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: 4634688
    Abstract: A new compound, 3'-fluoro-3'-deoxykanamycin A is now provided, which is active against gram-negative and gram-positive bacteria, including kanamycin-resistant strains of bacteria and is useful as antibacterial agent for therapeutic treatment of bacterial infections. This new compound is produced by a process comprising reacting a 6-azido-2,4-di-O-protected-3,6-dideoxy-3-fluoro-.alpha.-D-glucopyranosyl bromide with the 4-hydroxyl group of a 6-O-(2'-O-protected-3'-N-protected-3'-amino-4',6'-di-O-protected-3'-deoxy- .alpha.-D-glucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the azido group of the resulting reaction product into an amino group, and removing the remaining protective groups from the reduction product.
    Type: Grant
    Filed: July 25, 1985
    Date of Patent: January 6, 1987
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Yoshiaki Takahashi
  • Patent number: 4612372
    Abstract: Novel tylosin derivatives are represented by formula: ##STR1## wherein R represents a hydrogen atom, an acetyl group or a propionyl group; X represents a group --CO-- or --SO.sub.2 --; Y represents a fluorine atom, an acetyl group, a methanesulfonyl group, a methylthio group, a benzoyl group or a methoxy group bound to the benzyl group at the 2-position or 4-position; and Z represents a hydrogen atom or a D-mycinose residue: ##STR2## The tylosin derivatives which are antibiotics of macrolide type provide improved antibacterial activity and improved ability of absorption and excretion in vivo.
    Type: Grant
    Filed: July 12, 1985
    Date of Patent: September 16, 1986
    Assignee: Sanraku Incorporated
    Inventors: Takeo Yoshioka, Miharu Maeda, Rokuro Okamoto, Yasutaka Shimauchi, Tomoyuki Ishikura, Tsutomu Sawa, Tomio Takeuchi, Hamao Umezawa
  • Patent number: 4612371
    Abstract: Novel anthracycline antibiotics characteristic of Ring A of the anthracycline skeleton are produced by microorganisms belonging to the genus Streptomyces and are useful as anti-cancer agents.
    Type: Grant
    Filed: July 18, 1985
    Date of Patent: September 16, 1986
    Assignee: Sanraku Incorporated
    Inventors: Akihiro Yoshimoto, Shizuka Fujii, Katsuro Kubo, Tomoyuki Ishikura, Tsutomu Sawa, Tomio Takeuchi, Hamao Umezawa
  • Patent number: 4603015
    Abstract: Glyoxylylspermidine, an intermediate for 15-deoxyspergualin-related compounds, is prepared in an oxidative cleavage reaction.
    Type: Grant
    Filed: February 27, 1985
    Date of Patent: July 29, 1986
    Assignees: Takara Shuzo Col., Ltd., Nippon Kayaku Kabushiki Kaisha
    Inventors: Yoshihisa Umeda, Makoto Moriguchi, Teruya Nakamura, Akio Fujii, Tomio Takeuchi, Hamao Umezawa
  • Patent number: 4595698
    Abstract: 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: Grant
    Filed: June 2, 1983
    Date of Patent: June 17, 1986
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Masaaki Ishizuka
  • Patent number: 4592999
    Abstract: This invention is to provide a new microbial process for producing daunomycin by a mutant strain belonging to the genus Streptomyces.
    Type: Grant
    Filed: July 18, 1983
    Date of Patent: June 3, 1986
    Assignee: Sanraku Incorporated
    Inventors: Hamao Umezawa, Tomio Takeuchi, Kageaki Kouno, Tomoyuki Ishikura, Akihiro Yoshimoto, Yukio Takatsuki, Hiroyasu Tobe
  • Patent number: 4576931
    Abstract: Novel 23-C-substituted mycaminosyl tylonolide of the general formula (I) ##STR1## wherein R.sup.1 represents a lower alkyl group, an aryl group, a lower alkenyl group or a lower alkynyl group, R.sup.2 represents a hydrogen atom or a hydroxyl group.These compounds have excellent antibacterial activities.
    Type: Grant
    Filed: April 3, 1985
    Date of Patent: March 18, 1986
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai (Microbial Chemistry Research Foundation)
    Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Tomio Takeuchi, Akihiro Tanaka, Shuichi Sakamoto
  • Patent number: 4568490
    Abstract: An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.
    Type: Grant
    Filed: June 12, 1985
    Date of Patent: February 4, 1986
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Akio Fujii, Yasuhiko Muraoka, Tokuji Nakatani, Takeyo Fukuoka, Katsutoshi Takahashi
  • Patent number: 4567165
    Abstract: As new semi-synthetic antibiotic derivatives are provided N-methanesulfonic acid derivatives of 3-demethoxyistamycin B which are less toxic than the parent 3-demethoxyistamycin B but retain usefully high antibacterial activity of the parent antibiotic. The new derivatives are produced by a method of N-sulfomethylation where 3-demethoxyistamycin B is reacted with an aldehyde such as paraformaldehyde and sulfurous acid or sulfite reagent.
    Type: Grant
    Filed: May 8, 1984
    Date of Patent: January 28, 1986
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Shinichi Kondo
  • Patent number: 4565861
    Abstract: An anthracycline, serirubicin, of the formula: ##STR1## wherein R represents the substituent: ##STR2## is produced by a process which comprises cultivating a strain of Streptomyces in a suitable culture medium under aerobic conditions, said strain having the ability to produce the anthracycline compound, serirubicin, and then recovering the anthracycline compound, serirubicin, from the cultured medium. This serirubicin, or an acid addition salt of the serirubicin, can be contained as the active ingredient in anti-tumor agents and in pharmaceutical compositions for treatment of infections induced by gram-positive microorganisms, whereby good results are attainable.
