Abstract: The present invention relates to pyrrolo[2.1-a]isoquinolines which are inhibitors of phosphodiesterase 10a, a process for preparing these compounds and a method of treating cancer in humans and animals by administering these compounds.

Abstract: The invention relates to novel aryl and heteroaryl sulfonates of formula (Ia) and to methods for producing them and to novel aryl and heteroaryl sulfonates of formula (I) for treating and/or preventing diseases, especially for treating pain and neurodegenerative diseases, A representing (C6-C10)-aryl or 5-10-membered heteroaryl, D representing (C6-C10)-arylene or 5-10-membered heteroarylene, R1 representing (C4-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—, —SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl, in formula (Ia); and R1 representing (C3-C8)-alkyl, (C2-C8)-alkyl, the carbon chain being interrupted by one or two heteroatoms or groups chosen from the following group: —O—, —S—,—SO—and —SO2—, (C2-C8)-alkenyl or (C2-C8)-alkinyl.

Abstract: Substituted tetrahydro-naphthalenes and analogous compounds are prepared by reducing or condensing appropriate functional substituents in substituted tetrahydro-naphthalenes and analogous compounds by customary methods and converting functional groups in this manner into the desired groups. The compounds according to the invention are suitable for use as active compounds in pharmaceuticals, in particular in pharmaceuticals for treating arteriosclerosis and also dyslipidaemias.

Abstract: The invention relates to novel phenoxyphenyl alkanesulphonates, processes for their preparation, their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment of states of pain and neurodegenerative disorders

Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hypertipoproteinaemia and arteriosclerosis.

Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The, cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hyperlipoproteinaemia and arteriosclerosis.

Abstract: The invention relates to a process and intermediates for the preparation of enantiomerically pure cycloalkanoindolecarboxylic acids and azaindolecarboxylic acids and pyrimido?1,2a!indolecarboxylic acids and their activated derivatives, characterized in that the tolyl acetic acid is first esterified with a chiral alcohol, then diastereoselective substitution at .alpha.-carbon atoms is carried out and this product is halogenated in the tolyl group and then reacted with appropriate cycloalkanoindoles, cycloalkanoazaindoles or pyrimido?1,2a!indoles. It is possible by this method to prepare specifically, in high purity, the enantiomerically pure carboxylic acids which are intermediates for valuable medicaments.

Abstract: The invention relates to new ?3-amino!-tetrahydrocarbazole-propanoic acid esters which can be used as intermediates for the preparation of known thromboxane-antagonistic active compounds, and to a method for the purification of these active compounds.

Abstract: The present invention relates to a one-pot process for the preparation of 7-heterocyclyl-substituted 3-quinolonecarboxylic acid derivatives. They possess a strong anti-microbial effect. They include active compounds such as, for example, ofloxacin, ciprofloxacin or enrofloxacin.

Abstract: (7-APCA) having the formula (I) ##STR1## which is an important synthesis intermediate in the preparation of cephalosporin-like antibiotics, is prepared by treating a compound of the formula (II) ##STR2## in which R.sub.1 and R.sub.2 represent alkyl, aryl and aralkyl radicals, with a strong protonic acid or with a Lewis acid. Compound (II) is prepared by adding triphenylphosphine and alkali metal iodide to a compound of the formula (VI) ##STR3## then reacting with acetaldehyde in base. Compound (VI) is prepared by treating a compound of the formula (VII) ##STR4## with a base in a polar solvent at -70.degree. C. to 0.degree. C. Compound (VII) is prepared by treating a compound of the formula (VIII) ##STR5## with a chlorinating agent in an organic solvent.

Abstract: Known quinolone carboxylic acid derivatives of the formula ##STR1## are treated so as to become readily administrable parenterally, the treatment comprising dissolving the active compound using an acid, allowing the solution to stand for about 0.15 to 150 hours at a temperature from room temperature to the boiling point of the solution, filtering the solution, precipitating the active compound from the solution using a basic reagent, and converting the precipitated active compound into a form which can be administered parenterally.

Abstract: In the preparation of nitrenedipine by reaction of an ylidene compound of the formula ##STR1## with an enamine compound of the formula ##STR2## the improvement which comprises effecting the reaction in the presence of a catalytic amount of diisopropylamine acetate or dimethylbenzylamine acetate. The product is produced in high yield with reduced amounts of symmetrical by-products.

Abstract: The new compounds of the formula ##STR1## in which Acyl is alkylcarbonyl optionally substituted by halogen or aryl, or arylcarbonyl, which is substituted by lower alkoxy, halogen or nitro,R.sup.1 is an alkyl or alkenyl radical, andR.sup.4 is an optionally substituted branched or straight-chain C.sub.1 -C.sub.6 -alkyl radical or a cycloalkyl radical,are produced by reacting a 2-halogenoacetylacrylic acid ester of the formula ##STR2## with an acylthiourea of the formula ##STR3## The reaction can be conducted in aqueous DMF, substantially pure Z-isomer selectively crystallizing out.

Abstract: In the preparation of a 1,4-dihydropyridine of the formula ##STR1## in which R is a phenyl radical which is optionally substituted once or twice by nitro and/or chlorine,R.sub.1 is a C.sub.1 -C.sub.4 -alkyl radical which is optionally substituted by a C.sub.1 -C.sub.4 -alkoxy group, andR.sub.2 is a C.sub.1 -C.sub.12 -alkyl radical which is optionally substituted by a C.sub.1 -C.sub.4 -alkoxy group, a trifluoromethyl group or the radical (C.sub.6 H.sub.5 CH.sub.2) (CH.sub.3)N,by preparing an ylidene compound of the formula ##STR2## and reacting such ylidene compound with an enamine compound of the formula ##STR3## the improvement which comprises preparing the ylidene compound by reaction of a ketocarboxylic ester of the formula ##STR4## with an aldehyde of the formula RCHO, in a solvent in the presence of a catalytic amount of any acetate salt of an amine, at a temperature from about -10.degree. C. up to 100.degree. C. The products symmetrical or unsymmetrical, are produced in high yield and purity.

Abstract: A 3-.beta.-(vic-dihydroxyphenylmethyleneamino-2-oxo-imidazolidine)- or 3-.beta.-(vic-dihydroxyphenyl-methyleneamino-2,3-dioxo-piperazine)-1-carbo nylamino-acetamidoazetidin-2-one having an acidic grouping on .sub.1 N, e.g. of the formula ##STR1## The compounds are antibiotically active, especially against Pseudomonas bacteria and can be used in combating bacterial infection, as a preservative and as a growth promoting agent in animal feeds.

Abstract: A .beta.-lactam of the formula ##STR1## or a hydrate thereof, in whichR represents a hydrogen atom or a methoxy group,n is 1 or 2,Z represents a group of the formula ##STR2## wherein R.sup.