Patents by Inventor Masaji Ishiguro
Masaji Ishiguro 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: 9069700Abstract: The present invention provides a method for constructing a three-dimensional structural model of an activated intermediate of a G protein-coupled protein receptor (GPCR) or a complex between a GPCR and a ligand. The three-dimensional structural model may be used to identify, screen, search, evaluate, or design GPCR agonists or antagonists. In a representative embodiment, a three-dimensional structural model of a photoactivated intermediate of rhodopsin is constructed using molecule modeling software and structural coordinates of the crystal structure of rhodopsin. The three-dimensional structural model of rhodopsin is subsequently used to construct structural models of activated intermediates of other GPCRs.Type: GrantFiled: December 3, 2012Date of Patent: June 30, 2015Assignee: SUNTORY HOLDINGS LIMITEDInventor: Masaji Ishiguro
-
Publication number: 20140025345Abstract: The present invention provides a method for constructing a three-dimensional structural model of an activated intermediate of a G protein-coupled protein receptor (GPCR) or a complex between a GPCR and a ligand. The three-dimensional structural model may be used to identify, screen, search, evaluate, or design GPCR agonists or antagonists. In a representative embodiment, a three-dimensional structural model of a photoactivated intermediate of rhodopsin is constructed using molecule modeling software and structural coordinates of the crystal structure of rhodopsin. The three-dimensional structural model of rhodopsin is subsequently used to construct structural models of activated intermediates of other GPCRs.Type: ApplicationFiled: December 3, 2012Publication date: January 23, 2014Inventor: Masaji ISHIGURO
-
Patent number: 8318781Abstract: Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I).Type: GrantFiled: April 25, 2008Date of Patent: November 27, 2012Assignees: Japan Science and Technology Agency, Kyoto University, Nagoya City UniversityInventors: Gozoh Tsujimoto, Akira Hirasawa, Naoki Miyata, Takayoshi Suzuki, Yoshiyuki Takahara, Masaji Ishiguro, Mie Hata
-
Publication number: 20110184031Abstract: Disclosed is a novel aralkyl carboxylic acid compound which has an agonistic activity on GPR-120 and/or GPR-40, particularly GPR-120, and is therefore useful as an appetite regulator, an anti-obesity agent, a therapeutic agent for diabetes, a pancreatic beta differentiating cell growth enhancer, a therapeutic agent for metabolic syndrome, a therapeutic agent for a gastrointestinal disease, a therapeutic agent for a neuropathy, a therapeutic agent for a mental disorder, a therapeutic agent for a pulmonary disease, a therapeutic agent for a pituitary hormone secretion disorder or a lipid flavoring/seasoning agent. The aralkyl carboxylic acid compound is represented by the general formula (I).Type: ApplicationFiled: April 25, 2008Publication date: July 28, 2011Inventors: Gozoh Tsujimoto, Akira Hirasawa, Naoki Miyata, Takayoshi Suzuki, Yoshiyuki Takahara, Masaji Ishiguro, Yoshie Hata
-
Publication number: 20070010948Abstract: The present invention provides a method for constructing a structural model of a complex that a G protein-coupled protein receptor forms with a ligand capable of binding the G protein-coupled receptor and a three-dimensional structural model of an activated intermediate in the structural model of the complex. The present invention also provides a method for identifying, screening for, searching for, evaluating, or designing a ligand capable of binding a GPCR by using the three-dimensional model. In one specific method by the present invention, a three-dimensional structural model of a photoactivated intermediate of rhodopsin is constructed by using a molecule modeling software and by using the three-dimensional structural coordinate of the crystal structure of rhodopsin in such a manner that amino acid residues highly conserved among GPCRs are taken into consideration.Type: ApplicationFiled: April 1, 2002Publication date: January 11, 2007Inventor: Masaji Ishiguro
