Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.

Abstract: The present invention is directed to organic light emitting devices comprising a heterostructure for producing electroluminescence having a hole transporting layer with a glass structure. The hole transporting layer comprises a compound having a symmetric molecular structure. The end groups of the symmetric molecule are hole transporting amine moieties having an unsaturated linkage between two arenes.

Abstract: The invention provides compounds of formula ##STR1## as described in the claims, or an optical isomer, diastereomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable amide, ester, or imide thereof are useful as inhibitors of metalloproteases.Also disclosed are pharmaceutical compositions and methods of treating diseases, disorders and conditions characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.

Abstract: A compound of formula ##STR1## wherein n is 0 or 1; m is 0 or 1; p is 0 or 1; X is oxygen or sulfur; Y is CH, N or NO; W is oxygen, H.sub.2 or F.sub.2 ;A is N or C(R.sup.2); G is N or C(R.sup.3); D is N or C(R.sup.4);with the proviso that no more than one of A, G, and D is nitrogen, but at least one of Y, A, G, and D is nitrogen or NO;R.sup.1 is hydrogen or C.sub.1 to C.sub.4 alkyl;R.sup.2, R.sup.3, and R.sup.4 are independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, aryl, heteroaryl, OH, OC.sub.1 -C.sub.4 alkyl, CO.sub.2 R.sup.1, --CN, --NO.sub.2, --NR.sup.5 R.sup.6, --CF.sub.3, --OSO.sub.2 CF.sub.3 or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4, respectively, may together form another six membered aromatic or heteroaromatic ring sharing A and G, or G and D, respectively, containing between zero and two nitrogen atoms, and substituted with one to two of the following substituents: independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.

Abstract: Compounds defined by the following general structure are disclosed: ##STR1## These compounds display pharmacological activities, including inhibition of tyrosine kinase activity and enhancement of the function and/or survival of trophic factor responsive cells, e.g., cholinergic neurons.

Abstract: The subject invention concerns a process for the preparation of a compound of formula (2), which comprises phenolic oxidation of a compound of formula (1) wherein X.sup.1 and X.sup.2 are independently selected from H or a protecting group for the phenolic function, e.g. acyl or trialkylsilyl; groups A.sup.1, A.sup.2, B.sup.1, B.sup.2 and Y are selected so as to render the nitrogen atom non-basic; Z is a blocking group, e.g. Br or t-butyl; and R is H, C.sub.1-20 alkyl, C.sub.3-20 aryl, C.sub.4-20 arylalkyl, and wherein the process is carried out in a two-phase liquid system comprising an aqueous base and an organic solvent having a dielectric constant below 4.8.

Abstract: Compounds of formula (I) ##STR1## and the salts of these compounds, are efficacious PDE (phosphodiesterase) inhibitors.

Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.

Abstract: The present invention relates to a novel class of tracer compounds for fluorescence polarization imunoassays. The novel 4'-methyl fluorescein derivatives are conjugated to ligands via cyclic linkers.

Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.

Abstract: Novel piperidine derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments for the treatment of CNS disorders are disclosed.

Abstract: Novel amide derivatives of formula (I), processes for their preparation, pharmaceutical compositions containing them and their use as medicaments are disclosed.

Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.

Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.

Abstract: A spiro (indolino) oxazine compound of general formula (I) ##STR1## wherein R.sub.1 represents a group of the formula --NR.sub.2 R.sub.3 wherein each of R.sub.2 and R.sub.3, which may be the same or different, independently represents an alkyl group, or a carbocyclic group, preferably aryl, or a heterocyclic group, or R.sub.2 and R.sub.3 taken together with the nitrogen atom to which they are attached represent a heterocyclic ring having one or more heteroatoms and which may optionally carry at least one substituent selected from alkyl, aryl or heteroaryl groups;--X-- is selected from --O--, --S--, --Se--, --NH-- or --NR-- wherein R represents an alkyl group, andring A is a carbocyclic or heterocyclic ring which can be optionally substituted with a group of formula R.sub.8 as defined above, or may optionally have a carbocyclic or heterocyclic ring fused thereto; and wherein R.sub.4 -R.sub.8 are as defined in the specification.

