Patents by Inventor Manabu Sasho
Manabu Sasho 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: 7858809Abstract: Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; Rl represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.Type: GrantFiled: April 8, 2005Date of Patent: December 28, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Shigeto Negi, Toshikazu Shimizu, Hiroshi Kuroda, Naoyuki Shimomura, Manabu Sasho, Yorihisa Hoshino, Manabu Kuboto
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Patent number: 7816405Abstract: The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy) -2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. There is need for (2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4 -chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S) -3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.Type: GrantFiled: April 18, 2006Date of Patent: October 19, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Masanobu Shinoda, Fumiyoshi Matsuura, Kaoru Murata, Masaharu Gotoda, Kenji Hayashi, Manabu Sasho, Naoki Ozeki, Susumu Inoue, Katsutoshi Nishiura, Yoshihiko Hisatake, Teiji Takigawa, Mamoru Miyazawa, Shigeto Negi, Keisuke Matsuyama
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Patent number: 7803949Abstract: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.Type: GrantFiled: December 20, 2006Date of Patent: September 28, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Manabu Sasho, Keizo Sato, Jun Niijima, Mamoru Miyazawa, Shigeto Negi, Atsushi Kamada
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Patent number: 7790887Abstract: The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.Type: GrantFiled: January 28, 2008Date of Patent: September 7, 2010Assignees: Eisai R&D Management Co., Ltd., Mercian CorporationInventors: Hiroshi Ishihara, Manabu Sasho, Keizo Sato, Takashi Kamahara, Masashi Yoshida
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Publication number: 20090192316Abstract: An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.Type: ApplicationFiled: December 20, 2006Publication date: July 30, 2009Inventors: Manabu Sasho, Keizo Sato, Jun Niijima, Mamoru Miyazawa, Shigeto Negi, Atsushi Kamada
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Publication number: 20090069591Abstract: The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. [Problem] There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution] Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.Type: ApplicationFiled: April 18, 2006Publication date: March 12, 2009Applicant: EISAI R & D MANAGEMENT CO., LTD.Inventors: Masanobu Shinoda, Fumiyoshi Matsuura, Kaoru Murata, Masaharu Gotoda, Kenji Hayashi, Manabu Sasho, Naoki Ozeki, Susumu Inoue, Katsutoshi Nishiura, Yoshihiko Hisatake, Teiji Takigawa, Mamoru Miyazawa, Shigeto Negi, Keisuke Matsuyama
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Publication number: 20080214564Abstract: The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.Type: ApplicationFiled: January 28, 2008Publication date: September 4, 2008Applicants: Eisai R&D Management Co., Ltd., MERCIAN CORPORATIONInventors: Hiroshi ISHIHARA, Manabu Sasho, Keizo Sato, Takashi Kamahara, Masashi Yoshida
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Patent number: 7375236Abstract: In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon.Type: GrantFiled: August 18, 2005Date of Patent: May 20, 2008Assignee: Eisai Co., Ltd.Inventors: Naoyuki Shimomura, Manabu Sasho, Akio Kayano, Kazuhiro Yoshizawa, Masahiko Tsujii, Hiroshi Kuroda, Ken Furukawa
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Publication number: 20070191613Abstract: An object of the invention is to find out intermediates usful for the synthesis of pyrazol-fused ring derivatives (such as 7-phenylpyrazolo[1,5-a]pyridine derivatives) and a method for producing the same. A method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; R1 represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.Type: ApplicationFiled: April 8, 2005Publication date: August 16, 2007Inventors: Shigeto Negi, Toshikazu Shimizu, Hiroshi Kuroda, Naoyuki Shimomura, Manabu Sasho, Yorihisa Hoshino, Manabu Kubota
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Publication number: 20070117866Abstract: The present invention relates to calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate] represented by formula (I), a hydrate thereof, a crystal of the compound of formula (I), and a crystal of the hydrate of the compound of formula (I) which are useful as pharmaceuticals, and to processes for producing the same, and intermediates therefore, and processes for production thereof. [Problem]There is need for (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, in the form of a drug substance, purified so as to minimize a residual solvent content and having a uniformized specification and a highly favorable workability, and a process for producing the same. [Solution]Crystalline calcium bis[(2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionate], a calcium salt of (2S)-3-[3-[(2S)-3-(4-chloro-2-cyanophenoxy)-2-fluoropropoxy]phenyl]-2-isopropoxypropionic acid, solves the above problem.Type: ApplicationFiled: April 18, 2006Publication date: May 24, 2007Applicant: Eisai Co., Ltd.Inventors: Masanobu Shinoda, Fumiyoshi Matsuura, Kaoru Murata, Masaharu Gotoda, Kenji Hayashi, Manabu Sasho, Naoki Ozeki, Susumu Inoue, Katsutoshi Nishiura, Yoshihiko Hisatake, Teiji Takigawa, Mamoru Miyazawa, Shigeto Negi, Keisuke Matsuyama
