Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): in which Z is a divalent radical selected from among —O—, —S— or —Nr′— and Ar is either a radical having the following structural formula (II): or a radical having the following structural formula (III): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Sulfonamide-substituted chromans, processes for their preparation, their use as a medicament or a diagnostic, and medicament comprising them Chromans of the formula I and of the formula 1a having the meanings R(A), R(B), R(C) and R(1) to R(8) indicated in the claims are outstandingly suitable for preparing a medicament for blocking the K+ channel which is opened by cyclic adenosine monophosphate (cAMP); and further for preparing a medicament for inhibiting gastric acid secretion; for the treatment of ulcers of the stomach and of the intestinal region, in particular of the duodenum, for the treatment of reflux esophagitis, for the treatment of diarrheal illnesses, for the treatment and prevention of all types of arrhythmias including ventricular and supraventricular arrhythmias, and for the control of reentry arrhythmias and for the prevention of sudden heart death as a result of ventricular fibrillation.

Abstract: Compounds of the formula I having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.

Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure ##STR1## where A, B, D, Q, X.sup.1, R, R.sup.1, X.sup.2 and R.sup.2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.

Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the pyran portion or on the pyran portion and the naphtho- or benzo-portion thereof. These compounds may be represented by one of the following graphic formula: ##STR1## wherein B and/or B' is an alkylaminoalkylamino-substituted aryl group and R.sub.1 may also be an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.

Abstract: Methods of treating anxiety with flavonoid compounds according to Formula (I) and dimers thereof, compounds of Formula (I) and dimers thereof, use of compounds of Formula (I) and pharmaceutical formulations comprising flavonoids of Formula (I) and dimers thereof.

Abstract: Chromans of formula I ##STR1## with the meanings of R(A), R(B) and R(1) to R(8) stated in the specification are suitable for producing a medicament for blocking the K.sup.+ channel that is opened by cyclic adenosine monophosphate (cAMP); also for producing medicaments for inhibiting gastric acid secretion; for the treatment of ulcers of the stomach and the intestinal region, in particular the duodenum, for the treatment of reflux esophagitis, for the treatment of diarrheal disorders, for the treatment and prevention of all types of arrhythmias, including atrial, ventricular and supraventricular arrhythmias, for controlling reentry arrhythmias and for preventing sudden heart death as a result of ventricular fibrillation.

Abstract: A compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein X, O R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are defined in the specification; compositions containing such compounds; intermediates used in the preparation of such compounds; and methods for treating a disease associated with the altered tone and/or motility of smooth muscle, for example chronic obstructive airways disease, asthma, urinary incontinence, irritable bowel syndrome, diverticular disease, oesophageal achalasia, and hypertension.

Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.

Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I' ##STR1## wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.

Abstract: This invention relates to novel formulations of salts of certain benzopyran compounds, to compositions containing them and their use in the treatment of certain disorders.

Abstract: Sulfonamide-substituted benzopyran derivatives, processes for their preparation, their use as a medicament, and pharmaceutical preparations comprising them Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal diseases.

Abstract: Novel benzopyran and benzoxazine derivatives represented by the general formula: wherein R.sub.1 and R.sub.2 represent a lower haloalkyl group, R.sub.3 represents a hydrogen atom, etc., R.sub.4 represents a heterocyclic group or A--O-- wherein A represents a cyclic structure, etc., R.sub.5 and R.sub.6 represent a lower haloalkyl, X represents .dbd.N--, N.fwdarw.O, etc, are disclosed. These compounds exhibit K.sup.+ channel opening activating and can be widely used as an anti-asthma drug, an anti-epilepsy drug, etc.

Abstract: Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly efficacious substances for producing medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.

Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.

Abstract: Derivatives of oxazolidin-2-one of general formula (I) ##STR1## in which: n is equal to 0 or 1,R.sub.1 represents a cyano group, an alkyl group or a fluoroalkyl group,R.sub.2 represents a hydrogen atom or a hydroxyl group, andR.sub.3 represents a hydrogen atom or a methyl group.Application in therapeutics.

