Patents by Inventor Hirotsune Itahana

Hirotsune Itahana 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: 8076348
    Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
    Type: Grant
    Filed: August 7, 2006
    Date of Patent: December 13, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
  • Publication number: 20100168096
    Abstract: [Problem] To provide a compound which can be used in the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in the treatment of irritable bowel syndrome (IBS) and/or prevention of migraine. [Means for Resolution] It was found that an acylguanidine derivative having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having antagonism to both of the receptors showed superior pharmacological action in comparison with the case of the single use of an antagonist selective for either one of the receptors. Based on the above, the compound of the present invention is useful in preventing and/or treating diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly in treating irritable bowel syndrome (IBS) and/or preventing migraine.
    Type: Application
    Filed: August 7, 2006
    Publication date: July 1, 2010
    Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Eisuke Nozawa, Shinobu Akuzawa, Koichiro Harada
  • Publication number: 20080200551
    Abstract: This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof. The compound of the invention has an advantage in that it has high affinity for serotonin receptor subtypes, particularly for 5-HT2B receptor and 5-HT7 receptor, and shows excellent pharmacological effects in comparison with the conventional compounds which have only one of the antagonistic activities of 5-HT2B receptor and 5-HT7 receptor, this is useful as a prophylactic antimigraine agent having high safety and excellent effect.
    Type: Application
    Filed: February 17, 2005
    Publication date: August 21, 2008
    Inventors: Hiroyoshi Yamada, Hirotsune Itahana, Ayako Moritomo, Takaho Matsuzawa, Koichiro Harada, Jiro Fujiyasu, Yuji Koga, Makoto Oku, Toshio Okazaki, Shinobu Akuzawa, Toshihiro Watanabe
  • Patent number: 7250429
    Abstract: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.
    Type: Grant
    Filed: March 19, 2003
    Date of Patent: July 31, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Hirotsune Itahana, Jiro Fujiyasu, Satoshi Hayashibe, Toshihiro Watanabe, Masamichi Okada, Takashi Toya
  • Publication number: 20050148642
    Abstract: This invention relates to the provision of novel aminomethyl-substituted thiazolobenzimidazole derivatives represented by the following general formula (I) or a salt thereof. The aforementioned derivative or a salt thereof has a metabotropic glutamate receptor action and excellent oral activity and is therefore useful as a medicament. (In the formula, R1: an oxygen-containing saturated hetero ring or the like, Alk1: a lower alkylene, m: 0 or 1, Alk2: a lower alkylene which may be substituted with oxo group, n: 0 or 1, X: a bond, O, S or NR5, R3: H or the like, and R2, R4, R5, R6 and R7: the same or different from one another and each represents H or the like. Provided that R3 does not represent a lower alkyl or a halogeno-lower alkyl when X is a bond and n is 1. Also, R4 represents a group other than Me when m is 1, R1 is OH or OMe and Alk1 is a C1-3 alkylene, and further 1) when X is a bond, n is 1 and R3 is H, or 2) when X is a bond, n is 0 and R3 is cyclohexane.
    Type: Application
    Filed: March 19, 2003
    Publication date: July 7, 2005
    Inventors: Hirotsune Itahana, Jiro Fujiyasu, Satoshi Hayashibe, Toshihiro Watanabe, Masamichi Okada, Takashi Toya
  • Patent number: 6642264
    Abstract: This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention. (Symbols in the formula represent the following meanings. R1: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R2: hydrogen, lower alkyl or the like; and R3, R4 and R5: hydrogen, lower alkyl and the like which may be the same or different from one another.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: November 4, 2003
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Satoshi Hayashibe, Hirotsune Itahana, Masamichi Okada, Atsuyuki Kohara, Kyoichi Maeno, Kiyoshi Yahiro, Itsuro Shimada, Kazuhito Tanabe, Kenji Negoro, Takashi Kamikubo, Shuichi Sakamoto
  • Patent number: 5834499
    Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.
    Type: Grant
    Filed: August 26, 1996
    Date of Patent: November 10, 1998
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Kiyoshi Iwaoka, Hideki Anan, Naoki Imanishi, Kenichi Kazuta, Hiroyuki Koshio, Takeshi Suzuki, Hirotsune Itahana, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta