Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof:Y-CO-L-Z (I)whereinL is NH or O; Y is a group of formula (a), (b) or (c): ##STR1## wherein R.sub.1 and R.sub.2, R.sub.5 and R.sub.6, R.sub.9 and R.sub.10, are independently selected from hydrogen or halogen;X is N or CR.sub.3whereinR.sub.3 is hydrogen or C.sub.1-6 alkoxy;R.sub.4 is hydrogen, halogen, CH.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;one of R.sub.7 and R.sub.8 is C.sub.

Abstract: A compound selected from the group consisting a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of phenyl, cycloalkyl of 4 to 6 carbon atoms and ##STR2## R.sub.4 and R.sub.5 are individually hydrogen or alkyl of 1 to 5 carbon atoms, R.sub.6 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, phenyl, halogen, alkoxycarbonyl of 2 to 5 carbon atoms, cyano, amido and mono- and dialkylamido of 1 to 5 alkyl carbon atoms, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and cycloalkyl of 3 to 5 carbon atoms or taken together form alkylene of 3 to 5 carbon atoms, X and Y are individually selected form the group consisting of hydrogen, halogen, --NO.sub.2, azido, --CN, --CF.sub.

Abstract: A compound for treating disorders of the central nervous system, which is of the formulawherein A taken together with the two carbon atoms denoted by .alpha. and .beta. is one of the following groups: ##STR1## R.sup.1 is one of the following groups:--CH.dbd.CH--R.sup.6 (d)and--C.tbd.C--R.sup.6, (e)R.sup.2 is hydrogen, R.sup.3 is lower alkyl, or R.sup.2 and R.sup.3 together are dimethylene or trimethylene, R.sup.4 and R.sup.5 are independently hydrogen, halogen, trifluoromethyl or lower alkyl, and R.sup.6 is hydrogen, halogen, aryl or a saturated lower hydrocarbon group which is optionally mono- or di-substituted by hydroxy, lower alkoxy, (C.sub.3 -C.sub.7)-cycloalkyl or oxo, wherein the compound has the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.3 together are dimethylene or trimethylene and, further, the double bond present in group (d) has the E- and/or Z-configuration when R.sup.6 is different from hydrogen.

Abstract: The known compound, t-butyl (S)-8-bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][ 1,4]benzodiazepine-1-carboxylate of the formula ##STR1## is effective in the prevention or interruption in a human being of panic states, accompanying phobias and the associated social consequences such as anticipatory anxiety and avoidance behavior. In particular, it is effective in the discontinuous, purely attack-based prevention or interruption of panic states.

Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, halogen or trifluoromethyl; Z is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 CH.sub.2 --; R is ##STR2## R.sub.2 being hydrogen, loweralkyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl or phenoxycarbonyl; and R.sub.1 is hydrogen, loweralkanoyl, loweralkyl, ethoxycarbonyl, 2,2,2-trichloroethoxycarbonyl or phenoxycarbonyl; the dotted line within the seven-membered ring and the dotted line between R.sub.1 and the ring nitrogen being optional bonds such that the former is absent and the latter present when R is ##STR3## whereas the former is present and the latter absent when R is ##STR4## These compounds display antiinflammatory activities and analgesic activities.

Abstract: Phenyl-3-aminoalkyl-4-methyl-2,6-dioxopiperidines of the Formula I ##STR1## wherein: R.sub.1 represents methoxy, ethoxy or hydroxy,R.sub.2 represents methoxy, ethoxy, hydroxy or hydrogen;each R.sub.3 independently represents methyl or ethyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents hydrogen or methyl; andn represents 2 or 3,and a pharmacologically acceptable acid addition salt thereof (a) have anxiolytic activity, (b) antagonize the anxiogenic activity of benzodiazepine inverse agonists, (c) reduce chronic abnormally high brain levels of serotonin or its metabolite 5-hydroxy-indoleacetic acid and (d) have antibacterial and antiviral activity. These activities are believed to be related to a reduction in serotonin turnover caused by blocking the depolarization activation of tryptophan hydroxylase. Novel compositions comprise the compounds with a benzodiazepine agonist or benzodiazepine inverse agonist.

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

Abstract: An improved antiinflammatory composition and method of treating inflammation which employs a combination of antiinflammatory piroxicam, or a pharmaceutically acceptable salt thereof, with analgesic acetaminophen, antidepressant doxepin, bronchodilator pirbuterol, minor tranquilizer diazepam, or antihypertensive trimazosin.

