Abstract: Stable, rapidly soluble, lyophilized injectable preparations comprising an anthracycline glycoside, or a pharmaceutically acceptable salt thereof, as the active drug substance, and use of said preparations in the treatment of tumors.

Abstract: As a new antifungal and antiviral antibiotic is provided benanomicin A 4"'-O-sulfate or a salt thereof having formula (I) ##STR1## wherein M.sup.1 denotes a mono-valent alkali metal atom or a di-valent alkaline earth metal atom or a hydrogen atom and A denotes an organic base; n is zero when M.sup.1 is an alkali metal atom or alkaline earth metal atom but n is 1 or zero when M.sup.1 is a hydrogen atom, and M.sup.2 denotes a hydrogen atom or an alkali metal atom or an alkaline earth metal atom. This new compound is useful as antifungal agent to treat fungal infections in mammals and as antiviral agent to inhibitingly treat HIV.

Abstract: Stable, rapidly soluble, lyophilized injectable preparations comprising an anthracycline glycoside, or a pharmaceutically acceptable salt thereof, as the active drug substance, and use of said preparations in the treatment of tumors.

Abstract: A compound having the structure: ##STR1## wherein R is CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, t--C.sub.4 H.sub.9 or C.sub.6 H.sub.5 ; R.sup.1 is NH.sub.2, NHCH.sub.3, NHC.sub.2 H.sub.5, NHC.sub.3 H.sub.7, NHC.sub.4 H.sub.9, NHCH.sub.2 CH.sub.2 Cl, NHC.sub.6 H.sub.5, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, N(C.sub.3 H.sub.7).sub.2, NCH.sub.3 (C.sub.2 H.sub.5), NCH.sub.3 (C.sub.3 H.sub.7), N(CH.sub.2 CH.sub.2 Cl).sub.2, NHOH, NHNHCO.sub.2 CH.sub.2 C.sub.6 H.sub.5, NHNHCO.sub.2 C(CH.sub.3).sub.3, OCH.sub.3, OC.sub.2 H.sub.5, OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, OC.sub.6 H.sub.5, OC.sub.2 C.sub.6 H.sub.5, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, CH.sub.2 NO.sub.2 or CH.sub.2 NH.sub.2 ; and R.sup.2 is NHCH.sub.2 CH.sub.2 Cl or N(CH.sub.2 CH.sub.2 Cl).sub.2.These compounds may be used to eliminate occult leukemic clonogenic cells from bone marrow by contacting the bone marrow with a solution comprising levels of said compound sufficient to eliminate occult leukemic clonogenic cells.

Abstract: The invention relates to novel compounds of the formulae ##STR1## wherein S is H, alkyl or alkoxy and R is a good leaving group, and to the preparation of these compounds in a stereospecific manner to obtain a configuration wherein OH at C-3 and OR at C-1 are in the cis-position, which compounds can be used for the synthesis of daunomycinone and derivatives thereof.Daunomycinone can be used for the preparation of daunomycin and adriamycin.

Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.

Abstract: Two new antibiotics which are now nominated as benanomicin A and benanomicin B, respectively, are fermentatively produced by the cultivation of a new microorganism, designated as MH193-16F4 strain, of Actinomycetes. Benanomicins A and B each show antifungal activity and are useful as a therapeutic antifungal agent. A new compound, dexylosylbenanomicin B is now produced by chemical conversion of benanomicin B, and this semi-synthetic antibiotic also shows antifungal activity and is useful as a therapeutic antifungal agent.

Abstract: 7-O-Glycosyl-rhodomycins which correspond to the general formula I below ##STR1## in which the radicals have the following meaning: R.sup.1 is a hydrogen atom or a hydroxyl group,R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl group,R.sup.3 a hydroxyl group, an O-acyl protective group or the methyloxycarbonyl group,R.sup.4 is a hydrogen atom, an O-acyl protective group, an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group andR.sup.5 is an azido group, amino or trifluoroacetylamino group, a di-C.sub.1 -C.sub.4 -alkylamino group or cyanomethylamino group,where acyl protective group denotes an acetyl, mono-, di- or trihalogenoacetyl group with fluorine or chlorine as halogen or the p-nitrobenzoyl group, and a process for the preparation thereof and the use thereof as pharmaceuticals, are described.

