Patents by Inventor Yoshiaki Yoshikuni
Yoshiaki Yoshikuni 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: 5700918Abstract: The present invention has for its object to provide a trisaccharide Lewis sugar-chain epitope derivative of the following structural formula, which is of value as a medicine and has a novel structure containing moranoline. ##STR1## wherein R.sup.1 represents hydrogen or lower alkyl; R.sup.2 and R.sup.3 are dissimilar and each represents galactopyranosyl or fucopyranosyl, which is substituted by hydroxysulfonyl or a metal salt thereof. The compounds of the invention have cell adhesion-inhibitory activity and is useful for the prevention and treatment of inflammation, inflammation-associated thrombosis, rheumatism, immune diseases, viral infections, and cancer.Type: GrantFiled: September 20, 1996Date of Patent: December 23, 1997Assignee: Nippon Shinyaku Co., Ltd.Inventors: Akira Hasegawa, Makato Kiso, Yoshiaki Yoshikuni
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Patent number: 5498604Abstract: The object of the present invention is to provide a new SLe-type sugar chain derivative represented by the following formula (I), which is useful as a pharmaceutical and which contains moranoline: ##STR1## wherein R.sub.1 represents hydrogen, a lower alkyl, a lower alkenyl or a lower alkynyl; R.sup.2 and R.sup.3 differ from each other and represent a galactosyl, sialylgalactosyl or fucosyl group; R.sub.4 represents a hydroxyl group or an acetamido group. The present invention comprises a sugar chain derivative containing a moranoline, and having a new structure. Possessing cell adhesion inhibitory activity, the compounds of the present invention antagonizes selectin, serving well in the treatment of inflammation, inflammation-associated thrombosis, asthma and rheumatism, and in the prevention and treatment of immunological diseases and cancer.Type: GrantFiled: November 17, 1994Date of Patent: March 12, 1996Assignees: Nippon Shinyaku Company, Limited, Akira HasegawaInventors: Akira Hasegawa, Makoto Kiso, Yoshiaki Yoshikuni
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Patent number: 5292750Abstract: Compounds are described which are useful for lowering the activity of .alpha..sub.2 -PI, for the treatment of myocardial infarctions and cerebral infarctions, as urokinase secretion accelerators, as antithrombotic agents and to accelerate the fibrinolysis accelerating effect.Type: GrantFiled: September 8, 1992Date of Patent: March 8, 1994Assignee: Nippon Shinyaku Co. Ltd.Inventors: Yoshiaki Yoshikuni, Nobutoshi Ojima, Kazuya Mori
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Patent number: 5192772Abstract: Compounds are described which are useful for lowering the activity of .alpha..sub.2 -PI, for the treatment of myocardial infarctions and cerebral infarctions, as urokinase secretion accelerators, as antithrombotic agents and to accelerate the fibrinolysis accelerating effect.Type: GrantFiled: August 12, 1991Date of Patent: March 9, 1993Assignee: Nippon Shinyaku Co. Ltd.Inventors: Yoshiaki Yoshikuni, Nobutoshi Ojima, Kazuya Mori
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Patent number: 4859767Abstract: Compounds of formula I are useful in the prophylaxis or treatment of hyperglycemic symptoms ##STR1## wherein R is alkyl substituted by one or more hydroxy.Type: GrantFiled: October 10, 1986Date of Patent: August 22, 1989Assignee: Nippon Shinyaku Co., Ltd.Inventors: Makoto Sugiyama, Yoji Ezure, Yoshiaki Yoshikuni, Takayuki Ozaki, Nobutoshi Ojima
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Patent number: 4855415Abstract: A compound of formula (I) ##STR1## wherein: B is a divalent substituted or unsubstituted, cyclic or acyclic, saturated or unsaturated hydrocarbon group;A is a linking group selected from the group consisting of --O--, --S--, --N(H)--, --N(R)--, --C(O)-- and combinations of two or more thereof or A is a direct bond; andR is a monovalent substituted or unsubstituted, cyclic or acyclic, saturated or unsaturated hydrocarbon group, a monovalent substituted or unsubstituted aromatic hydrocarbon group, or a monovalent substituted or unsubstituted heterocyclyl provided that B--A--R may not represent hydrogen, lower alkyl, or a monovalent cyclic or acyclic hydrocarbon group having one or more hydroxyl groups, which is useful for inhibiting an increase in blood glucose in humans and for the treatment of diabetes mellitus.Type: GrantFiled: September 1, 1987Date of Patent: August 8, 1989Assignee: Nippon Shinyaku Co., Ltd.Inventors: Makoto Sugiyama, Yoji Ezure, Yoshiaki Yoshikuni, Yukio Fujita
