Abstract: Ergot alkaloids having interesting pharmacological activities, for instance in the therapy of migraine or hypertension. Such compounds are obtained in a fermentative process using mutant strains of Claviceps purpurea eventually hydrogenating the products thus obtained.

Abstract: [14-.sup.14 C]-daunorubicin and doxorubicin are prepared by reacting 9-desacetyl-9-formyl-N-trifluoroacetyl daunorubicin with [.sup.14 C]-diazomethane to form [14-.sup.14 C]-N-trifluoroacetyl daunorubicin from which the protecting group is removed by mild alkaline hydrolysis to afford [14-.sup.14 C]-daunorubicin which is then, in the form of the hydrochloride, reacted with bromine to form the corresponding labelled 14-bromo derivative, which, upon treatment with sodium formate leads to [14-.sup.14 C]-doxorubicin.

Abstract: New ergoline derivatives are disclosed which are compounds of formula (I) having the structure: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or methyl; andX is hydroxy, R.sub.3 COO, S--R.sub.4 or NR.sub.5 R.sub.6 in which R.sub.3 is a straight or branched alkyl having from 1 to 6 carbon atoms, unsubstituted- or substituted-phenyl, the substituents being selected from the class consisting of chlorine, bromine, alkyl or alkoxy having from 1 to 4 carbon atoms, cycloalkyl containing from 3 to 6 carbon atoms, or a heterocycle;R.sub.4 is phenyl or a heterocycle, andR.sub.5 and R.sub.6 are alkyl having from 1 to 4 carbon atoms, or together with the N atom to which they are attached, forming a heterocycle.

Abstract: Anthracycline disaccharides having antitumor activity are prepared by condensing N-trifluoroacetyldaunomycin with a 1-halosugar in the presence of a silver salt such as AgSO.sub.3 CF.sub.3 as catalyst to form a protected di-glycoside which upon mild alkaline hydrolysis yields the novel disaccharides.

Abstract: Disclosed are antitumor compounds of the formula: ##STR1## wherein R.sub.1 is a C.sub.2 -C.sub.4 alkyl; a C.sub.3 -C.sub.6 cycloalkyl; a C.sub.3 -C.sub.6 cycloalkyl substituted by a halogen, hydroxy, methoxy, amino or dimethylamino group; phenyl or phenyl substituted with nitro, chlorine or methoxy; thiazyl, pyridyl, pyrazyl; or a phenyl-alkyl group of the formula X--Phe--(CH.sub.2).sub.n --, in which X is hydrogen, halogen, hydroxyl, amino, or nitro and n is an integer from 1 to 2; R.sub.2 is hydrogen, hydroxyl or acyloxy (R--COO--), where R is an alkyl having from 1 to 11 carbon atoms; and R.sub.3 is hydrogen or trifluoroacetyl and salts thereof with pharmaceutically acceptable acids. Compounds I are prepared by condensing the aglycones thereof with 2,3,6-trideoxy-3-trifluoroacetamido-4-O-trifluoro-acetyl-.alpha.-L-lyxopyr anosyl chloride according to a conventional technique.

Abstract: A method is disclosed for inhibiting prolactin secretion in a female mammal which comprises administering to the mammal an effective dose of 6-methyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline, or 1,6-dimethyl-8.beta.-carbobenzyloxy-aminomethyl-10.alpha.-ergoline, or a pharmaceutically acceptable acid addition salt thereof.

Abstract: 7-Acylamino-3-pyrazinylthiomethyl-3-cephem-4-carboxylic acids are disclosed having the general formula: ##STR1## wherein R is an alkyl having from 1 to 5 carbon atoms or ##STR2## wherein Y = Y.sup.1 = HY = y.sup.1 = clY = cl, Y.sup.1 = FY = h,y .sup.1 = cl andIn which n is an integer from 1 to 4, X is O or S, and R.sub.2 is thienyl, phenyl, 1,4-cyclohexadienyl, phenoxy, pyrazinyl and substituted phenyl, thienyl, pyrazinyl and phenoxy, the substituent being selected from the group consisting of hydroxy, chlorine, bromine, and alkyl and alkoxy having from 1 to 4 carbon atoms;R.sub.3 is alkali metal such as sodium or potassium, hydrogen, alkyl having from 1 to 4 carbon atoms, benzyl, trichloroethyl, methoxybenzyl, benzhydryl, pivaloyloxymethyl, and an alkaline earth metal; R.sup.1 may be a pyrazinyl of the general formulae: ##STR3## in which R.sup.4, R.sup.5, R.sup.

Abstract: Disclosed are new antitumor compounds of the formula: ##STR1## wherein R is hydrogen or trifluoroacetyl and the hydrochlorides thereof and a process for making same. Also disclosed is a novel intermediate (9-desacetyl-9-formyl-N-trifluoroacetyldaunorubicin) used in the process.

Abstract: A process is disclosed for preparing compounds of structure: ##STR1## where R.sup.1 is hydroxyl, alkoxy with 1 to 4 carbon atoms, trichloroethoxy, benzyloxy, p-methoxybenzyloxy, p-nitrobenzyloxy, benzhydryloxy, triphenylmethoxy, phenacyloxy, or p-halophenacyloxy;Z is hydrogen, hydroxyl, --O-alkyl, --O--CO-alkyl, --Br, --I, --N.sub.3, --O--CO--CH.sub.3, O--CO--NH.sub.2, or an S-mononuclear heterocyclic ring,Starting from ##STR2## where R is hydrogen, alkyl having from 1 to 4 carbon atoms, cyano-methyl, thienyl-methyl, furyl-methyl, naphthyl-methyl, phenyl-methyl, phenoxy-methyl, phenyl-isopropyl, phenoxy-isopropyl, pyridyl-4-thiomethyl, or tetrazolyl-1-methyl;R.sup.2 and R.sup.3 are lower alkyl, a mononuclear aryl ring, CN, a mononuclear heterocyclic ring or the radicals --COR.sup.4, --COOR.sup.4, ##STR3## --CONHR.sup.4, or R.sub.2 and R.sub.3 together represent ##STR4## where T represents ##STR5## and R.sup.

