Patents by Inventor Mitsugi Yasumoto
Mitsugi Yasumoto 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: 5447944Abstract: The present invention provides carbamoyl-2 -pyrrolidinone compounds useful as medicaments for improving cerebral functions and activating cerebral metabolism or protecting against anoxic brain damage.Type: GrantFiled: March 22, 1994Date of Patent: September 5, 1995Assignee: Taiho Pharmaceutical Company, LimitedInventors: Makoto Kajitani, Etsuo Hasegawa, Akihiro Kawaguchi, Junji Yamamoto, Katsuo Toide, Takaji Honna, Mitsugi Yasumoto, Nobuo Kasahara
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Patent number: 5420117Abstract: This invention provides a 5-substituted uridine derivative of the formula ##STR1## wherein X is F or CF.sub.3, R.sub.1 and R.sub.2 each represent a group --OSi--(R.sub.4)(R.sub.5)(R.sub.6) (wherein R.sub.4, R.sub.5 and R.sub.6 represent C.sub.1 -C.sub.10 alkyl or the like), OH, aminoacyloxy group wherein the amino group may be substituted with lower alkyl group or carboxylalkylcarbonyloxy group, R.sub.3 is a group --OSi(R.sub.4)(R.sub.5)(R.sub.6), H, OH, aminoacyloxy group wherein the amino group may be substituted with lower alkyl group, or carboxylalkylcarbonyloxy group, and at least one of R.sub.1, R.sub.2 and R.sub.3 is a group --OSi--(R.sub.4)(R.sub.5)(R.sub.6), with the proviso that when X is fluorine atom, R.sub.3 is not hydrogen, and an intermediate for the preparation thereof, preparation processes of the derivative and anti-tumor agent containing the derivative as an active ingredient.Type: GrantFiled: October 19, 1992Date of Patent: May 30, 1995Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Junichi Yamashita, Mitsugi Yasumoto, Setsuo Takeda, Junji Uchida, Konstanty Wierzba, Yuji Yamada
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Patent number: 5318970Abstract: A isoxazole compound represented by the formula (1): ##STR1## wherein R represents a hydrogen atom or a lower alkoxy group, R.sub.1 is a group represented by the formula (2): ##STR2## (wherein A represents --NH-- or --O--, B represents a methylene group or a carbonyl group, m is 0 or 1, n is an integer of 1 to 12, X represents a hydrogen atom, a hydroxy group or a lower alkoxycarbonyl group, Y represents a phenyl group which can be substituted with one or more halogen atoms, or a hydrogen atom), a group represented by the formula (3): ##STR3## (wherein Z represents a pyrimidinyl group), or a group represented by the formula (4): ##STR4## (wherein R.sub.2 represents a styryl group which can be substituted with one or more hydroxy groups); a pharmaceutically acceptable salt thereof; or a medical use thereof in a method of inhibiting lipoxygenase, inhibiting 5-lipoxygenase or inhibiting cyclooxygenase.Type: GrantFiled: March 17, 1993Date of Patent: June 7, 1994Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Masahiro Suzuki, Kenji Nozaki, Makoto Kajitani, Mitsugi Yasumoto, Naohiko Ono, Takashi Shindo
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Patent number: 5310926Abstract: The present invention provides a process for producing isoxazole derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each a hydrogen atom or lower alkoxyl, and R.sup.3 is cyano or alkoxycarbonyl, the process being characterized by oxidizing an .alpha., .beta.-unsaturated ketoxime derivative represented by the formula ##STR2## wherein R.sup.1 , R.sup.2 and R.sup.3 are as defined above. The isoxazole derivatives (II) to be produced by the process of the present invention are useful as intermediates for preparing (3,4-diarylisoxazol-5-yl) acetic acid derivatives which are useful as anti-inflammatory agents, analgesics and antipyretics.Type: GrantFiled: September 16, 1993Date of Patent: May 10, 1994Assignee: Taiho Pharmaceutical Co., LimitedInventors: Yu-ichi Hagiwara, Motoaki Tanaka, Makoto Kajitani, Mitsugi Yasumoto
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Patent number: 5250673Abstract: Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.Type: GrantFiled: October 17, 1989Date of Patent: October 5, 1993Assignee: Taiho Pharmaceutical Company, Ltd.Inventors: Setsuro Fujii, Jun-ichi Yamashita, Hiroshi Matsumoto, Setsuo Takeda, Tadafumi Terada, Mitsugi Yasumoto, Norio Unemi
