Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: The present invention provides a compound having sPLA2 inhibiting activity. The compound represented by the formula (I): wherein R1 is (a) C1 to C20 alkyl, C2 to C20 alkenyl, C2 to C20 alkynyl, carbocyclic groups, heterocyclic groups or the like; R2 is CONH2 or CONHNH2; one of R3 and R4 is —(L2)-(acidic group) wherein L2 is a group connecting with an acid group and the length of the connecting groups 1 to 5 atoms, and the other is a hydrogen atom; its prodrug, their pharmaceutically acceptable salt, or solvate thereof.

Abstract: The present invention relates to pyrrolo[2.1-a]isoquinolines which are inhibitors of phosphodiesterase 10a, a process for preparing these compounds and a method of treating cancer in humans and animals by administering these compounds.

Abstract: The invention relates to an electroluminescent device, in which the luminescent layer contains a luminescent compound and a compound of the general formula I as doping agent, wherein B is an unsaturated carbocyclic or heterocyclic 4-8-link ring, which can also contain an alicyclic bridge, the rings D and E are five- or six-link rings, which each can contain one more hetero-atom N, O and S, the radicals R are one or more substituents H or straight-chain or branched C1-C6-alkyl, X and Y are carbon or nitrogen, R1, R2 and R9 are H or straight-chain or branched C1-C6-alkyl, R3 and R8 are hydrogen, straight-chain or branched C1-C6-alkyl, hydroxy, -OR16, -COOR16, N,N-dialkylamino, acetylamino or halogen, wherein R16 is hydrogen, or straight-chain or branched C1-C6-alkyl, R1 and R2 or R2 and R3 and/or R8 and R9 together can form an alicyclic, heterocyclic or aromatic ring, and A1 and A2, which can be the same or different, are cyan, nitro or -COOR16. The compounds I are partly new.

Abstract: The invention relates to the new arginine salt forms of RS-(±)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, R-(+)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating microbial infections.

Abstract: The present invention provides selective kinase inhibitors of formula (I).

Abstract: A red fluorescent material comprising a compound of Formula I: wherein R1, R2, R3, R4, R5, and R6 each independently represents a linear or branched aliphatic group having from 1 to 10 carbon atoms or an aromatic group having from 5 to 20 carbon atoms.

Abstract: The present invention relates to optically pure S-(−)-benzoquinolizlne carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(−)-benzoquinoluzie carboylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantlly free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(+)-benzoquinolizie carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.

Abstract: A process for easily and industrially advantageously producing both a tricyclic fused heterocyclic derivative having acetylcholinesterase inhibitory activity and an intermediate for the derivative. The process for producing the target compounds comprises the following reaction.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: The present invention relates to novel aminomethylene substituted non-aromatic heterocycles and, specifically, to compounds of formula (Ia) or (Ib) wherein W, R1, R2, R3, A, X′, Y′ and Z′ are as defined in the specification, and to intermediates used in the syntheses of such compounds. The novel compounds of formulae (Ia) and (Ib) are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.

Abstract: The present invention is a chemical compound of formula (I) or a pharmaceutically acceptable salt, solvate and ester thereof, wherein R1 to R4 and n are as defined in the specification. A compound of formula 1 is useful as a pharmaceutical composition for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

Abstract: The present invention relates to optically pure 8-(substituted piperidino)-benzo[i,j]quinolizines, their isomers, derivatives, salts, pseudopolymorphs, polymorphs prodrugs and hydrates thereof, to processes for their preparation, and to pharmaceutical compositions comprising 8-(substituted piperidino)-benzo[i,j]quinolizines their isomers, derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof. These compounds and compositions possess potent activity in treating local and systemic infections, particularly infections caused by sensitive and resistant Gram-positive organism infections, Gram-negative organism infections, mycobacterial infections and nosocomial pathogens, and particularly those belonging to the staphylococcus, streptococcus and enterococcus groups. Methods for treating the diseases and disorders arising from the foregoing infections in humans and animals are described by administering the compounds of the invention to said humans and animals.

Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I):

Abstract: The present invention provides a compound of formula I 1

Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.

Abstract: Novel compounds of formula (I): wherein X1, X2, X3 and X4, n, R1, R2 and R3 are defined in the specification, and pharmaceutically acceptable salts and prodrugs of the compounds of formula (I) have therapeutic uses. These compounds are useful for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea. They are particularly useful for the treatment of obesity.

Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: The invention relates to the new arginine salt forms of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid, a process for their preparation and pharmaceutical formulations which comprise those arginine salt forms as the active ingredient for its use in treating antimicrobial infections.

Abstract: The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases.

Abstract: Disclosed are compounds of formula wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.

