Patents Assigned to Zaidan Hojin
-
Patent number: 4209588Abstract: New anthracycline glycosides designated MA 144-G1, -G2, -L,-S1, -N1, -U1 and -Y which inhibit the growth of gram-positive bacteria and mammalian tumors are produced by fermentation of certain species of Streptomyces and by the chemical or enzymatic conversion of certain anthracycline glycosides. New microbiological and chemical processes are also provided for preparation of the anthracycline glycosides MA 144-S2 and -U2 which have been found to be identical with the previously reported anthracyclines, marcellomycin and musettamycin.Type: GrantFiled: July 27, 1978Date of Patent: June 24, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Toshikazu Oki, Taiji Inui
-
Patent number: 4209511Abstract: Aminoglycoside antibiotics biochemically transformed from Kanamycin A or Kanamycin B, which are represented by the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a methyl group and R.sub.2 represents an amino group or a hydroxyl group.Type: GrantFiled: January 3, 1979Date of Patent: June 24, 1980Assignees: Yamanouchi Pharmaceutical Co., Ltd., Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Yoshihiko Oka, Hitoshi Ishida, Moto Morioka, Yoso Numasaki, Tsutomu Yamafuji, Takashi Osono, Hamao Umezawa
-
Patent number: 4207313Abstract: New anthracycline glycosides designated MA 144-G1, -G2, -L, -S1, -N1, -U1 and -Y which inhibit the growth of gram-positive bacteria and experimental animal tumors are produced by fermentation of certain species of Streptomyces and by the chemical or enzymatic conversion of certain anthracycline glycosides. New microbiological and chemical processes are also provided for preparation of the anthracycline glycosides MA 144-S2 and -U2 which have been found to be identical with the previously reported anthracyclines, marcellomycin and musettamycin.Type: GrantFiled: October 3, 1977Date of Patent: June 10, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Toshikazu Oki, Taiji Inui
-
Patent number: 4204038Abstract: New antitumor agents designated MA 144-M.sub.1 and MA 144-M.sub.2, which are anthracycyline glycosides and inhibit the growth of gram-positive bacteria, e.g. Staphyococcus aureus, 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: GrantFiled: February 21, 1978Date of Patent: May 20, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Hiroshi Naganawa, Masaaki Ishizuka, Norio Shibamoto, Toshikazu Oki, Taiji Inui
-
Patent number: 4202824Abstract: Three, new physiologically active derivatives of esterastin are now provided, which inhibit the activity of esterase similarly to the parent esterastin and further exhibit a higher inhibiting activity against cholesterol esterase than the parent esterastin. These three new derivatives are tetrahydroesterastin which is produced by catalytic hydrogenation of esterastin; 3,5-di-hydroxy-2-hexylhexadeca-7,10-dienoic 1,3-lactone which is produced by alkaline hydrolysis of esterastin; and 3,5-di-hydroxy-2-hexylhexadecanoic 1,3-lactone which is produced either by alkaline hydrolysis of said tetrahydroesterastin or by catalytic hydrogenation of the product of the alkaline hydrolysis of esterastin.Type: GrantFiled: April 26, 1979Date of Patent: May 13, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi
-
Patent number: 4198480Abstract: 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: GrantFiled: March 15, 1978Date of Patent: April 15, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Masa Hamada, Masaaki Ishizuka, Hiroshi Naganawa, Toshikazu Oki, Taiji Inui
-
Patent number: 4198648Abstract: An integrated semiconductor device comprising: a first and a second static induction transistor each including a drain and a source, each having a first conductivity type, a current channel having the first conductivity type and located between the drain and the source, and a gate having a second conductivity type opposite to the first conductivity type and located adjacent to the current channel; and a third bipolar transistor including a collector and an emitter each having the second conductivity type, and a base having the first conductivity type and located between the collector and the emitter, the collector being connected to the gates of the first and second transistors and also to the drain of the second transistor, the source of the second transistor being connected to the source of the first transistor. The second transistor is operative for suppressing the occurrence of an unrequired excessive minority carrier injection in the first transistor.Type: GrantFiled: May 4, 1978Date of Patent: April 15, 1980Assignee: Zaidan Hojin Handotai Kenkyu ShinkokaiInventor: Jun-ichi Nishizawa
-
Patent number: 4196280Abstract: By protecting the aldehyde group of a macrolide series antibiotics with a cyclic acetal or thioacetal, novel macrolide derivatives can be produced from the macrolide series antibiotics by releasing successively, the sugar moieties bonded to the macrolide antibiotics.The novel macrolide derivatives obtained by this invention, that is, the derivatives of a macrolide series antibiotics produced by releasing partially or wholly the sugar moieties bonded are useful as intermediates for producing novel macrolide series antibiotics.Type: GrantFiled: March 3, 1978Date of Patent: April 1, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Sumio Umezawa, Hamao Umezawa, Kuniaki Tatsuta
-
Patent number: 4195170Abstract: New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.Type: GrantFiled: February 23, 1978Date of Patent: March 25, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Sumio Umezawa, Shigeo Seki, Shunzo Fukatsu, Shuntaro Yasuda
