Abstract: A process is disclosed for preparing 5-sulfamoylbenzoic acids substituted in 4-position by various substituents and in 3-position by a cyclic amino group having sali-diuretic properties. Novel intermediate compounds are also disclosed.

Abstract: L-3,4-dehydroproline is produced in good yield from D,L-3,4-dehydroproline by resolution via the tartaric acid salt and thermal racemization of the D-3,4-dehydroproline tartaric acid salt containing mother liquors.

Abstract: The invention concerns a process for the manufacture of 7.beta.-amino-3-cephem-3-ol-4-carboxylic acid compounds by ring closure of esters of 2-[4-(substituted-thio)-3-acylamino-2-oxoazetidin-1-yl]-3-substituted-amin o-crotonic acids and solvolysing the enamino group in the resulting 7.beta.-acylamino-3-substituted-amino-cephem-4-carboxylic acid esters.

Abstract: Novel alkylenetris- and alkylenetetrakis-[1,2,3,4-tetrahydroisoquinoline] and -[3,4-dihydroisoquinoline] compounds, the pharmaceutically acceptable acid addition salts thereof and compositions containing such substances have been found useful for inhibiting the formation of blood clots in mammals and/or dissolving blood clots in mammals after they have been formed.

Abstract: The imidyl compounds, according to the invention, of the formula I are suitable for the manufacture of polymers which can be crosslinked by light, which polymers can be, for example, polyesters, polyamides, polyamide-imides, polyimides, polyester-polyamides, polyester-amide-imides, polyethers, polyamines, polysaccharides and polysiloxanes. Polymers of this type are suitable for carrying out photochemical processes. Compared with known polymers, the polymers based on the imidyl compounds according to the invention have the advantage that they are photochemically substantially more sensitive. In addition, this sensitivity can also be further increased effectively by a combination with sensitizers.

Abstract: New proline derivatives and related compounds which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.

Abstract: Glycyrrhetinic acid esters of the formula: ##STR1## wherein R is hydrogen or an acyl radical of 2 to 20 carbon atoms and R.sub.1 is a lower alkyl of 1 to 4 carbon atoms and the haloacid or alkylsulfate quaternary ammonium salts thereof as well as a process for preparing same are provided. The compounds of the invention display anti-inflammatory, antihistaminic, and anti-ulcer pharmacological activity.

Abstract: Imidazo[2,1-a]isoquinolines useful as anorexics and antidepressants are prepared from a dilithium derivative of a 2-(o-tolyl)-2-imidazoline.

Abstract: Cis-1-cyclopropylmethyl-3a-(substituted-phenyl) decahydroisoquinoline, useful as analgetic agonist and analgetic antagonist.

Abstract: Imidazo[2,1-a]isoquinolines useful as anorexics and anti-depressants, e.g. 5-(2-thienyl)-2,3,5,6-tetrahydroimidazo[2,1-a]isoquinolin-5-ol, are prepared from a dilithium derivative of a 2-(o-tolyl)-2-imidazoline.

Abstract: Ergolines are chlorinated with SO.sub.2 Cl.sub.2 /BF.sub.3 .multidot.etherate, preferentially in the 2 position.

Abstract: Process for resolving enantiomers of 1-t-butylamino-2,3-dihydroxypropane using a pyroglutamic acid or a tartaric acid as resolving agent. The enantiomers of 1-t-butylamino-2,3-dihydroxypropane are useful in preparing .beta.-adrenergic blocking agents.

Abstract: Novel 5-(2-pyrroyl) and 5-(N-lower alkyl-2-pyrroyl)-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid compounds represented by the formula: ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein each of R and R.sup.1 is independently hydrogen or a lower alkyl group having from 1 to 4 carbon atoms and process for the production of such compounds; 5-(N-methyl-2-pyrroyl)-1,2-dihydro-3H-pyrrolo?1,2-a!pyrrole-1-carboxylic acid is representative of the class. These compounds are useful as anti-inflammatory analgesic and anti-pyretic agents and as smooth muscle relaxants.

