序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
1 Macrolide antibiotics, microbial production and relative microbes, novel intermediates and pharmaceutical composition JP218082 1982-01-09 JPS57140779A 1982-08-31 RUCHIAANO TOSUKANO; REONARUDO EMU KATSUPERETSUTEI
2 New macrolide compound, preparation thereof and microorganism using and producing same JP218182 1982-01-09 JPS57138384A 1982-08-26 REONARUDO EMU KATSUPERETSUTEI; ROBERUTO SUPAGUNORI; RUCHIAANO TOSUKANO
3 JPH0224279B2 - JP218082 1982-01-09 JPH0224279B2 1990-05-29 RUCHIAANO TOSUKANO; REONARUDO EMU KATSUPERETSUTEI
4 Anti/malignanttumor containing the same as active ingredients JP3968876 1976-04-07 JPS52136159A 1977-11-14 UMEZAWA KENJI; TAKEUCHI TOMIO; OSANAWA HIROSHI; ISHIZUKA MASAAKI; SHIBAMOTO NORIO; OKI SHIYUNICHI; INUI TAIJI
PURPOSE:Anthracycline'glycocides of formula (R is H or OH), their nontoxic acid salts and their complexes, e.g. MA144-M1 (R=H), MA144-M2 (R=OH).
5 JPH0365944B2 - JP218182 1982-01-09 JPH0365944B2 1991-10-15
6 Clavam derivative JP1257582 1982-01-30 JPS57144290A 1982-09-06 HANSU TSUEENERU; MARUTEIN BANNINGU; BERUNDO KURONE; AKUSERU TSUIIKU; HEINRITSUHI PETERU
The novel antibiotic "Tü 1718", which has been produced by the fermentation of a novel microorganism, and the components and derivatives of this antibiotic, in particular its main component, a clavam compound of the following formula and its derivatives, such as esters, ethers, thioesters and thioethers. The novel microorganism is strain Tü 1718 of the species Streptomyces antibioticus, subsp. antibioticus, which has been isolated from a soil sample from Northern Thailand. The novel antibiotic and its components and derivatives have an antibacterial, antifungal and tumour-inhibiting action.
7 JPS5438100B2 - JP3968876 1976-04-07 JPS5438100B2 1979-11-19
8 Streptomyces antibioticus ATCC 31771 and process for obtaining same US548323 1983-11-03 US4560662A 1985-12-24 Leonardo M. Cappelletti; Roberto Spagnoli; Luciano Toscano
The fermentation of a substrate selected among erythronolide B, erythronolide A and erythronolide A oxime with a novel mutant, Streptomyces antibioticus ATCC 31771, obtained from an industrial stock for the production of oleandomycin, said novel mutant being incapable of producing the same oleandomycin, permits novel macrolide antibiotics to be produced, having not only an activity range like that of erythromycin, but characterized by a greater stability in acidic environment, whereby for the administration of the antibiotic it is no longer necessary to have recourse to esters and/or salts highly toxic for the organism.
9 Process for producing new antitumor anthracycline antibiotics US928637 1978-07-27 US4209588A 1980-06-24 Hamao Umezawa; Tomio Takeuchi; Toshikazu Oki; Taiji Inui
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.
10 Anthracycline antibiotics US838617 1977-10-03 US4207313A 1980-06-10 Hamao Umezawa; Tomio Takeuchi; Toshikazu Oki; Taiji Inui
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.
11 2-Hydroxyaclacinomycin A and 2-hydroxyaklavinone and process for preparing same US184518 1980-09-05 US4386198A 1983-05-31 Toshikazu Oki; Akihiro Yoshimoto; Kageaki Kouno; Taiji Inui; Tomio Takeuchi; Hamao Umezawa
New anthracycline compounds, 2-hydroxyaclacinomycin A having potent antitumor activity and lower toxicity, 2-hydroxyaklavinone as an useful precursor for producing anthracycline glycosides, and a process for the production thereof by microbial conversion method are disclosed.
12 Method of producing anthracycline antibiotics US37804 1979-05-10 US4245045A 1981-01-13 Hamao Umezawa; Tomio Takeuchi; Toshikazu Oki; Taiji Inui
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.
13 Process for producing antibiotics MA 144-M.sub.1 and MA 144-M.sub.2 US17525 1979-03-05 US4219622A 1980-08-26 Hamao Umezawa; Tomio Takeuchi; Hiroshi Naganawa; Masaaki Ishizuka; Norio Shibamoto; Toshikazu Oki; Taiji Inui
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 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.
