Patents by Inventor Toshiyuki Kusayama
Toshiyuki Kusayama 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: 8076367Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.Type: GrantFiled: March 18, 2010Date of Patent: December 13, 2011Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Isao Kinoyama, Shunichiro Matsumoto, Kei Ohnuki, Kazuyoshi Obitsu, Toshiyuki Kusayama
-
Patent number: 7960562Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.Type: GrantFiled: March 30, 2006Date of Patent: June 14, 2011Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Isao Kinoyama, Shunichiro Matsumoto, Eiji Kawaminami, Kei Ohnuki, Hirofumi Yamamoto, Kazuhiko Osoda, Tatsuhisa Takahashi, Takashi Shin, Takanori Koike, Itsuro Shimada, Hiroyuki Hisamichi, Toshiyuki Kusayama
-
Publication number: 20100173946Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.Type: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: ASTELLAS PHARMA INCInventors: Masaaki Hirano, Eiji Kawaminami, Isao Kinoyama, Shunichiro Matsumoto, Kei Ohnuki, Kazuyoshi Obitsu, Toshiyuki Kusayama
-
Patent number: 7709519Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.Type: GrantFiled: June 2, 2005Date of Patent: May 4, 2010Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Isao Kinoyama, Shunichiro Matsumoto, Kei Ohnuki, Kazuyoshi Obitsu, Toshiyuki Kusayama
-
Patent number: 7569688Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: June 20, 2005Date of Patent: August 4, 2009Assignee: Astellas Pharma Inc.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
-
Publication number: 20090181964Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.Type: ApplicationFiled: March 30, 2006Publication date: July 16, 2009Inventors: Masaaki Hirano, Isao Kinoyama, Shunichiro Matsumoto, Eiji Kawaminami, Kei Ohnuki, Hirofumi Yamamoto, Kazuhiko Osoda, Tatsuhisa Takahisa, Takashi Shin, Takanori Koike, Itsuro Shimada, Hiroyuki Hisamichi, Toshiyuki Kusayama
-
Publication number: 20090018177Abstract: Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which has benzene or thiophene ring substituted with a group derived from 1-hydroxymethyl, shows excellent availability, in addition to its excellent GnRH receptor antagonism, thereby accomplishing the invention. Since the compound of the invention shows excellent availability, in addition to its strong GnRH receptor antagonism, it can be expected that it exerts superior drug effect in the living body, and it is useful for the treatment of sex hormone dependent diseases such as prostate cancer, breast cancer, endometriosis, uterine leiomyoma, benign prostatic hypertrophy and the like.Type: ApplicationFiled: June 2, 2005Publication date: January 15, 2009Inventors: Masaaki Hirano, Eiji Kawaminami, Isao Kinoyama, Shunichiro Matsumoto, Kei Ohnuki, Kazuyoshi Obitsu, Toshiyuki Kusayama
-
Publication number: 20050267110Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: ApplicationFiled: June 20, 2005Publication date: December 1, 2005Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
-
Patent number: 6960591Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: GrantFiled: July 4, 2001Date of Patent: November 1, 2005Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama
-
Publication number: 20030191164Abstract: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.Type: ApplicationFiled: December 19, 2002Publication date: October 9, 2003Inventors: Masaaki Hirano, Eiji Kawaminami, Akira Toyoshima, Hiroyuki Moritomo, Norio Seki, Ryutaro Wakayama, Minoru Okada, Toshiyuki Kusayama