Patents by Inventor Akihiro ISHIHATA
Akihiro ISHIHATA 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: 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: 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: 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: 10023583Abstract: 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-(bi-cyclic 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.Type: GrantFiled: November 27, 2015Date of Patent: July 17, 2018Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi Kawaguchi, Akihiro Ishihata, Akira Kanai, Yusuke Inagaki, 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: 20180022755Abstract: 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-(bi-cyclic 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.Type: ApplicationFiled: November 27, 2015Publication date: January 25, 2018Applicants: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Kenichi KAWAGUCHI, Akihiro ISHIHATA, Akira KANAI, Yusuke INAGAKI, 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