Abstract: Compounds of the formula (I) ##STR1## wherein R.sub.1 is(a) hydrogen or halogen;(b) a C.sub.1 -C.sub.6 alkyl group, unsubstituted or substituted by C.sub.1 -C.sub.4 alkoxy or by halogen;(c) a phenyl ring unsubstituted or substituted by a group chosen from halogen, C.sub.1 -C.sub.4 alkyl and C.sub.1 -C.sub.4 alkoxy;(d) a C.sub.1 -C.sub.6 alkylthio group;R.sub.2 is hydrogen or halogen;R.sub.3 is 2-pyridyl, 3-pyridyl or 4-pyridyl, wherein each pyridyl group is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; and the pharmaceutically acceptable salts thereof. The compounds possess anti-ulcerogenic and gastric anti-secretory activity.

Abstract: Novel ergoline derivatives formed by reaction of an 8-carboxy ergoline with a carbodiimide and having hypotensive and antiprolatinic activity.

Abstract: Disclosed is a process for preparing the glycoside antitumor anthracyclines 7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-daunomycinone (Ia); 4-demethoxy-7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-daunomycinon e (Ib); 7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-adriamycinone (Ic); 4-demethoxy-7-0-(2,6-dideoxy-.alpha.-L-arabino-hexopyranosyl)-adriamycinon e (Id); 7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-daunomycinone (IIa); 4-demethoxy-7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-daun omycinone (IIb); 7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-adriamycinone (IIc); and 4-demethoxy-7-0-(2,3,6-trideoxy-.alpha.-L-erythro-hex-2-enopyranosyl)-adri amycinone (IId). Compounds Ia, Ib, IIa, IIb are prepared by condensing daunomycinone and 4-demethoxydaunomycinone with 3,4-di-0-acetyl-2,6-dideoxy-.alpha.

Abstract: Compounds of the formula (1) ##STR1## wherein n is 1 or 2;R.sub.1 represents a hydrogen or a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a --CN group, a --CONH.sub.2 group or a --COOR.sub.8 group, wherein R.sub.8 represents hydrogen or a C.sub.1 -C.sub.6 alkyl group, unsubstituted or substituted by di(C.sub.1 -C.sub.4) - alkylamino;each of R.sub.2, R.sub.3 and R.sub.4 independently represents a hydrogen or a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group or a C.sub.3 -C.sub.4 alkenyloxy group;A completes a bond, thereby providing a double bond or, when R.sub.1 is --COOR.sub.8 wherein R.sub.8 is as defined above, A may represent also a --CH.sub.2 -- group, thereby providing a cyclopropane ring fused to the pyrido ring;R is (a) furyl, thienyl or pyridyl; or(b) a group of formula ##STR2## wherein each of R.sub.5, R.sub.6 and R.sub.7 represents, independently, a hydrogen or a halogen atom, hydroxy, formyloxy, C.sub.2 -C.sub.8 alkanoyloxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.

Abstract: 13, 14 didehydro-15 cyclic prostacyclins have been prepared.

Abstract: A process for the preparation of a pyrazine derivative of the formula ##STR1## wherein R.sub.1 represents hydroxy, C.sub.1 -C.sub.6 alkoxy, or a group of the formula NR.sub.2 R.sub.3 in which R.sub.2 and R.sub.3 are independently a hydrogen atom or C.sub.1 -C.sub.6 alkyl or, together with the nitrogen atom to which they are linked, form a saturated ring having five or six atoms which may contain one or more additional heteroatoms; which process comprises reacting a compound of the formula: ##STR2## wherein R represents a hydrogen atom, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkoxy, Y represents a hydrogen atom or a sodium, lithium, or potassium ion, and A is a nitrile group or a substituent of the formula COR.sub.1 where R.sub.1 is as defined above either with pyruvic aldehyde oxime of the formula: ##STR3## or with a pyruvic aldehyde oxime acetal derivative of the formula: ##STR4## wherein R.sub.4 and R.sub.5 are independently a hydrogen atom or C.sub.1 -C.sub.

