Patents by Inventor Kentaro Enjo
Kentaro Enjo 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: 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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
Patent number: 8513422Abstract: As a result of studies on compounds having a selective inhibitory activity against 17?HSD type 5, the present inventors have confirmed that a {1-[(indol-2-yl)carbonyl]piperidyl}alkanol derivative has a potent selective inhibitory activity against 17?HSD type 5. The invention has been completed based on these findings. The compound of the present invention can be used as an agent for treating and/or an agent for preventing diseases associated with 17?HSD type 5, such as benign prostatic hyperplasia and prostate cancer, without accompanying adverse effects due to a decrease in testosterone.Type: GrantFiled: August 28, 2008Date of Patent: August 20, 2013Assignee: Astellas Pharma Inc.Inventors: Akio Kakefuda, Kazushi Watanabe, Akio Kamikawa, Kentaro Enjo, Takashi Furutani, Minoru Yasuda
-
Publication number: 20110282066Abstract: [Object] A screening method for a compound which is useful as an agent for treating 17?HSD type 5-related diseases and/or an agent for treating 17?HSD type 5-related cancer such as prostate cancer is provided. [Means for Solution] The present invention has been completed by establishing a screening method for a compound which is useful for treating 17?HSD type 5-related diseases, by manifesting a tumor by transplanting tumor cells to, for example, an immunodeficient mouse, topically administering a steroid which is a biosynthetic substance for a hormone into the tumor, and measuring the level of a hormone produced in the tumor.Type: ApplicationFiled: January 26, 2010Publication date: November 17, 2011Inventors: Takashi Furutani, Kentaro Enjo, Aya Kikuchi, Sadao Kuromitsu, Yukitaka Ideyama, Tomoyuki Suzuki, Ryoko Kurihara
-
Publication number: 20110071146Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: ApplicationFiled: November 10, 2010Publication date: March 24, 2011Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
-
Patent number: 7855225Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: GrantFiled: March 1, 2007Date of Patent: December 21, 2010Assignee: Astellas Pharma Inc.Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
-
Publication number: 20100190826Abstract: Provided is a novel and excellent method for treating and/or preventing benign prostatic hyperplasia, prostate cancer, and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an indole or benzimidazole derivative, where a nitrogen atom of the indole ring or benzimidazole ring is substituted with a phenyl group substituted with COOH, has a potent selective inhibitory activity against 17?HSD type 5 and may become an agent for treating and/or an agent for preventing a disease associated with 17?HSD type 5, such as benign prostatic hyperplasia, prostate cancer and the like, without accompanying adverse effects due to a decrease in testosterone; and the present invention has thus been completed.Type: ApplicationFiled: July 23, 2008Publication date: July 29, 2010Inventors: Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano, Akio Kamikawa, Kentaro Enjo, Takashi Furutani
-
Publication number: 20090181960Abstract: To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17?HSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17?HSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone, and the present invention has thus been completed.Type: ApplicationFiled: March 1, 2007Publication date: July 16, 2009Inventors: Tatsuya Niimi, Akio Kamikawa, Yasushi Amano, Tomohiko Yamaguchi, Kenichi Suzumura, Kentaro Enjo, Takashi Furutani, Akio Kakefuda, Yutaka Kondoh, Masaaki Hirano
-
Publication number: 20050233304Abstract: A screening tool and a convenient screening method for obtaining a renal failure treating agent, and a pharmaceutical composition for treating renal failure and a production method thereof are disclosed. The aforementioned screening tool is a G protein coupling type receptor FGK which is a polypeptide capable of activating CTGF promoter, a functionally equivalent modified substance thereof or a homologous polypeptide, or a cell expressing the aforementioned polypeptide. The screening method is a method which employs inhibition of the aforementioned polypeptide as the index.Type: ApplicationFiled: October 9, 2003Publication date: October 20, 2005Applicant: YAMANOUCHI PHARMACEUTICAL CO., LTD.Inventors: Kentaro Enjo, Sadao Kuromitsu