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Patent number: 4831055Abstract: Compounds of formula (I) ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydrogen, halogen or alkyl and R.sup.2 is hydrogen or alkyl are useful to reduce serum lipids in animals, including humans.Type: GrantFiled: June 8, 1987Date of Patent: May 16, 1989Assignee: Nippon Shinyaku Co., Ltd.Inventors: Yoshiaki Yoshikuni, Shoichi Chokai, Takayuki Ozaki, Hirotsugu Yoshida, Haruo Tanaka, Jun Segawa
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Patent number: 4755523Abstract: Abietamide derivatives of the formula I ##STR1## wherein X is NZ wherein Z is hydrogen, alkyl, unsubstituted or substituted phenyl or X is a sulphur atom; when X is NZ, V is nitrogen, W is , and R is hydrogen or alkyl and when X is a sulphur atom, V is , W is nitrogen, and R is hydrogen, alkyl, phenyl or --CH.sub.2 COOR'; wherein R' is hydrogen or alkyl and is a single or double bond, are useful for treating hyperlipemia and particularly for the prevention and therapy of arteriosclerosis.Type: GrantFiled: February 17, 1987Date of Patent: July 5, 1988Assignee: Nippon Shinyaku Co., Ltd.Inventors: Yoshiaki Yoshikuni, Shoichi Chokai, Yukio Fujita, Takayuki Ozaki
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Patent number: 4533668Abstract: N-aralkylmoranoline and N-aralkenylmoranoline, and their pharmaceutical acceptable non-toxic acid addition salts thereof, pharmaceutical compositions containing the same and methods of inhibiting the increase in blood sugar level by administration of the same.Type: GrantFiled: April 27, 1979Date of Patent: August 6, 1985Assignee: Nippon Shinyaku Co. Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoshiaki Yoshikuni, Kohei Kura, Masahiro Yagi, Ichiro Shirahase
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Patent number: 4363802Abstract: Bisglucosyl moranoline of the formula (I) ##STR1## is useful in inhibiting increase of blood sugar in sugar-loaded animals and humans, and particularly for treatment of diabetes mellitus.Type: GrantFiled: November 30, 1981Date of Patent: December 14, 1982Assignee: Nippon Shinyaku Co. Ltd.Inventors: Shingo Matsumura, deceased, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoji Ezure, Yoshiaki Yoshikuni, Shigeaki Maruo, Nobutoshi Ojima, Kiyotaka Konno
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Patent number: 4339585Abstract: Moranoline, or 2-hydroxymethyl-3,4,5-trihydroxy piperidine, is prepared by directly reducing an actinomycetes culture solution containing nojirimycin, followed by isolation, as for example, through the utilization of an ion exchange resin. The corresponding N-methyl derivative can be obtained through the addition of formaldehyde to the culture solution prior to the reduction.Type: GrantFiled: November 9, 1978Date of Patent: July 13, 1982Assignee: Nippon Shinyaku Co., Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoji Ezure, Yoshiaki Yoshikuni, Masahiro Yagi
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Patent number: 4338433Abstract: Moranolines are produced which are useful for controlling blood sugar levels.Type: GrantFiled: December 8, 1980Date of Patent: July 6, 1982Assignee: Nippon Shinyaku Co. Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoji Ezure, Yoshiaki Yoshikuni, Masahiro Yagi, Nobutoshi Ojima
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Patent number: 4336373Abstract: Bis(2-hydroxymethyl-3,4,5-trihydroxypiperidine-1-yl-propenyl) compounds and their acid addition salts are antihyperglycemic agents. Typical examples are 1,4-bis[3-(2-hydroxymethyl-3,4,5-trihydroxypiperidin-1-yl)prop-2-enyl] benzene and 1,3-bis-{4-[3-(2-hydroxymethyl-3,4,5-trihydroxy-piperidin-1-yl)prop-2-enyl ]phenoxy}propane.Type: GrantFiled: March 26, 1981Date of Patent: June 22, 1982Assignee: Nippon Shinyaku Company, Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoshiaki Yoshikuni, Masahiro Yagi, Kohei Kura, Ichiro Shirahase
