Abstract: The compounds are of the class 1,4-benzodiazepines of the formula: An illustrative compound is (S)-6-chloro-2,3,4,5-tetrahydro-3-methyl-4-(3-methyl-2-butenyl)-1H-1,4-benzodiazepin-9-amine. The compounds are useful as intermediates in the preparation of tetrahydroimidazo[1,4]benzodiazepin-2-(thi)ones.

Abstract: The present invention concerns extended release formulations comprising cisapride-(L)-tartrate, in particular an oral formulation, the use thereof as a medicine, especially in treating gastrokinetic disorders.

Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk.sup.1 is C.sub.1-6 alkanediyl optionally substituted with hydroxy, C.sub.1-4 alkyloxy or C.sub.1-4 alkylcarbonyloxy; --Z.sup.1 --Z.sup.2 -- is a bivalent radical; R.sup.1, R.sup.2 and R.sup.3 are each independently selected from hydrogen, C.sub.1-6 alkyl, hydroxy, halo and the like; or when R.sup.1 and R.sup.2 are on adjacent carbon atoms, R.sup.1 and R.sup.2 taken together may form a bivalent radical; R.sup.4 is hydrogen or C.sub.1-6 alkyl; A is a bivalent radical of formula --NR.sup.6 --Alk.sup.2 -- (b-1), or --Npiperidinyl--(CH.sub.2).sub.m (b-2) wherein m is 0 or 1; R.sup.5 is a radical of formula ##STR1## wherein n is 1 or 2; p.sup.1 is 0, and p.sup.2 is 1 or 2; or p.sup.1 is 1 or 2, and p.sup.2 is 0; X is oxygen, sulfur or .dbd.NR.sup.9 ; Y is oxygen or sulfur; R.sup.7 is hydrogen, C.sub.1-6 alkyl, C.sub.

Abstract: The present invention concerns pharmaceutical dosage forms comprising cisapride-(L)-tartrate or a precursor form thereof, contained in a porous structure consisting essentially of one or more polymers which are insoluble or practically insoluble in water or gastro-intestinal fluids and wherein the pores of the porous structure comprise a substance soluble in water or gastro-intestinal fluids adjacent to the surface of the dosage form. The present invention is further concerned with processes for preparing such pharmaceutical dosage forms and with the use of these pharmaceutical dosage forms as a medicine, especially in treating gastro-intestinal disorders, more particularly gastro-oesophagal reflux disease.

Abstract: The present invention concerns sustained release sufentanil compositions for intramuscular administration, the preparation of said compositions and the use of said compositions for inhibiting pain, in particular post-operative pain, in animals, particularly in companion animals.

Abstract: The present invention concerns novel (2-morpholinylmethyl)benzamide derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sup.2 is hydrogen, halo or C.sub.1-6 alkylsulfonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is a radical of formula R.sup.4 --C(.dbd.O)--Alk-- (a); R.sup.5 --C(.dbd.O)--N(R.sup.6)--Alk-- (b); or R.sup.7 --C(.dbd.O)--O--Alk-- (c); wherein each Alk is independently C.sub.1-12 alkanediyl; R.sup.4 is hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.5 and R.sup.7 each independently are hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, amino, mono- or di(C.sub.1-6 alkyl)amino or an optionally substituted heterocyclic ring; R.sup.6 is hydrogen or C.sub.

Abstract: The present invention of compounds of formula (I), ##STR1## a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, R.sup.1 is C.sub.1-6 alkyloxy, C.sub.2-6 alkenyloxy or C.sub.2-6 alkynyloxy; R.sup.2 is hydrogen or C.sub.1-6 alkyloxy, or when taken together R.sup.1 and R.sup.2 may form a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C.sub.1-6 alkyl; R.sup.3 is hydrogen or halo; R.sup.4 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.2-6 alkenyl optionally substituted with aryl, or L is a radical of formula -Alk-R.sup.5 -, Alk-X--R.sup.6, -Alk-Y--C(.dbd.O)--R.sup.8, or -Alk-Y--C(.dbd.O)--NR.sup.10 R.sup.11 wherein each Alk is C.sub.1-12 alkanediyl; and R.sup.5 is hydrogen, cyano, C.sub.1-6 alkylsulfonylamino, C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, aryl, di(aryl)methyl or a heterocyclic ringsystem; R.sup.6 is hydrogen, C.sub.

Abstract: The present invention relates to a composition comprising an antimigraine compound of formula (I) and chitosan, which is particularly suited for intranasal administration. ##STR1## Process for preparing said composition, its use as a medicine and a nasal spray device, especially a unidose nasal spray device containing said composition.

Abstract: The present invention concerns oral dosage forms of some particular salts of cisapride, more particularly cisapride-(L)-tartrate, cisapride-(D)-tartrate, cisapride-sulfate, or cisapride citrate, which avoid drugfood interaction and which allow comedication of agents that increase the pH of the stomach. The invention particularly relates to solid oral dosage forms suitable for rapid dissolution. The present invention also concerns tablets which can be prepared via direct compression.

Abstract: The present invention concerns the use of receptor antagonists of the 5HT4 receptor for avoiding, alleviating, suppressing or overcoming the gastrointestinal side-effects of serotonin reuptake inhibitors. The present invention also concerns pharmaceutical formulations comprising 5HT4-receptor antagonists for alleviating, suppressing or overcoming the gastrointestinal side-effects of serotonin reuptake inhibitors, as well as pharmaceutical compositions comprising 5HT4 receptor antagonists and serotonin reuptake inhibitors.

