Patents by Inventor Itsuro Shimada

Itsuro Shimada 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: 10774082
    Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.
    Type: Grant
    Filed: December 12, 2019
    Date of Patent: September 15, 2020
    Assignee: Astellas Pharma Inc.
    Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
  • Publication number: 20200140437
    Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.
    Type: Application
    Filed: December 12, 2019
    Publication date: May 7, 2020
    Applicant: Astellas Pharma Inc.
    Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
  • Patent number: 10556906
    Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.
    Type: Grant
    Filed: June 5, 2019
    Date of Patent: February 11, 2020
    Assignee: ASTELLAS PHARMA INC.
    Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
  • Patent number: 10532048
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Grant
    Filed: July 5, 2018
    Date of Patent: January 14, 2020
    Assignee: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Publication number: 20190292182
    Abstract: [Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.
    Type: Application
    Filed: June 5, 2019
    Publication date: September 26, 2019
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Kazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike
  • Publication number: 20190000832
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Application
    Filed: July 5, 2018
    Publication date: January 3, 2019
    Applicant: Selder Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 10016410
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Grant
    Filed: November 14, 2016
    Date of Patent: July 10, 2018
    Assignee: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 9526719
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Grant
    Filed: August 26, 2015
    Date of Patent: December 27, 2016
    Assignee: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 9487491
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: November 8, 2016
    Assignees: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.
    Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
  • Publication number: 20150359787
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Application
    Filed: August 26, 2015
    Publication date: December 17, 2015
    Applicant: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 9150541
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: October 6, 2015
    Assignee: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 9085540
    Abstract: Compounds of formula (I): in which the variables are defined herein, are useful for the treatment of cancer in patients which express the EGFR T790M mutation.
    Type: Grant
    Filed: January 15, 2013
    Date of Patent: July 21, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Takahiro Matsuya, Yutaka Kondoh, Itsuro Shimada, Shigetoshi Kikuchi, Maiko Iida, Kenichi Onda, Hiroki Fukudome, Yukihiro Takemoto, Nobuaki Shindou, Hideki Sakagami, Hisao Hamaguchi
  • Patent number: 8969336
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: March 3, 2015
    Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.
    Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
  • Publication number: 20140371196
    Abstract: Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicants: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.
    Inventors: Itsuro SHIMADA, Kazuo KUROSAWA, Takahiro MATSUYA, Kazuhiko IIKUBO, Yutaka KONDOH, Akio KAMIKAWA, Hiroshi TOMIYAMA, Yoshinori IWAI
  • Publication number: 20140323463
    Abstract: [Problem] A compound which is useful as an inhibitor on EGFR T790M mutation kinase activity is provided. [Means for Solution] The present inventors have investigated a compound having an inhibitory action on an EGFR T790M mutation kinase, and have found that a pyrazinecarboxamide compound has an inhibitory action on an EGFR T790M mutation kinase, thereby completing the present invention.
    Type: Application
    Filed: January 15, 2013
    Publication date: October 30, 2014
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Takahiro Matsuya, Yutaka Kondoh, Itsuro Shimada, Shigetoshi Kikuchi, Maiko Iida, Kenichi Onda, Hiroki Fukudome, Yukihiro Takemoto, Nobuaki Shindou, Hideki Sakagami, Hisao Hamaguchi
  • Publication number: 20140058100
    Abstract: To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Application
    Filed: July 15, 2013
    Publication date: February 27, 2014
    Applicant: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Patent number: 8486970
    Abstract: [Problems] To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). [Means for Solving Problems] It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS.
    Type: Grant
    Filed: May 26, 2008
    Date of Patent: July 16, 2013
    Assignee: Seldar Pharma Inc.
    Inventors: Hiroyuki Hisamichi, Itsuro Shimada, Tsukasa Ishihara, Tomofumi Takuwa, Takafumi Shimizu, Noriko Ishikawa, Kyoichi Maeno, Norio Seki
  • Publication number: 20130096100
    Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.
    Type: Application
    Filed: September 14, 2012
    Publication date: April 18, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Yutaka KONDOH, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano
  • Publication number: 20130059855
    Abstract: Provided are crystals of compound A which have properties suitable for industrial production. MEANS FOR SOLVING As the results of intensive studies to provide crystals of compound A having an inhibitory activity on the kinase activity of an EML4-ALK fusion protein and a mutant EGFR protein, crystals of compound A were found. Moreover, it was found that A04-type crystal of compound A, from among the aforesaid crystals of compound A, unexpectedly have preferred properties as a drug substance.
    Type: Application
    Filed: May 16, 2011
    Publication date: March 7, 2013
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Itsuro Shimada, Yutaka Hirakura, Kouji Yamazaki, Kazuhiro Takeguchi, Norihiro Ueda
  • Patent number: 8318702
    Abstract: The present invention provides a compound which is useful as an inhibitor against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. As a result of extensive and intensive studies on compounds having an inhibitory effect against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins, the inventors of the present invention have found that the di(arylamino)aryl compound of the present invention has inhibitory activity against the kinase activity of EML4-ALK fusion proteins and mutant EGFR proteins. This finding led to the completion of the present invention.
    Type: Grant
    Filed: July 4, 2008
    Date of Patent: November 27, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Yutaka Kondoh, Kazuhiko Iikubo, Sadao Kuromitsu, Nobuaki Shindo, Takatoshi Soga, Takashi Furutani, Itsuro Shimada, Takahiro Matsuya, Kazuo Kurosawa, Akio Kamikawa, Hiroyuki Mano