    Type: Grant
    Filed: January 3, 1984
    Date of Patent: January 21, 1986
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Hiroshi Naganawa, Tsutomu Sawa, Takeshi Uchida, Masaya Imoto
  • Patent number: 4559362
    Abstract: This invention relates to an immunopotentiator or an immunopotentiating method using spermidine or its pharmacologically acceptable salt as an active ingredient.
    Type: Grant
    Filed: November 9, 1983
    Date of Patent: December 17, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masaaki Ishizuka
  • Patent number: 4556735
    Abstract: The invention relates to Spergualin-related compounds of the formula: ##STR1## (wherein R.sub.1 is a lower alkylene group which may be substituted by a hydroxymethyl group; X is a hydrogen atom or a halogen atom; m and n are each 0 or an integer of 1 to 5) and salts thereof and a process for producing the same.
    Type: Grant
    Filed: February 27, 1985
    Date of Patent: December 3, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyukai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Rinzo Nishizawa, Katsutoshi Takahashi, Teruya Nakamura, Yoshihisa Umeda
  • Patent number: 4550159
    Abstract: An anthracycline compound, ditrisarubicin, of the formula: ##STR1## wherein R represents one of the following substituents (A), (B), and (C): ##STR2## is produced by a process which comprises cultivating a strain of Streptomyces in a suitable culture medium under aerobic conditions, said strain having the ability to produce the anthracycline compound, ditrisarubicin, and then recovering the anthracycline compound, ditrisarubicin, from the cultured medium. This ditrisarubicin, or an acid addition salt of the ditrisarubicin, can be contained as the active ingredient in antitumor agents and in pharmaceutical compositions for treatment of infections induced by gram-positive microorganisms, whereby good results are attainable.
    Type: Grant
    Filed: October 25, 1983
    Date of Patent: October 29, 1985
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Hiroshi Naganawa, Tsutomu Sawa, Takeshi Uchida, Masaya Imoto
  • Patent number: 4547567
    Abstract: This invention relates to novel 4'-demethyl-4-epipodophyllotoxin derivatives represented by the general formula (I), and salts thereof: ##STR1## wherein R is a lower alkyl group, and X.sub.1 and X.sub.2 are independently a hydroxyl group or an amino group, the one being an amino group and the other being a hydroxyl group. These novel derivatives have a high carcinostatic activity and a relatively high water solubility and hence are expected to be useful as carcinostatics.
    Type: Grant
    Filed: July 18, 1984
    Date of Patent: October 15, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Shinichi Kondo, Wataru Tanaka, Tomohisa Takita, Yoshio Nishimura, Hiroshi Yoshikawa
  • Patent number: 4547492
    Abstract: 1-N-(L-3-amino-2-hydroxypropionyl)-2',-3'-dideoxykanamycin A and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'-dideoxykanamycin A are now provided which each is a new compound useful as antibacterial agent. The new compounds each is produced by acylating the 1-amino group of 2',3'-dideoxykanamycin A with L-3-amino-2-hydroxypropionic or L-4-amino-2-hydroxybutyric acid.
    Type: Grant
    Filed: August 10, 1984
    Date of Patent: October 15, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya, Toshio Yoneta, Shunzo Fukatsu
  • Patent number: 4537880
    Abstract: An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.
    Type: Grant
    Filed: July 27, 1984
    Date of Patent: August 27, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Akio Fujii, Yasuhiko Muraoka, Tokuji Nakatani, Takeyo Fukuoka, Katsutoshi Takahashi
  • Patent number: 4530998
    Abstract: This invention relates to 2'-deoxy-oxanosine represented by the following formula: ##STR1## and process for the preparation thereof. This new compound exhibits a growth inhibiting action to gram-negative bacteria and has a carcinostatic action.
    Type: Grant
    Filed: March 5, 1984
    Date of Patent: July 23, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku KenkyuKai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Masaaki Ishizuka, Tomohisa Takita, Nobuyoshi Shimada, Kuniki Kato
  • Patent number: 4529549
    Abstract: This invention relates to a novel spergualin-related compound and a process for the production thereof. The novel compound, which has a high antitumor activity, is represented by the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, hydroxyl group, or an aliphatic acyloxy group having 1 to 10 carbon atoms, R.sub.2 represents an amino acid residue (except for the residue of .alpha.-hydroxyglycine) formed by removing one hydrogen atom and hydroxyl group from respectively the .alpha.- or .omega.-amino group and the .alpha.-carboxyl group of an .alpha.- or .omega.-amino acid, said amino acid residue forming acid amide linkages with the adjacent carbonyl group and amino group, and m is an integer of 4 to 6.
    Type: Grant
    Filed: August 18, 1983
    Date of Patent: July 16, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Rinzo Nishizawa, Katsutoshi Takahashi, Teruya Nakamura, Yoshihisa Umeda
  • Patent number: 4525299
    Abstract: (-)-15-Deoxyspergualin represented by the following formula ##STR1## a salt thereof having antitumor activity, process for the preparation thereof and intermediate thereof.
    Type: Grant
    Filed: May 10, 1983
    Date of Patent: June 25, 1985
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tomio Takeuchi, Shinichi Kondo
  • Patent number: 4525465
    Abstract: A biospecific adsorbent comprising pyroglutamyl-lysyl-leucyl-argininal combined with a water-insoluble support is provided. This biospecific adsorbent is useful as an adsorbent for use in affinity chromatography and can be utilized for the purification of proteases such as urokinase.
    Type: Grant
    Filed: October 7, 1983
    Date of Patent: June 25, 1985
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Tetsuya Someno, Kazuo Kato, Tetsushi Saino, Shinichi Ishii, Tomio Takeuchi, Hamao Umezawa