Abstract: A 6- or 8-monooxy- or 6,8-dioxy-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline in which the 3-position is unsubstituted, is useful as a pharmaceutical, in particular as a prolactin secretion inhibitor, dopaminergic agent and dopamine receptor stimulating agent.

Abstract: Compounds according to the formula ##STR1## , its optical isomers, or a pharmaceutically acceptable salt thereof wherein:m and n are integers of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl and its aliphatic acylates of 1 to 6 carbon atoms or aryl acylates of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl or .alpha.-amino acid side chains;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.6, halo, --NH.sub.2, --N(R.sub.6).sub.2, --NHCOR.sub.6, --COOH, or --COO(R.sub.6) group wherein R.sub.

Abstract: Antidopaminergic agents having selective limbic activity, comprising (S)-enantiomers of aporphine compounds of either the following structures: ##STR1## wherein R.sub.1 is lower alkyl, alkyl substituted lower alkyl, alkyl substituted cycloalkyl, lower alkenyl, alkyl substituted lower alkenyl, lower alkynyl, alkyl substituted lower alkynyl, phenyl lower alkyl, phenyl lower alkenyl, and phenyl lower alkynyl, and the following structure where R.sub.1 is above and R.sub.2 and R.sub.3 are hydrogen, methyl, or R.sub.1 ##STR2## R.sub.1 is as above R.sub.4 is H, CH.sub.3 lower alkyl, or R.sup.1 C0--where R.sup.1 =CH.sub.3 or lower alkyl.

Abstract: Very pure riboflavin (I) is obtained by a process in which the riboflavin is dissolved in dilute aqueous alkali metal hydroxide solution, if necessary the alkaline solution is purified by treatment with active carbon or with a solvent which is insoluble or only slightly soluble in water, the resulting alkaline solution of I is introduced into water which is at 90.degree.-100.degree. C. and to which an acid has been added in an amount such that the reaction mixture is brought to a pH of from 6.5 to 0.8, the temperature being maintained at from 40.degree. to 100.degree. C., the reaction mixture is kept at from 90.degree. to 100.degree. C. for from 10 to 80 minutes and cooled, and I is then isolated.

Abstract: The invention relates to new aqueous pharmaceutical compositions containing as active ingredient a pharmaceutically acceptable complex of a bis-indole compound with a bi- or multivalent metal ion in a therapeutically effective amount. The invention further relates to complexes formed between a bis-indole compound and a bi- or multivalent metal ion.According to another aspect of the invention there is provided a process for the preparation of a pharmaceutically acceptable metal complex of a bis-indole compound and optionally stable aqueous pharmaceutical compositions containing said metal complex, in which a solution of a bis-indole compound or a pharmaceutically acceptable salt thereof in an aqueous medium is reacted with a non-toxic water soluble salt of a bi- or multivalent metal capable of complexation, at a pH of 3.0 to 6.0, optionally in the presence of or followed by the addition of a conventional pharmaceutical carrier and/or further additive, or, if desired, the obtained complex is isolated.

Abstract: A process for the transesterification of a carboxylic or carbonic acid ester comprises reacting the carboxylic or carbonic acid ester under transesterification conditions with an alcohol in the presence, as catalyst, of either (i) a Group V element-containing Lewis base and an epoxide or (ii) a cyclic amidine.The Lewis base can be an organic compound containing trivalent phosphorus or nitrogen and can be an amine, for example an amidine.The process can be operated in the liquid phase at a temperature of from 15.degree. to 150.degree. C., and the catalyst is employed in solution.Preferred catalysts are those where the cyclic amidine forms part of a fused ring system containing six and five membered rings, six and seven membered rings or two six membered rings.

Abstract: The invention relates to new apovincaminol derivatives of the formula /I/ ##STR1## wherein R.sub.1 is hydrogen, nitro or halogen,R.sub.2 is a substituted or unsubstituted alkyl or phenyl group,R.sub.3 and R.sub.4 together form a valency bond or each independently represents hydrogen, hydroxyl or an --OR.sub.5 group, in whichR.sub.5 is substituted or unsubstituted alkanoyl or benzoyl group,with the proviso that if R.sub.2 stands for a 3,4,5-trimethoxyphenyl group and R.sub.1 is hydrogen, R.sub.3 and R.sub.4 together do not form a valency bond, or if R.sub.2 is a 3,4,5-trimethoxyphenyl group and R.sub.3 and R.sub.4 both are hydrogen, R.sub.1 is other than hydrogen, nitro or bromine, and acid addition salts thereof.The compounds may be used in the therapy of various skin diseases accompanied by a pathological cell proliferation, preferably psoriasis.

