Patents by Inventor Hamao Umezawa
Hamao Umezawa 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: 5288898Abstract: As new compounds are now provided N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters which are effective as an .alpha.-adrenergic and .beta.-adrenergic agent to stimulate the .alpha.-adrenergic and .beta.-adrenergic functions of the central nervous system of mammalian animals and are expectable to be useful for therapeutic treatment of disorders as invoked by reduced biological activities or functions of the .alpha.- and/or .beta.-adrenergic neurons. N-methyl-L-threo-3-(3,4-dihydroxyphenyl)serine (C.sub.1 -C.sub.6) alkyl esters are preferred amongst the new compounds of this invention.Type: GrantFiled: May 4, 1993Date of Patent: February 22, 1994Assignee: Zaidan Hojim Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Toshiharu Nagatsu, Tomio Takeuchi, Hajime Morishima, Yoshio Sawasaki, Hiroshi Takezawa, Fujinori Sasaki
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Patent number: 5202427Abstract: A DNA segment of this invention is a DNA fragment of a length of about 3.8 kb which is obtained by excising with a restriction endonuclease Bgl II a hybrid plasmid pST 141 having a length of about 12.6 kb of Streptomyces griseus 4-1 strain (FERM P-7984, namely, FERM BP-1198) to give a Bgl II-Bgl II DNA fragment, and then excising with a restriction endonuclease Sph I the resultant Bgl II-Bgl II DNA fragment having a length of about 7.0 kb and having the restriction endonuclease sites as shown in the restriction endonuclease map of FIG. 1 . This DNA fragment is a DNA which contains a streptomycin resistance gene and contains, in the vicinity of this gene, such a DNA region possessing a function to control the expression of the streptomycin resistance gene. An insertion of this DNA fragment having a length of about 3.8 kb into a suitable actinomycetes plasmid vector can produce such a hybrid plasmid which acts reliably as a selected marker of the streptomycin resistance.Type: GrantFiled: February 25, 1991Date of Patent: April 13, 1993Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, deceased, Yoji Umezawa, heir, Yoji Umezawa, heir, Yoshiro Okamo, heir
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Patent number: 5101022Abstract: Mycaminosyl tylonolide derivatives represented by the following general formula ##STR1## (wherein R.sup.1 denotes hydroxyl group, a lower alkanoyloxy group, benzoyloxy group, azido group, or amino group which may optionally be substituted with a lower alkyl or a lower alkanoyl radical; R.sup.2 stands for hydrogen atom or hydroxyl group; R.sup.3 expresses hydrogen atom or formyl group; and means a double bond or a radical represented by ##STR2## and salts thereof.Type: GrantFiled: February 4, 1991Date of Patent: March 31, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Tomio Takeuchi, Akihiro Tanaka, Shuichi Sakamoto
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Patent number: 5034517Abstract: 2,6-Dideoxy-2-fluoro-L-talopyranose and 1-substituted derivatives thereof, including methyl 2,6-dideoxy-2-fluoro-L-talopyranoside and 3,4-di-O-protected-2,6-dideoxy-2-fluoro-L-talopyranosyl halides, are now provided and these new compounds are useful as intermediates for use in the synthesis of new compounds having antitumor activity, especially 7-O-(2,6-dideoxy-2-fluoro-.alpha.-L-talopyranosyl) daunomycinone or -adriamycinone. 2,6-Dideoxy-2-fluoro-L-talopyranose shows antibacterial activity. 2,6-Dideoxy-fluoro-L-talopyranose and the 1-substituted derivatives thereof may be produced by a multi-stage process starting from L-fucose.Type: GrantFiled: March 6, 1990Date of Patent: July 23, 1991Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Tomio Takeuchi, Yasushi Takagi