Abstract: The present invention provides a pyrrolidine compound of the formula (I) wherein each symbol is as defined in the specification, an optically active compound thereof and a pharmaceutically acceptable salt thereof. The present invention further provides a pharmaceutical composition containing a compound of the formula (I), an optically active compound thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable additive. The compound of the present invention has a serotonin 2 receptor antagonistic action along with a platelet aggregation suppressive action, a peripheral circulation improving action and a lacrimation promoting action. Therefore, the compound of the present invention can be a useful medicine showing effect against thrombotic embolism, dry eye and the like.

Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.

Abstract: An organic light-emitting device material is described, comprising at least one compound represented by formula (I) or a precursor thereof: wherein R1 to R7 each independently represents hydrogen atom, a halogen atom, a cyano group, a formyl group or a substituted or unsubstituted alkyl, alkenyl, alkynyl, aryl, heterocyclic, primary, secondary or tertiary amino, imino, alkoxy, aryloxy, alkylthio, arylthio, carbonamido, sulfonamido, carbamoyl, sulfamoyl, alkylcarbonyl, arylcarbonyl, alkylsulfonyl, arylsulfonyl, alkoxycarbonyl, aryloxycarbonyl, alkylcarbonyloxy, arylcarbonyloxy, urethane, ureido or carboxylic acid ester group, two or more groups selected from R1 to R7 may combine with each other to form an aliphatic carbon ring, an aromatic carbon ring, a non-aromatic heterocyclic ring or an aromatic heterocyclic ring and R4 may further represent R8 and R9 each represents hydrogen atom, an alkyl group, an aryl group or a heterocyclic group, R8 and R9 may combine with each oth

Abstract: This invention concerns intermediates in the preparation of compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alky

Abstract: Benzo[b]quinolizidine and benzo[f]indolizidine derivatives are provided which are useful for the treatment of Alzheimer's disease, senile dementia or other conditions characterized by memory loss. Pharmaceutical compositions containing these compounds, and methods for their use, are also provided.

Abstract: An 8-hydroxyjulolidine compound, having the formula: (wherein R1 and R2 represent independently H, halogen, hydroxyl or alkyl) is prepared by the following chemical reaction: wherein X and Y represent independently halogen, acyloxyl, sulfonyloxyl or phosphoryloxyl and R1 and R2 are as defined above.

Abstract: A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity

Abstract: The invention related to novel 3, 5, and/or 6 swainsonine analogues, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.

Abstract: The object of the present invention is novel photochromic [indole]naphthopyran compounds and their methods of preparation.

Abstract: Photochromic spirofluorenopyran compounds corresponding to the general formula (I): in which B, B′, R1 to R4 and G have the meanings defined herein. The compounds of the invention are useful in the production of photochromic articles, particularly articles made of synthetic resin materials, and exhibit rapid darkening and brightening rates, as well as long useful service lives. By appropriate selection of substituents, it is possible to adjust the properties of the compounds such as absorption maxima (color), brightening rate, etc.

Abstract: The invention relates to novel compounds which show high affinity for cocaine receptors in the brain, particularly dopamine and serotonin transporter sites. The compounds may be used as imaging or pharmaceutical agents, in the diagnosis and treatment of drug addiction, depression, anorexia and neurodegenerative diseases or in determining the doses of therapeutic agents that occupy significant numbers of receptors.

Abstract: A treatment process is disclosed that comprises administering an effective amount of an aromatic sulfone hydroxamic acid that exhibits excellent inhibitory activity of one or more matrix metalloprotease (MMP) enzymes, such as MMP-2, MMP-9 and MMP-13, while exhibiting substantially less inhibition at least of MMP-1 to a host having a condition associated with pathological matrix metalloprotease activity. Also disclosed are metalloprotease inhibitor compounds having those selective activities, processes for manufacture of such compounds and pharmaceutical compositions using an inhibitor.

Abstract: Photochromic spirofluorenopyran compounds corresponding to the general formula (I): in which B, B′, R1 to R4 and G have the meanings defined herein. The compounds of the invention are useful in the production of photochromic articles, particularly articles made of synthetic resin materials, and exhibit rapid darkening and brightening rates, as well as long useful service lives. By appropriate selection of substituents, it is possible to adjust the properties of the compounds such as absorption maxima (color), brightening rate, etc.

Abstract: A compound of the formula: wherein X′ is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value equal to 0; A, A′ and A″ are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z′ is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z″ is hydrogen or a substituent other than hydrogen; Y is C═O, C(OH)R′ or C—A, where R′ is hydrogen or lower alkyl is provided.

