Abstract: An object of this invention is to provide a novel process for the synthesis of a 2'-deoxy-2'-halocoformycin having an inhibitory activity against adenosine deaminase in a practically high yield. Thus, there is provided a process comprising multi-stage reactions with using as the starting intermediate a tert-butyl 1-(3,5-di-O-acyl-2-deoxy-2-halo-.beta.-D-ribofuranosyl or arabinofuranosyl)-5-aminoimidazole-4-carboxylate of formula (II) ##STR1## whereby there are produced a 2'-deoxy-2'-halocoformycin or a 2'-deoxy-2'-epi-2'-halocoformycin of formula (I-a) ##STR2## and also a 2'-deoxy-8-epi-2'-halocoformycin or a 2'-deoxy-8,2'-diepi-2'-halocoformycin of formula (I-b) ##STR3## It is expectable that a 2'-deoxy-2'-halocoformycin and epimers thereof are useful as a drug for lymphocytic leukemias and as drugs for various diseases attributable to the actions of adenosine deaminase.

Abstract: Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group, and 7-O-(2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)adriamycinon e derivative which is an adriamycinone derivative represented by formula (II): ##STR2## have now been newly synthesized. The novel anthracycline derivatives having the general formula (I) and formula (II), respectively, show excellent anticancer or antitumor activities and are of low toxicities. These novel compounds are very useful as anticancer or antitumor agents and are expected to be useful for the therapeutic treatments of a variety of cancers and tumors, similarly to daunomycin or adriamycin.

Abstract: A novel amino acid derivative represented by the general formula (I) shown below or a salt thereof have now been provided by chemical synthesis, and it has been found that these new compounds stimulate proliferation and physiological activities of the T cells of mammals, have an immunomodulating activity and also have an antitumor activity or a carcinostatic activity. It has also been found that these new compounds have an effect of stimulating the proliferation of hematopoietic stem cells. ##STR1## wherein y is 0 or 1; R.sup.1 represents an unsubstituted C.sub.1 -C.sub.8 alkyl group or others;R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group or others;R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.8 alkyl group or others;R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.3 alkyl group or others;R.sup.5 represents a group --OR.sup.42, a group ##STR2## or others.

Abstract: To provide novel fluorine-containing anthracycline derivatives having high antitumor activities and a solubility in water, there have now been synthesized a 7-O-(2,6-dideoxy-2-fluoro-3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-.alpha.-L-talopyranosyl)daunomycinone or -adriamycinone of general formula (I) shown below, as well as a 7-O-(3-O- or -4-O- or -3,4-di-O-aminoalkanoyl-2,6-dideoxy-2,6,6,6-tetrafluoro-.alpha.-L-talopyra nosyl- or -2,6-dideoxy-6,6,6-trifluoro-.alpha.-L-lyxo-hexopyranosyl)adriamycinone of general formula (II) shown below:General formula (I) ##STR1## General formula (II) ##STR2## wherein either one or both of A.sup.1 and A.sup.2 is or are an .alpha.-amino acid residue or an .omega.-amino acid residue and T denotes a fluorine or hydrogen atom. The novel fluorine-containing anthracycline derivatives of general formulae (I) and (II) are highly active against tumors and soluble in water, and they are useful as antitumor agents administrable in the form of injectable solution.

Abstract: 2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin are synthesized in this invention through a multi-stage process via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.- and -.beta.-D-ribofuranosyl bromides. Further, according to this invention, 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin are synthesized by a multi-stage process starting from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-.alpha.-D-arabinofuranosyl bromide. These four 2'-fluoro derivatives of coformycin are novel compounds and have high enzyme-inhibitory activities against adenosine deaminase. In particular, these novel compounds are useful substances which exhibit therapeutic effects on acute lymphocytic leukemias due to their high enzyme-inhibitory activities above-mentioned. In addition, a variety of intermediates are obtained as novel compounds which are useful for the synthesis of the aforesaid novel 2'-fluoro derivatives of coformycin.