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Patent number: 4336374Abstract: 2-Hydroxymethyl-3,4,5-trihydroxypiperidines bearing a quaternary ammonium-substituted cinnamyl group on the piperidine nitrogen atom and their acid addition salts are antihyperglycemic agents. A typical example is 1-(4-trimethylammoniumcinnamyl)-2-hydroxymethyl-3,4,5-trihydroxypiperidine chloride.Type: GrantFiled: March 26, 1981Date of Patent: June 22, 1982Assignee: Nippon Shinyaku Co., Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoshiaki Yoshikuni, Masahiro Yagi, Kohei Kura, Ichiro Shirahase
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Patent number: 4210671Abstract: A process for the preparation of amide derivatives of abietic acid, dehydroabietic acid, dihydroabietic acid or tetrahydroabietic acid which comprises reacting abietic acid, dehydroabietic acid, dihydroabietic acid or tetrahydroabietic acid or a reactive derivative thereof with an amine of the following formula:HNRR'wherein R and R' are each hydrogen, a straight chain or branched alkyl group having 3 to 15 carbon atoms, a lower alkenyl group, a cycloalkyl group, a phenyl group, a phenylalkyl group and a phenylalkyl group having a lower alkyl group at the .alpha.-position, with the proviso that such amines where both R and R' are hydrogen or where one of R and R' is hydrogen and the other is phenyl are excluded.The invention further comprises the resulting abietamide derivative reaction products, compositions containing effective blood serum cholesterol-reducing amounts of said abietamide derivatives and their use as anti-arteriosclerotic agents.Type: GrantFiled: May 12, 1975Date of Patent: July 1, 1980Inventors: Hiromu Murai, Katsuya Ohata, Hiroshi Enomoto, Kenji Sempuku, Koji Kitaguchi, Yukio Fujita, Yoshiaki Yoshikuni, Kohei Kura, Katsuhide Saito, Tamiki Mori, Yasuo Yasutomi
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Patent number: 4198481Abstract: 2-Hydroxymethyl-3,4,5-trihydroxy piperidine, or moranoline, is prepared by culturing a moranoline-producing strain of microorganism of the genus Streptomyces in an appropriate culture medium and thereafter isolating moranoline from the culture medium.Type: GrantFiled: November 15, 1978Date of Patent: April 15, 1980Assignee: Nippon Shinyaku Co., Ltd.Inventors: Shingo Matsumura, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoji Ezure, Yoshiaki Yoshikuni, Masahiro Yagi
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Patent number: 4182767Abstract: 2-Hydroxymethyl-3,4,5-trihydroxy-N-alkylpiperidines and their acid addition salts are antihyperglycemic agents. A typical example is 2-hydroxymethyl-3,4,5-trihydroxy-N-methylpiperidine.Type: GrantFiled: May 10, 1978Date of Patent: January 8, 1980Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Hiroshi Enomoto, Yoshiaki Aoyagi, Yoshiaki Yoshikuni, Masahiro Yagi, Ichiro Shirahase
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Patent number: 4137231Abstract: 2-Hydroxymethyl-3,4,5-trihydroxypiperidine is obtained from the mulberry plant through extraction, optionally with further purification through ion exchange or chromatographic treatment.Type: GrantFiled: December 20, 1976Date of Patent: January 30, 1979Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Hiroshi Enomoto, Yoshiaki Yoshikuni, Tatsuhiko Kono, Masahiro Yagi
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Patent number: 4117159Abstract: N-Phenyl and N-benzyl .DELTA..sup.8 -dihydropimaramides are antiphlogistic and serum cholesterol lowering agents. The compounds, of which N-(2-ethylphenyl)-.DELTA..sup.8 -dihydropimaramide is a representative embodiment, are prepared from reactive derivatives of .DELTA..sup.8 -dihydropimaric acid and the appropriate amine.Type: GrantFiled: February 14, 1977Date of Patent: September 26, 1978Assignee: Nippon Shinyaku Co., Ltd.Inventors: Hiromu Murai, Yukio Fujita, Tamiki Mori, Hiroshi Enomoto, Yoshiaki Yoshikuni
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Patent number: RE30886Abstract: 2-Hydroxymethyl-3,4,5-trihydroxypiperidine possesses antidiabetic and lipid biosynthesis inhibitory properties. The use of the compound for such indications and pharmaceutical compositions adapted to this use are described.Type: GrantFiled: December 15, 1978Date of Patent: March 23, 1982Assignee: Nippon Shinyaku Company Ltd.Inventors: Katsuya Ohata, Hiroshi Enomoto, Yoshiaki Yoshikuni, Tatsuhiko Kono, Masahiro Yagi