Abstract: This invention relates to the method of treatment and/or prophylaxis of anxiety and/or disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy, using compounds of the formula (Ia): ##STR1##

Abstract: The invention provides novel 2,2-di(C.sub.1-5 alkyl)- or trans-2,2-di(C.sub.1-5 alkyl)-3,4-dihydro-3-hydroxy- -4-carboxamido-6-(N-arylsulfonamido)-2H-1-benzopyrans; and N-oxides, esters and salts thereof; processes for their production; and their uses as pharmaceuticals, e.g. as K.sup.+ -channel openers, bronchodilators and agents for the suppression of airways hyperreactivity, e.g., for use in the treatment of asthma.

Abstract: Benzopyran-3-ols having anxiolytic and anticonvulsant activity are claimed.

Abstract: Described are novel water soluble photochromic naphthopyran and benzopyran compounds having an alkylaminoalkylamino group on the naphtho- or benzo-portions and/or pyran portions thereof. These compounds may be represented by one of the following graphic formulae: ##STR1## wherein R.sub.1 is an alkylaminoalkylamino group. Articles such as ophthalmic lenses or other plastic transparencies and coating compositions such as paints and inks that incorporate the novel water soluble compounds are also described.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.

Abstract: 3-amidochromanylsulfonyl(thio)ureas of the formula (I): ##STR1## which are valuable pharmaceutically active compounds for the treatment of disturbances of the cardiovascular system, in particular for the treatment of arrhythmias, for preventing sudden cardiac death or for influencing a reduced contractility of the heart, and processes for their preparation, their use and pharmaceutical preparations comprising them.

Abstract: Novel pharmaceutically/cosmetically-active polyaromatic heterocyclic compounds have the structural formula (I): ##STR1## in which Z is a divalent radical selected from among --O--, --S-- or --Nr'-- and Ar is either a radical having the following structural formula (II): ##STR2## or a radical having the following structural formula (III): ##STR3## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.

Abstract: Novel benzpyran derivatives and the use of these derivatives in producing novel anti-cannabinoid antibodies are disclosed. Also disclosed is the use of these antibodies as reagents in improved immunoassays for tetrahydrocannabinol metabolites in biological fluid samples.

Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.

Abstract: A new process for preparing a compound of the formula: ##STR1##

Abstract: The present invention relates to a process for preparing protected amines or amino acids. The invention furthermore relates to the use of tocopheryl radicals or radicals derived therefrom as protective groups for amines and amino acids, and to compounds obtained in this process as intermediates and to processes for preparing dipeptides and oligopeptides.

Abstract: Amino(thio)ether derivatives of formula I ##STR1## wherein R.sup.0, R.sup.1, R.sup.2, R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.9, X and Z are as defined herein, and their salts, are active on the central nervous system.

Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.

Abstract: Compounds such as ##STR1## or pharmaceutically acceptable salts thereof, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.

Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.

Abstract: The invention relates to a substituted amidine derivative which has an excellent platelet aggregation inhibiting action on the basis of fibrinogen antagonism and is particularly excellent in effectiveness on oral administration, and the platelet aggregation inhibitor containing the substituted amidine derivative of the invention as an effective ingredient is effective for prevention and treatment of thrombosis, and restenosis or reocclusion after percutaneous transluminal coronary angioplasty or percutaneous transluminal coronary recanalization.

