Patents Assigned to Kotobuki Pharmaceutical Co., Ltd.
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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
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Publication number: 20170152232Abstract: As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: ApplicationFiled: September 27, 2016Publication date: June 1, 2017Applicants: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Minoru KAMEDA, Ikumi KURIWAKI, Kazuhiko IIKUBO, Hiroyuki HISAMICHI, Yuichiro KAWAMOTO, Hiroyuki MORITOMO, Tomoyuki SUZUKI, Takashi FUTAMI, Atsushi SUZUKI, Kazuhisa TSUNOYAMA, Makoto ASAUMI, Hiroshi TOMIYAMA, Atsushi NODA, Yoshinori IWAI, Kazuo TOKUZAKI, Haruki OKADA, Kozo MIYASAKA
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Patent number: 9487491Abstract: 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: GrantFiled: August 29, 2014Date of Patent: November 8, 2016Assignees: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
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Patent number: 9464077Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: GrantFiled: February 26, 2013Date of Patent: October 11, 2016Assignees: Astellas Pharma Inc., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Minoru Kameda, Ikumi Kuriwaki, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Hiroyuki Moritomo, Tomoyuki Suzuki, Takashi Futami, Atsushi Suzuki, Kazuhisa Tsunoyama, Makoto Asaumi, Hiroshi Tomiyama, Atsushi Noda, Yoshinori Iwai, Kazuo Tokuzaki, Haruki Okada, Kozo Miyasaka
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Patent number: 8969336Abstract: 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: GrantFiled: May 6, 2010Date of Patent: March 3, 2015Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Itsuro Shimada, Kazuo Kurosawa, Takahiro Matsuya, Kazuhiko Iikubo, Yutaka Kondoh, Akio Kamikawa, Hiroshi Tomiyama, Yoshinori Iwai
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Publication number: 20140371196Abstract: 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: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicants: ASTELLAS PHARMA INC., KOTOBUKI PHARMACEUTICAL CO., LTD.Inventors: Itsuro SHIMADA, Kazuo KUROSAWA, Takahiro MATSUYA, Kazuhiko IIKUBO, Yutaka KONDOH, Akio KAMIKAWA, Hiroshi TOMIYAMA, Yoshinori IWAI
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Publication number: 20140142084Abstract: Provided is a compound useful as a prophylactic and/or therapeutic agent for bladder cancer. As a result of studies on compounds having FGFR inhibitory action, the present inventors have found that the nitrogen-containing aromatic heterocyclic compounds of the present invention have inhibitory action on FGFR1, FGFR2, and/or FGFR3, particularly, mutant FGFR3, and thus, the present invention has been accomplished. The nitrogen-containing aromatic heterocyclic compound of the present invention can be used as a therapeutic agent for various cancers related to FGFR1, FGFR2, and/or FGFR3, such as lung cancer and hormone therapy-resistant breast cancer, stomach cancer, triple negative breast cancer, endometrial cancer, bladder cancer, and glioblastoma, particularly as a prophylactic and/or therapeutic agent for mutant FGFR3-positive bladder cancer.Type: ApplicationFiled: February 26, 2013Publication date: May 22, 2014Applicants: KOTOBUKI PHARMACEUTICAL CO., LTD., Astellas Pharma Inc.Inventors: Minoru Kameda, Ikumi Kuriwaki, Kazuhiko Iikubo, Hiroyuki Hisamichi, Yuichiro Kawamoto, Hiroyuki Moritomo, Tomoyuki Suzuki, Takashi Futami, Atsushi Suzuki, Kazuhisa Tsunoyama, Makoto Asaumi, Hiroshi Tomiyama, Atsushi Noda, Yoshinori Iwai, Kazuo Tokuzaki, Haruki Okada, Kozo Miyasaka
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Patent number: 8198464Abstract: The present invention provides a method for producing a C-glycoside derivative, which can produce the C-glycoside derivative at a high yield and at a low cost, which conforms to environmental protection, and which is applicable industrially. The C-glycoside derivative is useful for treating and preventing diabetes such as insulin-dependent diabetes (type 1 diabetes), non-insulin-dependent diabetes (type 2 diabetes) and the like and various diabetes-related diseases including insulin-resistant diseases and obesity.Type: GrantFiled: December 20, 2007Date of Patent: June 12, 2012Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Kousuke Komenoi, Atsushi Nakamura, Makoto Kasai, Masakazu Imamura, Ryota Shiraki, Keita Nakanishi
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Patent number: 8097592Abstract: A cocrystal of (1S)-1,5-anhydro-1-[3-(1-benzothien-2-ylmethyl)-4-fluorophenyl]-D-glucitol and L-proline. It is a cocrystal of known compound A, which has a constant quality, is superior in storage stability, has no moisture absorptivity, and is suitable as a crystal of a drug substance used for preparing pharmaceuticals.Type: GrantFiled: April 4, 2007Date of Patent: January 17, 2012Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co. Ltd.Inventors: Masakazu Imamura, Keita Nakanishi, Ryota Shiraki, Kenichi Onda, Daisuke Sasuga, Masamichi Yuda
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Patent number: 8044206Abstract: The invention provides a novel nitrogen-containing heterocyclic derivative having 2,6-disubstituted styryl and a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the nitrogen-containing heterocyclic derivative and a pharmaceutically acceptable salt thereof, in particular, a pharmaceutical composition effective as a sodium channel inhibitor, having an excellent analgesic action especially on neuropathic pain with minimized side effects.Type: GrantFiled: March 5, 2004Date of Patent: October 25, 2011Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Kazumi Kikuchi, Makoto Oku, Jiro Fujiyasu, Norio Asai, Toshihiro Watanabe, Yukinori Nagakura, Hiroshi Tomiyama, Motoharu Sonegawa, Kazuo Tokuzaki, Yoshinori Iwai
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Patent number: 7977466Abstract: The present invention provides C-glycoside derivatives and salts thereof, wherein B ring is bonded to A ring via —X— and A ring is directly bonded to the glucose residue, and it is usable as a Na+-glucose cotransporter inhibitor, especially for a therapeutic and/or preventive agent for diabetes such as insulin-dependent diabetes (type 1 diabetes) and insulin-independent diabetes (type 2 diabetes), as well as diabetes related diseases such as an insulin-resistant diseases and obesity.Type: GrantFiled: July 15, 2008Date of Patent: July 12, 2011Assignees: Astellas Pharma Inc., Kotobuki Pharmaceutical Co., Ltd.Inventors: Masakazu Imamura, Takeshi Murakami, Ryota Shiraki, Kazuhiro Ikegai, Takashi Sugane, Fumiyoshi Iwasaki, Eiji Kurosaki, Hiroshi Tomiyama, Atsushi Noda, Kayoko Kitta, Yoshinori Kobayashi