Abstract: Antitumour anthracycline glycosides of formula I: ##STR1## wherein R.sub.1 is hydrogen or a hydroxyl group, and pharmaceutically acceptable acid addition salts thereof.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group. The N-trifluoroacetyl 7S:9S and 7R:9R derivatives of the .alpha.-glycosides of formula XV can be separated by chromatography on silica gel to obtain, after mild alkaline hydrolysis the wanted 7S:9S .alpha.-glycosides (R.sub.1 =H) as free bases and can eventually be transformed into their corresponding doxorubicin derivatives (R.sub.1 =OH) by known procedures.

Abstract: The present invention relates to anthracycline derivatives of the formula I ##STR1## in which at least one of the two substitutents R.sub.1 and R.sub.2 represents an N-oxidized sugar or an N-oxidized sugar combination, and a chemical process for the preparation of these compounds and their use as medicaments for the treatment of malignant tumors.

Abstract: 2,6-Dideoxy-2-fluoro-L-talopyranose and 1-substituted derivatives thereof, including methyl 2,6-dideoxy-2-fluoro-L-talopyranoside and 3,4-di-O-protected-2,6-dideoxy-2-fluoro-L-talopyranosyl halides, are now provided and these new compounds are useful as intermediates for use in the synthesis of new compounds having antitumor activity, especially 7-O-(2,6-dideoxy-2-fluoro-.alpha.-L-talopyranosyl) daunomycinone or -adriamycinone. 2,6-Dideoxy-2-fluoro-L-talopyranose shows antibacterial activity. 2,6-Dideoxy-fluoro-L-talopyranose and the 1-substituted derivatives thereof may be produced by a multi-stage process starting from L-fucose.

Abstract: Cytorhodin S derivatives, especially cytorhodin S-immunoglobulin complexes are disclosed. Cytorhodin S possesses very high anticancer activity, but the complexes act more selectively on cancer cells and are more useful as an anticancer agent. New intermediate derivatives are also useful as an anticancer agent.

Abstract: Process for the preparation of finely divided porous cellulose in the form of essentially spherical particles by formation of a suspension, in which an organic solution of a cellulose ester of aromatic or aromatic-aliphatic carboxylic acids containing a C.sub.5 -C.sub.12 alkanol is stirred into an aqueous solution of an anionic surfactant, the solvent is removed and the particles are isolated and hydrolyzed under heterogeneous conditions. They are suitable as adsorbents in e.g. chromatographic processes.

Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of target cell an agent free of its targeting molecular carrier.

Abstract: A new species of Micromonospora, in particular Micromonospora spartanea ATCC 53803, is described. The species produces antifungal compounds spartanamicins A and B. Methods for the production, isolation and characterization of the compounds are described. The compounds contain deoxy-L-fucose, as well as another hexose and an amino sugar.

Abstract: An improved process for the preparation of doxorubicin, by means of hydrolysis of a doxorubicin ester of a dicarboxylic acid, in acid medium.

Abstract: As new compounds are now provided 14-O-(3,4-disubstituted benzoyl)adriamycins which are of low cytotoxicity and exhibit a high activity inhibitory to the reverse transcriptase of human immunodeficiency virus (HIV) and which can inhibit propagation of HIV.

Abstract: Prodrugs of bio-active hydroxyaromatic drugs having the structural formula:A pharmaceutically acceptable prodrug of a biologically active, therapeutically effective hydroxyaromatic drug, said prodrug being selected from the group consisting of, (A) compounds having the structural formula:DRUG--O--CR'R"--Z].sub.nwherein:DRUG --O-- is the hydroxyaromatic O-dehydro residue of said drug;R' and R' may be the same or different and may be H, alkyl, aryl or electron withdrawing groups;Z is a displaceable leaving group; andn is an integer in the range of from 1 to 3, and (B) pharmaceutically acceptable salts thereof.