14 Semisynthetic macrolidic antibiotics, intermediate compounds for their preparation and related pharmaceutical compositions containing compounds for their preparation and related pharmaceutical compositions containing them US570833 1984-01-16 US4540662A 1985-09-10 Luciano Toscano; Leonard M. Cappelletti
From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-B-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-B-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A,B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the marcolide antibiotics are obtained.The preparation of the aforesaid substrate comprises the convention of erythronolide A, erythronolide B or 3-O-mycarosyl-erythronolide B into the corresponding hemiacetal, the reaction of the latter with a compound capable of generating electrophlic fluorine and the opening of the resulting acetal with aqueous acid.
15 Semisynthetic macrolidic antibiotics, intermediate compounds for their preparation and related pharmaceutical compositions containing them US338105 1982-01-08 US4439426A 1984-03-27 Luciano Toscano; Leonardo M. Cappelletti
From the fermentation carried, out with mutants blocked in the synthesis respectively of erythromycin and of oleandomycin, namely Streptomyces erythreus ATCC 31772 and Streptomyces antibioticus ATCC 31771, using as the substrate a derivative of erythronolide A, namely (8S)-8-fluoroerythronolide A, a derivative of erythronolide B, namely (8S)-8-fluoroerythronolide B, or a derivative of 3-O-mycarosyl-erythronolide B, namely 3-O-mycarosyl-(8S)-fluoroerythronolide B, the corresponding (8S)-8-fluoro derivatives of the erythromycins A, B, C and D, as well as 3-O-oleandrosyl-5-desosaminyl-(8S)-8-fluoroerythronolide A and 3-O-oleandrosyl-5-O-desosaminyl-(8S)-8-fluoroerythronolide B, all belonging to the class of the macrolide antibiotics are obtained.The preparation of the aforesaid substrate comprises the convention of erythronolide A, erythronolide B or 3-O-mycarosyl-erythronolide B into the corresponding hermiacetal, the reaction of the latter with a compound capable of generating electrophlic fluorine and the opening of the resulting acetal with aqueous acid.
16 3-O-Oleandrosyl-5-O-desosaminyl erythronolide compounds US338117 1982-01-08 US4429115A 1984-01-31 Leonardo M. Cappelletti; Roberto Spagnoli; Luciano Toscano
The fermentation of a substrate selected among erythronolide B, erythronolide A and erythronolide A oxime with a novel mutant, Streptomyces antibioticus ATCC 31771, obtained from an industrial stock for the production of oleandomycin, said novel mutant being incapable of producing the same oleandomycin, permits novel macrolide antibiotics to be produced, having not only an activity range like that of erythromycin, but characterized by a greater stability in acidic environment, whereby for the administration of antibiotic it is no longer necessary to have recourse to esters and/or salts highly toxic for the organism.
17 2-Pyridyl-2-thiazoline-4-carboxylic acid derivatives US285909 1981-07-23 US4406905A 1983-09-27 Hans Zahner; Hans-Ulrich Naegeli; Heinrich Peter
The invention relates especially to 2-(3'-hydroxypyrid-2'-yl)-2-thiazoline-4-carboxylic acid derivatives of the formula (I) and salts and also certain metal complexes of these compounds, processes for their manufacture, pharmaceutical agents containing such compounds and the use of these compounds. ##STR1## In the formula, R.sup.1 represents free, etherified or esterified hydroxy, R.sup.2 represents hydrogen or an aliphatic, carbocyclic or carbocyclic-aliphatic radical having 1-12 carbon atoms, and R.sup.3 represents hydrogen or an unsubstituted aliphatic radical having 1-7 carbon atoms.The compounds of the formula (I) can be used, for example, for the abstraction of heavy metals from the organism of warm-blooded animals and/or they have an antibiotic action.
18 Process for preparing antibiotics MA 144-M.sub.1 and MA 144-M.sub.2 US879536 1978-02-21 US4204038A 1980-05-20 Hamao Umezawa; Tomio Takeuchi; Hiroshi Naganawa; Masaaki Ishizuka; Norio Shibamoto; Toshikazu Oki; Taiji Inui
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.
19 Anthracycline glycosides from streptomyces US898065 1978-04-20 US4192915A 1980-03-11 Hamao Umezawa; Tomio Takeuchi; Masa Hamada; Masaaki Ishizuka; Hiroshi Naganawa; Toshikazu Oki; Taiji Inui
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).
20 Antibiotic 1745A/X and methods for the production thereof US887160 1978-03-16 US4152424A 1979-05-01 Richard W. Kierstead; Ronald A. LeMahieu; David Pruess
A new antibiotic, designated as antibiotic 1745A/X, is produced by the fermentation of the known microorganism Streptomyces antibioticus, ATCC 11891, using the novel compound erythronolide A oxime as the substrate. This new antibiotic is useful an an antibacterial agent.
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