Abstract: Tetralin derivatives, such as 7-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)-amino!tetralin and 8-hydroxy-2-(N-n-propyl-N-3 '-iodo-2'-propenyl)amino-tetralin, are disclosed which have affinity and specificity for dopamine D-3 and/or serotonin 5-HT.sub.1A receptors.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ; (c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) R.sub.1 is hydrogen or straight, branched or cyclic alkyl, aryl or C(.dbd.NH)--NHR.sub.4 ; and(f) R.sub.2, R.sub.3, and R.sub.4, are independently hydrogen, straight, branched or cyclic alkyl having from one to 10 carbon atoms, or aryl; R.sub.2 and R.sub.3 can be bonded together to form a ring having 5 or 6 atoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from 1 to about 3;(b) X is selected from the group consisiting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen;(e) W is O or S; and(f) R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, straight, branched or cyclic alkyl having from 1 to 10 carbon atoms, aryl, heterocyclyl, heteroaryl, hydroxy, or alkoxy; or R1, R2 or R3 may be bonded to form one or more rings each ring having from 3 to about 7 atoms wherein from 1 to 3 atoms may be heteroatoms.pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pain using such compounds.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification have retinoid-like biological activity.

Abstract: This invention relates to novel diastereomeric acid addition salts of homochiral hydroxylamines, to processes for obtaining such, to processes for the conversion thereof to the corresponding homochiral hydroxylamines, to certain novel homochiral hydroxylamines and the processes for using these as intermediates.

Abstract: There is disclosed a process of producing a 2-cyano-4-oxo-4H-benzopyran compound of the general formula (2): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, hydroxy, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, nitro or a group of the RCONH wherein R is C.sub.1 -C.sub.20 alkyl, phenyl, phenyl-substituted (C.sub.1 -C.sub.20) alkyl, phenyl (C.sub.1 -C.sub.20)alkoxyphenyl or (C.sub.1 -C.sub.20) alkoxyphenyl. This production process is characterized in that a carboxamide of the general formula (1): ##STR2## wherein R.sup.1 and R.sup.2 are each as defined above, is reacted with a dehydrating agent in the presence of a pyridine compound of the general formula (4): ##STR3## wherein A.sup.1 and A.sup.2 are independently hydrogen or C.sub.1 -C.sub.5 alkyl.

Abstract: 3-amino-5-carbonylchromans, as well as enantiomers and salts thereof are disclosed. Pharmaceutical compositions containing the compounds as active ingredients are also disclosed. The compounds are useful in the treatment of 5-hydroxytryptamine-mediated disorders of the central nervous system.

Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.

Abstract: A process for preparing (R)-3-amino-5-methoxychroman is provided. The process comprises the steps of (i) dissolving racemic 3-amino-5-methoxychroman and L(+)tartaric acid in water to form the tartrate salt; (ii) heating the solution until a clear solution is obtained; and (iii) crystallizing the tartrate salt by allowing the solution to cool to room temperature.

Abstract: Protein tyrosine kinase inhibitors are provided of formula (I): ##STR1## wherein R.sup.2 is H, OH, halo or O(C.sub.1 -C.sub.4)alkyl; R.sup.2 is OH, halo or O(C.sub.1 -C.sub.4)alkyl; R.sup.1 is ##STR2## wherein R.sup.4 is H, OH, halo, CH.sub.2 OH, C(O)CH.sub.3, C(O)N(R).sub.2 wherein each R is H or (C.sub.1 -C.sub.4)alkyl; or C(O)R wherein R.sup.6 is OH or O(C.sub.1 -C.sub.4)alkyl; and R.sup.5 is OH, CH.sub.2 OH, C(O)CH.sub.3, C(O)N(R).sub.2 or C(O)R.sup.6 ; or a pharmaceutically acceptable salt thereof, which inhibit the pathological proliferation or growth of mammalian cells, such as cancer cells.

Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents .dbd.O, .dbd.S, .dbd.N--Z, etc. (Z represents a lower alkyl group, etc.); Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 each represents a hydrogen atom, a lower alkyl group, etc, are disclosed. The benzopyran derivative exhibit K.sup.+ channel opening activities and are widely applicable as antiasthmatics, antiepileptics, and the like.

Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are employed as intermediates in the synthesis of aminochroman compounds useful in the treatment of CNS disorders.

Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes and 3-aminochromanes which exhibit binding activity at the serotonin 1A receptor.