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).

  • Patent number: 4151347
    Abstract: A known nucleoside, coformycin and its related substances such as isocoformycin, 2'-deoxycoformycin and formycins present as a mixture of them may be separated from each other when an aqueous solution containing them is chromatographed on a column of a cation-exchanger having partially activated carboxylic groups as the ion-exchange function with using water or a buffer solution as the developing solvent.
    Type: Grant
    Filed: February 27, 1978
    Date of Patent: April 24, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Shinichi Kondo
  • Patent number: 4147861
    Abstract: A number of 1N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-6'N-methyl-3',4'-dideoxykanamyc in B derivatives have been found to possess excellent antibacterial activity against most kanamycin susceptible and resistant organisms. In particular, 1N-(DL-isoseryl)-6'N-methyl-3',4'-dideoxykanamycin B, 1N-(L-isoseryl)-6'-N-methyl-3',4'-dideoxykanamycin B, 1N-(L-4-amino-2-hydroxybutyryl)-6'N-methyl-3',4'-dideoxykanamycin B and 1N-(L-5-amino-2-hydroxyvaleryl)-6'N-methyl-3',4'-dideoxykanamycin B, or an acid addition salt thereof possess these highly desirable attributes.
    Type: Grant
    Filed: December 29, 1977
    Date of Patent: April 3, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Kenji Maeda, Shinichi Kondo, Sumio Umezawa
  • Patent number: 4147778
    Abstract: A novel anthracycline antibiotic complex designated herein as baumycin complex is produced by fermentation of a baumycin-producing strain of Streptomyces, e.g. Streptomyces coeruleorubidus ME 130-A4 (FERM-P3540, ATCC 31276). The complex and four bioactive components thereof designated baumycin A.sub.1, A.sub.2, B.sub.1 and B.sub.2 are useful as antibacterial and antitumor agents.
    Type: Grant
    Filed: May 16, 1977
    Date of Patent: April 3, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Masaaki Ishizuka, Hiroshi Naganawa, Toshikazu Oki, Taiji Inui
  • Patent number: 4144329
    Abstract: New antitumor agents designated MA 144-M.sub.1 and MA 144-M.sub.2, which are anthracycline glycosides and inhibit the growth of gram-positive bacteria, e.g. Staphyococcus aureaus, Bacillus subtilis and Sarcina lutea, and inhibit the growth of animal tumors such as leukemia L 1210, P 388 and sarcoma 180 are produced by fermentation of MA 144-producing strains of streptomyces and by the chemical or enzymatic conversion of aclacinomycin A or cinerubin A.
    Type: Grant
    Filed: March 24, 1977
    Date of Patent: March 13, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku KenkyuKai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Hiroshi Naganawa, Masaaki, all of Ishizuka, Norio Shibamoto, Toshikazu Oki, Taiji Inui
  • Patent number: 4140849
    Abstract: 1-N-(L-4-amino-2-hydroxybutyryl) derivatives of kanamycin C, 3'-deoxykanamycin C and 3',4'-dideoxykanamycin C have been prepared which possess high antibacterial activity against a wide variety of drug-resistant bacteria. These new derivatives are prepared by reacting L-4-amino-2-hydroxybutyric acid or a functional equivalent thereof with the 1-amino group of kanamycin C, 3'-deoxykanamycin C or 3',4'-dideoxykanamycin C.
    Type: Grant
    Filed: September 19, 1977
    Date of Patent: February 20, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Shinichi Kondo
  • Patent number: 4127714
    Abstract: New antitumor agents designated rhodirubin A and B, which are anthracycline glycosides and inhibit the growth of gram-positive bacteria and mammalian tumors, are produced by fermentation of rhodirubin-producing strains of Streptomyces, e.g. Streptomyces sp. ME 505-HEI (ATCC 31273).
    Type: Grant
    Filed: August 9, 1977
    Date of Patent: November 28, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Masaaki Ishizuka, Hiroshi Naganawa, Toshikazu Oki, Taiji Inui
  • Patent number: 4126606
    Abstract: The present invention relates to new physiologically active peptides, derivatives thereof and a process for preparation thereof. In particular, it relates to new tetrapeptides designated amastatins A.sub.1, A.sub.2, A.sub.3, B.sub.1 and B.sub.2 and derivatives thereof which have an inhibitory effect on aminopeptidase A and also show stimulation of antibody formation and to a process for preparation thereof by cultivating a strain belonging to the genus Streptomyces.FIELD OF THE INVENTIONThe present invention relates to new physiologically active peptides, derivatives thereof and a process for preparation thereof. In particular, it relates to new tetrapeptides designated amastatins A.sub.1, A.sub.2, A.sub.3, B.sub.1 and B.sub.2 and derivatives thereof which have an inhibitory effect on aminopeptidase A and also show stimulation of antibody formation and to a process for preparation thereof by cultivating a strain belonging to the genus Streptomyces.