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Patent number: 4983328Abstract: N-[4-(3-Aminopropyl)aminobutyl]-2-(.omega.-guanidino-fatty acid-amido)-2-substituted-ethanamides represented by the general formula ##STR1## wherein Y represents --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH or ##STR2## R represents a hydrogen atom, an alkyl group of 1 to 4 carbon atoms which may have a hydroxyl group as substituent, or a benzyl group, and n is an integer of from 1 to 8, provided that when Y is ##STR3## and n is 4, R represents the groups other than the hydrogen atom; salt thereof having antitumor activity in experimental animal tumors and a process for the preparation thereof is provided.Type: GrantFiled: March 15, 1988Date of Patent: January 8, 1991Assignee: Bristol-Myers CompanyInventors: Hamao Umezawa, Tomio Takeuchi, Shinichi Kondo, Hironobu Iinuma, Daishiro Ikeda, Teruya Nakamura, Akio Fujii
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Patent number: 4956504Abstract: The present invention relates to novel Spergualin-related compounds represented by the general formula [I] ##STR1## (wherein X is ##STR2## R is --H or --CH.sub.2 OH; R.sub.1 is --H, ##STR3## R.sub.2 is a residue obtained by removing, from an amino acid or peptide, the hydroxyl group of the carboxyl group and, when R.sub.1 is a group other than --H, R.sub.2 is same as R.sub.1), or a pharmacologically acceptable salt thereof. Said compounds or salts thereof have an immuno-modulating action.Type: GrantFiled: April 1, 1987Date of Patent: September 11, 1990Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Tetsushi Saino, Masao Yoshida, Katsutoshi Takahashi, Teruya Nakamura, Hamao Umezawa, deceased
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Patent number: 4945081Abstract: Mycaminosyl tylonolide derivatives represented by the following general formula ##STR1## (wherein R.sup.1 denotes hydroxyl group, a lower alkanoyloxy group, benzyloxy group, azido group, or amino group which may optionally be substituted with a lower alkyl or a lower alkanoyl radical; R.sup.2 stands for hydrogen atom or hydroxyl group; R.sup.3 expresses hydrogen atom or formyl group; and means a double bond or a radical represented by ##STR2## and salts thereof.Type: GrantFiled: August 16, 1988Date of Patent: July 31, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Tomio Takeuchi, Akihiro Tanaka, Shuichi Sakamoto
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Patent number: 4925877Abstract: The present invention provides new physiological active substance erbstatin analogue compounds of a general formula (I), which have excellent tyrosine-specific protein-kinase inhibitory activity, antitumor activity and antimicrobial activity. ##STR1## (in which R.sup.1 represents a hydrogen atom, a lower alkanoyl group or a lower alkyl group; n represents a positive integer of 1 to 3;X represents a hydrogen atom or a halogen atom;Y represents a group of formula --CH.dbd.CH--NC, --CH.dbd.CH--NHR.sup.2 or --CH.sub.2 --CH.sub.2 --NHR.sup.2(where R.sup.2 represents a formyl group or a lower alkanoyl group; with the exception of the cases where X is hydrogen atom, (R.sup.1 O).sub.n group is 2,5-dihydroxy group and Y is --CH.dbd.CH--NHCHO or --CH.sub.2 --CH.sub.2 --NHCHO).The present invention further provides a tyrosine-specific protein-kinase inhibitor, tumoricide or bactericide containing at least one compound of the said formula (I).Type: GrantFiled: February 20, 1987Date of Patent: May 15, 1990Assignee: Zaidanhojin Biseibutsu Kagaku KenkyukaiInventors: Hamao Umezawa, deceased, Tomio Takeuchi, Kuniaki Tatsuta, Kunio Isshika, Masaya Imoto
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Patent number: 4914192Abstract: Mycaminosyl tylonolide derivatives represented by the following general formula ##STR1## (wherein R.sup.1 denoted hydroxyl group, a lower alkanoyloxy group, benzyloxy group, azido group, or amino group which may optionally be substituted with a lower alkyl or a lower alkanoyl radical; R.sup.2 stands for hydrogen atom or hydroxyl group; R.sup.3 expresses hydrogen atom or formyl group; and means a double bond or a radical represented by ##STR2## and salts thereof.Type: GrantFiled: September 14, 1988Date of Patent: April 3, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Tomio Takeuchi, Akihiro Tanaka, Shuichi Sakamoto
