Abstract: The invention relates to aminoalkyl-substituted 5,6-dihydro-dibenz[b,e]azepine-6,11-dione-11-oximes, to processes for their preparation and to their use as antiretroviral agents.

Abstract: A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m -- wherein m is an integer of 0 to 2; W represents ##STR2## and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.CH or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, ##STR3## and Q represents N or CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents CH.sub.2 CH.sub.2 ; and Z.sup.1 --Z.sup.2 represents N--(CH.sub.2).sub.n -- wherein n is an integer of 1 to 3 or a pharmaceutically acceptable salt thereof.

Abstract: Drug-resistant malarial infection in humans can be effectively treated with standard antimalarial agents if administered in conjunction with desipramine.

Abstract: Novel benzazepines of the formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R represents H, alkyl, allyl or ##STR2## A represents --[CR.sup.1 R.sup.2].sub.n --; n represents 3 or 4; R.sup.1 and R.sup.2 may be the same or different and each independently represents H, OH, atkyl, alkoxy, phnenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.2 on the same carbon atom are not both OH, or R.sup.1 and R.sup.2 on the same carbon atom together represent=O;G represents H, R.sup.3 (CO)-- or ArNHCO--;R.sup.3 represents H, alkyl, alkoxy, phenyl or substituted phenyl;Ar represents phenyl or substituted phenyl; andY and Z may be the same or different and each is independently selected from H, halo, alkyl, alkoxy or halpalkyl;the pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, useful in the treatment of psychoses, drug dependence, D1 dependent neurological disorder or pain are disclosed.

Abstract: Novel polycyclic compounds represented by the following formula: A--(CH.sub.2).sub.n --COOR.sup.1, wherein R.sup.1 represents a hydrogen atom or a lower alkyl group; n represents an integer of from 0 to 5; and A is a group represented by the following formula: ##STR1## wherein X represents a hydrogen atom or a halogen atom; and Y represents a methylene group, an oxygen atom, or a sulfur atom, or A is a group represented by the following formula: ##STR2## and pharmacologically acceptable salts thereof are disclosed. Also disclosed are a method for preparing the same, a pharmaceutical composition comprising the same, an antiallergic agent and an agent for bronchial asthma comprising the same, and a method for treatment of an allergic disease or bronchial asthma comprising the step of administering the same.

Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6 alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 --O, CH.sub.2 --(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.

Abstract: The use of a pharmaceutically acceptable cholinesterase inhibitor or a prodrug therefor for the treatment of fatigue syndromes, including chronic fatigue syndrome, post-infectious fatigue syndromes, fatigue syndromes associated with human immunodeficiency virus (HIV) infection or with preeclampsia. The acetyl cholinesterase is preferably one that acts substantially selectively at nicotinic receptor sites, and which has selectivity for acetyl cholinesterase as opposed to butyryl cholinesterase. Compounds of the invention include galanthamine and galanthamine derivatives.

Abstract: Potentiating agents which enhance the efficacy of antineoplastic agents are disclosed. The potentiating agents disclosed are dibenz[b,e]oxepins such as doxepin.

Abstract: The compounds are 3-[ (benzocycloalkyl)alkyl amino alkyl] -1,3,4,5-te trahydro 2H- 3-benzazepin-2 ones useful in cardiovascular field.A compound disclosed is (R,S)-7,8-dimethoxy-3-{3-{N-[(4,5-dimethoxybenzocyclobut-1-yl) methyl]-N-methyl amino}propyl}-1,3,4,5-tetrahydro-2H-3-benzazepin-2-one.

Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.

Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.

Abstract: Diacylpiperazines of general structure ##STR1## are: angiotensin II (A-II) antagonists selective for the type 2 (AT.sub.2) subtype useful in the treatment of cerebrovascular, cognitive, and CNS disorders; tachykinin receptor antagonists useful in the treatment of inflammatory diseases and pain or migraine; and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: The invention relates to a method for increasing blood flow to the retina and choroid in subjects with decreased retinal or choroidal blood flow. The method involves the topical administration of loxapine and is useful for the treatment of low pressure glaucoma and ischemic retinal degeneration.