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Patent number: 5229402Abstract: The present invention provides a carbamoyl-2-pyrrolidinone compound which has the following formula (2) and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.3 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having lower alkoxyl, lower alkylamino, a halogen atom or halogenomethyl as a substituent.Further, the present invention provides novel carbamoyl-2-pyrrolidinone compounds represented by the formula ##STR2## wherein R.sup.1 is a hydrogen atom, hydroxyl or lower alkyl substituted or unsubstituted with hydroxyl, and R.sup.2 is phenyl, tetrahydronaphthyl, pyridyl or thiazolyl having or not having methoxy or lower alkylamino as a substituent, provided that when R.sup.1 is a hydrogen atom or unsubstituted lower alkyl, R.sup.2 is not unsubstituted phenyl.Type: GrantFiled: December 13, 1989Date of Patent: July 20, 1993Assignee: Taiho Pharmaceutical Company, Ltd.Inventors: Makoto Kajitani, Etsuo Hasegawa, Akihiro Kawaguchi, Junji Yamamoto, Katsuo Toide, Takaji Honna, Mitsugi Yasumoto, Nobuo Kasahara
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Patent number: 5214039Abstract: The present invention provides a bicyclolactam derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.Type: GrantFiled: August 5, 1992Date of Patent: May 25, 1993Assignee: Taiho Pharmaceutical Co., LimitedInventors: Akihiro Kawaguchi, Atsushi Satoh, Makoto Kajitani, Mitsugi Yasumoto, Junji Yamamoto
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Patent number: 5206261Abstract: The present invention provides an oxindole derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is hydrogen atom, halogen atom, lower alkyl group or lower alkoxyl group, R.sup.2 is hydrogen atom or lower alkyl group, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being alkyl group which may form a ring; benzodioxanyl group; or phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group, diethylamino group, trifluoromethyl group, nitrile group, nitro group and benzyloxy group), R.sup.2 and R.sup.3 may form together .dbd.CH--R.sup.5 (R.sup.5 being same as above), R.sup.Type: GrantFiled: March 20, 1991Date of Patent: April 27, 1993Assignee: Taiho Pharmaceutical Company, LimitedInventors: Akihiro Kawaguchi, Atsushi Sato, Makoto Kajitani, Mitsugi Yasumoto, Junji Yamamoto
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Patent number: 5185344Abstract: The present invention provides a bicyclolactam derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R is benzoyl group which may be substituted with halogen atom, lower alkyl group, lower alkoxyl group, nitro group, cyano group or amino group; l is 1 or 2; m is 0 or 1; and n is 0, 1 or 2, provided that m and n are not 0 at the same time.Type: GrantFiled: October 1, 1991Date of Patent: February 9, 1993Assignee: Taiho Pharmaceutical Company, Ltd.Inventors: Akihiro Kawaguchi, Atsushi Satoh, Makoto Kajitani, Mitsugi Yasumoto, Junji Yamamoto
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Patent number: 5182284Abstract: Disclosed are a piperazine compound of the formula below or a pharmaceutically acceptable salt thereof, medical uses thereof, and processes for preparing the same: ##STR1## wherein each of R and R' is --OH, a lower alkoxy, a halo, H, a di(lower alkyl) hydrogenphosphate residue or a group --OR" (R" is an aralkyl group, etc.), etc., Y is --CH.dbd.CH-- or --(CH.sub.2).sub.m -- (m is 0, 1 or 2), and Y.sub.1 is a group of the formula ##STR2## (wherein A is --NH-- or --O--, A.sub.1 is a methylene or a carbonyl, n is 6-20, X is --OH, H or a lower alkoxycarbonyl, and X.sub.1 is an optionally halo-substituted phenyl or H) or a group of the formula ##STR3## (wherein X and n are as defined above), provided that when Y.sub.1 is the group of the formula (3), each of R and R' is an --OH group.Type: GrantFiled: September 25, 1991Date of Patent: January 26, 1993Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Masahiro Suzuki, Kenji Nozaki, Makoto Kajitani, Mitsugi Yasumoto, Naohiko Ono, Takashi Shindo
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Patent number: 5142091Abstract: The present invention provides an .alpha., .beta.-unsaturated ketone and ketoxime derivative represented by the formula ##STR1## wherein Y is oxygen atom or hydroxyimino group, Z is cyano or alkoxycarbonyl group, R.sup.1 and R.sup.2 are the same or different and are each hydrogen atom or lower alkoxyl group.The .alpha., .beta.-unsaturated ketones and ketoxime derivatives of the invention are useful as an intermediate for preparing a (3,4-diarylisoxazol-5-yl)acetic acid derivatives which is useful as an anti-inflammatory agent, analgesic and antipyretic.Type: GrantFiled: July 10, 1991Date of Patent: August 25, 1992Assignee: Taiho Pharmaceutical Company LimitedInventors: Motoaki Tanaka, Yu-ichi Hagiwara, Makoto Kajitani, Mitsugi Yasumoto
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Patent number: 5068235Abstract: The present invention provides a diazabicycloalkane derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is phenyl group, thiazolyl group or furyl group, the phenyl group may have lower alkoxy, lower alkyl or halogen atom as a substituent, R.sup.2 is oxygen atom or sulfur atom, m is 3 or 4, n is 1 or 2.Type: GrantFiled: August 16, 1990Date of Patent: November 26, 1991Assignee: Taiho Pharmaceutical Company, LimitedInventors: Etsuo Hasegawa, Akihiro Kawaguchi, Makoto Kajitani, Mitsugi Yasumoto, Nobuo Kasahara, Junji Yamamoto
