Patents by Inventor Isamu Shiina
Isamu Shiina 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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Publication number: 20240140918Abstract: A compound represented by formula (1) below, useful for treating cancer. In the formula, R1 and R3-R8 each independently represents a hydrogen atom or an alkyl group, R2 represents a hydrogen atom or a group represented by —ORa, R9 represents a group represented by —C(O)NRcRf, Ra, Re, and Rf each independently represents a hydrogen atom, an arylalkyl group that may have a substituent, or a heteroarylalkyl group.Type: ApplicationFiled: January 28, 2022Publication date: May 2, 2024Inventors: Isamu SHIINA, Motoyuki SHIMONAKA, Takatsugu MURATA, Yuuki OBATA, Toshirou NISHIDA, Koji OKAMOTO
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Patent number: 10696703Abstract: Provided are: eushearilides; a method for producing eushearilides; a production intermediate; and a pharmaceutical composition containing eushearilides. By having the Wittig reaction process, Mukaiyama Aldol reaction process and Macrolactonizaion process serve as key processes, eushearilides represented by formula (I) are efficiently produced.Type: GrantFiled: October 28, 2015Date of Patent: June 30, 2020Assignee: TOKYO UNIVERSITY OF SCIENCE FOUNDATIONInventors: Isamu Shiina, Takayuki Tonoi
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Publication number: 20190382425Abstract: Provided are: eushearilides; a method for producing eushearilides; a production intermediate; and a pharmaceutical composition containing eushearilides. By having the Wittig reaction process, Mukaiyama Aldol reaction process and Macrolactonizaion process serve as key processes, eushearilides represented by formula (I) are efficiently produced.Type: ApplicationFiled: October 28, 2015Publication date: December 19, 2019Inventors: Isamu SHIINA, Takayuki TONOI
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Patent number: 9796640Abstract: Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an ?-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.Type: GrantFiled: February 2, 2015Date of Patent: October 24, 2017Assignee: TOKYO UNIVERSITY OF SCIENCE FOUNDATIONInventor: Isamu Shiina
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Publication number: 20170008820Abstract: Provided is a method for producing an optically active carboxylic acid ester at a high yield and with high enantioselectivity using dynamic kinetic resolution, said optically active carboxylic acid ester having an ?-nitrogen substituent. This method for producing an optically active carboxylic acid ester includes a step in which racemic carboxylic acid represented by formula (a) and a specific alcohol or phenol derivative are reacted in a polar solvent having a dipole moment of at least 3.5 in the presence of an acid anhydride and an asymmetric catalyst, one enantiomer of the racemic carboxylic acid is selectively esterified, and the other enantiomer is racemized. In formula (a), Ra1 represents a nitrogen-containing heteroaromatic ring group bonded to an assymetric carbon via a nitrogen atom constituting a ring, and Ra2 is an organic group.Type: ApplicationFiled: February 2, 2015Publication date: January 12, 2017Inventor: Isamu SHIINA
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Patent number: 9315442Abstract: A method that manufacturers an optically active carboxylic acid ester at high yield and high enantioselectivity is provided. An optically active carboxylic acid ester is manufactured at high yield and high enantioselectivity by reacting a racemic carboxylic acid and a specific alcohol or phenol derivatives in a polar solvent having a dipole moment of 3.0 or higher in the presence of an acid anhydride and an asymmetric catalyst, esterifying one enantiomer of the racemic carboxylic acid at high selectivity, and increasing the amount of esterified carboxylic acid by racemizing the optically active carboxylic acid which is the other enantiomer not used in esterification.Type: GrantFiled: June 7, 2012Date of Patent: April 19, 2016Assignee: TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION ADMINISTRATIVE ORGANIZATIONInventors: Isamu Shiina, Kenya Nakata, Keisuke Ono
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Publication number: 20140135520Abstract: A method that manufacturers an optically active carboxylic acid ester at high yield and high enantioselectivity is provided. An optically active carboxylic acid ester is manufactured at high yield and high enantioselectivity by reacting a racemic carboxylic acid and a specific alcohol or phenol derivatives in a polar solvent having a dipole moment of 3.0 or higher in the presence of an acid anhydride and an asymmetric catalyst, esterifying one enantiomer of the racemic carboxylic acid at high selectivity, and increasing the amount of esterified carboxylic acid by racemizing the optically active carboxylic acid which is the other enantiomer not used in esterification.Type: ApplicationFiled: June 7, 2012Publication date: May 15, 2014Applicant: Tokyo University of Science Educational Foundation Administration OrganizationInventors: Isamu Shiina, Kenya Nakata, Keisuke Ono