-
Patent number: 6867297Abstract: An azetidinone derivative represented by the general formula (1) (wherein OR1 is a protected hydroxyl group; R2 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group or a substituted or unsubstituted aromatic group) is reacted with an ester compound represented by the formula (2) (wherein CO2R3 is an esterified carboxyl group; X and Y are the same or different and represent individually a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted alkyloxy group, a substituted or unsubstituted alkenyloxy group, a substituted or unsubstituted aralkyloxy group, a substituted or unsubstituted aryloxy group, a substituted or unsubsType: GrantFiled: October 26, 1998Date of Patent: March 15, 2005Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Masaji Ishiguro, Takashi Nakatsuka, Rie Tanaka, Tetsuo Shimamoto, Takuro Yoshida
-
Publication number: 20050004092Abstract: A penem derivative represented by the following formula (I): wherein R1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof. The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA.Type: ApplicationFiled: April 26, 2004Publication date: January 6, 2005Applicant: DAIICHI SUNTORY PHARMA CO., LTD.Inventors: Masaji Ishiguro, Takashi Nakatsuka, Rie Tanaka, Koshi Namikawa, Shinsuke Matsuki
-
Patent number: 6051569Abstract: A carbapenem derivative represented by the following formula (I), ##STR1## wherein R.sub.1 represents a hydrogen atom, a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, R.sub.2 indicates a hydrogen atom or a protective group for a carboxyl group, and R.sub.3 is a methyl group or an ethyl group; or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising this carbapenem derivative or a salt thereof as an active ingredient. The carbapenem derivative exhibits a wide and strong antimicrobial activity, particularly a strong antimicrobial activity against MRSA. An intermediate compound for preparing the carbapenem derivative is also disclosed.Type: GrantFiled: August 15, 1997Date of Patent: April 18, 2000Assignee: Suntory LimitedInventors: Masaji Ishiguro, Takashi Nakatsuka, Hidekazu Inoue
-
Patent number: 6049009Abstract: A method for producing an optically active trans-vinylsulfide alcohol having the formula: ##STR1## wherein R.sup.1 represents an alkyl group or an aryl group, comprising the step of reducing a trans-vinylsulfide ketone with a borane reducing agent in the presence of an optically active oxazaborolidine and an additive.Type: GrantFiled: June 30, 1997Date of Patent: April 11, 2000Assignee: Suntory LimitedInventors: Kazuto Sekiuchi, Masahiro Imoto, Masaji Ishiguro, Takashi Nakatsuka, Rie Tanaka, Hidekazu Inoue
-
Patent number: 5885981Abstract: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R.sub.1 is a hydrogen atom or linear or branched C.sub.1 --C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.Type: GrantFiled: June 6, 1995Date of Patent: March 23, 1999Assignee: Suntory LimitedInventors: Hiromitsu Iwata, Takashi Nakatsuka, Rie Tanaka, Masaji Ishiguro
-
Patent number: 5830889Abstract: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R.sub.1 is a linear or branched C.sub.1 -C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.Type: GrantFiled: February 19, 1993Date of Patent: November 3, 1998Assignee: Suntory LimitedInventors: Hiromitsu Iwata, Takashi Nakatsuka, Rie Tanaka, Masaji Ishiguro
-
Patent number: 5821362Abstract: Method of desilylating a silylether compound by reacting a silylether compound of the general formula (I): ##STR1## or a salt thereof with an amine hydrogen fluoride salt or a pyridine hydrogen fluoride salt in an organic solvent to produce a compound of the general formula (IV): ##STR2## According to this method, silylether compounds that are labile under strong acidic or basic conditions can be desilylated efficiently using inexpensive reagents.Type: GrantFiled: December 27, 1995Date of Patent: October 13, 1998Assignee: Suntory LimitedInventors: Akira Kaneko, Tsutomu Kaku, Masaji Ishiguro, Takashi Nakatsuka
-