Abstract: Disclosed are indole derivatives of formula (I) ##STR1## wherein Y represents H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halogen;Z represents --CH.sub.2 N(R.sub.5)--;R represents H or --CH.sub.2 CH.sub.2 X where X represents pyridyl, aralkyloxy or substituted amino of NR.sub.6 R.sub.7 where R.sub.6 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl, C.sub.1 -C.sub.6 alkoxycarbonyl, aralkyloxycarbonyl or halogenated C.sub.1 -C.sub.6 alkoxycarbonyl and R.sub.7 represents H, C.sub.1 -C.sub.6 alkyl or aralkyl, or together with R.sub.2 may form a ring of --(CH.sub.2).sub.n -- (n is 1-4) or ##STR2## R.sub.1 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or arylsulfonyl; R.sub.2 represents C.sub.1 -C.sub.6 alkyl, hydroxy, C.sub.1 -C.sub.6 alkoxy or aralkyloxy;R.sub.3 represents H, C.sub.1 -C.sub.6 alkyl, aralkyl or halogenated C.sub.1 -C.sub.6 alkyl;R.sub.4 and R.sub.5 may be the same or different and each represents H, C.sub.1 -C.sub.6 alkyl or aralkyl or both may together form a ring of --(CH.sub.2).sub.

Abstract: Compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein m is 0, 1 or 2 and n is 0 or 1;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is C.sub.1 -C.sub.6 -alkyl substituted with a heterocyclic group or C.sub.7 -C.sub.16 -arylalkyl, wherein the aryl group is unsubstituted or substituted with from one to three non-hydrogen members independently selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkyl, halo-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxy, amino and C.sub.1 -C.sub.6 -alkylamino;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, halogen, and halo-C.sub.1 -C.sub.6 -alkyl, or any two of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 taken together form a methylenedioxy group; andR.sup.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl.

Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.

Abstract: The present invention relates to the derivatives of formula: ##STR1## as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.

Abstract: Pharmaceutical compositions containing aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings are disclosed which are useful in the treatment of panic disorder or anxiety disorder.

Abstract: Novel heterocyclic compounds, which are represented by the following general formula, useful as anticancer drug potentiaters having a potentiating effect on the incorporation of anticancer drugs into cancer cells, the compounds each synthesized by, for example, reacting a epoxy compound obtained by reacting a heterocyclic compound with an epihalogenohydrin, with an amine derivative.

Abstract: New 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines of formula I and their pharmaceutically acceptable salts were found to be suitable actives for the treatment of cardiac arrhythmia. Previously unknown 3-carbalkoxyamino-5-(alpha-halogenpropionyl)-5H-dibenz[b,f]azepines are obtained from 3-carbalkoxyamino-5H-dibenz[b,f]azepines by reaction with alpha-halogenpropionyl halides. Through their reaction with ammonia, primary amines or secondary amines, the new 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines are obtained, which can be optionally converted into their pharmaceutically acceptable acid addition salts.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.

Abstract: Aromatic 2-benzazepines with fused 5- or 6-membered heterocyclic rings which are antagonists of cholecystokinins and/or gastrin, and are useful in the treatment or prevention of CCK-related and/or gastrin-related disorders of the gastrointestinal, central nervous and appetite regulatory systems; compositions comprising these compounds; and methods of treatment of mammals or of increasing food intake of animals employing these compounds.

Abstract: The present invention relates to improved oral forms of administration, for example syrups, having a delayed release characteristic, of carbamazepine. The delayed release of carbamazepine is achieved by the manufacture of an advantageous cubic crystal form of suitable size of dihydrate crystals contained in the form of administration.

Abstract: Novel imidazo[2,1-b][3]benzazepines and pyrimido[2,1-b][3]benzazepines of formula I, pharmaceutical compositions containing them, methods for treating cardiac arrhythmia in mammals utilizing them, and processes for synthesizing them.