Abstract: A modified cellulose for biocompatible dialysis membranes having a structure represented by the formula ##STR1## wherein cell is cellulose or chitin, in each case without hydroxyl groups, s=3 in the case of cellulose and s=2 in the case of chitin, R' is CH.sub.3 and/or C.sub.2 H.sub.5 and/or C.sub.3 H.sub.7, X denotes specified functional groups, R" is H or R, R"' denotes R, x+t=0.75 to 2.85, t=0 to 2.85, x=0 to 2.85, and r=0 to 1. A process for preparation of the cellulose derivatives is also disclosed.

Abstract: Novel antibiotic herein designated as BU-3608, BU-3608 B, and BU-3608 C are produced by fermentation of Actinomadura hibisca Strain No. P157-2, ATCC 53557, and Strain No. Q278-4, ATCC 53646. The antibiotics possess antifungal and antiviral activities.

Abstract: Anthracycline glycoside compounds of general formula I or II: ##STR1## wherein R.sub.1 is hydrogen or a hydroxy group and R.sub.2 is hydrogen or a methoxy group, and their pharmaceutically acceptable acid addition salts, are antitumor agents.

Abstract: Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotised followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

Abstract: A modified cellulose for biocompatible dialysis membranes having a structure represented by the formula ##STR1## wherein Cell is cellulose or chitin, in each case without hydroxyl groups, s=3 in the case of cellulose and s=2 in the case of chitin, R' is CH.sub.3 and/or C.sub.2 H.sub.5 and/or C.sub.3 H.sub.7, X denotes specified functional groups, R" is H or R, Z corresponds to the following groups of atoms: SR", SO.sub.3 H and salts thereof, SO-R, SONR".sub.2, SO.sub.2 -R, SO.sub.2 NR".sub.2, SO.sub.2 H and salts thereof, F, Cl, Br, I, NR".sub.2, PR".sub.2, PO.sub.3 H.sub.2 and salts thereof, PO.sub.2 H(OR), PO(OR).sub.2, PO.sub.2 HR" and salts thereof, POR"(OR) and POR".sub.2, x+t=0.75 to 2.85, t=0 to 2.85, x=0 to 2.85, and z=0.01 to 0.45. A process for preparation of the cellulose derivatives is also disclosed.

Abstract: A modified cellulose for biocompatible dialysis membranes having a structure represented by the formula ##STR1## wherein cell is unmodified cellulose or chitin, in each case without hydroxyl groups, s=3 in the case of cellulose and s=2 in the case of chitin, R' is CH.sub.3 and/or C.sub.2 H.sub.5 and/or C.sub.3 H.sub.7, X denotes specified functional groups, m=0.75 to 2.85, and x=0.005 to 2.10. A process for preparation of the cellulose derivatives is also disclosed.

Abstract: This invention relates to a novel method for the delivery of cytotoxic drugs to tumor cells by the administration of a tumor-specific antibody-enzyme conjugate that binds to the tumor cells, and the additional administration of a prodrug that is converted at the tumor site, in the presence of the antibody-bound enzyme, to an active cytotoxic drug. According to preferred embodiments of this invention, antibody-enzyme conjugates containing the enzyme, alkaline phosphatase ("AP"), have been used in conjunction with the novel prodrug, etoposide-4'-phosphate or 7-(2'-aminoethyl phosphate)mitomycin or a combination thereof, to effect killing of tumor cells. According to another embodiment of the invention, an antibody-enzyme conjugate containing the enzyme, penicillin V amidase ("PVA"), has been used in conjunction with a novel prodrug, N-(p-hydroxyphenoxyacetyl)adriamycin to effect killing of tumor cells.

