Patents by Inventor Kazuyuki Tsuchiya
Kazuyuki Tsuchiya 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).
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Patent number: 11981644Abstract: Provided herein are compounds of formula (1): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X1, X2, Ry, Rz, R1, R2, R3, and R4 are as defined herein. Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided herein are methods of using a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to treat various diseases, disorders, and conditions responsive to the modulation of the contractility of the skeletal sarcomere.Type: GrantFiled: November 5, 2021Date of Patent: May 14, 2024Assignee: CYTOKINETICS, INC.Inventors: Bradley P. Morgan, Chris Evans, Pu-Ping Lu, Makoto Yamasaki, Wenyue Wang, Scott Collibee, Takuya Makino, Kazuyuki Tsuchiya, Toshio Kurosaki, Susumu Yamaki, Eriko Honjo, Yuka Koizumi, Naoto Katoh, Ryuichi Sekioka, Ikumi Kuriwaki
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Publication number: 20230083960Abstract: Provided herein are compounds of formula (I): or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein X1, X2, Ry, Rz, R1, R2, R3, and R4 are as defined herein. Also provided herein is a pharmaceutically acceptable composition comprising a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing. Also provided herein are methods of using a compound of formula (I), or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, to treat various diseases, disorders, and conditions responsive to the modulation of the contractility of the skeletal sarcomere.Type: ApplicationFiled: November 5, 2021Publication date: March 16, 2023Inventors: Bradley P. MORGAN, Chris Evans, Pu-Ping Lu, Makoto Yamasaki, Wenyue Wang, Scott Collibee, Takuya Makino, Kazuyuki Tsuchiya, Toshio Kurosaki, Susumu Yamaki, Eriko Honjo, Yuka Koizumi, Naoto Katoh, Ryuichi Sekioka, Ikumi Kuriwaki, Denise Andersen
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Patent number: 10975091Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: GrantFiled: August 19, 2019Date of Patent: April 13, 2021Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Yusuke Inagaki, Kazuyuki Tsuchiya, Tadaatsu Hanadate, Akira Kanai, Hiroyuki Kaizawa, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
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Publication number: 20200055868Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: ApplicationFiled: August 19, 2019Publication date: February 20, 2020Applicants: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi KAWAGUCHI, Akihiro ISHIHATA, Yusuke INAGAKI, Kazuyuki TSUCHIYA, Tadaatsu HANADATE, Akira KANAI, Hiroyuki KAIZAWA, Junichi KAZAMI, Hiroshi MORIKAWA, Masashi HIRAMOTO, Kentaro ENJO, Hajime TAKAMATSU
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Patent number: 10532979Abstract: Phenyldifluoromethyl-substituted prolinamide compounds that have a cathepsin S inhibitory effect, and are usable as active ingredients of pharmaceutical compositions for preventing and/or treating autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue.Type: GrantFiled: April 25, 2019Date of Patent: January 14, 2020Assignee: ASTELLAS PHARMA INC.Inventors: Yutaka Nakajima, Sunao Imada, Eriko Yamamoto, Kazuyuki Tsuchiya, Yu Harayama, Shunichiro Matsumoto
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Patent number: 10421762Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: GrantFiled: July 20, 2018Date of Patent: September 24, 2019Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Yusuke Inagaki, Kazuyuki Tsuchiya, Tadaatsu Hanadate, Akira Kanai, Hiroyuki Kaizawa, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
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Publication number: 20190248738Abstract: Phenyldifluoromethyl-substituted prolinamide compounds that have a cathepsin S inhibitory effect, and are usable as active ingredients of pharmaceutical compositions for preventing and/or treating autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue.Type: ApplicationFiled: April 25, 2019Publication date: August 15, 2019Applicant: Astellas Pharma Inc.Inventors: Yutaka Nakajima, Sunao Imada, Eriko Yamamoto, Kazuyuki Tsuchiya, Yu Harayama, Shunichiro Matsumoto
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Patent number: 10322997Abstract: Phenyldifluoromethyl-substituted prolinamide compounds that have a cathepsin S inhibitory effect, and are usable as active ingredients of pharmaceutical compositions for preventing and/or treating autoimmune diseases including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue.Type: GrantFiled: November 5, 2018Date of Patent: June 18, 2019Assignee: ASTELLAS PHARMA INC.Inventors: Yutaka Nakajima, Sunao Imada, Eriko Yamamoto, Kazuyuki Tsuchiya, Yu Harayama, Shunichiro Matsumoto
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Publication number: 20190071398Abstract: [Problem] To provide a compound useful as a cathepsin S inhibitor. [Means for Solution] The present inventors have examined a compound that has a cathepsin S inhibitory effect and is usable as an active ingredient of a pharmaceutical composition for preventing and/or treating autoimmune disease including systemic lupus erythematosus (SLE) and lupus nephritis, allergies, or graft rejection of an organ, bone marrow or tissue, and have found that a phenyldifluoromethyl-substituted prolinamide compound of the present invention has the cathepsin S inhibitory effect, thereby completing the present invention. The phenyldifluoromethyl-substituted prolinamide compound of the present invention has the cathepsin S inhibitory effect and is useful as an agent for preventing and/or treating autoimmune disease including SLE and nephritis, allergies, or graft rejection of an organ, bone marrow or tissue.Type: ApplicationFiled: November 5, 2018Publication date: March 7, 2019Applicant: ASTELLAS PHARMA INC.Inventors: Yutaka NAKAJIMA, Sunao IMADA, Eriko YAMAMOTO, Kazuyuki TSUCHIYA, Yu HARAYAMA, Shunichiro MATSUMOTO
