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like. A preparation containing [3-[2-[4-isopropyl-2-(4-trifluoroethyl)phenyl-5-thiazolyl]ethyl]-5-methyl-1,2-benzisoxazol-6-yl]oxyacetic acid, [4-[3-[2-(4-trifluoromethyl)phenyl-4-isopropyl-5-thiazolyl]propionyl]-2-methylphenoxy]acetic acid or [4-[3-[2-(2-hydroxy-4-chlorophenyl)-5-isopropyl-4-oxazolyl]propionyl]-2-methylphenoxy]acetic acid, or a pharmacologically acceptable salt thereof as an active ingredient is used as an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, as well as a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like.
    Type: Application
    Filed: May 20, 2008
    Publication date: October 25, 2012
    Applicants: SENJU PHARMACEUTICAL CO., LTD., NIPPON CHEMIPHAR CO., LTD.
    Inventors: Yoshikuni NAKAMURA, Ikuko HANANO, Jun INOUE
  • GPR119 AGONIST
    Publication number: 20120245344
    Abstract: A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: wherein each of R23, R24, and R25 is hydrogen, halogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkylsulfonyl, or the like; each of Q0 and T0 is CH2 or the like, or Q0 and T0 are combined to form CH?CH or the like; A0 is (CH2)p, C(O), or a bond; B0 is a bond or the like; one of U0 and V0 is N, and the other is CR31 or the like; each of X0 and Y0 is CH2CH2 or the like; Z0 is C(O)OR32 or the like; and each of R21 and R22 is hydrogen, a halogen atom, hydroxyl, C1-8 alkyl, or the like.
    Type: Application
    Filed: August 30, 2010
    Publication date: September 27, 2012
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Tsuyoshi Endo, Hiroto Tanaka, Toshihiro Takahashi, Toshihiro Kunigami
  • Methods of using an alpha-1-adrenergic receptor having altered ligand affinity
    Patent number: 8173378
    Abstract: A modified G-protein-coupled receptor (GPCR), having modified ligand affinity is provided by binding a G-protein-coupled receptor to a polypeptide consisting of an amino acid sequence of SEQ ID NO: 1. Furthermore, agonists for or antagonists against the modified GPCR are screened using a transformant in which the modified GPCR has been expressed. This makes it possible to provide a technique for analyzing the function of many putative GPCRs whose entities have not been clarified.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: May 8, 2012
    Assignees: Pharmacome LLC, Nippon Chemiphar Co., Ltd.
    Inventor: Ikunobu Muramatsu
  • DIAZEPINEDIONE DERIVATIVE
    Publication number: 20110319610
    Abstract: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
    Type: Application
    Filed: February 15, 2010
    Publication date: December 29, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Shogo Sakuma, Toshihiro Takahashi, Masatoshi Ushioda, Toshiyasu Imai, Kazuhide Inoue
  • AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT
    Publication number: 20110257201
    Abstract: An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Masuharu HIRANO, Tomio YAMAKAWA, Toshihisa ISHIKAWA, Hikaru SAITO
  • GPR119 AGONIST
    Publication number: 20110137032
    Abstract: A cyclic amine derivative represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes. wherein Ar0 is phenyl or phenyl having a substituent such as C1-8 alkylsulfonyl or the like, pyridyl, or pyridyl having a substituent such as C1-8 alkylsulfonyl; A0 is (CH2)p, O, or the like; B0 is (CH2)q, or the like, provided that B0 is neither O nor NR25 when A0 is O or NR24; one of U0 and V0 is N, and the other is N or CR26; each of X0 and Y0 is C1-3 alkylene or C1-3 alkylene having a substituent; R23 is a C1-8 alkyl group or the like; each of R21 and R22 is hydrogen, a halogen atom, or the like.
    Type: Application
    Filed: July 31, 2009
    Publication date: June 9, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Tsuyoshi Endo, Rie Takahashi, Hiroto Tanaka, Toshihiro Kunigami, Takaichi Hamano, Mai Okamura, Kaoru Hara
  • THERAPEUTIC OR PROPHYLACTIC AGENT FOR CEREBRAL ANEURYSM
    Publication number: 20110092484
    Abstract: [Problems] To provide a medicament which is effective for treatment and prophylaxis of cerebral aneurysms [Means for Solving the Problems] The invention provides a medicament for treatment and prophylaxis of cerebral aneurysms, wherein the medicament contains a cysteine protease inhibitor as an active ingredient. The cysteine protease inhibitor preferably is an epoxysuccinamide derivative or its salt.