Abstract: Disclosed are antibiotics BU-3608 FA-1 and FA-2 and alkyl derivatives thereof. These compounds are useful as antifungal agents. BU-3608 FA-1 and FA-2 are produced from Actinomadura hibisca in a medium containing a source of D-serine.

Abstract: Anthracycline glycosides of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from hydrogen, methyl, ethyl or methoxy and pharmaceutically acceptable acid addition salts thereof, which are useful in treatment of human cancer, are prepared by a stereospecific condensation of a derivative of daunosamine of general formula (II): ##STR2## wherein R.sub.3 is an alkyl, perfluoroalkyl or aryl group and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently selected from alkyl, aryl or aralkyl having up to ten carbon atoms, with a quinone quinizarine epoxide of general formula (III) ##STR3## and conversion of the product obtained to the anthracycline glycoside of formula (I) or salt thereof.

Abstract: N-2-chloroalkyl nitrosouredio derivatives of anthracycline-based compounds having antitumor activity are disclosed. Relative to the clinically-used drugs adriamycin and daunorubicin, substantially enhanced antitumor activity against parent murine P388 leukemia and an adriamycin-resistant P388 leukemia subline has been found for the N-2-chloroethylnitrosoureido derivatives of adriamycin, daunorubicin and epirubicin. Chemical stability has been found to be enhanced when employing the 4'-epi stereoisomeric family of these compounds.

Abstract: Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotized followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I ##STR1## wherein R.sup.1 is a CH.sub.3 (CH.sub.2).sub.n group with n=0 to 3,R.sup.2 is a hydrogen atom or a methyl group,R.sup.3 is a hydrogen atom, a methyl group or an acyl protective group, andR.sup.4 is a hydrogen atom or an acyl protective group,and which are optionally in the form of a salt of an inorganic or organic acid, to a process for their preparation and to their use in pharmaceuticals.

Abstract: Disclosed herein are N-alkyl derivatives of antibiotics BU-3608, BU-3608 B, C, D and E as well as the corresponding desxylosyl compounds. These novel compounds are useful as antifungal agents.

Abstract: Disclosed is an anthracycline compound of the formula (I): ##STR1## wherein Ra is -R.sup.1, ##STR2## or --OR.sup.3, R.sup.1 being (1) alkyl, alkenyl, alkynyl, fluoroalkyl, aryl or aralkyl, or (2) alkyl, alkenyl, alkynyl. fluoroalkyl, aryl or aralkyl having carboxyl, azido, amino, hydroxy, alkoxy or a halogen atom; R.sup.2 being R.sup.1, a hydrogen atom or hydroxy; and R.sup.3, which may be the same or different when one substituent has two R.sup.3 's, being R.sup.1 or a hydrogen atom; or the formula (II): ##STR3## wherein Rb is -R.sup.1, ##STR4## or --OR.sup.3, R.sup.1, R.sup.2 and R.sup.3 being as defined above; and R.sup.4 being the same as R.sup.3 except that methyl is not included; or an acid addition salt thereof.This compound can be contained as an active ingredient in an antitumor agent, whereby good results are attainable.

Abstract: This invention relates to a process for preparing an antibiotic D788-7 wherein, after culturing carborubicin-producing bacteria, the obtained culture liquid is extracted in acidic conditions while stirring to be absorbed to synthetic resin, followed by desorption from the resin and elution with acetone and the resulting acetone solution containing carborubicin is converted into an antibiotic D788-7 by photo radiation, for obtaining D788-7 in the purified form from the reaction solution. The production yield for D788-7 is extremely high and its use as an antitumor agent can be made possible.

Abstract: A stabilized preparation, particularly, freeze-drying injection, of anthracycline, for example, (7S, 9S)-9-acetyl-9-amino-7-[(2-deoxy-.beta.-D-erythropentopyranosyl)oxy]-7,8,9 ,10-tetrahydro-6,11-dihydroxynaphthacene-5,12-dione or salts thereof which comprises L-cysteine or salts thereof.