Abstract: The invention relates to dihydrobenzopyrrolobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --CH.sub.2 CH.sub.2 -- group; and R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --CH.sub.2 CH.sub.2 -- group and the pharmaceutically acceptable acid addition salts thereof.

Abstract: The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.

Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, trifluoromethyl or halogen; Z is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 CH.sub.2 --; n is 1, 2 or 3; R.sub.1 is hydrogen, loweralkanoyl, aroyl, ethoxycarbonyl, phenoxycarbonyl, loweralkylaminocarbonyl, arylaminocarbonyl, loweralkyl or arylmethyl; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is hydrogen, loweralkyl, ethoxycarbonyl, loweralkanoyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together is isopropylidene; with the proviso that when n is 3, X, Y and R.sub.1 are all hydrogen and Z is --CH.sub.2 CH.sub.2 --, R.sub.2 and R.sub.3 can not both be methyl. These compounds display antiinflammatory and analgesic activities.

Abstract: The invention relates to 1,3,4,16b-tetrahydro-2H,10H-indolo[2,1-c]pyrazino[1,2-a][1,4]benzodiazepin e derivatives of the formula I, ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, C.sub.3-7 -alkenyl, C.sub.3-7 -alkynyl, 3 to 7 ring-membered cycloalkyl, C.sub.2-7 -alkyl substituted by a substituent selected from hydroxy, amino, N-mono-lower alkyl-amino and N,N-di-lower alkyl-amino; or R.sup.1 is lower alkyl substituted by a substituent selected from 3 to 7 ring-membered cycloalkyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-mono-lower alkyl-carbamoyl, N,N-di-lower alkyl-carbamoyl and lower alkanoyl; or R.sup.1 is lower alkyl substituted by either phenyl or benzoyl each of said phenyl or benzoyl radicals being unsubstituted or substituted by up to three members selected from lower alkyl, lower alkoxy, lower alkylthio, halogen and trifluoromethyl; R.sup.2 and R.sup.3 represent hydrogen, lower alkyl, hydroxy, lowr alkoxy, halogen or trifluoromethyl; and R.sup.

Abstract: Antibacterially active new 1,8-bridged 4-quinolone-3-carboxylic acid derivatives of the formula ##STR1## in which Y is carboxyl or a derivative thereofR.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and X.sup.5 are H or various radicals,Z is O, NH, substituted NH, --CON< or --SO.sub.2 N<,m and n are 0 or 1, andA, B, D and E are CH or substituted C or up to three of them are N,and physiologically acceptable salts thereof. Novel intermediates are described as well as processes for making the intermediates and end products.

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

Abstract: Products of Aspergillus alliaceus fermentation having cholecystokinin (CCK) antagonist activity, their preparation and use are disclosed.

Abstract: Fused tetracyclic benzodiazepines of the formula (I): ##STR1## where R.sup.1 is a cyclic amine such as 1-piperazine and R.sup.2 is H or a substituent as defined herein are useful as LHRH antagonizing agents. Also, methods for their synthesis, intermediates used in such synthesis, methods for use as medicaments and pharmaceutical compositions are described.

Abstract: New oxadiazolyl imidazobenzodiazepine derivatives having the formula ##STR1## wherein R.sup.3 has the formula ##STR2## wherein R" is hydrogen, C.sub.1-6 alkyl C.sub.1-6 alkoxymethyl or C.sub.3-6 - cycloalkyl;R.sup.4 is hydrogen;R.sup.5 is C.sub.1-6 alkyl or R.sup.4 and R.sup.5 together form a 2-4 membered alkylene bridge; and R.sup.A is C.sub.1-6 alkyl, C.sub.1-6 alkoxy, or C.sub.1-3 trifluoroalkyl, pharmaceutical compositions thereof, and method of treating therewith, are disclosed.The compounds and pharmaceutical compositions are useful in the amelioration, mitigation, or elimination of central nervous system disorders related to benzodiazepine receptors and especially as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: Imidazothiadiazolealkenecarboxamides of the formula ##STR1## in which R.sup.1 is hydrogen, aryl, substituted aryl or a cyclic or aliphatic hydrocarbon radical which is optionally interrupted by O, S, N, N-alkyl, N-aryl or N-aralkyl and which is optionally substituted,R.sup.8 having the meaning indicated for R.sup.1, andX representing oxygen, sulphur or the radical NR.sup.9 R.sup.10,the other radical having various definitions, and acid addition salts thereof, exhibit hypotensive activity.

