Patents by Inventor Yoshikuni Tamao
Yoshikuni Tamao 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: 5834508Abstract: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 6, 1997Date of Patent: November 10, 1998Assignee: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5744487Abstract: A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful as an active ingredient of pharmaceutical compositions is provided.Type: GrantFiled: January 26, 1995Date of Patent: April 28, 1998Assignee: Mitsubishi Chemical CorporationInventors: Masahiro Ohshima, Norimichi Iwase, Shigeo Sugiyama, Koichi Sugawara, Misao Okitsu, Yoshikuni Tamao, Yasuhiro Morinaka
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Patent number: 5643911Abstract: A method is provided for treating a disease caused by smooth muscle cell hyperplasia.Type: GrantFiled: May 16, 1995Date of Patent: July 1, 1997Assignee: Mitsubishi Chemical CorporationInventors: Kumi Yamada, Yoshikuni Tamao, Masahiro Ohshima, Norimichi Iwase
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Patent number: 5639783Abstract: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: May 26, 1995Date of Patent: June 17, 1997Assignee: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5462941Abstract: A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed.Type: GrantFiled: March 21, 1994Date of Patent: October 31, 1995Assignee: Mitsubishi Chemical CorporationInventors: Norimichi Iwase, Yasuhiro Morinaka, Yoshikuni Tamao, Toshiji Kanayama, Kumi Yamada
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Patent number: 5424325Abstract: Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.Type: GrantFiled: December 22, 1993Date of Patent: June 13, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Naoko Ando, Hirokazu Masuda, Toshiro Sasaki, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5422359Abstract: Alpha-aminoketone derivatives of the present invention strongly inhibit thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L and calpain or the like and have excellent properties in absorbance on oral administration, tissue distribution and cell membrane permeability. The alpha-aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, amyotrophy, cardiac infarction, stroke, Alzheimer's disease, disturbance of consciousness or dyskinesia caused upon brain trauma, multiple sclerosis, peripheral nervous neuropathy, cataract, inflammation, allergosis, fulminant hepatitis, osteoporosis, hypercalcemia, breast carcinoma, prostatic carcinoma or prostatomegaly. They may also be used as therapeutic agents for suppressing growth of cancer cells, preventing metastasis of cancer or suppressing aggregation of plaques.Type: GrantFiled: December 22, 1993Date of Patent: June 6, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Toshiro Sakaki, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5141947Abstract: Disclosed herein is a fibrinolysis-enhancing agent comprising, as an effective ingredient, an N.sup.2 -arylsulfonyl-L-arginine amide represented by the general formula (I): ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## where R.sup.3 is an alkyl group having 3 to 5 carbon atoms or an alkoxyalkyl group having 2 to 4 carbon atoms and R.sup.4 is an alkyl group having 1 to 3 carbon atoms; and R.sup.2 is a group of the formula: ##STR3## where R.sup.5 and R.sup.6 are independently hydrogen atom, methyl group or methoxy group provided that they cannot be hydrogen atoms simultaneously, and R.sup.7 is an alkyl group having 1 to 3 carbon atoms; or a salt thereof. The agent is used in combination with a plasminogen activator.Type: GrantFiled: September 12, 1991Date of Patent: August 25, 1992Assignee: Mitsubishi Kasei CorporationInventors: Yoshikuni Tamao, Ryoji Kikumoto
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Patent number: 5089494Abstract: 4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.Type: GrantFiled: March 27, 1991Date of Patent: February 18, 1992Assignee: Mitsubishi Kasei CorporationInventors: Norimichi Iwase, Yasuhiro Morinaka, Yoshikuni Tamao, Toshiji Kanayama
