Patents by Inventor Takashi Shin
Takashi Shin 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: 9428501Abstract: Compounds of formula (I) and salts thereof: wherein the variables are defined herein, are useful for the treatment of breast cancer.Type: GrantFiled: June 9, 2014Date of Patent: August 30, 2016Assignee: Astellas Pharma Inc.Inventors: Kei Ohnuki, Hidenori Azami, Yuki Sawada, Takashi Shin, Kazuyuki Kuramoto, Shigetoshi Kikuchi, Tomoyuki Saito, Hisao Hamaguchi, Takeyuki Nagashima
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Publication number: 20150266869Abstract: [Problem] A compound which is useful as an agent for treating breast cancer is provided. [Means for Solution] As a result of intensive studies on a compound having a Complex I inhibitory effect and an AMPK activation effect, the present inventors found that a bicyclic nitrogen-containing aromatic heterocyclic amide compounds of the present invention has an excellent Complex I inhibitory effect and the AMPK activation effect, furthermore, has a cell proliferation inhibitory effect with respect to not only human PIK3CA mutation-positive breast cancer cell lines in which MCT4 is not expressed but also human breast cancer cell lines which do not have mutation of PIK3CA in which MCT4 is not expressed, and exhibits an anti-tumor effect in a human PIK3CA mutation-positive breast cancer cell line MDA-MB-453 cell in a cancer-bearing mouse in which the MCT4 is not expressed, thereby completing the present invention.Type: ApplicationFiled: June 9, 2014Publication date: September 24, 2015Applicant: ASTELLAS PHARMA INC.Inventors: Kei Ohnuki, Hidenori Azami, Yuki Sawada, Takashi Shin, Kazuyuki Kuramoto, Shigetoshi Kikuchi, Tomoyuki Saito, Hisao Hamaguchi, Takeyuki Nagashima
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Patent number: 8304547Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.Type: GrantFiled: October 23, 2008Date of Patent: November 6, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
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Patent number: 8163746Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: GrantFiled: April 19, 2007Date of Patent: April 24, 2012Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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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
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Publication number: 20100249088Abstract: [Object] To provide a therapeutic and/or prophylactic agent for urinary frequency, urinary urgency, and urinary incontinence associated with various lower urinary tract diseases including overactive bladder, various lower urinary tract diseases accompanied by lower urinary tract pain, such as interstitial cystitis, chronic prostatitis, and the like, and various diseases accompanied by pain, based on an excellent trkA receptor inhibitory action.Type: ApplicationFiled: October 23, 2008Publication date: September 30, 2010Applicant: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Nomura, Shunichiro Matsumoto, Takashi Shin, Hidenori Azami, Tomoaki Abe, Akira Suga, Ryushi Seo, Masayuki Tanahashi, Toru Watanabe
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Publication number: 20090286766Abstract: Provided is an agent for treating or preventing urinary frequency, urinary urgency and urinary, incontinence which are associated with overactive bladder, a lower urinary tract disease such as interstitial cystitis and chronic prostatitis accompanied by lower urinary tract pain, and various diseases accompanied by pain. A novel azolecarboxamide derivative in which an azole ring such as thioazole or oxazole is bonded to a benzene ring, pyridine ring or pyrimidine ring through carboxamide was confirmed to have a potent trkA receptor-inhibitory activity and found to be an agent for treating or preventing lower urinary tract disease and various diseases accompanied by pain, which is excellent in efficacy and safety, and thus the present invention was accomplished.Type: ApplicationFiled: April 19, 2007Publication date: November 19, 2009Applicant: ASTELLAS PHARMA INC.Inventors: Keizo Sugasawa, Kenichi Kawaguchi, Takaho Matsuzawa, Ryushi Seo, Hironori Harada, Akira Suga, Tomoaki Abe, Hidenori Azami, Shunichiro Matsumoto, Takashi Shin, Masayuki Tanahashi, Toru Watanabe
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Patent number: 7585886Abstract: [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).Type: GrantFiled: May 18, 2006Date of Patent: September 8, 2009Assignee: Astellas Pharma Inc.Inventors: Shunichiro Hachiya, Makoto Oku, Hana Mukai, Takashi Shin, Keisuke Matsuura, Ryushi Seo, Takashi Kamikubo, Yoh Terada, Masanao Sanagi, Kousei Yoshihara, Taisuke Takahashi
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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