Patent number: 5703068Abstract: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the following formula: ##STR2## in which R.sub.1 is a linear or branched, C.sub.1 -C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1 or 2, and R.sub.3 represents a specific substituted or unsubstituted alkyl, aryl or aralkyl group. Antibiotic compositions for oral administration are also described.Type: GrantFiled: February 19, 1993Date of Patent: December 30, 1997Assignee: Suntory LimitedInventors: Hiromitsu Iwata, Takashi Nakatsuka, Rie Tanaka, Masaji Ishiguro
-
Patent number: 5506225Abstract: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a physiological-hydrolyzable, ester-forming group. The physiologically hydrolyzable, ester-forming group useful in the penem compound of the present invention means a group which can be removed easily by in vivo hydrolysis, such as an acetyloxymethyl, 1-(acetyloxy)ethyl, pivaloyloxymethyl, 1-(ethoxycarbonyloxy)ethyl, 1-(isopropyloxycarbonyloxy)ethyl, 1-(cyclohexyloxycarbonyloxy)ethyl or 3-phthalidyl group. Antibiotic compositions for oral administration are also described.Type: GrantFiled: February 19, 1993Date of Patent: April 9, 1996Assignee: Suntory LimitedInventors: Hiromitsu Iwata, Takashi Nakatsuka, Rie Tanaka, Masaji Ishiguro
-
Patent number: 5116832Abstract: Novel penem compounds of the formula, ##STR1## wherein R is hydrogen or allyl, and A is an aliphatic 5- or 6-membered heterocyclic group having one or two oxygens in the ring and their pharmaceutically acceptable salts are produced from the compounds of the formula, ##STR2## wherein A is the same as above and respective R.sup.1 and R.sup.2 are protective groups for hydroxyl and carboxyl groups, through several steps. The compounds and their salts are useful as antibacterial agents.Type: GrantFiled: February 5, 1991Date of Patent: May 26, 1992Assignee: Suntory LimitedInventors: Masaji Ishiguro, Hiromitsu Iwata, Rie Tanaka
-
Patent number: 5026844Abstract: A process for producing 3-[1'-(R)-hydroxyethyl]-4-acyloxyazetidinone from 3-[1'-(R)-hydroxyethyl]-4-alkyl (or aryl) thioazetidinone using a copper salt of aliphatic or aromatic carboxylic acid is disclosed. The process is an effective route for producing 3-[1'-(R)-hydroxyethyl]-4-acyloxyazetidinone, and intermediate for synthesizing penems or carbapenems, without using a mercury salt which can cause an environmental hazard.Type: GrantFiled: October 13, 1989Date of Patent: June 25, 1991Assignees: Suntory Limited, Nippon Soda Company, Ltd.Inventors: Masaji Ishiguro, Hiromitsu Iwata, Takashi Nakatsuka, Yasuo Yamada
-
Patent number: 4997829Abstract: A penem compound represented by the general formula: ##STR1## (wherein R denotes hydrogen or allyl group, A denotes oxygen atom or methylene group and B denotes methylene, ethylene or carbonyl group) or a pharmacologically acceptable salt is produced through several processes.The compound exhibits stronger activities against wide variety of gram-positive and gram-negative bacteria as compared with known penem compounds.Type: GrantFiled: March 9, 1990Date of Patent: March 5, 1991Assignee: Suntory LimitedInventors: Masaji Ishiguro, Hiromitsu Iwata, Takashi Nakatsuka
-
Patent number: 4985575Abstract: A process for preparing an optically active tetrahydro-2-furoic acid is disclosed. The process comprises (i) reacting (.+-.)-tetrahydro-2-furoic acid with an optically active amine resolver of the following formula (I): ##STR1## wherein R.sub.1 is a lower alkyl group and R.sub.2 represents an alkyl group or ar aryl group, provided that R.sub.1 and R.sub.2 are different from each other, thus producing an optically active diastereomer salt, and (ii) decomposing the diastereomer salt. According to the process, a high purity, optically active tetrahydro-2-furoic acid can be prepared at a high yield using an amine resolver. The amine resolver can be recovered at a high yield and high purity.Type: GrantFiled: February 6, 1990Date of Patent: January 15, 1991Assignees: Suntory Limited, Nippon Soda Co., Ltd.Inventors: Masaji Ishiguro, Hiromitsu Iwata, Takashi Nakatsuka, Kiyoharu Nakayama, Osamu Miyahara, Kenichi Noguchi