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Publication number: 20060058370Abstract: In the present invention, the methods of producing a fluorinated cyclic benzamidine derivative (A), or a salt thereof, comprise the step of reacting a specific novel compound with ammonia or imide. The methods of this invention for producing a morpholine-substituted phenacyl derivative (B), or a salt thereof, comprise reaction of a specific novel compound with morpholine, reaction of the product with a halogenating reagent, and deketalization of the product. The methods of this invention for a producing cyclic benzamidine derivative (C), or a salt thereof, comprise the step of coupling compound (A), or a salt thereof, with compound (B), or a salt thereof, in the presence of an ether or a hydrocarbon.Type: ApplicationFiled: August 18, 2005Publication date: March 16, 2006Applicant: Eisai Co., Ltd.Inventors: Naoyuki Shimomura, Manabu Sasho, Akio Kayano, Kazuhiro Yoshizawa, Masahiko Tsujii, Hiroshi Kuroda, Ken Furukawa
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Patent number: 6642377Abstract: A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak—E means the alkali earth metal; and B means the inorganic acid, respectively.Type: GrantFiled: January 14, 2002Date of Patent: November 4, 2003Assignee: Eisai Co., Ltd.Inventors: Akio Kayano, Hiroyuki Chiba, Taiju Nakamura, Shin Sakurai, Hiroyuki Ishizuka, Hiroyuki Saito, Yuuki Komatsu, Manabu Sasho, Nobuaki Sato, Shigeto Negi
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Patent number: 6372914Abstract: The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate. A method for manufacturing which comprises the step of reacting a compound of the formula (I): (wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II): (wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).Type: GrantFiled: November 2, 2000Date of Patent: April 16, 2002Assignee: Eisai Co., Ltd.Inventors: Takaaki Suzuki, Isao Sugiyama, Manabu Sasho, Nobuaki Sato, Atsushi Kamada, Kazuhide Ashizawa
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Patent number: 6218550Abstract: The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate. A method for manufacturing which comprises the step of reacting a compound of the formula (I): (wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II): (wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).Type: GrantFiled: November 12, 1999Date of Patent: April 17, 2001Assignee: Eisai Co., Ltd.Inventors: Takaaki Suzuki, Isao Sugiyama, Manabu Sasho, Nobuaki Sato, Atsushi Kamada, Kazuhide Ashizawa
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Patent number: 6037341Abstract: Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, a high stability to .beta.-lactamases and DHP-I and a high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: ##STR1## wherein the ring A represents a 3- to 7-membered non-aromatic ring containing at least one nitrogen atom and optionally having a substituent other than R.sup.6 ; R.sup.1 represents hydrogen or methyl; R.sup.2 and R.sup.5 are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R.sup.3 represents hydrogen or a protecting group of the carboxyl group; R.sup.4 represents hydrogen, lower alkyl or a protecting group of the amino group; R.sup.6 represents: (1) hydrogen, (2) lower alkyl, optionally substituted by an optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or ##STR2## wherein R.sup.7 and R.sup.Type: GrantFiled: December 18, 1996Date of Patent: March 14, 2000Assignee: Eisai Co., Ltd.Inventors: Nobuaki Sato, Manabu Sasho, Atsushi Kamata, Takaaki Suzuki, Isao Sugiyama, Kanemasa Katsu, Takeshi Suzuki
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Patent number: 5151417Abstract: 3-Substituted vinyl cephalosporin derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a hydroxyl or lower alkoxyl group, X represents a nitrogen atom or a group represented by the formula --CH.dbd., R.sup.2 represents a carboxyl group or a carboxyl group protected with a protecting group, and R.sup.3 is as defined herein, and pharmaceutically acceptable salts thereof are potent antibacterial agents. Processes for their preparation, intermediates in such processes, and antibacterial compositions containing them as active ingredients are also described.Type: GrantFiled: July 10, 1990Date of Patent: September 29, 1992Assignee: Eisai Co., Ltd.Inventors: Manabu Sasho, Hiroshi Yamauchi, Motosuke Yamanaka, Takaharu Nakamura, Kanemasa Katsu, Isao Sugiyama, Yuuki Komatu, Shigeto Negi
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Patent number: 5128465Abstract: A cephem derivative represented by the following formula: ##STR1## wherein R.sub.1 means a fluorine-substituted lower alkyl and A.sub.1 denotes a cyclic or acyclic ammonio group, or a non-toxic salt thereof, is prepared by reacting a compound represented by the following formula: ##STR2## wherein A.sub.1 has the same meaning as defined above, with another compound represented by the following formula: ##STR3## wherein R.sub.1 has the same meaning as defined above, and if necessary, removing the protecting groups.Type: GrantFiled: January 22, 1990Date of Patent: July 7, 1992Assignee: Eisai Co., Ltd.Inventors: Takashi Kamiya, Toshihiko Naito, Yuuki Komatu, Yasunobu Kai, Takaharu Nakamura, Manabu Sasho, Shigeto Negi, Isao Sugiyama, Kanemasa Katsu, Hiroshi Yamauchi