Patents by Inventor Tsuyoshi Nagase

Tsuyoshi Nagase has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 8822453
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Grant
    Filed: August 20, 2010
    Date of Patent: September 2, 2014
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Takashi Oshiyama, Tsuyoshi Nagase, Masataka Ueda, Kuninori Tai
  • Patent number: 8420823
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: April 16, 2013
    Assignee: MSD K.K.
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Patent number: 8367698
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: February 5, 2013
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8314094
    Abstract: [PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: November 20, 2012
    Assignee: MSD K.K
    Inventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
  • Patent number: 8268842
    Abstract: The present invention provides a compound represented by formula (I) below, or a pharmaceutically acceptable salt thereof, which, having histamine H3 receptor antagonist or inverse agonist activity, is useful in the prophylaxis or therapy of metabolic diseases, circulatory diseases, or nervous system diseases. [where, for example, Ar is a divalent group formed by eliminating two hydrogen atoms from benzene, X1 is a nitrogen atom, sulfur atom or oxygen atom, R1 is a 5- to 6-membered heteroaryl group, Ring A is a 5- to 6-membered heteroaryl ring, R2 and R3 are amino groups or alkylamino groups, and X2 is represented by formula (II): (where R4 and R5 are lower alkyl groups, and n is an integer from 2 to 4).
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: September 18, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Publication number: 20120232109
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Application
    Filed: May 23, 2012
    Publication date: September 13, 2012
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20120225866
    Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.
    Type: Application
    Filed: August 20, 2010
    Publication date: September 6, 2012
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kunio Oshima, Shuuji Matsumura, Hokuto Yamabe, Naohiro Isono, Noriaki Takemura, Shinichi Taira, Takashi Oshiyama, Yasuhiro Menjo, Tsuyoshi Nagase, Masataka Ueda, Yasuo Koga, Sunao Nakayama, Kenji Tsujimae, Toshiyuki Onogawa, Kuninori Tai, Motohiro Itotani
  • Patent number: 8188280
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Grant
    Filed: February 4, 2009
    Date of Patent: May 29, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8163898
    Abstract: [PROBLEMS] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [MEANS FOR SOLVING PROBLEMS] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: April 24, 2012
    Assignee: MSD K. K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8138206
    Abstract: Disclosed is a substance having an antagonistic effect on the binding of histamine to a histamine H3 receptor or an inhibitory effect on the activity which a histamine H3 receptor constantly exhibits. A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof; (I) wherein R1 represents a phenyl group which may be substituted or the like and R2 represents a cyano group which may be substituted or the like, or R1 and R2 together form an aliphatic heterocylic ring which may be substituted; R3 represents a group represented by the formula (II-1) below; and all of X1 to X4 represent a carbon atom or the like: (II-1) where R4 and R5 represent a lower alkyl group or the like; and m1 represents an integer of 2 to 4.
    Type: Grant
    Filed: May 29, 2006
    Date of Patent: March 20, 2012
    Assignee: MSD. K.K.
    Inventors: Shiho Ishikawa, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi, Shigeru Tokita, Toshihiro Wada
  • Patent number: 8124807
    Abstract: [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: February 28, 2012
    Assignee: MSD K.K.
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 8106086
    Abstract: A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
    Type: Grant
    Filed: March 27, 2008
    Date of Patent: January 31, 2012
    Assignee: MSD K.K.
    Inventors: Toshiyuki Takahashi, Tsuyoshi Nagase, Nagaaki Sato
  • Patent number: 7960394
    Abstract: This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
    Type: Grant
    Filed: May 30, 2005
    Date of Patent: June 14, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Publication number: 20110009622
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Application
    Filed: April 17, 2009
    Publication date: January 13, 2011
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20100331360
    Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.
    Type: Application
    Filed: February 4, 2009
    Publication date: December 30, 2010
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20100249147
    Abstract: [Problem] To provide a compound that is useful as an agent in the prevention and treatment of circulatory system, nervous system, metabolic, reproductive system, and gastrointestinal diseases. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I): [wherein, Z represents formula (II-1), (II-2), or (II-3), wherein m and n are 0, 1, or 2, Y represents CR3 or N, R1 represents a C1-6 alkyl, C3-8 cycloalkyl, etc., R2 represents phenyl or a heteroaryl, etc., R3 and R4 each independently represent a hydrogen atom, a C1-6 alkyl, etc., M1, M2, M3, and M4 each independently represent a hydrogen atom, a C1-6 alkyl, etc.
    Type: Application
    Filed: December 16, 2008
    Publication date: September 30, 2010
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Publication number: 20100234392
    Abstract: [Problems] To provide compounds useful as preventives or remedies for circulatory diseases, nervous diseases, metabolic diseases, reproductive system diseases, and digestive diseases. [Means for Solving Problems] Compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof: wherein R1 is C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 is phenyl, heteroaryl, or the like; Q is N or CH; and M1, M2, M3 and M4 are each independently hydrogen or C1-6 alkyl, or alternatively M1 together with M2 or M3 forms —CH2-CH2- or the like, or M4 together with M2 or M3 forms —CH2-CH2- or the like, with the proviso that M1, M2, M3, and M4 are such that one —CH2- or —CH2-CH2- group is formed thereamong.
    Type: Application
    Filed: September 12, 2008
    Publication date: September 16, 2010
    Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
  • Patent number: 7790731
    Abstract: The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: September 7, 2010
    Assignee: Banyu Pharmaceutical Co. Ltd.
    Inventors: Akio Kanatani, Nagaaki Sato, Tsuyoshi Nagase, Shigeru Tokita
  • Publication number: 20100210636
    Abstract: [PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].
    Type: Application
    Filed: October 2, 2008
    Publication date: August 19, 2010
    Inventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
  • Publication number: 20100056597
    Abstract: A compound represented by the general formula (I-a): [wherein R1a and R2a each means hydrogen, lower cycloalkyl, lower alkyl, etc.; R3a means hydrogen, lower cycloalkyl, lower alkyl, etc.; R4a and R5a each means lower alkyl, lower cycloalkyl, etc. or R4a and R5a are bonded to each other to form lower cycloalkylidene; and R6a means lower alkyl, lower haloalkyl, etc.]. This compound functions as an LCE inhibitor and is useful as a therapeutic agent for various circulatory diseases, nervous diseases, metabolic diseases, reproductive diseases, digestive tract diseases, neoplasm, infectious diseases, etc.
    Type: Application
    Filed: March 27, 2008
    Publication date: March 4, 2010
    Inventors: Toshiyuki Takahashi, Tsuyoshi Nagase, Nagaaki Sato