Abstract: Novel imidazo[1,2-b][2]benzazepines and pyrimido[1,2-b][2]benzazepines of formula I, pharmaceutical compositions containing them, methods for treating cardiac arrhythmias in mammals utilizing them, and processes for synthesizing them.

Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

Abstract: The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates.

Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and X have the significances given herein, their acid addition salts and the preparation of these substances, pest control compositions which contain these substances as active ingredients and the use of the active substances or compositions for the control of pests.

Abstract: A method for treating abstructive respiratory passage disorders which comprises the use of 5,11-dihydro-11-[[(1-methyl-4-piperidinyl)-amino]carbonyl]-6H-dibenz[b,e]a zepin-6-one; 5,11-dihydro-11-[(1-methyl-4-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6H-dibenz[b,e]azepin-6-on e, alone or in combination.

Abstract: The instant invention is drawn to the use of clomipramine for treating trichotillomania and onchyphagia.

Abstract: Alpha-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce .alpha.-adrenoceptor antagonism in mammals.

Abstract: The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.

Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, which is (S)-1-[6-amino-2-[[hydroxy-(4-phenylbutyl)phosphenyl]oxy]-1-oxohexyl]-L-pr oline, fosinopril or zofenopril, alone or in combination with an antidepressant drug such as lithium, over a prolonged period of treatment.

Abstract: Disclosed are fused benzazepine compounds, pharmaceutical compositions including such compounds, methods of using such compounds, for example, in the treatment of psychoses and/or depression, and intermediates useful in the preparation of such compounds.

Abstract: Alpha-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonists to produce .alpha.-adrenoceptor antagonism in mammals.

Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereif, wherein: Z represents a residue of a substituted or unsubstituted aryl group,X represents o or NR.sup.o wherein R.sup.0 represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,n represents an integer 1 or 2,m represents an integer 1 or 2,p represents an integer 2 or 3,andq represents an integer in the range of from 1 to 12; pharmaceutical compositions containing such compounds and the use of such compounds and compositions in medicine.

Abstract: The invention relates to compounds of the formula ##STR1## wherein X is --CH.dbd.CH-- or S; R.sub.1 is lower alkyl, lower alkoxy or trifluoromethyl;R.sub.2 is hydrogen, lower alkyl, lower alkoxy, hydroxy or alkanoyloxy;R.sub.3 and R.sub.4, independently, are hydrogen, chlorine, fluorine, lower alkyl or lower alkoxy;s is an integer from 0 to 1, provided that when s is 1,R.sub.2 cannot be hydroxy, lower alkoxy or alkanoyloxy;R.sub.5 is a radical of the formula R.sub.6 --(CH.sub.2).sub.n -- or R.sub.7 --O--(CH.sub.2).sub.m --wherein R.sub.6 and R.sub.7 are aryl or a heterocyclic radical, n is an integer of from 0 to 2 and m is an integer of from 1 to 2, provided that, when n is 0, R.sub.6 must be attached through a carbon to carbon bond, and provided that R.sub.7 is always attached through a carbon to oxygen bond,and, when at least one asymmetric carbon is present, its enantiomers and racemates, and pharmaceutically acceptable acid addition salts thereof.

Abstract: .alpha.-adrenoceptor antagonists having the formula: ##STR1## which are useful to produce .alpha.-adrenoceptor antagonism, pharmaceutical compositions including these antagonists, and methods of using these antagonist to produce .alpha.-adrenoceptor antagonism in mammals.