Abstract: Choline or a natural or synthetic compound that dissociates to form choline is administered to a patient concomitantly with a drug in order to potentiate the effect of the drug by increasing acetylcholine levels in the brain or other tissues, and/or to suppress, or block the development of, unwanted side effects of the drug, by increasing acetylcholine levels in the brain or other tissues.

Abstract: Disclosed are the novel compounds of formula I ##STR1## wherein ring A is unsubstituted or substituted by one or two identical or different substituents selected from lower alkyl, halogen, trifluoromethyl, lower alkoxy, hydroxy and acyloxy; or ring A is substituted on adjacent carbon atoms by lower alkylenedioxy; R represents hydrogen, halogen or lower alkyl; and Ar represents carbocyclic aryl or heteroaryl;which are useful as benzodiazepine receptor agonists, processes for preparing the same, pharmaceutical compositions comprising said compounds and methods of treating nervous system disorders, such as anxiety and epilepsy, by administration of said compounds and pharmaceutical compositions to mammals.

Abstract: [1,2]-fused 1,4-benzodiazepine compounds are disclosed corresponding to the general formula I ##STR1## wherein X is an oxygen or sulfur atom or an optionally substituted imino group, R.sub.1 is a hydrogen or halogen atom, lower alkyl radical, a lower alkoxy radical or a nitro group and R.sub.2 is a hydrogen or halogen atom, a lower alkyl radical, a lower alkoxy radical or a nitro group, or if R.sub.1 is a hydrogen atom, R.sub.2 may also be a lower alkylthio radical, or, if R.sub.1 is a hydrogen atom and X is a sulfur atom or an imino group, R.sub.2 may be a trifluoromethyl radical; or R.sub.1 and R.sub.2 are bonded to adjacent carbon atoms and together denote a methylenedioxy or ethylenedioxy radical; R.sub.3 is an optionally substituted furyl, thienyl, pyrrolyl or pyridyl radical and n is zero or, if R.sub.3 is furyl or thienyl, n may be 0 or 1. The compounds may be in the form of their optical isomers or acid addition salts. The compounds exhibit neuroleptic properties.

Abstract: Fused tetracyclic benzodiazepines of the formula (I): ##STR1## where R.sup.1 is a cyclic amine such as 1-piperazine and R.sup.2 is H or a substituent as defined herein are useful as antiovulatory and contragestational agents. Also, methods for their synthesis, intermediates used in such synthesis, methods for use as medicaments and pharmaceutical compositions are described.

Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-diones, which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.

Abstract: Novel quinazolino-1,4-benzodiazepin-5,13-dione derivatives, which are soluble in aqueous media and which have been found to be antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.

Abstract: Novel indol-3-yl-quinazolino-1,4-benzodiazepin-5,13-diones, which are antagonists of the function of cholecystokinins (CCK), to the preparation of these compounds from compounds prepared by aerobic fermentation of certain Aspergillus alliaceus strains, and to the use of these compounds to antagonize the function of CCK, which antagonism is useful, e.g., for the treatment and prevention of disorders of the gastrointestinal, central nervous and appetite-regulatory systems of mammals, especially of humans.

Abstract: Tetracyclic compounds of the formula: ##STR1## and a process for their preparation are disclosed. The compounds have cholecystokinin inhibiting activity.

Abstract: Fused tetracyclic benzodiazepines of the formula (I): ##STR1## where R.sup.1 is an acyclic amine or cyclic amine such as 1-piperidine, 4-morpholine or 1-piperazine and R.sup.2 is H or a substituent as defined herein as useful as antiallergins. Also, methods for their synthesis, intermediate used in such synthesis, methods for use as medicaments and pharmaceutical compositions.

Abstract: This invention discloses novel imidazo[2,1-a]pyrrolo[2,1-c][1,4]benzodiazepine derivatives, processes for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful as antiobesity agents to reduce food intake in a mammal.

Abstract: According to the invention, the parenteral administration of water-insoluble pharmacologically active agents is enhanced wherein the agents are administered in the lipoid phase of a carrier emulsion comprising a microemulsion of a finely dispersed lipoid in an aqueous phase. The lipoid preferably has a mean particle size below 1 micron. This makes it possible to administer water-insoluble agents in high concentrations, and thus a lower dose, whereby a rapid onset of the pharmacological effect is accompanied by a markedly reduced incidence of injury to body tissues.