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Publication number: 20090062366Abstract: [Problem] To provide a compound which may be used in treating diseases in which a calcium sensing receptor (CaSR) is concerned, particularly hyperparathyroidism. [Means for Resolution] It was found that novel pyrrolidine derivatives which are characterized by the possession of aminomethyl group substituted with arylalkyl group or the like, or salts thereof, have excellent CaSR agonistic regulatory activity and also have excellent selectivity with CYP2D6 inhibitory activity having a possibility of causing drug interaction. Based on the above, these novel pyrrolidine derivatives are useful as therapeutic agents for treating diseases in which CaSR is concerned (hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like).Type: ApplicationFiled: May 18, 2006Publication date: March 5, 2009Applicant: ASTELLAS PHARAMA INC.Inventors: Shunichiro Hachiya, Makoto Oku, Hana Mukai, Takashi Shin, Keisuke Matsuura, Ryushi Seo, Takashi Kamikubo, Yoh Terada, Masanao Sanagi, Kousei Yoshihara, Taisuke Takahashi
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Patent number: 5494812Abstract: A novel trehalase inhibitor having the following physicochemical properties:(1) Activity: a specific inhibitory activity to trehalase;(2) Form: white powder, water-soluble;(3) Somogy-Nelson test: negative(4) Rydon-Smith test: positive(5) Optical rotation [.alpha.].sub.D.sup.23 : 113.8.degree. (C, 0.1, H.sub.2 O)(6) Molecular weight: 335 ([M+H].sup.+ =336)(7) Ultraviolet absorption spectrum: 258.5 nm (max.)(8) .sup.13 C-NMR(ppm): 28.9, 41.0, 56.9, 58.4, 64.3, 65.0, 71.3, 74.0, 75.2, 75.8, 76.0, 77.1, 123.0, 144.Type: GrantFiled: July 14, 1994Date of Patent: February 27, 1996Assignee: Sawao MuraoInventors: Sawao Murao, Takashi Shin, Kyoichi Sugawa, Amachi Teruo
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Patent number: 5372816Abstract: This invention relates to the substance Trehalostatin which is a white powder soluble in water but hardly or only slightly soluble in hexane, benzene, ethers and petroleum ether, shows no absorption maxima at 220 nm or above in its ultraviolet visible light absorption spectrum, is positive in Rydon-Smith reaction and negative in nynhydrin reaction, 3,6-dinitrophthalic acid reaction and Elson-Morgan reaction, and has an RF value of 0.37 in Merck Kieselgal 50 F.sub.254 thin-layer chromatography using 3:1:2 mixture on n-butanol, acetic acid and water as a developing solvent, Rt of 11.0 minutes in YMC PA03 (0.7 .times.27 cm) high performance liquid chromatography using 65% v/v acetonitrile (in H.sub.2 O) as a solvent at a flow rate of 1.0 ml/min, a molecular weight of 366, [alpha].sub.D of +115.degree., and specific NMR spectrum.Also disclosed is a process for preparing trehalostatin and a specific strain of Amycolatopsis trehalostatica which has FERM accession number BP-2784.Type: GrantFiled: September 21, 1992Date of Patent: December 13, 1994Assignee: Suntory LimitedInventors: Sawao Murao, Takashi Shin
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Patent number: 5354685Abstract: A novel trehalase inhibitor having the following physicochemical properties:(1) Activity: a specific inhibitory activity to trehalase;(2) Form: white powder, water-soluble;(3) Somogy-Nelson test: negative(4) Rydon-Smith test: positive(5) Optical rotation [.alpha.].sub.D.sup.23 : 113.8.degree. (C, 0.1 H.sub.2 O)(6) Molecular weight: 335 ([M+H].sup.+ =336)(7) Ultraviolet absorption spectrum: 258.5 nm (max.)(8) .sup.13 C-NMR(ppm): 28.9, 41.0, 56.9, 58.4, 64.3, 65.0, 71.3, 74.0, 75.2, 75.8, 76.0, 77.1, 123.0, 144.Type: GrantFiled: March 29, 1993Date of Patent: October 11, 1994Assignee: S. MuraoInventors: Sawao Murao, Takashi Shin, Kyoichi Sugawa, Amachi Teruo
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Patent number: 5180672Abstract: An ascorbate oxidase having an optimum pH range of 3.5-4.5 is isolated from Acremonium sp. Hi-25 BP-3124. The ascorbate oxidase is used in foods or drinks to oxidize ascorbate to prevent damage to the foods or drinks by oxidation.Type: GrantFiled: February 6, 1991Date of Patent: January 19, 1993Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Homare Itoh, Takashi Shin, Takahisa Yajima, Shigeki Fukuyasu
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Patent number: 5169778Abstract: This invention relates to a substance Trehalostatin which is a white powder soluble in water but hardly or only slightly soluble in hexane, benzene, ethers and petroleum ether, shows no absorption maxima at 220 nm or above in its ultraviolet visible light absorption spectrum, is positive in Rydon-Smith reaction and negative in ninhydrin reaction, 3,6-dinitrophthalic acid reaction and Elson-Morgan reaction, has an Rf value of 0.37 in Merk Kieselgal 60 G.sub.254 thin layer chromatography using a 3:1:2 mixture of n-butanol, acetic acid and water as a developing solvent, and Rt of 11.0 minutes in YMC PA03 (0.7.times.27 cm) high performance liquid chromatography using 65% v/v acetonitrile (in H.sub.2 O) as a solvent at a flow rate of 1.0 ml/min, has a molecular weight of 366 and a specific rotatory power [.alpha.].sub.D of +115.degree., and presents an NMR spectrum described below:H-NMR/D.sub.2 O 3.3 (ppm), dd, 1H, 3.5 (ppm), m, 1H, 3.5 (ppm), t, 1H, 3.6 (ppm), d, 1H, 3.6 (ppm), d, 1H, 3.7 (ppm), d, 1H, 3.Type: GrantFiled: December 6, 1990Date of Patent: December 8, 1992Assignee: Sawao MuraoInventors: Sawao Murao, Takashi Shin