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Patent number: 4946951Abstract: Disclosed is a 2'-deoxy-5-fluorouridine derivative of the formula ##STR1## wherein one of R.sub.1 and R.sub.2 is a benzyl group which may optionally have substituent selected from the group consisting of C.sub.1 -C.sub.6 alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.3 halogenated alkyl group, halogen atom, hydroxyl group and nitro group on the phenyl ring, and the other constitutes an amino acid residue, or a salt thereof. The compounds are useful for treating cancer.Type: GrantFiled: July 29, 1988Date of Patent: August 7, 1990Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Yukio Tada, Atsuhiko Uemura, Mitsugi Yasumoto, Setsuo Takeda, Hitoshi Saito, Norio Unemi
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Patent number: 4886877Abstract: Novel 2'-deoxy-5-substituted uridine derivative represented by the general formula, ##STR1## wherein R.sub.1 is a hydrogen atom, a benzoyl group or a tetrahydrofuranyl group; R.sub.2 is a fluorine atom or a trifluoromethyl group; and any one of R.sub.3 and R.sub.4 is a hydrogen atom and the other one is an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, a benzyl group having as the substituents selected from the group consisting of a halogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a nitro group, or an alkyl group having 1 to 3 carbon atoms having one or two phenyl groups as the substituents.The novel 2'-deoxy-5-substituteduridine derivative possesses excellent antitumor activity with less toxicity, thus it is useful as antitumor agent.Type: GrantFiled: February 26, 1988Date of Patent: December 12, 1989Assignee: Taiho Pharmaceutical Company LimitedInventors: Setsuro Fujii, Jun-ichi Yamashita, Hiroshi Matsumoto, Setsuo Takeda, Tadafumi Terada, Mitsugi Yasumoto, Norio Unemi
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Patent number: 4696929Abstract: A piperazine derivative represented by the formula (I) below ##STR1## wherein R.sup.1 is lower alkyl or phenyl, R.sup.2 is hydrogen or lower alkyl, n is an integer of 2 to 10, is useful as an effective component of anti-inflammatory agent or antiallergic agent.Type: GrantFiled: December 17, 1985Date of Patent: September 29, 1987Assignee: Taiho Pharmaceutical Company, LimitedInventors: Ichiro Yamawaki, Kazuo Ogawa, Naohiko Ono, Takaji Honna, Sekio Nagayama, Mitsugi Yasumoto
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Patent number: 4670583Abstract: This invention provides an amide compound represented by the formula ##STR1## wherein R.sub.1 is vinyl, 2-(methylsulfinyl)ethyl, 2-(methylsulfonyl)ethyl, 2-(2-acetylamino-2-carboxyethylthio)ethyl or 2-[2-(4-amino-4-carboxybutyrylamino)-2-(carboxymethylcarbamoyl)ethylthio]e thyl and R.sub.2 is hydrogen or lower alkyl, process for the preparation thereof, and antiallergic compositions cotaining the amide compound.Type: GrantFiled: September 5, 1985Date of Patent: June 2, 1987Assignee: Taiho Pharmaceutical Company, LimitedInventors: Akihide Koda, Mikio Hori, Mitsugi Yasumoto, Naosuke Matsuura, Ichiro Yamawaki, Yukio Tada
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Patent number: 4581372Abstract: Sulfonium compounds represented by the formula ##STR1## having immunostimulant activity and useful as the active components of drugs and agricultural chemicals.Type: GrantFiled: October 14, 1983Date of Patent: April 8, 1986Assignee: Taiho Pharmaceutical Company LimitedInventors: Akihide Koda, Mikio Hori, Mitsugi Yasumoto, Ichiro Yamawaki, Yuji Yamada, Katsuo Takikawa
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Patent number: 4556737Abstract: This invention provides novel sulfonium compounds, processes for the preparation of the sulfonium compounds, and pharmacological composition containing the sulfonium compound. The compounds of this invention are useful for treating allergy.Type: GrantFiled: February 27, 1984Date of Patent: December 3, 1985Assignee: Taiho Pharmaceutical Company LimitedInventors: Akihide Koda, Mikio Hori, Naosuke Matsuura, Mitsugi Yasumoto, Ichiro Yamawaki, Shuichi Ueda, Yukio Tada
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Patent number: 4340543Abstract: Sulfonium compounds represented by the formula ##STR1## have anticancer activity, immunostimulant activity and the like, and useful as the active components of drugs and agricultural chemicals.Type: GrantFiled: February 3, 1981Date of Patent: July 20, 1982Assignee: Taiho Pharmaceutical Company LimitedInventors: Akihide Koda, Mikio Hori, Mitsugi Yasumoto, Ichiro Yamawaki, Yuji Yamada, Katsuo Takikawa