Abstract: Carboxy-thiazolo[3,2-a]pyrimidine derivatives, and pharmaceutical compositions containing them. The compounds and compositions possess anti-allergic activity.

Abstract: A new antitumor anthracycline glycoside, 4-demethoxy-13-dihydrodaunorubicin, is disclosed.The new compound is prepared by reduction of the side-chain ketone function of the known 4-demethoxydaunorubicin, with sodium borohydride in aqueous solution at room temperature.

Abstract: Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond;each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different is(a) hydrogen; hydroxy; halogen; cyano; C.sub.1 -C.sub.6 alkyl; C.sub.1 -C.sub.6 alkoxy; a C.sub.2 -C.sub.4 acyl or C.sub.2 -C.sub.4 acylamino group; --SR', --N(R') (R"), --CH.sub.2 OR', --COR or --CH.sub.2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C.sub.1 -C.sub.6 alkyl; or(b) one of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is 5-tetrazolyl or a group selected from --COCH.sub.2 OR', --CH.dbd.C(R')--COR and --X--C(R')(R")--COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a);R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or a phenyl or 3-pyridyl ring, wherein the phenyl or pyridyl ring is unsubstituted or substituted by one to three substituents chosen from hydroxy and C.sub.

Abstract: (.+-.)4-demethoxy-6(and-11-)-deoxydaunomycinone which are starting materials for anthracycline antitumor antibiotics are prepared by reacting 1,2,3,6-tetrahydrophthalic anhydride with an alcohol of the formula ROH, wherein R is lower alkyl, substituted lower alkyl or aryl to form a monoester, subjecting the monoester to a Friedel-Crafts reaction with acetyl chloride, followed by mild alkaline treatment, to give the corresponding .alpha.,.beta. unsaturated ketone, catalytically reducing same to form the corresponding 4-acetyl-perhydrophthalate reacting the latter with 1,4-dimethoxynaphthalone in the presence of tritluoroacetic anhydride and trifluoroacetic acid to form a mixture of two isomeric compounds, submitting said mixture of isomers to a catalytic reduction of the benzylic carbonyl function, followed by treatment thereof with sulphuric acid at room temperature to afford a mixture of tetracyclic isomers, treating the mixture of tetracyclic isomers with sulphuric acid at 80.degree. C.

Abstract: The present invention relates to new condensed benzopyrone derivatives, to a process for their preparation and to pharmaceutical compositions containing them.

Abstract: Platelet aggregation inhibiting compositions and methods of use containing compounds of the formula ##STR1## where Z completes a bond or is a ##STR2## group; one of R.sub.1 and R.sub.2 is hydroxy and the other is hydrogen or alkyl, or R.sub.1 and R.sub.2, taken together, form an oxo group; and the remaining substituents are as defined in the specification.

Abstract: A new process is described for the preparation of (5R)-penem derivatives of the general formula I: ##STR1## wherein R.sub.1 represents a hydrogen atom or an organic group; R.sub.2 represents a hydrogen atom or a carboxy protecting group and Y represents a hydrogen or halogen atom or an organic group. A 2-thiacephem derivative of the general formula II: ##STR2## wherein R.sub.1, R.sub.2 and Y have the meanings/given above is oxidized by means of organic peracids to the corresponding sulphone of the general formula III: ##STR3## which is subsequently submitted to a desulphurative ring contraction by extrusion of SO.sub.2 to give exclusively the desired (5R)-penem derivatives of the general formula I.

Abstract: The present invention relates to new furyl derivatives of 16-substituted prostaglandins, to a process for their preparation and to pharmaceutical and veterinary compositions containing them.The new compounds of the invention are optically active or racemic prostaglandins of the following formula (I) ##STR1## wherein R is(1) --OH or --OR' wherein R' is C.sub.1 -C.sub.6 alkyl optionally substituted by phenyl or by a monocycloalkyl group or by a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N;(2) ##STR2## wherein each of R" and R"', is independently, hydrogen; C.sub.1 -C.sub.6 alkyl; phenyl; or a pentatomic or hexatomic heteromonocyclic ring containing at least one heteroatom chosen from O, S and N; or R" and R"', together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic heteromonocyclic ring optionally containing a further heteroatom chosen from O, S and N;(3) --W--(CH.sub.2).sub.

Abstract: Amino derivatives of benzylidene-Pyrrolo[2,1-b] Quinazolines are provided, together with pharmaceutical compositions containing them. The compounds and the compositions have pharmaceutical utility and are particularly useful as anti allergy agents.