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Patent number: 8552215Abstract: Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.Type: GrantFiled: March 8, 2010Date of Patent: October 8, 2013Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Isamu Shiina, Kenya Nakata
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Patent number: 8193394Abstract: Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.Type: GrantFiled: January 25, 2007Date of Patent: June 5, 2012Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Isamu Shiina, Yoshiyuki Sano, Kenya Nakata
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Patent number: 8183235Abstract: Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent.Type: GrantFiled: September 11, 2008Date of Patent: May 22, 2012Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventor: Isamu Shiina
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Patent number: 8115008Abstract: Disclosed is a method for producing an optically active ester by highly selectively esterifying one enantiomer of a racemic carboxylic acid, while producing an optically active carboxylic acid which is the other enantiomer. An optically active ester is produced while producing an optically active carboxylic acid at the same time by reacting a racemic carboxylic acid with a specific alcohol or phenol derivative in the presence of benzoic anhydride or a derivative thereof and a catalyst such as tetramisole or benzotetramisole, thereby selectively esterifying one enantiomer of the racemic carboxylic acid.Type: GrantFiled: March 4, 2009Date of Patent: February 14, 2012Assignee: Tokyo University of Science Education Foundation Administrative OrganizationInventors: Isamu Shiina, Kenya Nakata
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Publication number: 20110319650Abstract: Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.Type: ApplicationFiled: March 8, 2010Publication date: December 29, 2011Applicant: Tokyo University of Science Educational Foundation Administrative OrganizationInventors: Isamu Shiina, Kenya Nakata
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Patent number: 8034947Abstract: The invention relates to a pyridine oxide compound represented by formula (I), an optically active compound thereof, a salt thereof and a hydrate thereof, and, in the presence of the compound as a catalyst, performing 1) a method for producing an ester compound or an amide compound from a carboxylic acid equivalent and an alcohol or an amine, 2) an asymmetric esterification reaction or 3) an asymmetric amidation reaction.Type: GrantFiled: February 17, 2006Date of Patent: October 11, 2011Assignee: Tokyo University of Science Educational Foundation Administrative OrganizationInventor: Isamu Shiina
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Publication number: 20100249400Abstract: Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent.Type: ApplicationFiled: September 11, 2008Publication date: September 30, 2010Applicant: Tokyo University of Science Educational Foundation Administrative OrganizationInventor: Isamu Shiina
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Publication number: 20100234610Abstract: Disclosed is a method for producing an optically active ester by highly selectively esterifying one enantiomer of a racemic carboxylic acid, while producing an optically active carboxylic acid which is the other enantiomer. An optically active ester is produced while producing an optically active carboxylic acid at the same time by reacting a racemic carboxylic acid with a specific alcohol or phenol derivative in the presence of benzoic anhydride or a derivative thereof and a catalyst such as tetramisole or benzotetramisole, thereby selectively esterifying one enantiomer of the racemic carboxylic acid.Type: ApplicationFiled: March 4, 2009Publication date: September 16, 2010Inventors: Isamu Shiina, Kenya Nakata
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Publication number: 20090062548Abstract: The invention relates to a pyridine oxide compound represented by formula (I), an optically active compound thereof, a salt thereof and a hydrate thereof, and, in the presence of the compound as a catalyst, performing 1) a method for producing an ester compound or an amide compound from a carboxylic acid equivalent and an alcohol or an amine, 2) an asymmetric esterification reaction or 3) an asymmetric amidation reaction.Type: ApplicationFiled: February 17, 2006Publication date: March 5, 2009Inventor: Isamu Shiina
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Publication number: 20090012314Abstract: Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.Type: ApplicationFiled: January 25, 2007Publication date: January 8, 2009Applicant: TOKYO UNIVERSITY OF SCIENCE EDUCATIONAL FOUNDATION ADMINISTRATIVE ORGANIZATIONInventors: Isamu Shiina, Yoshiyuki Sano, Kenya Nakata