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Patent number: 4897470Abstract: New anthracycline antibiotics of a formula (I) are provided, which are usable as an anticancer agent ##STR1## (where R represents a hydrogen atom or a hydroxyl group). The antibiotics (I) can be produced by incubation of a dye-nonproductive or hardly dye-productive mutant strain which has an ability of converting .alpha.-citromycinone or .beta.-isorhodomycinone into the antibiotics (I), in the presence of .alpha.-citromycinone or .beta.-isorhodomycinone in a pertinent nutrient medium.Type: GrantFiled: April 6, 1987Date of Patent: January 30, 1990Assignee: Sanraku IncorporatedInventors: Akihiro Yoshimoto, Osamu Jodo, Yoshio Watanabe, Tomoyuki Ishikura, Tsutomu Sawa, Tomio Takeuchi, Hamao Umezawa, deceased
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Patent number: 4877870Abstract: Disclosed is a process for producing a 10-hydroxyanthracycline of the following formula (II) which comprises reacting a compound of the following formula (I) or an acid addition salt thereof with an N-oxide of a tertiary amine ##STR1## wherein: R.sup.1 through R.sup.6 each designate any of H, OH and OCH.sub.3 ; R.sup.7 designates any of H, OH and a sugar residue; and R.sup.8 designates any of C.sub.2 H.sub.5, COCH.sub.3, CH(OH)CH.sub.3, CH(OH)CH.sub.2 (OH) and COCH.sub.2 OH. In accordance with this process, it is possible to efficiently introduce a hydroxyl group into the 10-position of an anthracycline having no substitutent at the same position thereof.Type: GrantFiled: June 30, 1987Date of Patent: October 31, 1989Assignee: Kirin Beer Kabushiki KaishaInventors: Hamao Umezawa, deceased, Kuniaki Tatsuta, Hiroyuki Kawai, Shohachi Nakajima
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Patent number: 4876244Abstract: The present invention relates to a stable medical composition for injection containing (1) a Spergualin of the formula: ##STR1## [wherein R is ##STR2## (wherein R' is a lower alkyl group having 1 to 4 carbon atoms), ##STR3## or a salt thereof and (2) at least one stabilizer selected from the group consisting of mannitol, maltose, dextran, lactose, cyclodextrin, gelatin, chondroitin sulfate, and human serum albumin; when R is ##STR4## mannitol is excepted. A spergualin is useful as cancer control agents and immunomodulators.Type: GrantFiled: August 11, 1987Date of Patent: October 24, 1989Assignee: Zaidan Hojin Biseibutsu KagakuInventors: Hamao Umezawa, Shintaro Suzuki, Taka'aki Ohkuma, Fumihiro Sato, Teruya Nakamura
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Patent number: 4870207Abstract: Known compound, optically active arphamenine A can now be synthesized in an optically active pure form and in a favorable yield by a new process comprising consecutive steps with starting from L-arginine, wherein racemization of intermediate reaction products can be minimized.Type: GrantFiled: July 30, 1987Date of Patent: September 26, 1989Assignee: Zaiden Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, deceased, Takaaki Aoyagi, Kuniaki Tatsuta, Takeshi Nakamura, Shunzo Fukatsu
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Patent number: 4870172Abstract: A novel compound having anti-tumor activity is disclosed which is 1,12-dihydroxy-1,6,12,17-tetraazacyclodocosan-2,5,13,16-tetrone produced microbiologically by culturing a microorganism belonging to the genus of Alteromonas or, in particular, Alteromonas haloplanktis SB-1123. The characterization data of the compound and the microbiological properties of the microorganism are described. The results of in vitro assays are given for the anti-tumor activity of the compound against L-1210 and IMC carcinoma cells.Type: GrantFiled: July 16, 1987Date of Patent: September 26, 1989Assignee: Microbial Chemistry Research FoundationInventors: Yoshiro Okami, Shogo Kurasawa, Toshiyuki Kamayama, Atsushi Takahashi, Masaaki Ishizuka, Hamao Umezawa, deceased
