Abstract: For the preparation of 4'-0-tetrahydropyranyladriamycin b, the 9,14-position of the starting adriamycin is previously protected with phenylboronic acid and then the 4'-position of the thus protected adriamycin is selectively tetrahydropyranylated. After the tetrahydropyranylation, the by-product of 4'-0-tetrahydropyranyladriamycin a is converted to the aimed product of 4'-0-tetrahydropyranyladriamycin b. The yield of the product of 4'-0-tetrahydropyranyladriamycin b is high.

Abstract: Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.4 --Bwherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula ##STR1## in which R.sub.1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R.sub.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula ##STR2## in which R.sub.3 and R.

Abstract: As new 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives are provided four compounds, namely 2'-deamino-2'-hydroxyistamycin B; 2'-deamino-2'-hydroxy-3-O-demethylistamycin B; 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxyistamycin B.sub.o ; and 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxy-3-O-demethylistamycin B.sub.o which all exhibit high antibacterial activity and low acute toxicity in combination. These new compounds are useful as antibacterial agent.

Abstract: Mycaminosyl tylonolide derivatives represented by the following general formula ##STR1## (wherein R.sup.1 denotes hydroxyl group, a lower alkanoyloxy group, benzoyloxy group, azido group, or amino group which mat optionally be substituted with a lower alkyl or a lower alkanoyl radical; R.sup.2 stands for hydrogen atom or hydroxyl group; R.sup.3 expresses hydrogen atom or formyl group; and means a double bond or a radical represented by ), and salts thereof.

Abstract: A stable, non-hygroscopic, crystalline .gamma.-form of bestatin is prepared from the .alpha.- or .beta.-form of bestatin by heating at a temperature of from about 148.degree. C. to the melting point of bestatin, or by suspending or kneading in certan specified solvents.

Abstract: This invention relates to method for suppressing a transplantation immunity and treating an allergic disease and an autoimmune disease in a mammal which comprises administering spergualin or a pharmaceutically acceptable salt thereof in effective amount to the said mammal.

Abstract: A stable, non-hygroscopic, crystalline .gamma.-form of bestatin is prepared from the .alpha.- or .beta.-form of bestatin by heating at a temperature of from about 148.degree. C. to the melting point of bestatin, or by suspending or kneading in certain specified solvents.

Abstract: L-aminoacylases S.sub.1 and S.sub.2 derived from actinomycetes and having physicochemical characteristics such that it is a L-aminoacylase which acts on a N-acyl-L-amino acid to give a L-amino acid, its substrate profile is wide, and it acts not only on a N-acyl derivative of a natural L-amino acid, but also on a N-acyl derivative of a synthetic L-amino acid, while it does not act on a N-acyl-D-amino acid, a DL-N-acetyl-.alpha.methylbenzylamine and a N-acetyl-D-glucosamine, etc.

Abstract: Plipastatin represented by the general formula ##STR1## wherein R.sub.1 is --C.sub.13 H.sub.27 or --C.sub.14 H.sub.29 ; and R.sub.2 is Ala or Val, or salts thereof, which is prepared by culturing a Plipastatin-producing strain belonging to the genus Bacillus to produce and accumulate Plipastatin in a cultured broth and then isolating Plipastatin from the cultured broth. Plipastatin exhibits an enzyme inhibiting activity against phospholipase A.sub.2, C and D and which will be useful as an immunosuppressive agent or as a type I anti-allergic agent.

Abstract: The antibiotics designated obelmycins exhibit high proliferation inhibiting action against leukemia cells and are effective as anti-cancer agents.

Abstract: New 3-[N-(mercaptoacyl)]amino-4-arylbutanoic acid derivatives are now provided, which exhibit analgesic activity and are effective to enhance the analgesia induced by a known analgesic compound, ]D-ala.sup.2,met.sup.5 ]-enkephalin (DAME).

Abstract: This invention relates to a novel 4'-demethyl-4-epipodophylltoxin derivative of the formula: ##STR1## (wherein R.sub.1 is a lower alkyl group; X.sub.1 and X.sub.2 are each a hydroxyl group or an amino group substituted by one or two lower alkyls, provided that either one of X.sub.1 and X.sub.2 is an amino group substituted by one or two lower alkyls and the other is a hydroxyl group) and salts thereof.