Abstract: This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-???8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-?4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: A therapeutic agent for osteoporosis, comprising an azepine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as an active ingredient, a method for treating osteoporosis comprising administering said compound and a use of said compound for the production of a therapeutic agent for osteoporosis. The compounds of the formula (I) have superior bone resorption-inhibitory activity and act to reduce the increased amount of calcium in blood serum, which is caused by bone resorption.

Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.

Abstract: The invention provides novel 1,4-benzothiazepine compounds substituted with hydroxy or a group containing hydroxy, compositions comprising such compounds and their use in the treatment or prophylaxis of treating clinical conditions in which inhibition of bile acid uptake is indicated, for example, hyperlipidemia and atherosclerosis.

Abstract: The present invention relates to novel substituted benzylamino nitrogen containing non-aromatic heterocycles and, specifically, to compounds of the formula ##STR1## wherein W, R.sup.1, R.sup.2, R.sup.3 and A are as defined in the specification, and to intermediates used in the synthesis of such compounds. The novel compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The present invention relates to 1-benzyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.

Abstract: The present invention relates to therapeutic agents for thrombocytopenia which contain an indolocarbazole derivative represented by the formula (I) given below or a pharmaceutically acceptable salt thereof as an active ingredient, and to novel indolocarbazole derivatives.

Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.

Abstract: Spirocycles of general structural formula: ##STR1## are Class III antiarrhythmic agents.

Abstract: Polyalkylpiperidine compounds of the formula I ##STR1## in which Y is the group ##STR2## are very effective stabilizers for organic materials.

Abstract: New intramolecular charge-transfer organic dyes are described. The design of these molecules is based on the phenomenon of spiroconjugation, and it provides a modular approach to the preparation of unique materials with interesting optical properties. In the dyes of the invention, the lowest unoccupied molecular orbital (LUMO) of the acceptor part (based on indandione) is spiroconjugated with the highest unoccupied molecular orbital (HOMO) of the donor part (amines, alcohols and thiols). The interaction between the donor and acceptor is controlled by the energy and symmetry of the frontier orbitals. The novel dyes described herein, with predictable and tunable optical properties, can be used in many optical applications including nonlinear optics (NLO).

Abstract: A spiro compound represented by the formula: ##STR1## wherein ring A represents an optionally substituted aromatic ring; T represents an optionally substituted hydrogen atom or an optionally substituted hydrocarbon group; X represents --CH.sub.2 --, --CO-- or --CH(OH)--; D represents --CH.sub.2 --, --O-- or --NR-- wherein R is a hydrogen atom or an optionally substituted hydrocarbon group and m, e and f independently represent an integer from 1 to 3, or a salt thereof. The spiro compound inhibits monoamine uptake, monoamine oxidase B and/or Ca ion uptake, and is a prophylactic and therapeutic drug for a central nervous diseases.

Abstract: N.sub.1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: ##STR1## These compounds have patent antibacterial activities against a wide variety of infectious bacteria and are useful as antibacterial agents by oral or parenteral administration.

Abstract: Compounds of general formula (I), in which r is 1 or 2, R.sub.1 is selected independently from: unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, the 2(beta)-naphthyl group, and heterocyclic, monocyclic or dicyclic groups; R.sub.2 is selected independently from: heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups, and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group comprising from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group.

Abstract: There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

Abstract: This invention concerns the compounds of formula (I), the pharmaceutically acceptable salts and stereoisomeric forms thereof, and also the N-oxide forms thereof. ##STR1## wherein: R.sup.1 and R.sup.2 each independently are hydrogen; C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; C.sub.1-6 alkyl substituted with hydroxy, C.sub.1-6 alkyloxy, carboxyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkyloxycarbonyl or aryl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.9, R.sup.10, R.sup.11 or R.sup.12 each independently are hydrogen, halo, cyano, hydroxy, trifluoromethyl, trifluoromethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)-amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkyloxy-carbonyl; R.sup.7 and R.sup.