Abstract: 1,9-Alkano-bridged-2,3,4,5-tetrahydro-1H-3-benzazepines and the derivatives thereof, i.e., the compounds of Formula I: ##STR1## wherein: R is selected from the group consisting of: hydrogen, cyano, lower alkyl, lower alkenyl, and aralkyl;each of R.sup.1, R.sup.2 and R.sup.3 is independently selected from the group consisting of: hydrogen, hydroxy, halo, trifluoromethyl, nitro, amido, lower alkoxy, lower alkyl, and lower alkylthio; andY is lower alkylene having from two to four carbon atoms;and the pharmaceutically acceptable salts thereof, are useful as CNS agents, e.g., as antidepressants, anxiolytics and antihypertensives, and/or as precursors thereto.

Abstract: The invention relates to combination products with a synergistic action and antidepressant activity, containing substances having antidepressant activity and compounds having antagonistic activity and belonging to the class of dihydropyridines, and to the use of the dihydropyridines in antidepressants.

Abstract: Carpipramine, and its pharmaceutically acceptable salts, are useful for the treatment of anxiety and sleep disorder.

Abstract: An anticonvulsant composition comprising as an active ingredient an amount effective for controlling seizures in mammals of a compound selected from the group consisting of dextromethorphan and other non-narcotic, non-addictive, low-toxicity compounds that bind to the same central nervous system sites as dextromethorphan. The composition may also contain an antiepileptic hydantoin, which is potentiated by said compound.

Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine, Z is alkylene, alkenylene, oxygen or a sulfur atom and W is an oxygen or a sulfur atom.

Abstract: The present invention relates to new naphthyl derivatives of general formula ##STR1## wherein N represents the number 1 or 2,A represents a --CH.sub.2 --, --CO--, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## while the atom marked with an x is linked to the phenyl nucleus, E represents a straight chained alkylene group optionally substituted by an alkyl group,G represents a straight chained alkylene group optionally substituted by an alkyl group,L represents a bond or an oxygen atom, if G represents a straight chained alkylene group with 2 to 5 carbon atoms optionally substituted by an alkyl group,R.sub.1 and R.sub.2, which may be identical or different, represent alkyl or alkoxy groups or R.sub.1 and R.sub.2 together represent an alkylenedioxy group,R.sub.3 represents a hydrogen atom, or an alkyl or an allyl group,R.sub.4, R.sub.5 and R.sub.

Abstract: New 2,3,4,5,6,7-hexahydro-2,7-methano-1,5-benzoxazonine and -1,4-benzoxazonine compounds of the formula ##STR1## have useful pharmaceutical properites. They are prepared from ketones of the formula ##STR2## via a lactone intermediate. In the formula, the various R substitutes are generally hydrogen or alkyl, with R.sup.4 also being halogen or alkoxy and R.sup.3 R.sup.3' also being phenyl. R.sup.1 may be joined with R.sup.5 /R.sup.5' in a 5- to 7-membered ring possibly interrupted by O, S, SO.sub.2 or amino. One of X and Y is CH.sub.2 ; the other is amino. The starting ketones also have pharmaceutical properties. The lactone intermediates are new compounds.

Abstract: Compositions and methods are disclosed for the treatment of obesity, depression, drug abuse, and narcolepsy. The compositions comprise a norepinephrine precursor such as L-tyrosine or L-phenylalanine in combination with a norepinephrine re-uptake inhibitor such as desipramine. In another embodiment of the invention, the compositions further comprise enzymatic cofactors for the biosynthesis of norepinephrine.

Abstract: Compounds of formula (i) and pharmaceutically acceptable salts thereof: ##STR1## wherein: m and n are independently 1 or 2 and p is 0, 1 or 2 such that m+n+p.gtoreq.3;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl-C.sub.1-6 alkyl, which phenyl moieties may be substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;Ar is a group of formula (a): ##STR2## wherein either R.sub.3 is hydrogen or C.sub.1-7 alkanoyl; and X is chloro, bromo, methylthio or nitro; having gastric motility enhancing activity, anti-emetic activity and/or 5-HT antagonist activity, a process for their preparation, and their use as pharmaceuticals.

Abstract: 2,3,4,8,9,9a-Hexahydro-4-aryl-1H-indeno[1,7-cd;]-azepines are selective dopamine receptor site binding agents.