Abstract: The present invention is concerned with vasoconstricive [(benzodioxan, benzofuran or benzopyran)alkylamino]alkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein X is O, CH.sub.2 or a direct bond; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 may be taken together to form a bivalent radical of formula --(CH.sub.2).sub.m --, wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together may form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n --, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd., --CH.dbd.CH--N.dbd., or --CH.dbd.N--CH.dbd.; R.sup.4 is hydrogen or C.sub.1-6 alkyl;Alk.sup.1 is a bivalent C.sub.

Abstract: The present invention is concerned with antiretroviral (e.g. anti-HIV-1) compounds having the formula ##STR1## wherein R.sup.1 and R.sup.2 each independently are halo or methyl; R.sup.3 is hydrogen, halo, nitro or trifluoromethyl; R.sup.4 is trifluoromethyl or methylcarbonyl; or a radical -C(=X)-NR.sup.5 R.sup.6 wherein X is O or S, and R.sup.5 and R.sup.6 each independently are hydrogen or C.sub.1-4 alkyl; or a radical -Alk-R.sup.7, wherein Alk is C.sub.1-4 alkanediyl; and R.sup.7 is hydrogen or hydroxy; Het is a heterocyclic radical of formula: ##STR2## Pharmaceutical compositions containing said compounds of formula (I) and processes of preparing said compounds and compositions.

Abstract: The present invention relates to compounds of the formula ##STR1## wherein R represents hydrogen; C.sub.1-6 alkyl; C.sub.3-6 cycloalkyl; phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; or thienyl optionally substituted with halo or C.sub.1-6 alkyl; and.dbd.C.dbd.X is a radical of the formula:.dbd.C.dbd.O (a),.dbd.C.dbd.N--O--R.sup.1 (b), or.dbd.C.dbd.CH--R.sup.2 (c);the addition salts thereof and stereochemically isomeric forms thereof, said compounds being useful as intermediate to potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflications.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system.

Abstract: A compound of formula ##STR1## the racemic mixture, the (S)-form and the acid addition salts thereof, said compound having anti-stroke properties. Pharmaceutical compositions containing this compound as active ingredient and a method of preparing said compound and pharmaceutical compositions.

Abstract: There is disclosed a process for recovering sucralose-6-ester from a feed mixture of 6-O-acyl-4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose in a reaction medium comprising a tertiary amide (such as N,N-dimethylformamide), wherein said process comprises removing a major proportion of said tertiary amide by steam distillation. In preferred aspects of the invention, the steam distillation is followed by extraction and then purification by crystallization or crystal aging to recover sucralose-6-ester in good yield.

Abstract: The present invention relates to novel 6-aryl-5,6-dihydroimidazo[2,1-b]thiazole derivatives having immunostimulating properties, which are useful for treating humans and warm-blooded animals suffering from disorders and/or diseases wherein the immune system is impaired or suppressed. Processes of preparing said novel compounds and compositions containing the same as active ingredient.

Abstract: Novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifluoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.

Abstract: N-(3-hydroxy-4-piperidinyl)(dihydrobenzofuran, dihydro-2H-benzopyran or dihydrobenzodioxin)carboxamide derivatives, their N-oxide forms and pharmaceutically acceptable salts having gastrointestinal motility stimulating properties, compositions containing these compounds as active ingredient and methods of treating warm-blooded animals suffering from the decreased peristalsis of the gastrointestinal system are disclosed, wherein the compounds have the formula: ##STR1## A represents a group of the formula: --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --wherein one or two hydrogen atoms in the A moiety may be replaced by a C.sub.1-6 alkyl group.

Abstract: The present invention provides novel compounds of formula ##STR1## the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof, wherein A and B taken together form a bivalent radical of formula: --N.dbd.CH-- (a), --CH.dbd.N-- (b), --CH.sub.2 --CH.sub.2 -- (c), --CH.dbd.CH-- (d) --C(.dbd.O)--CH.sub.2 -- (e), --CH.sub.2 --C(.dbd.O)-- (f); R.sup.1 is hydrogen, C.sub.1-6 alkyl, or halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-6 cycloalkyl or C.sub.1-8 alkyl substituted with hydroxy, oxo, C.sub.3-6 cycloalkyl or aryl. Het is five- or six-membered optionally substituted heterocyclic ring. The use as a medicine, especially as a lipid lowering agent is disclosed as well as pharmaceutical compositions and processes for preparing compounds and compositions.