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Patent number: 5032614Abstract: A method of suppressing vasoconstriction in a warm-blooded animal which comprises administering to said warm-blooded animal an effective amount of a serotonin antagonist compound of the formula (I): ##STR1## wherein: R.sup.1 is hydrogen, halo, C.sub.1 -C.sub.5 alkoxy or C.sub.2 -C.sub.6 dialkyl amino;R.sup.2 is hydrogen, halo or C.sub.1 -C.sub.5 alkoxy;R.sup.3 is hydrogen, hydroxy, --O--(CH.sub.2).sub.n --COOH or --O--CO--(CH.sub.2).sub.l --COOH, wherein n is an integer of 1-5, and l is an integer of 1-3;R.sup.4 is ##STR2## wherein R.sup.5 and R.sup.6 are each independently hydrogen or C.sub.1 -C.sub.8 alkyl, and A is C.sub.3 -C.sub.5 alkylene or C.sub.3 -C.sub.5 alkylene substituted with carboxy; andm is an integer of 0-5,or a pharmaceutically acceptable salt thereof. The use of the compound (I) for the preparation of a pharmaceutical formulation useful as a serotonin antagonist is also provided.Type: GrantFiled: May 18, 1990Date of Patent: July 16, 1991Assignee: Mitsubishi Kasei CorporationInventors: Masanori Osakabe, Hiroto Hara, Yoshikuni Tamao, Ryoji Kikumoto
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Patent number: 4764618Abstract: Novel arginine derivatives represented by the general formula ##STR1## wherein R.sup.1 stands for a naphthalenesulfonyl, a naphthalenecarbonyl, a 1,2,3,4-tetrahydronaphthalenesulfonyl, a 1,2,3,4-tetrahydronaphthalenecarbonyl, a dioxa b-6,7-naphthalenesulfonyl, a dioxa b-6,7-naphthalenecarbonyl, a 1,2,3,4-tetrahydro-8-quinolinesulfonyl, a 1,2,3,4-tetrahydro-8-quinolinecarbonyl, a dibenzofuransulfonyl, a dibenzofurancarbonyl, a fluorenesulfonyl, a fluorenecarbonyl, a dibenzothiophenesulfonyl or a dibenzothiophene, and R.sup.2 stands for a piperidino or a piperazino are disclosed. These arginine derivatives and their pharmaceutically acceptable salts have trypsin-inhibiting activity and useful as a pancreatitis remedy.Type: GrantFiled: June 19, 1987Date of Patent: August 16, 1988Assignee: Mitsubishi Chemical Industries LimitedInventors: Ryoji Kikumoto, Yoshikuni Tamao, Shinji Tonomura, Akira Maruyama, Shosuke Okamoto, Akiko Okunomiya
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Patent number: 4670420Abstract: N.sup.2 -dansyl-L-arginine esters and amides having the formula ##STR1## or the acid addition salts thereof with a pharmaceutically acceptable acid, wherein R is selected from the group consisting of (1) alkoxy, alkenyloxy, alkynyloxy, and cycloalkoxy, respectively, containing not more than 10 carbon atoms, aralkyl of not more than 15 carbon atoms, tetrahydrofurfuryloxy, and alkoxy of not more than 10 carbon atoms substituted with an alkoxy group of not more than 10 carbon atoms, halogen or nitro; (2) ##STR2## wherein R.sub.1 and R.sub.Type: GrantFiled: February 4, 1980Date of Patent: June 2, 1987Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Ryoji Kikumoto, Yoshikuni Tamao, Shinji Tonomura, Kazuo Ohkubo
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Patent number: 4258192Abstract: N.sup.2 -Arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: May 22, 1979Date of Patent: March 24, 1981Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4227006Abstract: N.sup.2 -dansyl-L-arginine esters and amides or the acid addition salts thereof with a pharmaceutically acceptable acid have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis.Type: GrantFiled: June 1, 1976Date of Patent: October 7, 1980Assignee: Mitsubishi Chemical Industries Ltd.Inventors: Shosuke Okamoto, Ryoji Kikumoto, Yoshikuni Tamao, Shinji Tonomura, Kazuo Ohkubo
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Patent number: 4201863Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: August 31, 1978Date of Patent: May 6, 1980Assignees: Mitsubishi Chemical Industries, Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4173630Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: May 4, 1978Date of Patent: November 6, 1979Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4140681Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.Type: GrantFiled: June 7, 1977Date of Patent: February 20, 1979Assignee: Mitsubishi Chemical Industries, LimitedInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuni Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4139529Abstract: N.sup.2 -naphthalenesulfonyl-L-arginine esters and amides and the pharmaceutically acceptable acid addition salts thereof which have antithrombotic properties.Type: GrantFiled: August 31, 1977Date of Patent: February 13, 1979Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Hyogi Kikumoto, Yoshikuni Tamao, Kazdo Ohkubo, Tohru Tezuka, Shinji Tonomura