Abstract: Polyalkylpiperidine compounds of the formula I ##STR1## in which Y is one of the groups ##STR2## are distinguished by very low volatility at elevated temperature and are very effective stabilizers for organic substances.

Abstract: The invention features a method of treating a pathological condition of the prostate gland, e.g., benign prostatic hypertrophy or prostate cancer, in a mammal, said method comprising administering to said mammal a therapeutic amount of the indolocarbazole compound K-252a or a preferred derivative thereof. The invention also includes novel derivatives of K-252a.

Abstract: An improved process for the preparation of trans-6- 2-(substituted-pyrrole-1-yl)alkyl!pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N, 4-diphenyl-1- 2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl!-1H-pyrrol e-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Abstract: A compound of formula I, having antibacterial activity and a pharmaceutical composition containing the compound of formula I: ##STR1## wherein Q represents a partial structure of formula II: ##STR2## wherein all substituents are defined in the specification.

Abstract: A method of treating cognitive deficiencies is described by administering a quinazoline derivative of the general formula ##STR1## wherein A represents ##STR2## in which n is 1-10, P is a bond or (CH.sub.2).sub.m in which m is 0-10, and M is .dbd.O, .dbd.S, .dbd.NR, .dbd.CRR', ##STR3## novel compounds of the above are also described as well as methods of manufacture and pharmaceutical compositions.

Abstract: An improved process for the preparation of trans-6-[2-(substituted-pyrrole-1-yl)alkyl]pyran-2-ones by a novel synthesis is described where .alpha.-metalated N,N-disubstituted acetamide is converted in seven operations to the desired products, and specifically, a process for preparing (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahy dro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H pyrrole-3-carboxamide, as well as other valuable intermediates used in the processes and prodrugs which are bioconverted to hypolipidemic and hypocholesterolemic agents and pharmaceutical compositions of the same.

Abstract: Compounds of the invention have the formula: ##STR1## which have fibrinogen receptor antagonist activity, including, for example, ##STR2##

Abstract: Novel piperidine compounds of the formula (I) are suitable for use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.The definitions of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, A and n in the formula (I) are given in the text.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefor.

Abstract: This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT.sub.4 agonists or antagonists and 5-HT.sub.3 antagonists.

Abstract: A novel class of N-substituted triarylmethane sulfonamides is provided which undergo reversible oxidation into colored form and reversible reduction of the oxidized form into colorless form. The N-substituted triarylmethane sulfonamides can be represented by the formulae: ##STR1## wherein B is a carbocyclic ring or rings; T is a 5- or 6-membered ring; Y is a moiety selected from ##STR2## wherein E, positioned ortho or para to said --OH group, is selected from --OH, --NH.sub.2, --NHR', --NR'R" and --NHSO.sub.

Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.

Abstract: Fungicidally active compounds of the formula ##STR1## in which X represents oxygen or sulphur,R represents cycloalkyl, or represents optionally substituted aryl, or represents the radical ##STR2## R.sup.1 and R.sup.2 each independently is hydrogen or an organic radical, or together with the nitrogen atom form a heterocyclic radical,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl, andR.sup.4 represents alkyl or cycloalkyl, or represents optionally substituted aryl,but wherein and R.sup.3 and R.sup.4 may not simultaneously represent methyl,and acid addition salts thereof, as well as intermediates therefore.

Abstract: The invention relates to processes for preparing N-substituted heterocyclic compounds of formula (I) ##STR1## wherein the substituents are as described in the specification, and to intermediates. The compounds are useful for antagonizing angiotensin II.

Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.

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

Abstract: The present invention relates to spiro compounds of general formula I: ##STR1## wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.

Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.

Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.