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Publication number: 20180327418Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: ApplicationFiled: July 20, 2018Publication date: November 15, 2018Applicants: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi KAWAGUCHI, Akihiro ISHIHATA, Yusuke INAGAKI, Kazuyuki TSUCHIYA, Tadaatsu HANADATE, Akira KANAI, Hiroyuki KAIZAWA, Junichi KAZAMI, Hiroshi MORIKAWA, Masashi HIRAMOTO, Kentaro ENJO, Hajime TAKAMATSU
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Patent number: 10059720Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: GrantFiled: May 28, 2015Date of Patent: August 28, 2018Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICALS CO., LTD.Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Yusuke Inagaki, Kazuyuki Tsuchiya, Tadaatsu Hanadate, Akira Kanai, Hiroyuki Kaizawa, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
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Patent number: 10005762Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.Type: GrantFiled: December 4, 2015Date of Patent: June 26, 2018Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Akira Kanai, Kazuyuki Tsuchiya, Yusuke Inagaki, Junichi Kazami, Hiroshi Morikawa, Masashi Hiramoto, Kentaro Enjo, Hajime Takamatsu
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Publication number: 20170362209Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically an agent for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.Type: ApplicationFiled: December 4, 2015Publication date: December 21, 2017Applicants: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi KAWAGUCHI, Akihiro ISHIHATA, Akira KANAI, Kazuyuki TSUCHIYA, Yusuke INAGAKI, Junichi KAZAMI, Hiroshi MORIKAWA, Masashi HIRAMOTO, Kentaro ENJO, Hajime TAKAMATSU
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Publication number: 20170190715Abstract: The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia. The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and/or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-{[4-(substituted pyridine)-2-yl]methyl}-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production.Type: ApplicationFiled: May 28, 2015Publication date: July 6, 2017Applicants: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Kenichi KAWAGUCHI, Akihiro ISHIHATA, Yusuke INAGAKI, Kazuyuki TSUCHIYA, Tadaatsu HANADATE, Akira KANAI, Hiroyuki KAIZAWA, Junichi KAZAMI, Hiroshi MORIKAWA, Masashi HIRAMOTO, Kentaro ENJO, Hajime TAKAMATSU
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Patent number: 8901126Abstract: Substituted imidazo[1,5-a]quinoxalin-4-one compounds of formula (I) described herein exhibit PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hirofumi Yamamoto, Kazunori Kamijo, Kazuyuki Tsuchiya, Ryushi Seo, Satoshi Yamamoto
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Patent number: 8674096Abstract: Substituted imidazo[1,5-a]quinoxalin-4-ones are useful as phosphodiesterase 9 inhibitors.Type: GrantFiled: November 27, 2012Date of Patent: March 18, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
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Publication number: 20130296329Abstract: The present inventors have investigated a compound which has a PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibitory action, thereby completing the present invention.Type: ApplicationFiled: March 7, 2013Publication date: November 7, 2013Inventors: Hiroyuki KAIZAWA, Mari SUGITA, Hirofumi YAMAMOTO, Kazunori KAMIJO, Kazuyuki TSUCHIYA, Ryushi SEO, Satoshi YAMAMOTO
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Patent number: 8357688Abstract: Substituted imidazo[1,5-a]quinoxalin-4(5H)-ones are useful as PDE9 inhibitors.Type: GrantFiled: March 4, 2010Date of Patent: January 22, 2013Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
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Publication number: 20110319385Abstract: [Problem] Provided is a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like. [Means for Solution] The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibiting action, thereby completing the present invention. The imidazoquinoxaline compound or the triazoloquinoxaline compound of the present invention has a PDE9-inhibiting action and can be used as an agent for preventing and/or treating storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like.Type: ApplicationFiled: March 4, 2010Publication date: December 29, 2011Applicant: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Mari Sugita, Hidenori Azami, Ryushi Seo, Takaho Nomura, Satoshi Yamamoto, Hirofumi Yamamoto, Kazuyuki Tsuchiya, Hideki Kubota, Kazunori Kamijo
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Publication number: 20100267775Abstract: A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.Type: ApplicationFiled: October 22, 2008Publication date: October 21, 2010Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Kazuyuki Tsuchiya, Kazuyuki Kuramoto, Shigeru Yoshida, Takatoshi Soga