Abstract: 6-Phenyl-1,2,3,4,4a,5,6,10b-octahydrobenz(h)isoquinolines having anti-depressant activity and methods for their preparation.

Abstract: Novel derivatives of substituted pyrrolizine diones, isomers, and pharmaceutically acceptable derivatives thereof, have therapeutic utility for reducing amnesia induced by electroconvulsive shock and for treating senility.

Abstract: Benzobicyclic lactam acids having a fused aromatic carbocyclic and a saturated lactam ring of five- or six-members, their salts, esters, and amides, are useful in the treatment of senility and for reversing amnesia. Pharmaceutical compositions including these compounds, a method of preparing the compounds, and a method of treating senility and reversing amnesia area also disclosed.

Abstract: Bifunctional derivatives of a 3-carboxhydrazide of an antineoplastic dimeric indole-dihydroindole alkaloids, useful both in forming conjugates with immunoglobulins and as anti-tumor agents.

Abstract: Pyrimidoisoquinoline/compounds of the formula: ##STR1## where R.sup.1 is H, halogen or lower alkyl, R.sup.2 is NH.sub.2, NO.sub.2 or acylamino and R.sup.3 is carboxy or protected carboxy, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are disclosed in this application. Also disclosed is a method of treating allergies by administering the compounds of this invention.

Abstract: Riboflavin of the formula I ##STR1## is prepared by condensation of a 4,5-dimethyl-N-(D)-ribityl-2-phenylazoaniline of the formula II ##STR2## where X is H, --Cl, --NO.sub.2 or --CH.sub.3 in the o- or p-position, with barbituric acid of the formula III ##STR3## in the presence of an acidic condensing agent in an inert organic solvent by an improved process in which the reaction is carried out in an aliphatic diol or triol derivative of the general formula IV ##STR4## where R.sup.1 is H or CH.sub.3, R.sup.2 is H or CH.sub.3 -- or, when n is 0, is CH.sub.3 --CO--O--CH.sub.2 --, R.sup.3 is CH.sub.3 --, C.sub.2 H.sub.5 -- or CH.sub.3 --, R.sup.4 is CH.sub.3 --CO--, or is H when R.sup.3 is CH.sub.3 -- or C.sub.2 H.sub.5 --, and n is 0 or 2, preferably 0, having a boiling point of 80.degree.-180.degree. C., or in a mixture of these as a solvent. In this process, the riboflavin is obtained in particularly pure form and in very good yields.

Abstract: This invention relates to compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein the various substituents are defined herein. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents in mammals.

Abstract: Benzo(f)isoquinoline compounds, particularly, penta- and tetrahydrobenzo(f)isoquinoline dicarboxylic acid compounds, their preparation and their use as calcium entry blockers are disclosed.

Abstract: Novel compounds of the formula I ##STR1## where Cat.sym. is a secondary or tertiary alkylammonium cation of 16 to 30 carbon atoms and the aromatic rings can be further substituted by chlorine, bromine, methyl, methoxy or nitro, are useful for the preparation of low-electrolyte powder and liquid formulations or for coloring organic media.

Abstract: Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans are useful as analgesics or narcotic antagonists and provide enhanced bioavailability of 3-hydroxymorphinans from orally administered doses.

Abstract: Optically active 1-benzyl-3,4-bis-(diphenylphosphino)-pyrrolidine is produced in a three-step process from optically active 1-benzyl-2,5-dioxo-3,4-dihydroxy-pyrrolidine. The product is useful as a chiral ligand in rhodium complexes which serve as catalysts for the homogeneous asymmetric hydrogenation of prochiral substrates.

Abstract: An antineoplastic dimeric indole-dihydroindole (vinca) alkaloid carrying a hydrazine succinimide group at C-3, capable of forming conjugates with a diacid at C-4.