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Patent number: 4859593Abstract: New physiologically active substances, arphamenine A and arphamenine B which are generically termed arphamenine are produced from a new microorganism, BMG361-CF4 strain identified as FERM P-6521 or FERM BP-286 or ATCC No. 39373. Arphamenine is useful as a host defence stimulator having an activity to enhance cell-mediated immunity, and also as an anti-tumor agent.Type: GrantFiled: December 16, 1985Date of Patent: August 22, 1989Assignee: Zaidin Hojin Biseibutsu Kagaku Kenky KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Masaaki Ishizuka
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Patent number: 4855414Abstract: An anthracycline compound, R20X2, of the following formula (II) is produced by a process which comprises subjecting an anthracycline compound, R20X3, of the following formula (I) or a salt thereof to reaction in the co-presence of (1) acetone and/or dimethylformamide and (2) an aqueous solution containing ammonium ion and/or trialkylamine. ##STR1## The anthracycline compound, R20X2, can be produced not only by the cultivation of actinomycetes but also, in accordance with the process as shown above, by chemical conversion of the anthracycline compound, R20X3, in a high yield.Type: GrantFiled: June 30, 1987Date of Patent: August 8, 1989Assignee: Kirin Beer Kabushiki KaishaInventors: Hamao Umezawa, Atsuo Odagawa, Shiro Kataoka, Shohachi Nakajima
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Patent number: 4851446Abstract: The present invention relates to an immunosuppressing method which comprises administering a spergualin-related compound represented by the following formula ##STR1## (wherein R.sub.1 is --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.6 --, ##STR2## R.sub.2 is --(CH.sub.2).sub.2 -- or --CH.dbd.CH--; and R.sub.3 is ##STR3## or pharmacologically acceptable salts thereof in an effective amount to a warm-blood animal.Type: GrantFiled: March 6, 1987Date of Patent: July 25, 1989Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, deceased, Tomio Takeuchi, Masaaki Ishizuka, Fuminori Abe, Akio Fujii, Teruya Nakamura
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Patent number: 4845082Abstract: New compound, 3',4'-dideoxy-3'-fluorokanamycin B is now provided, which is useful as antibacterial agent.3',4'-Dideoxy-3'-fluorokanamycin B is prepared by a process comprising halogenating an N,O-protected derivative of 3'-deoxy-3'-fluoro-4'-O-sulfonylkanamycin B with a metal halide, reducing the resulting 4'- halogenated 3'-deoxy-3'-fluorokanamycin B derivative to convert its 4'-halo group into a hydrogen atom, and thereby to produce an N,O-protected derivative of 3',4'-dideoxy-3'-fluorokanamycin B, and removing the remaining amino-protecting groups and the remaining hydroxyl-protecting groups from the reduction product by conventional deprotecting methods.Type: GrantFiled: August 22, 1986Date of Patent: July 4, 1989Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Yoshihiko Kobayashi
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Patent number: 4833241Abstract: Disclosed is an anthracycline compound of the following formula (I) or an acid addition salt thereof: ##STR1## These compounds are useful as intermediates in the synthesis of an anthracycline compound, M-R20X or M-R20X2, which has antitumor activity.Type: GrantFiled: June 30, 1987Date of Patent: May 23, 1989Assignee: Kirin Beer Kabushiki KaishaInventors: Hamao Umezawa, Hiroyuki Kawai, Shohachi Nakajima
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Patent number: 4833268Abstract: DL- or L-Threo-3-(3,4-dihydroxyphenyl)-N-methyl-serine which may also be termed as DL- or L-threo-adrenalinecarboxylic acid are now provided, which are new compounds useful for therapeutic treatment of Parkinson's disease and mental depression disease.Type: GrantFiled: July 30, 1987Date of Patent: May 23, 1989Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Toshiharu Nagatsu, Hirotaro Narabayashi, Tomio Takeuchi, Shuichi Iwadare, Ikuo Matsumoto, Junji Yoshizawa, Hajime Morishima, Koji Tomimoto