Abstract: Compounds of the formula (I) ##STR1## wherein the symbol represents a single or a double bond; Z completes a single bond or is a --CH.sub.2 -- group; 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);one of R.sub.5 and R.sub.6 is hydrogen and the other is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.

Abstract: Azinomethyl-rifamycins I ##STR1## (wherein Y=H or COCH.sub.3 and either R.sub.1 =C.sub.1 -C.sub.7 alkyl or C.sub.3 -C.sub.4 alkenyl and R.sub.2 =C.sub.1 -C.sub.7 alkyl, C.sub.2 -C.sub.4 cloro-, hydroxy-, or alkoxy-alkyl C.sub.3 -C.sub.4 alkenyl, cycloalkyl having a C.sub.3 -C.sub.7 ring, cycloalkylalkyl having a C.sub.3 -C.sub.6 ring, phenyl or C.sub.7 -C.sub.8 aralkyl optionally monohalogen substituted in the aryl group or NR.sub.1 R.sub.2 = a cyclic moiety, said moiety being pyrrolidinyl, piperidinyl, hexahydroazepinyl or heptahydroazocinyl, each of which are unsubstituted or substituted with 1 or 2 methyl radicals, 4-alkyl-1-piperazinyl, morpholinyl or 1,2,3,4-tetrahydroisoquinolinyl) are prepared from rifamycin S by(a) dissolving the rifamycin S in tetrahydrofuran, CHCl.sub.3, dioxan, CH.sub.2 Cl.sub.2 or dichloroethane(b) adding (i) a Schiff's base CH.sub.2 =NR.sub.3 wherein R.sub.3 = t-alkyl or (ii) a compound R.sub.4 N(CH.sub.2 OR.sub.5).sub.2 wherein R.sub.

Abstract: There are provided ergoline derivatives of formula ##STR1## wherein R.sub.1 .dbd.H, CH.sub.3 ; R.sub.2 .dbd.H or halogen atom, or CH.sub.3,CN, alkyl- or phenyl-thio; R.sub.3 .dbd.H, OCH.sub.3 ; R.sub.4 .dbd.C.sub.1 -C.sub.4 hydrocarbon group; X.dbd.O, S, NH; A.dbd.CO, SO.sub.2 ; B.dbd.C.sub.1 -C.sub.4 hydrocarbon group, aryl, aralkyl, heterocyclic ring group, alkoxy, aryloxy; n.dbd.0, 1, 2; and pharmaceutically acceptable salts thereof.A process for preparing said compounds is also provided. The compounds show anti-hypertensive activity and are active on the gastroenteric system.

Abstract: New pharmaceutical sustained-release compositions, formulated as tablets, are prepared by mixing the active ingredient with excipient already granulated and coated with polymers and/or copolymers or a polymers- and/or copolymers-mixture substantially insoluble in water. Such pharmaceutical preparations enable one to enhance or to decrease very easily and precisely the sustained-release effect by regulating the granulometry of the excipient, the excipient/active ingredient ratio, the hardness, and the percentage of the polymers and/or copolymers or of the polymers- and/or copolymers-mixture.

Abstract: Substituted imino derivatives of 4 H-2, 3-dihydrobenzopyran and 4 H-2, 3-dihydrobenzothiopyran, and pharmaceutical compositions containing them. The compounds are active on the central nervous system, in particular as central nervous system depressants, i.e., sedatives, anticonvulsive agents, tranquilizers and sleep-inducing agents.

Abstract: 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. These compounds possess hypolipaemic properties.

Abstract: Compounds of the formula (I) ##STR1## wherein R.sub.1 is:(a) hydrogen, or C.sub.1 -C.sub.6 alkyl;(b) an unsubstituted 2-pyridyl or 3-pyridyl group;(c) a benzyl group, wherein the phenyl ring is unsubstituted or substituted by halogen, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl;(d) a phenyl ring, unsubstituted or substituted by one or two groups chosen from halogen, trihalomethyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkanoylamino, nitro and amino;each of R.sub.2 and R.sub.3 independently represents hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 represents a 2-pyridyl, 3-pyridyl or 4-pyridyl group, unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl;and the pharmaceutically acceptable salts thereof are disclosed. The compounds have activity in the gastroenteric system, particularly anti-ulcerogenic and gastric anti-secretory activity.

