Patents by Inventor Takaaki Aoyagi

Takaaki Aoyagi 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: 4185156
    Abstract: The compounds of this invention represented by the following formula: ##STR1## (wherein R is hydrogen atom, an alkyl group having C.sub.1 to C.sub.4, a hydroxy group or a halogen atom) can be obtained by condensing the compounds represented by the following formula: ##STR2## wherein R is as defined above, X is hydrogen atom, and Y is hydrogen atom or an amino protecting group or reactive derivatives thereof with (S)-arginine according to a method commonly employed in the peptide chemistry.The peptides according to this invention have strong inhibitory activity against aminopeptidase B, can raise immunity of the organisms and prove useful for inhibiting transfer of cancer and relapse thereof. Also, when used jointly with Bleomycin which is an antitumor agent, they can greatly enhance the antitumor effect of said agent.
    Type: Grant
    Filed: September 15, 1978
    Date of Patent: January 22, 1980
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Tetsushi Saino, Michinori Koyama
  • Patent number: 4179573
    Abstract: This invention provides the amino acid (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoic acid which is prepared by hydrolysis of bestatin. Bestatin is a chemical which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, has the following structure ##STR1## and is prepared by cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).
    Type: Grant
    Filed: August 19, 1977
    Date of Patent: December 18, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Yoshiro Okami
  • Patent number: 4167448
    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.
    Type: Grant
    Filed: June 16, 1978
    Date of Patent: September 11, 1979
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada
  • 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: 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
  • Patent number: 4055468
    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: October 25, 1977
    Assignee: Sanraku-Ocean Co., Ltd.
    Inventors: Hamao Umezawa, Tomio Takeuchi, Takaaki Aoyagi, Akira Takamatsu, Taiji Inui, Hiroshi Tone, Hajime Morishima
  • Patent number: 4052449
    Abstract: This invention provides a new chemical named bestatin which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine and has the following structure: ##STR1## and also provides a process for the production thereof which comprises cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).
    Type: Grant
    Filed: May 27, 1976
    Date of Patent: October 4, 1977
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Yoshiro Okami
  • Patent number: 4029547
    Abstract: This invention provides a new chemical named bestatin which inhibits aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase, enhances the antitumor effect of bleomycin, has the chemical name [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine and has the following structure: ##STR1## and also provides a process for the production thereof which comprises cultivating a strain of streptomyces which produces bestatin in a nutrient medium under aerobic conditions until substantial activity inhibitory to aminopeptidase B is imparted to said cultured medium and then recovering said bestatin from said cultured medium. A preferred strain is Streptomyces olivoreticuli FERM-P No. 2590 (A.T.C.C. 31159).
    Type: Grant
    Filed: May 27, 1976
    Date of Patent: June 14, 1977
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Yoshiro Okami
  • Patent number: 3975366
    Abstract: A process for producing new pepstatins having anti-pepsin activity by cultivating a pepstatin producing strain in a nutrient medium containing assimilable carbon sources and nitrogen sources, and extracting the new pepstatins from the cultivated broth or medium.
    Type: Grant
    Filed: February 4, 1975
    Date of Patent: August 17, 1976
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tetsuji Miyano, Kohtaro Funaishi, Tomio Takeuchi, Takaaki Aoyagi
  • Patent number: 3963579
    Abstract: A process for producing pepstatins by means of a microorganism belonging to Streptomyces and producing pepstatins, wherein at least one amino acid selected from the group consisting of L-leucine, L-valine, L-alanine, L-aspartic acid, L-glutamic acid, and L-lysine is added to the reaction medium, which also contains an energy source.
    Type: Grant
    Filed: October 10, 1974
    Date of Patent: June 15, 1976
    Assignee: Sanraku-Ocean Co., Ltd.
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Akira Takamatsu, Taiji Inui
  • Patent number: 3950405
    Abstract: A trans isomer of 4-cyanoncyclohexane-1-carboxylic acid or its lower alkyl ester is reduced in a solvent in the presence of a hydrogenating catalyst, and hydrolyzing the produced ester in case the starting trans-isomer is a lower alkyl ester, then the trans-4-aminomethyl-cyclohexane-1-carboxylic acid is recovered from the reaction mixture.
    Type: Grant
    Filed: June 4, 1969
    Date of Patent: April 13, 1976
    Assignee: Mitsubishi Chemical Industries Ltd.
    Inventors: Atsuji Okano, Shizuo Kadoya, Takeo Naito, Takaaki Aoyagi, Masao Shimizu