Abstract: Disclosed are naphthopyran-type compounds having a pyrrole group annelated in position 5.6, as well as compositions and particularly (co)polymer matrices containing them. These compounds, compositions, and matrices have photochromic properties. These [pyrrole]naphthopyran compounds have the general formula: Articles containing these photochromic compounds, such as ophthalmic and/or solar glasses, lenses, glazing, devices, and the like, are also disclosed.

Abstract: This invention concerns compounds of formula the pharmaceutically acceptable acid addition salts and the stereochemically isomeric forms thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; —A— is a bivalent radical of formula; R1 and R2 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, trihalomethyl, trihalomethoxy, C2-6alkenyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxyC1-6alkyloxy, C1-6alkyloxycarbonyl, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar, Ar—C1-6alkyl, Ar-oxy, Ar—C1-6alkyloxy; or when on adjacent positions R1 and R2 taken together may form a bivalent radical; R3 and R4 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy, Ar-oxy, C1-6alkylthio, di(C1-6alkyl)amino, trihalomethyl, trihalomethoxy, or when on adjacent positions R3 and R4 taken together may form a bivalent radical; R5 is an imidazolyl substituted with hydrogen or C1-6alkyl; R6 hydrogen, hydroxy, halo, cyano

Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.

Abstract: The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.

Abstract: The present invention relates to therapeutically active compounds of formula I ##STR1## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in the prevention or treatment of estrogen related diseases or syndromes.

Abstract: A process for producing pyridiondole derivatives represented by general formula (III) or their salts (wherein R.sup.1 represents hydrogen, lower alkyl or lower alkenyl; R.sup.2 represents hydrogen, lower alkyl or halogeno; and R.sup.3 represents optionally substituted imidazolyl), which comprises reacting a compound represented by general formula (I) or its salt (wherein R.sup.1 and R.sup.2 are each as defined above) with a compound represented by general formula (II) or its salt (wherein R.sup.3.sub.a represents optionally substituted imidazolyl having an imino protecting group; and X represents halogeno), followed by a reaction for eliminating the imino protecting group); and a process for producing optically active pyridoindole derivatives represented by general formula (IV) or their salts: which comprises reacting a racemic mixture of the pyridoindole derivative represent by formula (III) or its salt with (1R)-(-)-10-camphorsulfonic acid.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders.

Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.

Abstract: The present invention relates to the new use of 1,2-bridged 1,4-dihydropyridines which are known in some cases, of the general formula (I) ##STR1## in which R.sup.1 to R.sup.4 and a have the meaning indicated in the description, processes for their preparation and their use as medicaments, as selective potassium channel modulators, in particular for the treatment of the central nervous system.

Abstract: A compound of the formula: ##STR1## wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value equal to 0; A, A' and A" are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z" is hydrogen or a substituent other than hydrogen; Y is C.dbd.O, C(OH)R' or C--A, where R' is hydrogen or lower alkyl is provided.

Abstract: New N-arylpiperidine compounds of formula: ##STR1## wherein: A, m, R, E, n and Ar are as defined in the description, the isomers thereof and the addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same are useful in the treatment of disorders involving the serotininergic system.

Abstract: This invention relates to novel amide derivatives of certain 2,6-methano-2H-quinolizine-type compounds, to the intermediates and processes for their preparation, to their ability to antagonize the effects of serotonin at the 5HT.sub.3 receptors, and to their end-use application in the treatment of chemotherapeutically-induced nausea and vomiting, as anti-anxiety agents, in the symptomatic treatment of pain associated with migraine, as anti-arrhythmic agents, in the treatment of cognitive disorders, in treating hallucinatory endogenous psychoses of the type manifested in patients suffering from schizophrenia, and mania, in the treatment of glaucoma, for stimulating gastric motility, to combat drug abuse, to treat sleep apnea and to treat irritable bowel syndrome.

Abstract: A red fluorescent material includes a compound of the formula: ##STR1## wherein: R.sub.1, and R.sub.2 are individually alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; andR.sub.3, and R.sub.4 are individually alkyl of from 1 to 10 carbon atoms, and a branched or unbranched 5 or 6 member substituent ring connecting with R.sub.1, R.sub.2 respectively; andR.sub.5 is alkyl of from 2-20 carbon atoms; sterically hindered aryl and heteroaryl; andR.sub.6 is alkyl of from 1 to 10 carbon atoms, and a 5 or 6-member carbocyclic ring connecting with R.sub.5.

Abstract: Disclosed is a metal chelate dye which is composed of a metal ion and a ligand that is a methine dye having 2 or more bonding positions capable of coordinate bond to the metal ion at the bonding position. A thermal transfer recording material, an ink used for an ink jet image recording process and a color toner for electrostatic image recording process are also disclosed.