    Type: Application
    Filed: June 6, 2008
    Publication date: April 21, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Nobuo Hashimoto, Hiroharu Kataoka, Tomohiro Aoki
  • P2X4 RECEPTOR ANTAGONIST
    Publication number: 20110092703
    Abstract: A P2X4 receptor antagonist is a compound represented by the formula (I) or a pharmacologically acceptable salt thereof, which is used as a preventive or therapeutic agent for neuropathic pains: Wherein B is aryl or the like that can have a substituent; Y is C1-5 alkylene that can have a double bond; Z is O, S or the like; each of R1, R2 and R3 independently is hydrogen, C1-8 alkyl or the like; R4 is hydrogen, C1-8 alkyl or the like; each of P and Q independently is hydrogen, halogen, C1-8 alkyl or the like; W is C1-8 alkyl or the like; and each of n and m independently is 1 or 2.
    Type: Application
    Filed: August 8, 2008
    Publication date: April 21, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Shogo Sakuma, Tsuyoshi Endo, Noriko Kanakubo, Masahiko Arai, Toshihiro Takahashi, Toshiyasu Imai, Kumiko Taguchi, Eriko Nakata, Nobutaka Mochiduki, Masatoshi Ushioda, Makoto Tsuda, Kazuhide Inoue
  • SALT OF (2S, 3S) -3- [ [ (1S) -1- ISOBUTOXYMETHYL-3-METHYLBUTYL] CARBAMYL] OXIRANE-2-CARBOXYLIC ACID
    Publication number: 20110003993
    Abstract: The invention relates to purification of (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylic acid [hereinafter, referred to as the carboxylic acid] using the salt of the carboxylic acid with an organic amine selected from the group consisting of piperazine, adamantane amines and others. The invention also relates to providing crystalline sodium salt of the carboxylic acid. The sodium salt is usable as a material for preparing medicaments and improved in storage stability, and has the following characteristics: DSC: exothermic peak observed at a temperature in the range of 170 to 175° C. with weight decrease; and characteristic absorption bands of infrared absorption spectrum (KBr tablet): 3255, 2950, 2860, 1670, 1630, 1550, 1460, 1435, 1395, 1365, 1310, 1260, 1110, 890 cm×1.
    Type: Application
    Filed: September 13, 2010
    Publication date: January 6, 2011
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Atsushi TENDO, Toshihiro TAKAHASHI, Tomio YAMAKAWA, Kazuki OKAI, Susumu NIHASHI
  • REGULATOR FOR SIGNALING TOLL-LIKE RECEPTOR, WHICH COMPRISES CATHEPSIN INHIBITOR AS ACTIVE INGREDIENT
    Publication number: 20100331545
    Abstract: [Problems] To provide a modulator for signaling of TLR [Means for solving the problems] A medicament containing cathepsin inhibitor such as monosodium (2S,3S)-3-[[(1S)-1-isobutoxymethyl-3-methylbutyl]carbamoyl]oxirane-2-carboxylate as a active ingredient is used as a modulator for signaling of TLR, a therapeutic agent for treating diseases associated with TLR signaling, a therapeutic agent for treating diseases associated with induction of Th17 cells, a therapeutic agent for treating diseases associated with production of IL-6, IL-12, IL-17, or IL-23, or a therapeutic agent for treating systemic lupus erythematosus, lupus nephritis, crohn's disease, psoriasis, or acute disseminated encephalomyelitis.
    Type: Application
    Filed: October 23, 2008
    Publication date: December 30, 2010
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Hiroshi Takayanagi, Masataka Asagiri, Toshitake Hirai
  • P2X4 RECEPTOR ANTAGONIST
    Publication number: 20100256123
    Abstract: A compound having the following formula (II) or its pharmacologically acceptable salt is used as a P2X4 receptor antagonist: in which R11 represents hydrogen or an alkyl group having 1-8 carbon atoms; R21 represents an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms and having 1-3 halogen substituents, or hydroxyl; and R31 is hydrogen or a halogen atom.
    Type: Application
    Filed: August 24, 2007
    Publication date: October 7, 2010
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Shogo Sakuma, Tsuyoshi Endo, Toshiyasu Imai, Noriko Kanakubo, Masahiko Arai, Toshihiro Takahashi, Tomio Yamakawa, Makoto Tsuda, Kazuhide Inoue, Kenji Hirate, Takako Hirate
  • AGENT FOR OVERCOMING RESISTANCE TO ANTI-CANCER AGENT
    Publication number: 20100234399
    Abstract: An agent comprising, as an active ingredient, a xanthine oxidase inhibitor such as 2-[3-cyano-4-(4-fluorophenoxy)phenyl]-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-[3-cyano-4-(4-fluorophenoxy)phenyl]thiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine, 2-(3-cyano-4-phenoxyphenyl)-4-hydroxythiazolo[5,4-d]pyrimidine potassium salt, 2-(3-cyano-4-phenoxyphenyl)thiazolo[5,4-d]pyrimidine, TMX-67, and FYX-051, which can be used as an agent for overcoming anti-cancer agent resistance.
    Type: Application
    Filed: June 22, 2007
    Publication date: September 16, 2010
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Masuharu Hirano, Tomio Yamakawa, Toshihisa Ishikawa, Hikaru Saito