-
Patent number: 4189604Abstract: Bestatin, which is [(2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl]-L-leucine, and related compounds which inhibit aminopeptidase B, leucino aminopeptidase and Bleomycin hydrolase, enhance the anti-tumor effect of Bleomycin and exhibit an antifertility effect were synthesized and tested.Type: GrantFiled: June 24, 1977Date of Patent: February 19, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomohisa Takita, Rinzo Nishizawa, Tetsushi Saino
-
Patent number: 4189438Abstract: A new physiologically active substance named esterastin is now provided, which inhibits the activity of esterase and is useful as an immunosuppressive drug. Esterastin is produced by cultivating a microorganism Streptomyces MD4-C1 identified as FERM-P 3723 or ATCC. 31336 in a culture medium under aerobic conditions and recovering it from the resulting culture.Type: GrantFiled: January 30, 1978Date of Patent: February 19, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Masaaki Ishizuka
-
Patent number: 4185156Abstract: 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: GrantFiled: September 15, 1978Date of Patent: January 22, 1980Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Tetsushi Saino, Michinori Koyama
-
Patent number: 4179573Abstract: 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: GrantFiled: August 19, 1977Date of Patent: December 18, 1979Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada, Yoshiro Okami
-
Patent number: 4170642Abstract: Novel derivatives of kanamycin, 1-N-(L-4-amino-2-hydroxy butyryl)-6'-N-alkylkanamycins, have been prepared which possess improved antibacterial activity against gram-positive and gram-negative bacteria including kanamycin-resistant strains.Type: GrantFiled: March 12, 1975Date of Patent: October 9, 1979Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Kenji Maeda, Shinichi Kondo, Sumio Umezawa, Osamu Tsuchiya, Shunze Fukatsu
-
Patent number: 4169939Abstract: A clinically valuable antibiotic, 3',4'-dideoxykanamycin B is now produced by a reduced number of consecutive steps in an improved overall yield by new processes starting from kanamycin B via intermediate derivatives of kanamycin B in which all the five amino groups are protected with an unsubstituted or substituted benzyloxycarbonyl group and possibly the 2"-hydroxyl group may be protected with a lower alkylsufonyl, arylsulfonyl or aralkylsulfonyl group.Type: GrantFiled: November 14, 1977Date of Patent: October 2, 1979Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya
-
Patent number: 4167448Abstract: 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: GrantFiled: June 16, 1978Date of Patent: September 11, 1979Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Takaaki Aoyagi, Tomio Takeuchi, Masa Hamada
-
Patent number: 4164567Abstract: There is provided a process for recovering macromomycin (hereinafter referred to as MCR) which comprises adding coagulants or coagulants and neutralizers to a culture filtrate saturated with ammonium sulfate and collecting the resulting precipitate containing MCR in a high yield at low centrifugal force. From the precipitate obtained, MCR powders can be prepared according to the methods described in U.S. Pat. No. 3,595,954 and others.Type: GrantFiled: May 31, 1977Date of Patent: August 14, 1979Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi
-
Patent number: 4163839Abstract: A novel, unique nucleoside, 3-.beta.-D-ribofuranosyl-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-7-o l, named isocoformycin, of the formula ##STR1## is provided by ring expansion of derivatives of 9-.beta.-D-ribofuranosyl-6-hydroxymethyl-1,6-dihydropurine. Isocoformycin markedly inhibits deaminating enzymes which inactivate formycin and adenine arabinoside (also known as ara-A and Vidarabine). Formycin and adenine arabinoside are used as antiviral and antitumor agents in mammals and birds and isocoformycin is advantageous to prolong the activity and effect of formycin and adenine arabinoside.Type: GrantFiled: December 9, 1977Date of Patent: August 7, 1979Assignee: Zaidan Hojin Biselbutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Tomio Takeuchi, Shinichi Kondo, Masami Shimazaki
-
Patent number: 4160259Abstract: In a transistor structure having a pair of current electrodes and a control electrode, at least one control electrode is added to vary the negative feed-back resistance in the current path. In a typical example, both the triode-like and the pentode-like characteristics are provided by the control in the voltage applied to the additional control electrode for varying the negative feed-back resistance r.sub.s, thereby changing the product G.sub.m .multidot.r.sub.s from less than unity to greater than unity where G.sub.m is the transconductance.Type: GrantFiled: December 27, 1976Date of Patent: July 3, 1979Assignee: Zaidan Hojin Handotai Kenkyu ShinkokaiInventor: Jun-ichi Nishizawa
-
Patent number: 4156078Abstract: A useful antibiotic, 3',4'-dideoxykanamycin B can be prepared in shortened steps and in an improved overall yield by a new process starting from kanamycin B via new intermediate derivatives of kanamycin B in which all the amino groups and possibly the 2"-hydroxyl group are protected with sulfonyl-type protecting groups selected from lower alkyl-, aryl- and aralkyl-sulfonyl groups.Type: GrantFiled: November 26, 1976Date of Patent: May 22, 1979Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Hamao Umezawa, Sumio Umezawa, Tsutomu Tsuchiya