Abstract: The present invention relates to a stable medical composition for injection containing (1) a Spergualin of the formula: ##STR1## [wherein R is ##STR2## --(CH.sub.2).sub.6 --, --(CH.sub.2).sub.4 --CH.dbd.CH--, ##STR3## (wherein R' is a lower alkyl group having 1 to 4 carbon atoms), --(CH.sub.2).sub.8 --, or ##STR4## or a salt thereof and (2) at least one stabilizer selected from the group consisting of mannitol, maltose, dextran, lactose, cyclodextrin, gelatin, chondroitin sulfate, and human serum albumin; when R is ##STR5## mannitol is expected. A spergualin is useful as cancer control agents and immunomodulators.

Abstract: A protease adsorbent wherein valyl-glycyl-argininal is bound to a water-insoluble carrier and a process for purifying TPA utilizing the same.

Abstract: N-acyl-DL-3-(3,4-dihydroxyphenyl)serine or a catecholic hydroxyl-protected derivative thereof is stereospecifically de-acylated by reaction with a microorganism of the genus Streptomyces or Streptoverticillium having an acylase or with an extract of said microorganism containing said acylase, to produce L-3-(3,4-dihydroxyphenyl)serine or the hydroxyl-protected derivative thereof, with the N-acyl-D-3-(3,4-dihydroxyphenyl)serine compound remaining unaltered. The L-3-(3,4-dihydroxyphenyl)serine compound so produced can be separated from the N-acyl-D-3-(3,4-dihydroxyphenyl)serine compound owing to the difference in the properties of them.

Abstract: Disclosed is a novel physiologically active substance, MH435, represented by the formula: ##STR1## wherein R represents either of the following groups A and B A: --CH.dbd.CH--NHCHOB: --CH.sub.2 --CH.sub.2 --NHCHO.The substance MH435 has an inhibitory activity against tyrosine specific protein kinase, and the 50% inhibitory concentrations of the substances MH435-A and MH435-B are respectively 0.55 .mu.g/ml and 6.0 .mu.g/ml.

Abstract: A compound of the formula (I) ##STR1## which is identified as an actinonin has now been found to potentiate the immune response in animals bearing Ascites Sarcoma 180 tumor cells.

Abstract: New compounds, 2',3'-dideoxy-2'-fluorokanamycin A and 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives thereof, particularly 1-N-(DL- or L-3-amino-2-hydroxypropionyl)- and 1-N-(L-4-amino-2-hydroxybutyryl)-2',3'-dideoxy-2'-fluorokanamycins A are now provided, which are each useful as antibacterial agent. 2',3'-Dideoxy-2'-fluorokanamycin A is prepared by a process comprising condensing a 6-azido-4-O-protected-2,3,6-trideoxy-2-fluoro-.alpha.-D-ribo-hexopyranosyl bromide with the 4-hydroxyl group of a 6-O-(2',4',6'-tri-O-protected-3'-N-protected-3'-amino-3'-deoxy-.alpha.-D-g lucopyranosyl)-1,3-bis-N-protected-2-deoxystreptamine, reducing the resulting condensation product to convert its azido group into an amino group, and removing the remaining amino-protecting and hydroxyl-protecting groups from the reduction product.

Abstract: New arphamenine-related compounds are now provided, which are represented by the formula ##STR1## wherein R.sub.1 denots a hydrogen atom or an amino-protecting group, R.sub.2 denotes a dimethylpyrimidinyl group, R.sub.3 denotes a hydrogen atom or a hydroxyl group, and R.sub.4 denotes a hydrogen atom or a carboxyl-protecting group. The new arphamenine-related compounds exhibit a carboxypeptidase-inhibitory activity and also an immunopotentiating activity and are useful for potentiating the immune response in a living animal.

Abstract: The novel compound N-[(3-aminoproypl)aminobutyl]-Z-(F-guandino-3-hydroxyheptanamido)-2-methox yethanamide or a pharmaceutically acceptable salt thereof which has antitumor activity in experimental animals.