Abstract: The invention relates to novel pyrrolidine derivatives represented by formula (1): ##STR1## wherein: R1 represents (1) a lower alkyl group having 1 to 6 carbon atoms, or (2) a 3- to 15-membered mono- or fused cyclic hydrocarbon group which may contain a hetero atom on the ring, or which may be substituted with a substituent(s); each of n and m represents an integer and the sum of n and m is an integer of 0 to 2; each of X and E represents oxygen, NR' (wherein R' is hydrogen or a lower alkyl group having 1 to 6 carbon atoms), sulfur, phenylene, CH.dbd.CH or CH.sub.2 ; A represents an amino acid residue or an imino acid residue, which functional group may be optionally protected, or a glycine residue which may be substituted at the amino moiety thereof; and, Y1 represents a cycloalkyl group having 3 to 8 carbon atoms; or a salt thereof. The pyrrolidine derivatives inhibit a prolyl endopeptidase and are expected to be effective for the treatment of amnesia.

Abstract: Novel anthracycline derivatives have now been produced, which exhibit higher antitumor activities and lower toxicities than those of daunomycin, adriamycin etc. that have been clinically used as anticancer agents. That is, a daunomycinone or adriamycinone derivative represented by the general formula (I): ##STR1## wherein R is a hydrogen atom or a hydroxyl group.

Abstract: An aqueous solution of kasugamycin or its salt is either mixed with a strongly acidic ion-exchange resin of the H.sup.+ -form in a reaction vessel, or is brought into contact with a strongly acidic ion-exchange resin of the H.sup.+ -form in a column containing said resin, followed by heating said aqueous solution and the resin under an atmospheric pressure or an elevated pressure, thereby to effect hydrolytic reaction of kasugamycin. By this reaction, an acidic reaction solution containing D-chiro-inositol is produced. This acidic reaction solution containing D-chiro-inositol is separated from the strongly acidic ion-exchange resin. Subsequently, D-chiro-inositol is recovered from the reaction solution. For this recovery, the acidic reaction solution is passed successively through a column of a strongly acidic ion-exchange resin of the H.sup.+ -form and through a column of a strongly basic ion exchange resin of the OH.sup.- -form, so that a neutral aqueous eluate containing D-chiro-inositol is obtained.

Abstract: Desalaninebenanomicin A has been synthesized by chemical conversion of benanomicin A. Amino acid derivatives of desalaninebenanomicin A having the general formula (Ia): ##STR1## where R.sup.a represents a hyhrogen atom, a C.sub.1-5 alkyl group, a C.sub.1-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group have been synthesized by condensing the 2-carboxyl group of desalaninebenanomicin A with a variety of amino acids. Among the derivatives of the formula (Ia) having antifungal activities, such desalaninebenanomicin A derivatives in which R.sup.a is a C.sub.2-5 alkyl group, a C.sub.2-5 hydroxyalkyl group, carboxyl group or a lower alkoxycarbonyl group are novel semi-synthetic antibiotics having antifungal activities.

Abstract: D-.beta.-Lysylmethanediamine represented by the formula (I) ##STR1## or a salt or a hydrate thereof has now been found to have an activity of inhibiting the infection with AIDS virus (a virus causative of acquired human immunodeficiency syndrome), mamely HIV. A pharmaceutical composition comprising the above compound or a salt or hydrate thereof as active ingredient is provided and expectable as one of remedial agents for treating AIDS which is now thought to be difficult to cure.

Abstract: As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

Abstract: A compound of the following formula is provided: ##STR1## wherein A represents a carbonyl group which may be protected; B represents an aldehyde group which may be protected; R.sup.1 represents a hydroxyl group which may be protected; R.sup.2 represents a hydrogen atom or acyl group; W represents a hydrogen atom, hydroxyl group, lower alkanoyloxy group or substituted sulfonyloxy group; Y represents a hydrogen atom, halogen atom, hydroxyl group or substituted sulfonyloxy group; and broken line "-------" represents a double bond or single bond. This compound is useful for producing 3,4'-dideoxymycaminosyltylonolide useful as an antimicrobial agent.

