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: Orally administrable pharmaceutical compositions comprising 3-(N-piperidinomethyl-azino)methylrifamycin S as the active substance are disclosed. The active substance is easily soluble in water even at low pH values and is provided with good bioavailability. Such compositions are useful in the treatment of bacterial infections.

Abstract: 6-substituted penem esters of formula (I): ##STR1## wherein R.sub.1 is halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, phenyl, phenoxy, benzyl, or sulphonyloxy group; R.sub.2 is a C.sub.1 -C.sub.4 alkyl, benzyl diphenylmethyl ##STR2## group where A is C.sub.1 -C.sub.4 is C.sub.1 -C.sub.4 alkyl, benzyl, p-nitrobenzyl or p-methoxybenzyl; and R.sub.3 is an organic radical, are elastase inhibitors and thereby useful antiinflammatory and antidegenerative agents.

Abstract: A substantially (.gtoreq.95%) optically pure (5R,6S,1'R) penem of formula ##STR1## and the pharmaceutically acceptable salts and the ester prodrugs thereof, are endowed with antibacterial activity.

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 device includes a syringe and an apparatus for coupling the syringe to a drug holding bottle and the like, the apparatus defining an enclosed chamber wherein there is housed a needle to be coupled to the syringe and the free end of which is arranged is front of a tightness resilient member located at a seat adapted to receive the mouth of the bottle, the syringe being firmly and fixedly clamped, in a tight way, in a syringe seat formed in the apparatus.

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 6-alkylidenadrosta-1,4-diene-3,17-dione derivatives, having the following general formula ##STR1## wherein each of R and R.sub.2, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl, which are useful in therapy, in particular in the treatment of hormone-dependent cancers.

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.

Abstract: There are provided compounds of formula I: ##STR1## wherein R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl group either unsubstituted or substituted by one or more substituents chosen from a free or protected hydroxy or halogen atom;R.sup.2 is a free or esterified carboxy group or carboxylate anion;R.sup.3 and R.sup.4 are each independently hydrogen or organic group,X is --O--, ##STR2## --S--, Q is either(a") free or protected hydroxy, or(b") a C.sub.1 -C.sub.1 acyloxy, or(c") carbamoyloxy OCONH.sub.2, or(d") an optionally substituted heterocyclylthio group, or(e") an optionally substituted imido group, or(f") an optionally substituted quaternary ammonium group or(g") a halogen atom,A and the pharmaceutically or veterinarily acceptable salts thereof. There are provided also methods for preparing compounds of formula I. The compounds of formula I are useful as antibacterial agents.

Abstract: A pharmaceutical compositon having activity against nephropathies comprising, as an active agent, a therapeutically effective amount of a compound of formula (I) ##STR1## wherein (a) ##STR2## wherein Y completes a single bond or is oxygen or a --CH.sub.2 -- group and the symbol ##STR3## represents a single bond or (b) ##STR4## ##STR5## and the symbol ##STR6## represents a double bond; one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is --CH.sub.2 OH, C.sub.2 -C.sub.4 acyl, ##STR7## in which each of R.sub.1, R.sub.8 and R.sub.9 is independently hydrogen or C.sub.1 -C.sub.4 alkyl and the others are independently chosen from hydrogen, hydroxy, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and --COOR, wherein R.sub.7 is as defined above, and one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier and/or diluent.

Abstract: The invention relates to a new process for the preparation of known aromatase inhibitors of the following formula ##STR1## wherein each of R.sub.1 and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl andR.sub.4 is hydrogen or fluorine; the process comprising subjecting to Mannich reaction a compound of formula ##STR2## wherein R.sub.1,R.sub.2,R.sub.3 and R.sub.4 are as defined above, and then oxidizing the respective 6-methylene derivative thus obtained by methods known per se.

Abstract: The invention relates to an apparatus for connecting a bottle containing a medicament to a syringe the needle of which is housed in a closed chamber defined by the apparatus and from which the needle can be made to emerge by sliding the separate constituent parts of the appartus along each other. To prevent the needle from emerging from the chamber when no bottle is housed in the appropriate seat provided in the apparatus, there extends from one of the parts of the apparatus an elongated flexible appendix having at least one protuberance which projects into the seat and against which the bottle presses when inserted into the seat, so bending the appendix outwards. In front of the free end of the appendix there is provided a stop tooth projecting from that consituent part of the apparatus which is projecting from that constituent part of the apparatus which is mobile along the first part and extends totally around the seat.

Abstract: The invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula ##STR1## wherein each of R and R.sub.3, independently, is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or fluorine;R.sub.5 is (a) hydrogen or C.sub.1 -C.sub.6 alkyl; (b) phenyl unsubstituted or substituted by one or two substituents independently chosen from C.sub.1 -C.sub.6 alkyl, halogen and amino; (c) an acyl group; or (d) a hydroxy protecting group; and the pharmaceutically acceptable salts thereof,which are useful in therapy, in particular as anti-cancer agents.