Abstract: Novel antineoplastic amine-containing derivatives and methods for synthesizing such derivatives of anthracycline antibiotics are disclosed. The derivatives are useful to prepare site-selectively attached therapeutic antibody-anthracyline antibiotic conjugates which retain substantial immunospecificity of the unconjugated antibody molecule. Using the conjugates, targeted delivery of the attached antineoplastic amine derivatives of anthracycline antibiotics is achieved in vivo. Such conjugates are thus therapeutically effective against a variety of neoplastic cellular disorders when administered in vivo. Methods for preparing the antibody conjugates and for use of the conjugates in vivo are also disclosed.

Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I, which are optionally in the form of a salt of an inorganic or organic acid, ##STR1## in which the substituents have the following meaning: R.sup.1 is hydrogen or a hydroxyl group,R.sup.2 is hydrogen or a hydroxyl or a methoxy group,R.sup.3 is hydrogen or a hydroxyl group,R.sup.4 is hydrogen or a hydroxyl group,R.sup.5 is hydrogen, a hydroxyl or a methoxycarbonyl group, or a substituent of the general formula II, ##STR2## in which R.sup.8a has the meaning indicated for R.sup.8, or a substituent of the formula III, ##STR3## R.sup.6 is ethyl, methylcarbonyl, hydroxymethylcarbonyl, hydroxyalkyl or a dihydroxyalkyl,R.sup.7 is hydrogen or a substituent of the general formula IV, ##STR4## and R.sup.8 is hydrogen or a cyanomethyl group or a substituent of the general formula COR.sup.9 or CH.sub.2 R.sup.10, R.sup.9 being hydrogen, CH.sub.3, CF.sub.3 or CCl.sub.3, and R.sup.10 being C.sub.1 - to C.sub.

Abstract: According to the invention there is provided a sterile, pyrogen-free, ready-to-use solution of an anthracycline glycoside, especially doxorubicin, which consists essentially of a physiologically acceptable salt of an anthracycline glycoside dissolved in a physiologically acceptable solvent therefor, which has not been reconstituted from a lyophilizate and which has a pH of from 2.5 to 6.5. The solution of the invention is particularly advantageous for the administration by injection of the anthracycline glycoside drugs, e.g. doxorubicin, in the treatment of both human and animal tumors.

Abstract: The novel compounds are provided with good antibacterial and antitumour activity.

Abstract: A new process for the preparation of 6-deoxyanthracyclinones of general formula I: ##STR1## wherein R represents a hydrogen atom, a hydroxy group or a lower alkoxy group is described. The process provides a total synthesis of the 6-deoxyanthracyclinones of formula I using 1,2,3,6-tetrahydro-phthalate as starting material. The obtained racemic mixture of the compounds of formula I, if desired, can be submitted to optical resolution by the conventional method of conversion to diastereomeric derivatives using a chiral resolving agent. Alternatively, the racemic mixture can be used as such for the condensation with a suitably protected halosugar derivative to obtain alpha glycosidic derivatives of formula XV: ##STR2## wherein R.sub.1 represents a hydrogen atom or a hydroxy group, one of R.sub.2 and R.sub.3 represents a hydrogen atom, the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxy group and X is a hydrogen atom or a trifluoro acetyl group.

Abstract: The O-acyl derivatives of urdamycin A exhibit an antibiotic or antitumoral activity.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.

Abstract: Disclosed are anthracycline antibiotics of a formula (I): ##STR1## in which R.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.2 are hydroxyl groups, R.sup.3 is 1-hydroxyethyl group, R.sup.4 is hydrogen atom and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1, R.sup.2 and R.sup.4 are hydroxyl groups, R.sup.3 is ethyl group and X represents daunosamine-rhodenose, daunosamine-deoxyfucose, rhodosamine-rhodenose, N-monomethyldaunosamine-rhodenose or N-monomethyldaunosamine-deoxyfucose; orR.sup.1 is methoxy group, R.sup.2 is hydroxyl group, R.sup.3 is ethyl group, R.sup.4 is methoxycarbonyl group and X represents daunosamine-rhodenose or daunosamine-deoxyfucose; orR.sup.1 and R.sup.4 are hydroxy groups, R.sup.2 is hydrogen atom, R.sup.