Abstract: A process for the preparation of compounds of formula (I) ##STR1## wherein R.sub.1 is hydrogen or an organic group;R.sub.2 is hydrogen or a carboxy protecting group; andY is a group-S-heterocyclic, acyloxy, alkoxy, alkylthio, pyridyl, which group may be substituted, or azido, and penem derivatives falling within the scope of formula (I) and pharmaceutically or veterinarily acceptable salts thereof.The process involves displacing a group L in the Y position with a reagent Y-H.

Abstract: The invention relates to a device to one end of which a syringe can be connected and to the other end of which the mouth or opening of a bottle containing a drug or medicine can be connected. The device comprises a closed chamber having enclosed therein a needle which is in connection with the syringe. Members are provided by means of which the mouth or opening of the bottle is steadily connected to the device and means enabling the needle to perforate a seal plug and then a small rubber plug mounted on the bottle only when the device is blocked onto the bottle so that in any case it cannot be disconnected therefrom. Such a device can be disconnected from the bottle only after the needle has been caused to reenter the closed chamber, so as to prevent any possible dripping of the liquid outside of the device.

Abstract: Disclosed is a process for purifying Tylosin by selective adsorption of the fermentation broth previously brought to 7.5-10.0 pH on polymeric resins and by subsequent deadsorption of the purified product with a aqueous-alcoholic or aqueous-acetonic solution and further purification of the eluate by filtration through macroreticular weak anion resins.

Abstract: Anthracycline glycosides of the formula (I) ##STR1## wherein one of R.sub.1 and R.sub.2 is hydrogen and the other of R.sub.1 and R.sub.2 is hydroxy, each of R.sub.3, R.sub.4 and R.sub.5 is independently selected from the group consisting of hydrogen and hydroxy and X is hydrogen or trifluoroacetyl, with the provisos that R.sub.4 and R.sub.5 are not simultaneously hydroxy and that if R.sub.3 is hydroxy, then X is hydrogen, which are useful in treating certain mammalian tumors are prepared by condensing an aglycone of the formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are defined as above, with a suitable protected halosugar, after which the protecting groups are removed.

Abstract: Substituted carboxy-thiazolo [3,2-a] pyrimidine derivatives are disclosed, together with compositions containing them and methods of using. These derivatives are useful as anti-allergic agents.

Abstract: There are disclosed .beta.-lactam-containing compounds of the formula: ##STR1## where R is hydrogen, lower alkyl, trichloroethyl, acetonyl, benzyl, substituted benzyl, phenyl, substituted phenyl, benzidryl or a residue that will undergo metabolic activation "in vivo" and have favorable pharmacokinetic properties; R.sup.1 is a hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, or hydroxyalkyl, with the alcoholic function of the hydroxyalkyl being free or protected; Z is hydrogen, halogen, hydroxy, amino, carbamoyloxy, mercapto, pyridinium, OR.sup.2, OCOR.sup.2, NHCOR.sup.2, or SR.sup.3 wherein each of R.sup.2 and R.sup.3 is any of lower alkyl, aryl, or a heterocyclic ring, each of which may be substituted or unsubstituted, and n is 0 or 1. The compounds have broad spectrum antibacterial activity and .beta.-lactamase inhibiting activity. Processes for the production of the .beta.-lactam-containing compounds and various intermediates in the production of those compounds are also disclosed.

Abstract: There are provided compounds of formula 1: ##STR1## wherein R=halogen atom or CN, NH.sub.2 and NO.sub.2 group, and pharmaceutically acceptable salts thereof.The compounds are antipsycotic agents.

Abstract: Omega furyl prostenynoic acids have been prepared.

Abstract: Pharmacologically active thiazolo[3,2-a]pyrimidines of the formula ##STR1## wherein A is a bond between the .alpha.- and .beta.-carbon atoms or (--CH.sub.2 --) group; R.sub.1 and R.sub.2 represent hydrogen, C.sub.1 -C.sub.4 alkyl, cyano, CF.sub.3, thienyl, pyridyl, biphenyl, naphtyl, phenyl optionally substituted, ##STR2## wherein R' and R" are hydrogen or alkyl; R.sub.3 represents hydrogen, halogen, alkyl, OH, formyloxy, alkanoyloxy, alkenyloxy; R.sub.4 represents substituted pyrrole, substituted phenyl or substituted thiazolyl. The compounds have antiinflammatory, antiulcerorgenic and antigastric secretory activity.

Abstract: A process for deformylation and separation of N-formyl-L- .alpha.-aspartyl-L-phenylalanine methyl ester from a mixture containing both .alpha. and .beta. isomers thereof, which comprises admixing with said isomeric mixture hydrogen peroxide and an organic acid.

Abstract: Esters of 13,14-didehydro prostaglandins have been prepared.