Abstract: This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.

Abstract: A process for separating, in the liquid phase, a reaction mixture which comprises a first chlorinated sucrose and at least one additional component selected from the group consisting of at least one other chlorinated sucrose different from said first chlorinated sucrose, salt and solvent, by injecting said reaction mixture onto a fixed bed of solid adsorbent and treating with a desorbent such that:(a) the first chlorinated sucrose passes through the adsorbent into a first recoverable product stream rich in said first chlorinated sucrose at a rate, which is different than the rate at which,(b) at least one of said additional components passes through the adsorbent into at least a second recoverable stream rich in said additional component.

Abstract: A process is described for clarifying a crude inulin extract by ultrafiltration and separating an aqueous inulin solution containing carbohydrates having a range of degrees of polymerization into fractions having different average degrees of polymerization which comprises subjecting an aqueous inulin solution to ultrafiltration through a membrane having a predetermined pore size whereby inulin fractions having average degrees of polymerization less than a predetermined value pass through said membrane as permeate and inulin fractions having average degrees of polymerization greater than said predetermined value are collected as retentate.

Abstract: The present invention is concerned with the method of using a 2,3-dihydro-imidazo?2,1-b!benzothiazole derivative for the manufacture of a medicament for the therapeutic or prophylactic treatment of humans suffering from ageing of, or degenerative diseases of the nervous and vascular system which are associated with oxidative stress.

Abstract: The present invention is concerned with a novel benzamide derivative for 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: Antiallergic triazolobenzazepines of formula ##STR1## wherein each of the dotted lines independently represents an optional bond; R.sup.1 represents hydrogen, halo, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkyloxy; R.sup.2 represents hydrogen, halo, C.sub.1-4 alkyl, hydroxy or C.sub.1-4 alkyloxy; R.sup.3 represents hydrogen, C.sub.1-4 alkyl or halo; --B.dbd.D-- is a bivalent radical of formula --C(R.sup.4).dbd.N--(a-1); or --N.dbd.C(R.sup.5)-- (a-2); R.sup.4 and R.sup.5 represent hydrogen, C.sub.1-4 alkyl, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; R.sup.5 also represents phenyl or pyridinyl; L represents hydrogen; C.sub.1-6 alkyl; substituted C.sub.1-6 alkyl, C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl or, L represents a radical of formula -Alk-Y-Het.sup.1 (b-1), -Alk-NH--CO--Het.sup.2 (b-2) or --Alk-Het.sup.3 (b-3).

Abstract: The present invention provides novel compounds of formula ##STR1## the N-oxides, 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 concerns novel compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl or C.sub.1-6 alkyl substituted with C.sub.3-7 cycloalkyl; R.sup.2 is hydrogen or C.sub.1-6 alkyl; Alk represents C.sub.1-3 alkanediyl; --A-- represents a bivalent radical of formula --CH.dbd.CH--N.dbd.CH-- (a), --N.dbd.CH--N.dbd.CH-- (b), --CH.dbd.N--N.dbd.CH-- (c), --CH.dbd.CH--CH.dbd.N-- (d); in said bivalent radicals a hydrogen atom may be replaced by C.sub.1-6 alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof.

Abstract: Use of 3-aryl-5,6-dihydro-1,4,2-oxathiazines and their oxides having the formula ##STR1## wherein n is 0, 1 or 2; R.sup.1 is hydrogen, C.sub.1-4 alkyl or benzyl; and R represents (a) phenyl; phenyl substituted with 1 to 3 substituents independently selected from hydroxyl, halo, C.sub.1-12 alkyl, C.sub.5-6 cycloalkyl, trihalomethyl, phenyl, C.sub.1-5 alkoxy, C.sub.1-5 alkylthio, tetrahydropyranyloxy, phenoxy, C.sub.1-4 alkylcarbonyl, phenylcarbonyl, C.sub.1-4 alkylsulfinyl, C.sub.1-4 alkylsulfonyl, carboxy or its alkali metal salt, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkylaminocarbonyl, phenylaminocarbonyl, tolylaminocarbonyl, morpholinocarbonyl, amino, nitro, cyano, dioxolanyl or C.sub.1-4 alkyloxyiminomethyl; naphthyl; pyridinyl; thienyl, preferably when n is not 2; furanyl; or thienyl or furanyl substituted with one to three substituents independently selected from C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, C.sub.1-4 alkylthio, halo, cyano, formyl, acetyl, benzoyl, nitro, C.sub.

Abstract: The present invention is concerned with novel benzoate derivatives having the formula ##STR1## the N-oxide forms, the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein R.sup.1 is halo or C.sub.1-6 alkylsulfonylamino; either R.sup.2 is hydrogen and R.sup.3 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; or R.sup.2 and R.sup.3 taken together form a bivalent radical of formula --CH.dbd.CH-- (a), --(CH.sub.2).sub.2 -- (b), or --(CH.sub.2).sub.3 -- (c); in the bivalent radicals of formula (a), (b) or (c) one or two hydrogen atoms may be replaced by C.sub.1-6 alkyl; Alk is C.sub.1-6 alkanediyl; R.sup.4 is hydrogen or C.sub.1-6 alkyloxy; R.sup.5, R.sup.6 and R.sup.7 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy; or R.sup.5 and R.sup.6 taken together may also form a bivalent radical of formula: --NR.sup.8 C(O)NR.sup.9 --, --NH--C(NHR.sup.10).dbd.N--, --O--(CH.sub.2).sub.m --O--; R.sup.8 and R.sup.