Abstract: Compounds of general formula (I) ##STR1## wherein R.sub.1 is a 2-pyridyl, 3-pyridyl or 4-pyridyl group; (b) a phenyl ring, unsubstituted or substituted by one or two groups chosen from halogen, trihalo-C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.6 alkyl, nitro, amino and C.sub.2 -C.sub.6 alkanoylamino; (c) benzyl; or (d) C.sub.1 -C.sub.6 alkyl;each of R.sub.2 and R.sub.3 independently is a hydrogen or a halogen atom or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl;R.sub.5 is (a') ##STR2## wherein each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sub.6 and R.sub.7, taken together with the nitrogen atom to which they are linked, form a morpholino, piperidino, N-pyrrolidinyl or N-piperazinyl ring, wherein the N-piperazinyl ring is unsubstituted or substituted by C.sub.1 -C.sub.6 alkyl;(b') a ##STR3## wherein R.sub.8 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen;(c') --NHR.sub.9, wherein R.sub.

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: Disclosed is a process for preparing the new antitumor glycosides: 4'-deoxy-3'-epi-daunorubicin and 4'-deoxy-3'-epi-doxorubicin starting from the known 3'-epi-4'-keto-N-trifluoroacetyl-daunorubicin.Reduction of the 4'-keto group with sodium borohydride to the corresponding 4'-hydroxy group, reacting the so obtained intermediate with trifluoromethanesulphonic anhydride followed by treatment with n-tetrabutylammonium iodide, dehalogenated reductively, by treatment with tributyl tin hydride to 4'-deoxy-3'-epi-N-trifluoroacetyl-daunorubicin.A mild alkaline hydrolysis removes the N-protecting group to give 4'-deoxy-3'-epi-daunorubicin which is successively transformed, via its 14-bromo derivative, in its doxorubicin analogue.

Abstract: Peptides of the formulaX-A-Pro-Pro-Ile-Ser-B-C-Leu-D-E-F-G-WwhereinX is H, a terminal N atom protecting group of acyl, aromatic urethane, aliphatic urethane, alkyl or aralkyl type, or a residue of a natural L-amino acid, the free amino group of the residue optionally being protected by a terminal N atom protecting group as aforesaid;A is a L-amino acid residue or a glycine residue;B is a neutral L-amino acid residue;C is a neutral L-amino acid residue or an acidic L-amino acid residue;D is a L-amino acid residue which contains in the side chain an alcoholic hydroxyl group; the latter may be free or protected by a usual protecting group for the hydroxy function, said protecting group being t-butyl, trityl, benzyl, 2,4-dichloro-benzyl, benzyloxycarbonyl, 2-bromobenzyloxycarbonyl t-butoxycarbonyl or lower acyl;E is a valence bond or a neutral L-amino acid residue;F is a valence bond or a L-amino acid residue;G is a valence bond or a neutral L-amino acid residue;W is OH, NH.sub.2, OR, NHR, NR.sub.

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: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.

Abstract: A method is disclosed for purifying non-homogeneous systems, known as liposomic suspensions, from non-entrapped drugs wherein said suspensions are treated with liquid or solid polymers of synthetic and organic nature having chemical functionality, which are used as ion-exchangers. The liquid or solid polymers are based on styrene, divinylbenzene, acrylic acid, methacrylic acid, and the like, normally known as ion-exchange resins, and may include carboxylic, phosphonic, or sulphonic functions of different matrices. The ion-exchange resins may also include salified quaternary ammonium, primary, secondary and tertiary amminic or phosphinic functions or other functions with different matrices, including phenolformaldehyde, styrene-divinylbenzene, acrylates, methacrylates, hydrocarbons and condensation-resins.