Abstract: New 4,5,6,7-tetrahydroimidazo-[4,5-c]-pyridine derivatives are disclosed, and more particularly derivatives of Formula I ##STR1## where R.sub.1 is hydrogen or an alkyl having from 1 to 4 carbon atoms;R.sub.2 is hydrogen, an alkyl having from 1 to 4 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, phenyl or a heterocycle;R.sub.3 is hydrogen, a saturated or unsaturated straight or branched alkyl having from 1 to 6 carbon atoms, a cycloalkyl having from 3 to 6 carbon atoms, benzoyl or phenyl; andX is O, S or NR.sub.4 where R.sub.4 is hydrogen, an alkyl having from 1 to 4 carbon atoms, cyano, amino, nitro or acylamino;Or pharmaceutically acceptable acid addition salts thereof.

Abstract: Aglycones of the formula ##STR1## and Toslyhydrazones of the formula ##STR2## wherein R.sub.1, R.sub.2 and Ts have meanings described in the specification, and process for preparing a compound of formula (V).

Abstract: Novel antitumor antibiotics, which are daunomycin analogues of the formula: ##STR1## wherein R.sub.1 is hydrogen or a C.sub.1 -C.sub.4 lower alkyl, R.sub.2 is a C.sub.1 -C.sub.4 lower alkyl, a C.sub.3 -C.sub.6 cycloalkyl, phenyl, lower alkyl phenyl, lower alkoxy phenyl or halophenyl, and R.sub.3 is hydrogen or trifluoroacetyl are prepared by condensing 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxopyra nosyl chloride with novel aglycones of the formula: ##STR2## which are in turn prepared by a novel method from 14-bromodaunomycinone through a series of novel intermediates.

Abstract: Optically active anthracyclinones are prepared by reacting an optically active (-) 1,4-dimethoxy-6-hydroxy-6-acetyl-tetralin with a phthalic anhydride in the presence of AlCl.sub.3 or AlBr.sub.3 and an alkali metal chloride at 130-180.degree. C. for 1 to 10 minutes.

Abstract: Daunorubicin (also known as daunomycin) derivatives of the formula ##STR1## wherein X is ##STR2## and R is --COCF.sub.3 or H which are prepared by hydrogenating 9-desacetyl-9-keto-N-trifluoroacetyldaunorubicin, an unexpectedly stable key-intermediate which is itself a new compound, are useful in treating certain mammalian tumors.

Abstract: Disclosed is a class of novel daunosaminyl anthracyclinones which are useful in treating Sarcoma 180 ascites.

Abstract: Amino- and oxygen-protected pseudotrisaccharide is disclosed, which has been proved to be a useful intermediate for preparing aminoglycoside antibacterial antibiotics related to paromomycin and neomycin. Process for its preparation is also disclosed.

Abstract: Novel substituted pyrazine derivatives are disclosed having the general formula (I): ##STR1## where R.sub.1 and R.sub.2 may be methyl, methoxy, halogen (particularly chlorine, bromine or fluorine), or hydrogen, with the proviso that R.sub.1 and R.sub.2 cannot both be hydrogen, and X may be S or NH.These novel substituted pyrazine derivatives show a remarkable activity as inhibitors of platelet aggregation at very low dosages.

Abstract: Disclosed is a process for preparing glycoside antitumor antibiotics, including the known compounds daunomycin, adriamycin, 4'-epi-daunomycin and 4'-epi-adriamycin and the novel antibiotics, 3',4'-epi-6'-hydroxydaunomycin, 3',4'-epi-6'-hydroxyadriamycin. 3',4'-epi-daunomycin, 3',4'-epi-adriamycin, 4-demethoxy-4'-epi-daunomycin and 4-demethoxy-4'-epi-adriamycin. Process involves reacting daunomycinone or 4-demethoxy-daunomycinone with a protected 1-halo derivative of 3,4-epi-6-hydroxydaunosamine, 3,4-epi-daunosamine or 4-epi-daunosamine in an inert solvent in the presence of a soluble silver salt catalyst to form a protected derivative of the glycoside antibiotic and removing the protecting groups.

Abstract: Racemic anthracyclinones of the general formula II ##STR1## when condensed with 2,3,6-trideoxy-3-trifluoroacetamido-4-0-trifluoroacetyl-.alpha.-L-lyxo-pyr anosyl chloride in the presence of silver trifluoromethane sulphonate yield an easily separable mixture of equimolar amounts of exclusively the .alpha.-glycoside of the 7S : 9S diastereomer and the .beta.-glycoside of the 7R : 9R diastereomer. In this way the biologically important .alpha.-glycosides of the 7S : 9S diastereomer of the general formula I (below) are easily prepared from a racemic anthracyclinone.

Abstract: The known antibiotics adriamycin and its .beta.-anomer, and the novel compounds, 4'-epiadriamycin (both .alpha.- and .beta.-anomers) are prepared by condensing a novel, reactive protected derivative of adriamycinone with reactive intermediates which are 1-halo-2,3,6-trideoxy-3-trifluoroacetamido-4-trifluoroacetoxy-.alpha.-L-ly xo (or arabino) hexopyranoses.