Abstract: Method of treating 5-HT.sub.3 -mediated disorders, which comprises systemic administration of an effective amount of a compound of formula (I) ##STR1## the pharmaceutically acceptable acid addition salt forms and the stereochemically isomeric forms thereof, wherein R.sup.1 and R.sup.2 represent hydrogen, or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH-- (a), --CH.dbd.C(Cl)--CH.dbd.CH--(b) or --CH.dbd.CH--C(Cl)=CH-- (c); n represents 2, 3 or 4; R.sup.3 represents hydrogen or methoxy; m represents 1 or 2; R.sup.4 represents hydrogen, amino or C.sub.1-3 -alkylcarbonylamino; and R.sup.5 represents hydrogen or halo; novel compounds; compositions; processes for preparing novel compounds and intermediates.

Abstract: The present invention is concerned with a novel benzamide derivative of formula (I). ##STR1## Pharmaceutical compositions comprising said novel compounds, processes for preparing compounds and compositions, and the use thereof as a medicine, in particular in the treatment of conditions involving a decreased motility of the intestine are described.

Abstract: The present invention concerns novel oxadiazole derivatives of formula (I) ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sup.3 is hydrogen; or R.sup.2 and R.sup.3 taken together may form a C.sub.2-3 alkanediyl radical wherein one or two hydrogen atoms may be replaced by C.sub.1-4 alkyl; R.sup.4 is hydrogen or C.sub.1-6 alkyloxy; X is a bivalent radical of the formula ##STR2## L is a radical of formula -Alk-R.sup.5 or -Alk--O--R.sup.6, Alk is C.sub.1-12 alkanediyl; R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkylsulfinyl, C.sub.1-6 alkylsulfonyl, aryl, arylcarbonyl, tetrahydrofuran, dioxolane, dioxolane substituted with C.sub.1-6 alkyl, dioxane, dioxane substituted with C.sub.1-6 alkyl; R.sup.6 is hydrogen, aryl, C.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.

Abstract: There is disclosed a process for preparing (l)-(-)-2-aminocarbonyl)-N-(4-amino-2,6-dichlorophenyl)-4-?5,5-bis(4-fluor ophenyl)pentyl!-1-piperazineacetamide which comprises the steps of (a) cyclizing (-)-(S,S)-N.sup.1,N.sup.

Abstract: A method and apparatus for indicating when a female stock animal has been ridden or mounted by another stock animal comprises providing indicator means which is mounted on a female animal to be monitored. The apparatus is directly engaged by the other stock animal during riding or mounting and pressure applied to a smoothly curved actuator causes release of a signalling element to provide a visually observable signal. The device is re-setable by simple manual intervention and can be transferred to another animal after use.

Abstract: The present invention relates to the use of a cyclodextrin or a derivative thereof as a mucoadhesive in an emulsion or aqueous solution, said cyclodextrin or derivative thereof being used in an amount from 10% to 70% by weight based on the total weight of the composition.

Abstract: The present invention is concerned with a film coated tablet comprising as active ingredients the analgesic agent paracetamol and the antiemetic agent domperidone, and with a process of preparing such tablets.

Abstract: The invention is concerned with the compounds having the formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X is O or S; Y is CH or N; R.sup.1, R.sup.2 and R.sup.3 each independently are hydrogen or C.sub.1-4 alkyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy; R.sup.6 is C.sub.1-4 alkyl; C.sub.1-4 alkyl substituted with arylcyclohexyl; aryl or arylcarbonyl; wherein aryl is phenyl optionally substituted with one or two substituents selected from halo and C.sub.1-4 alkyl;Z is C=O or CHOH; and ##STR2## Compositions comprising said compounds, processes for preparing the same and the use of these compounds as a medicine.

Abstract: Synergistic fungicidal compositions containing a fungicidal triazole and metconazole for treating plants or the loci thereof, or for use in wood-preservation or protection of biodegradable materials. Method of treating plants comprising the administration of a fungicidal triazole and metconazole. Method of protecting wood, wood-products and biodegradable materials from fungal attack and destruction.

Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.

Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3 to R.sup.10 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxycarbonyl; R.sup.11 is hydrogen, C.sub.1-6 alkyl, or trifluoromethyl; R.sup.12 is hydrogen, C.

Abstract: The present invention relates to pharmaceutical compositions containing as active ingredient micronized nebivolol of formula (I) and ways of preparing said compositions.

Abstract: A process for preparing (+)-6-?(4-chlorophenyl)(1H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole comprising the resolution of (.+-.)-6-!(4-chlorophenyl)-hydrazinomethyl)-1-methyl-1H-benzotriazole and converting the appropriate enantiomerically pure hydrazine intermediate into (+)-6-?(4-chlorophenyl)(H- 1,2,4-triazol-1-yl)methyl!-1-methyl-1H-benzotriazole.

Abstract: A solution is disclosed for intravenous administration containing lubeluzole or a pharmaceutically acceptable addition salt thereof, an isotonizing agent, water and acid and base substances to adjust the pH of the solution in the range from 2.5 to 3.6.

Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.

Abstract: Compounds of the formula: ##STR1## in which R.sup.1, R.sup.2 represent H or methyl and R.sup.3, R.sup.4 represent H, C.sub.1-4 alkyl or C.sub.2-4 alkenyl; R.sup.3 and R.sup.4 together can also be butylidene are interesting camphor derivatives. They exhibit valuable odor characteristics.

Abstract: The invention relates to a process for the preparation of N-tert.butyl-decahydro-2-?2(R)-hydroxy-4-phenyl-3(S)-phthalimidobutyl!-(4a S,8aS)-isoquinoline-3(S)-carboxamide of the formula ##STR1## as well as novel intermediates. The compound of formula I, specifically described in Example 1 of European Patent Publication 0,432,694, is a valuable intermediate for pharmacologically active compounds. The compound of formula I can be converted into pharmacologically active compounds which are suitable for the treatment of viral infections, such as those caused by HIV and other retroviruses.

Abstract: A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host requiring such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, halogen, lower-alkoxy or nitro;R.sub.2 is hydrogen, lower alkyl or trifluoromethyl; andR.sup.3 is hydrogen, lower alkyl, trifluoromethyl, benzyl, hydroxy-lower-alkyl, lower alkoxy, lower-alkyl-carbonyl-amino, carbonyl-lower-alkyl, benzyl, di-lower-alkyl-amino-carbonyl, carbonylamino or amino-carbonyl-amino; orR.sup.2 and R.sup.3 together optionally are a fused benzene ring andR.sup.4 is hydrogen or halogen,or a pharmaceutically acceptable salt of a compound of formula I, and a pharmaceutically inert carrier material.

Abstract: A pharmaceutical composition suitable for the treatment of cardiovascular disorders is described which comprises an inhibitor of the Renin Angiotensin System and an endothelin antagonist.

Abstract: A process for the manufacture of 4H-imidazo?1,5-a!?1,4!benzodiazepine derivatives of formula I ##STR1## wherein R.sup.1 is phenyl or mono- or disubstituted phenyl;R.sup.2 is hydrogen, halogen, nitro, cyano, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or lower alkyl; andR.sup.4 is hydrogen or lower alkyland of pharmaceutically usable salts of these compounds by decarboxylating a 4H-imidazo?1,5-a!?1,4!benzodiazepinecarboxylic acid of formula II ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the above significances, at elevated temperature and under elevated pressure in the presence of an organic solvent. The compounds of formula I and their pharmaceutically usable acid addition salts are known muscle relaxants, sedatives and anticonvulsants.