    Type: Grant
    Filed: September 19, 1977
    Date of Patent: November 21, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada
  • Patent number: 4125706
    Abstract: A 1-N-(.alpha.-substituted-.omega.-aminoacyl)-3'-deoxyribostamycin, which is a useful antibiotic active against various drug-resistant bacteria, can be prepared advantageously by a process starting from a protected derivative of ribostamycin in the form of 1,6-carbamate and comprising the 3'-deoxygenation, the splitting of the carbamate linkage and the 1-acylation.
    Type: Grant
    Filed: April 14, 1976
    Date of Patent: November 14, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya
  • Patent number: 4120955
    Abstract: Kanamycin C, 3'-deoxykanamycin C and 3'4'-dideoxykanamycin C are obtained by a new process comprising treating the primary 6'-amino group of a tetra-N-protected derivative of kanamycin B, 3'-deoxykanamycin B and 3', 4'-dideoxykanamycin B with a nitrite to convert said amino group into hydroxyl group and then removing the protective groups. 3'-Deoxykanamycin C and 3', 4'-dideoxykanamycin C are new semi-synthetic aminoglycosidic antibiotics.
    Type: Grant
    Filed: May 23, 1977
    Date of Patent: October 17, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Shinichi Kondo
  • Patent number: 4107424
    Abstract: A new and useful 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivative of an aminoglycosidic antibiotic, including its deoxy derivative, such as kanamycin B, 3'-deoxyneamine, 3',4'-dideoxyneamine, 3',4'-dideoxyribostamycin or 3',4'-dideoxykanamycin B is now synthetized from the parent substance, aminoglycosidic antiobiotic. The new 1-N-[(S)-.alpha.-hydroxy-.omega.-aminoacyl] derivative shows a wider and/or higher antibacterial activity than the parent substance and is useful in the treatment of infections by gram-negative and gram-positive bacteria, including drug-resistant strains thereof. The preparation of this new derivative may be made by 1-N-acylating the parent aminoglycosidic antibiotic with (S)-.alpha.-hydroxy-.omega.-aminocarboxylic acid with the amino group being protected, and chromatographically separating the acylated products to isolate the desired 1-N-acyl derivative, followed by the removal of the amino-protecting group.
    Type: Grant
    Filed: July 23, 1976
    Date of Patent: August 15, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Sumio Umezawa, Kenji Maeda, Osamu Tsuchiya, Shinichi Kondo, Shunzo Fukatsu
  • Patent number: 4105658
    Abstract: There are disclosed two new antibiotics formerly denominated MC916-A and MC916-B and now called neothramycin A and neothramycin B which are potent inhibitors of the growth of leukemia cells, e.g. Leukemia L-1210 cells in mice. They are produced by controlled fermentation of Streptomyces FERM-P 2452 (A.T.C.C. 31123).
    Type: Grant
    Filed: February 19, 1976
    Date of Patent: August 8, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Shinichi Kondo, Masaaki Ishizuka, Hiroshi Naganawa
  • Patent number: 4104372
    Abstract: 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl)-derivatives of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A are provided as new and useful compounds which are active against gram-negative and gram-positive bacteria, including drug-resistant strains of these bacteria. Examples of these compounds include 1-N-((SR)-.beta.-amino-.alpha.-hydroxypropionyl)-3'-deoxykanamycin A, 1-N-((S)-.gamma.-amino-.alpha.-hydroxybutyryl)-3'-deoxykanamycin A, 1-N-((S)-.delta.-amino-.alpha.-hydroxyvaleryl)-3'-deoxykanamycin A and 1-N-((S)-.gamma.-amino-.alpha.-hydroxybutyryl)-6'-N-methyl-3'-deoxykanamyc in A. The compounds may be prepared by selective acylation of the 1-amino group of 3'-deoxykanamycin A or 6'-N-methyl-3'-deoxykanamycin A with a corresponding .alpha.-hydroxy-.omega.-amino-alkanoic acid.