Abstract: The present invention relates to new tetralins and their use for the preparation of anthracyclinones and anthracyclins. These tetralins contain at least one chiral carbon atom and correspond to the formula (V) below: ##STR1## in which: R.sub.1 and R.sub.2 denote a hydrogen atom, or a halogen atom or the group OCH.sub.3, provided that one of the two substituents (R.sub.1 or R.sub.2) must denote OCH.sub.3, andR.sub.3 denotes a hydrogen atom or the OR' group, R' being hydrogen or a hydroxyl-protecting group. Application: synthesis of glycosides of great therapeutic value.

Abstract: The invention relates to new anthracycline derivatives having cytostatic activity and the general formula I ##STR1## in which the radicals R.sup.1 is hydrogen or a hydroxyl group, R.sup.2 is hydrogen or a hydroxyl group or a structure of the formula II, and R.sup.3 is a hydroxyl group or a structure of the formula II ##STR2## in which R.sup.4 is an aliphatic or aromatic acyl group, with the proviso that at least one of the radicals R.sup.2 and R.sup.3 has a structure of the formula II, which are optionally in the form of a salt of an inorganic or organic acid, as well as to the process for the preparation thereof, and to the use thereof in pharmaceuticals.

Abstract: Anti-retroviral agents comprising, as active ingredient, an antibiotic of anthracycline family (e.g., daunorubicin and doxorubicin) have higher effect with less toxicity, compared with conventional antiretroviral substances, such as azidothymidine and bleomycin.

Abstract: Anthracycline glycosides of the general formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom or a hydroxyl group, one of R.sub.2 and R.sub.3 represents a hydrogen atom and the other of R.sub.2 and R.sub.3 represents a hydrogen atom or a hydroxyl group; and pharmaceutically acceptable acid addition salts thereof are antitumor agents. These glycosides may be prepared from a daunomycinone derivative of formula (II): ##STR2## in which the 4-amino group is protected. 4-Demethoxy-4-amino-daunomycinone (II) and an earlier intermediate in its preparation, 4-demethoxy-4-amino-7-deoxy-daunomycinone (IX), can be diazotized followed by mild reduction to form 4-demethoxy-daunomycinone or 4-demethoxy-7-deoxy-daunomycinone respectively. 4-Demethoxy-daunomycinone can be converted into another antitumor anthracycline glycoside, 4-demethoxy-daunorubicin.

Abstract: New anthracycline antibiotics of a formula (I) are provided, which are usable as an anticancer agent ##STR1## (where R represents a hydrogen atom or a hydroxyl group). The antibiotics (I) can be produced by incubation of a dye-nonproductive or hardly dye-productive mutant strain which has an ability of converting .alpha.-citromycinone or .beta.-isorhodomycinone into the antibiotics (I), in the presence of .alpha.-citromycinone or .beta.-isorhodomycinone in a pertinent nutrient medium.

Abstract: 4'-Deoxy-13(S)-dihydro-4'-iododoxorubicin having the formula (II): ##STR1## and pharmaceutically acceptable salts thereof are anti-tumor agents.

Abstract: Anthracycline glycosides having the general formula (A): ##STR1## wherein R.sub.1 is hydrogen, hydroxy or methoxy; R.sub.2 is amino, R.sub.3 is hydrogen or hydroxy and X is hydrogen; and their pharmaceutically acceptable salts; are antitumor agents. The compounds are obtained by reduction of the corresponding 6-nitro derivatives with stannous chloride in presence of sodium acetate or with palladium or charcoal in presence of cyclohexene.