Patents by Inventor Shinobu Akuzawa

Shinobu Akuzawa 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: 8222274
    Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
    Type: Grant
    Filed: February 19, 2007
    Date of Patent: July 17, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
  • 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
  • Patent number: 7985764
    Abstract: It was found that a compound according to the following formula: or a pharmaceutically acceptable salt thereof, has a strong antagonism for both the 5-HT2B and 5-HT7 receptors. In addition, the compound shows good pharmacological action as compared to antagonists selective for only one of these receptors. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
    Type: Grant
    Filed: February 7, 2007
    Date of Patent: July 26, 2011
    Assignee: Astellas Pharma Inc.
    Inventors: Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Ryushi Seo, Shinobu Akuzawa
  • Publication number: 20110158930
    Abstract: A method for treatment of a patient suffering from irritable bowel syndrome with diarrhea or mixed irritable bowel syndrome, which comprises administering to the patient a therapeutically effective amount of ramosetron or a pharmaceutically acceptable salt thereof in combination with a therapeutically effective amount of polycarbophil or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: August 27, 2009
    Publication date: June 30, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takuya Hirata, Toshiyuki Funatsu, Yoshihiro Keto, Shinobu Akuzawa
  • 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: 20090062363
    Abstract: [Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
    Type: Application
    Filed: February 7, 2007
    Publication date: March 5, 2009
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Ryushi Seo, Shinobu Akuzawa
  • Publication number: 20090036421
    Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).
    Type: Application
    Filed: February 19, 2007
    Publication date: February 5, 2009
    Applicant: ASTELLAS PHARMA INC
    Inventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
  • 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
  • Publication number: 20080171788
    Abstract: The invention relates to a medicament for IBS, which comprises a dual antagonist for 5-HT2B and 5-HT7 receptors having selective binding affinities for 5-HT2B and 5-HT7 receptors. The pharmaceutical composition of the invention is useful as a drug which is excellent in the therapeutic effect on IBS and shows lessened side effects occurring in the existing remedies for IBS, because it showed good pharmacological actions in comparison with the case of independently using a 5-HT2B receptor antagonist having selective binding affinity for 5-HT2B receptor or a 5-HT7 receptor antagonist having selective binding affinity for 5-HT7 receptor.
    Type: Application
    Filed: February 7, 2006
    Publication date: July 17, 2008
    Inventors: Shinobu Akuzawa, Hiroyuki Ito, Toshihiro Watanabe, Hiroyoshi Yamada
  • Publication number: 20080161419
    Abstract: The present invention relates to prophylactic antimigraine agents comprising as an active ingredient a dual antagonist for the 5-HT2B and 5-HT7 receptors, the antagonist having a binding affinity selective for the 5-HT2B and 5-HT7 receptors. Since these prophylactic antimigraine agents show an excellent pharmacological effect in comparison with the cases in which a 5-HT2B receptor antagonist having a selective binding affinity to the 5-HT2B receptor or a 5-HT7 receptor antagonist having a selective binding affinity to the 5-HT7 receptor is used alone, they are useful as drugs which are excellent in prophylaxis of migraine and in which the side effects found in the existing prophylactic antimigraine agents are reduced.
    Type: Application
    Filed: February 17, 2005
    Publication date: July 3, 2008
    Inventors: Shinobu Akuzawa, Toshihiro Watanabe