    Type: Grant
    Filed: April 20, 1976
    Date of Patent: August 1, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya
  • Patent number: 4102999
    Abstract: There is provided a process for producing a stable macromomycin (hereinafter often referred to as MCR) powder which comprises adding a stablilizer selected from the group consisting of saccharides, amino acids and salts thereof, organic acid salts, inorganic acid salts and a chelating agent to a solution of macromomycin purified from fermentation broth prior to dehydration as by lyophilization.
    Type: Grant
    Filed: June 1, 1977
    Date of Patent: July 25, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi
  • Patent number: 4101650
    Abstract: Increased duration of inhibition of secretion of pepsin in man by oral administration of pepstatin is achieved by the use of a formulation in which pepstatin is coated on very small granules of sodium bicarbonate to form floating minicapsules.
    Type: Grant
    Filed: April 6, 1977
    Date of Patent: July 18, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventor: Hamao Umezawa
  • Patent number: 4091097
    Abstract: Compounds having the general formula ##STR1## wherein R.sup.2 is substituted either at the 4'-position or at the 5'-position and is hydrogen, fluoro, bromo, chloro, hydroxy or lower alkyl; R.sup.3 is chloro, bromo or lower alkyl; R.sup.4 is hydroxy, amino or lower alkoxy, and Z is hydrogen or lower alkyl and the nontoxic, pharmaceutically acceptable metal salts of said compounds when Z is hydrogen exhibit strong activities in inhibiting histidine decarboxylase and anthine oxidase.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: May 23, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Akira Takamatsu, Kenji Kayahara
  • Patent number: 4091202
    Abstract: As new semi-synthetic antibiotic derivative are provided N-methanesulfonic acid derivatives of 3',4'-dideoxykanamycin B which are less toxic than the parent antibiotic and have useful high antibacterial activity. They are produced by interacting 3',4'-dideoxykanamycin B, an aldehyde such as paraformaldehyde and sulfurous acid or an alkali metal sulfite reagent.
    Type: Grant
    Filed: September 16, 1976
    Date of Patent: May 23, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Sumio Umezawa, Shunzo Fukatsu, Shigeo Seki, Masao Murase, Shuntaro Yasuda
  • Patent number: 4078138
    Abstract: 3',4'-.alpha.-Epoxyneamine and its related aminoglycosidic antibiotic derivatives containing 3',4'-.alpha.-epoxyneamine moiety in the molecule thereof are now provided, which may be in the form of their amino-protected and partially hydroxyl-protected product and which are useful as intermediates for use in the synthetic production of therapeutically valuable 3'-deoxy derivatives of aminoglycosidic antibiotics.
    Type: Grant
    Filed: December 5, 1975
    Date of Patent: March 7, 1978
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Eiichi Akita, Yukio Horiuchi, Takeo Miyazawa, Toshio Yoneta, Sumio Umezawa, Hamao Umezawa
  • Patent number: 4072753
    Abstract: Compounds having the formula ##STR1## (the meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are indicated hereinafter) exhibit suppressive activity to various immune responses and can be employed in the therapy of immunological diseases, especially autoimmune diseases.
    Type: Grant
    Filed: February 17, 1977
    Date of Patent: February 7, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Akira Takamatsu, Shunro Mori
  • Patent number: 4071411
    Abstract: New antitumor agents named aclacinomycins A and B, which are anthracycline glycosides and inhibit the growth of various microorganisms e.g., Staphylococcus aureus, Micrococcus flavus, Corynebacterium bovis and inhibit the growth of animal tumors such as leukemia L1210 and P388 and lymphoma 6C3HED in mice and hepatomas in rats are produced by the fermentation of a microorganism belonging to the genus Streptomyces which has been designated Streptomyces galilaeus (MA144-M1 and A.T.C.C. 31133); they are recovered from the broth by conventional methods for recovering antibiotics.
    Type: Grant
    Filed: June 4, 1976
    Date of Patent: January 31, 1978
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Akira Takamatsu, Toshikazu Oki
  • Patent number: 4070458
    Abstract: A novel physiologically active peptide Val-X-Ala-X, in which X is 4-amino-3-hydroxy-6-methylheptanoic acid, which is prepared from R-Val-Val-X-Ala-X by the action of a microbial enzyme, N-acyl derivatives thereof which are produced by acylating said new peptide, and the processes for producing thereof and the microbial enzyme are disclosed.
    Type: Grant
    Filed: November 3, 1976
    Date of Patent: January 24, 1978
    Assignee: Sanraku-Ocean Co., Ltd.
    Inventors: Hamao Umezawa, Tomio Takeuchi, Takaaki Aoyagi, Akira Takamatsu, Taiji Inui, Hiroshi Tone, Hajime Morishama