Abstract: As new compounds are now synthetized 5-deoxy-5,5-difluoro derivatives of aminoglycosidic antibiotics of neamine, kanamycin A-series, kanamycin B-series, gentamicin-series and seldomycin-series. Further, the 1-N-(.alpha.-hydroxy-.omega.-aminoalkanoyl) derivatives are synthetized from 5-deoxy-5,5-difluorokanamycins A and B, as well as their analogues now obtained. The 5-deoxy-5,5-difluoro derivatives of the aminoglycosidic antibiotics now provided according to this invention have such antibacterial activities enhanced much more than or equal to those of the respectively corresponding parent aminoglycosidic antibiotics, while these 5-deoxy-5,5-difluoro derivatives exhibit values of the 50% lethal dosage (LD.sub.50) which are improved remarkably better when they are intravenously administered to mice, so that they have remarkedly reduced toxicities to mammals.

Abstract: As new antibiotics are obtained delaminomycins A, B and C having a formula (I) or (I') shown below, or salts thereof. Delaminomycins preferentially inhibit T cells and are useful as immunosuppressants, antineoplastic agents and antibacterial agents. ##STR1## wherein X is a hydroxyl group for delaminomycin A, a methoxy group for delaminomycin B and a hydrogen atom for delaminomycin C.

Abstract: As new dibekacin derivatives and new arbekacin derivatives are now provided 2"-amino-2"-deoxydibekacin, 2"-amino-5,2"-dideoxydibekacin, 2"-amino-2"-deoxyarbekacin, 2"-amino-5,2"-dideoxyarbekacin, 2"-amino-5,2"-dideoxy-5-epi-fluoroarbekacin and 2"-amino-5,2"-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

Abstract: A novel, biologically active substance, poststatin, has been isolated from a culture medium of microorganism belonging to Streptomyces. The novel substance is a peptide compound having a novel structure, wherein the peptide chains have ketone radicals. Thus substance has a high endopeptidase inhibition activity. It is possible to chemically synthesize poststatin related compound having ketone radicals in the peptide chains. These compounds also have an endopeptidase inhibition activity.

Abstract: As new compounds are now provided N-methyl-3-(3,4-dihydroxyphenyl)serine alkyl esters which are effective as an .alpha.-adrenergic and .beta.-adrenergic agent to stimulate the .alpha.-adrenergic and .beta.-adrenergic functions of the central nervous system of mammalian animals and are expectable to be useful for therapeutic treatment of disorders as invoked by reduced biological activities or functions of the .alpha.- and/or .beta.-adrenergic neurons. N-methyl-L-threo-3-(3,4-dihydroxyphenyl)serine (C.sub.1 -C.sub.6) alkyl esters are preferred amongst the new compounds of this invention.

Abstract: Benanomicin A and Benanomicin B are fermentatively produced by the cultivation of a new microorganism Actinomadura spadix, designated as MH193-16F4 strain.

Abstract: The present invention discloses a new .alpha.-keto amide derivative or a salt thereof represented by the formula (1): ##STR1## wherein X represents (1) a peptide residue or amino acid residue in which the functional group may be protected, (2) a hydrogen atom or (3) an amino-protective group, Y represents a peptide residue or amino acid residue in which the functional group may be protected, E represents a substituent on the alkylene (C.sub.n H.sub.2n-1) and is a halogen, lower alkoxy or hydrogen, A represents a carbonyl group or mono- or di-substituted methylene (the substituent being a hydroxy, lower alkoxy, phenylimino or benzylimino), and n represents an integer of 2 to 6.The compound of the present invention is effective in inhibiting prolyl endopeptidase activity and useful as an active ingredient of an enzyme inhibitor.

Abstract: In this invention, a new microbial strain which is a strain of Actinomycetes and belongs to the genus Actinomadura, namely Actinomadura sp. MI215-NF3 strain is cultured, and MI215-NF3 substance, a novel antibiotic classifiable as a polyether antibiotic, is recovered from the resultant culture. MI215-NF3 substance and its salts obtained according to this invention are useful for therapeutic treatment of chicken coccidiosis and also have useful antibacterial activities against certain species of bacteria.