Abstract: The present invention relates to novel 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-one derivatives of formula ##STR1## wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, phenyl optionally substituted with from 1 to 3 substituents each independently selected from halo, hydroxy, C.sub.1-6 alkyloxy, C.sub.5-6 cycloalkyloxy, C.sub.1-6 alkyl or trifiuoromethyl; pyridinyl; thienyl optionally substituted with halo or C.sub.1-6 alkyl; and>C.dbd.X is a radical of formula>C.dbd.O (a),>C.dbd.N--O--R.sup.1 (b),or>C.dbd.CH--R.sup.2 (c);the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, said compounds being potent inhibitors of both phosphodiesterase III and IV, which are useful in the treatment of warm-blooded animals suffering from allergic disorders, atopic diseases and related afflictions. Intermediates in the preparation thereof. Pharmaceutical compositions containing said compounds as an active ingredient.

Abstract: The present invention relates to a topical liposomal formulation comprising piroxicam, a phospholipid, a solvent system for piroxicam and said phospholipid, water and conventional auxiliary formulating agents, and a method of preparing said formulation.

Abstract: A method for treating skin disorders in warm-blooded animals, said method comprising administering to said warm-blooded animals an effective amount of an appropriately substituted benzimidazole or benzotriazole which suppresses the metabolism of retinoids. Compositions comprising said compounds and an effective amount of a retinoid.

Abstract: Piperidinyl substituted benzamides of formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereoisomeric forms thereof, wherein R.sup.1 is hydrogen or halo; R.sup.2 is halo; R.sup.3 is hydrogen or halo; R.sup.4 and R.sup.5 each independently are hydrogen, C.sub.1-4 alkyl or haloC.sub.1-4 alkyl; and the group NR.sup.4 R.sup.5 may also be azido, Alk is C.sub.2-4 alkanediyl; pharmaceutical compositions containing said compounds of formula (I) as active ingredient; use of said compounds as a medicine; process of preparing said compounds; compounds of formula (I) containing a radioactive isotope; process of marking 5HT.sub.2 -receptor sites; and process for imaging an organ are disclosed.

Abstract: There is disclosed a process for producing sucralose from sucralose-6-ester whereby the sucralose-6-ester is deacylated directly either prior to or after removal of the tertiary amide reaction vehicle from the neutralized chlorination reaction mixture, to produce an aqueous solution of sucralose plus salts and impurities, from which sucralose is recovered by extraction and is then preferably purified by crystallization.

Abstract: Pyrroloimidazolyl and imidazopyridinyl substituted 1H-benzimidazole derivatives having the formula ##STR1## wherein n is 0 or 1;R.sup.1 is hydrogen, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, halo, C.sub.1-6 alkyl, hydroxy or C.sub.1-6 alkyloxy;R.sup.2 is hydrogen; C.sub.1-10 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkynyl; C.sub.3-7 cycloalkyl; phenyl; substituted phenyl; C.sub.1-4 alkyl substituted with phenyl, substituted phenyl, naphthalenyl, thienyl, furanyl, C.sub.1-4 alkylfuranyl, C.sub.3-7 cycloalkyl; andR.sup.3 is hydrogen; C.sub.1-8 alkyl; C.sub.3-7 cycloalkyl; hydroxy; amino; C.sub.1-6 alkyloxy; C.sub.1-6 alkyloxycarbonylamino; phenyl; C.sub.1-4 alkyl substituted with phenyl, piperazinyl, 4-(C.sub.1-4 alkyl)piperazinyl or morpholinyl;each substituted phenyl independently is phenyl substituted with a substituent independently selected from halo, hydroxy, hydroxymethyl, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.

Abstract: Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl,D is a bicyclic heterocycle of formula ##STR2## wherein R.sup.1 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, carboxaldehyde, carboxyl, C.sub.1-10 alkylcarbonyloxyC.sub.1-4 alkyl; each R.sup.2 represents hydrogen or C.sub.1-4 alkyl; R.sup.3 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R.sup.4 represents C.sub.1-3 alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl.

Abstract: The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and processes of preparing said compounds and compositions.

Abstract: A method of topically treating subjects suffering from acne, hyperkeratotic dermatoses and photo-aging of the skin, by administering to the skin of said subjects an effective amount of the antifungal compound ketoconazole and a retinoid is disclosed. Compositions comprising an inert carrier and as active ingredients the compound ketoconazole and a retinoid are described.