Abstract: Compounds of the formula (I): ##STR1## and salts thereof wherein X is a group: ##STR2## R is hydrogen, methyl or ethyl; R.sub.1 is phenyl or naphthyl or phenyl substituted by fluorine, chlorine, bromine, methyl, methoxy or trifluoromethyl; R.sub.2 is hydrogen or methyl; R.sub.3 is hydrogen, methyl, ethyl or benzyl; R.sub.4 is hydrogen or methyl; and R.sub.5 is hydrogen or methyl; have been found to be mood modifying agents and anorexic agents.

Abstract: This invention relates to certain structural and pharmacological analogs of prostacyclin (PGI.sub.2) wherein a nitrogen atom is substituted for the 6,9.alpha.-epoxy-oxygen of prostacyclin. These novel nitrogen-containing prostacyclin-type compounds are useful for the pharmacological purposes for which prostacyclin is used, e.g., as antithrombotic agents, smooth muscle stimulators, gastric antisecretory agents, antihypertensive agents, antiasthma agents, nasal decongestants, or regulators of fertility and procreation.

Abstract: Quinine, quinidine, their antipodes or racemates and derivatives thereof, are prepared by (a) cyclizing the correspondingly substituted 4-[3-(1-chloro-3(R)-alkyl(or alkenyl)-4-(R)-piperidyl)-1-oxopropyl]quinolines, antipodes or racemates thereof, to the corresponding 4-[5(R)-alkyl(or alkenyl)-4-(S)-quinuclidin-2(S) or 2(R)-ylcarbonyl]quinolines, antipodes or racemates thereof; and (b) stereoselectively reducing the products of step (a) to .sup.a (S)-[5(R)-alkyl(or alkenyl)-4(S)-quinuclidin-2(R)-yl]-4-quinoline-methanols, antipodes or racemates thereof, and .alpha.(R)-[5(R)-alkyl(or alkenyl)-4(S)-quinuclidin-2(S)-yl]-4-quinolinemethanols, antipodes or racemates thereof. Various intermediates and the end products are useful antimalarial and antiarrhythmic agents.

Abstract: This invention relates to novel indolothiopyrones having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, nitro-substituted-aryl, or .omega.-substituted lower alkyl wherein the substituent is: ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen, lower alkyl, or together with the nitrogen atom, form a heterocyclic ring; and R.sub.6 is lower alkoxy or amino, and novel intermediates used in their preparation. The indolothiopyrones are prepared by reacting a 3-mercaptoindole with sodium propiolate or a substituted sodium propiolate followed by acidification to obtain an intermediate acid; the intermediate acid cyclizes in the presence of an acid catalyst to obtain the indolothiopyrone structure which may be additionally subjected to halogenation, alkylation or hydrolysis to obtain derivatives having the various substituent groups disclosed.

Abstract: An N-perfluoroacyl-L-.alpha.-amino acid is converted to the corresponding acid halide which is useful as a resolving agent for the resolution of racemic amines.

Abstract: Novel 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein R is hydrogen or a lower alkyl group containing from 1 to 4 carbon atoms and R.sup.1 is hydrogen, a lower alkyl group having from 1 to 4 carbon atoms, a lower alkoxy group of 1 to 4 carbon atoms, chloro, fluoro or bromo, the R.sup.1 substitution being at the ortho, meta or para positions of the aroyl group and process for the production of such compounds; 5-p-toluoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid is representative of the class. These compounds, as the racemic mixture or the (1)-isomer, are useful as anti-inflammatory, analgesic and antipyretic agents and as smooth muscle relaxants.

Abstract: A process is disclosed for the preparation of a compound of the formula I ##STR1## where R is hydrogen or methyl, X is sulphur or the NH group, Y is selected from the class consisting of methyl, methoxy, chlorine, bromine, iodine, nitro or cyano, m is 0, 1 or 2, and n is 1 or 2, characterized in that a compound of the formula II: ##STR2## where R and n have the above-mentioned meanings, is reacted in a suitable polar aprotic solvent, such as dimethylforamide or dimethylsulphoxide, under a nitrogen atmosphere and at a temperature between 50.degree. and 100.degree. C, with the sodium salt of an appropriate 2-aminopyridine or 2-mercaptopyridine to give, after evaporation of the solvent in vacuo, the desired compound of formula I which is then purified by methods known "per se".The invention also includes the compounds of general formula I, where R, X, Y, m and n have the same meanings, and their pharmaceutically acceptable salts.