Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.

Abstract: There is provided a charge transport material which can easily be coated to form a film, is less likely to be crystallized during or after film formation, has excellent charge transport capability, and high applicability to electronic devices. A charge transport monomer comprising conventional CBP with a specific substituent introduced thereinto is polymerized to prepare a polymer which is brought to a charge transport material comprising this polymer.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: There is provided a process for preparation of a monoketal compound of the structure that includes reacting 1,4-cyclohexanedione of the structure with a diol of the structure in a halogenated organic solvent in the presence of an acid catalyst, wherein X is a substituted or unsubstituted ethylene or propylene. Various embodiments and variants are provided.

Abstract: Disclosed herein are a gelling agent composed of an isoleucine derivative having a carbazolyl group, and a process for preparing a gelling agent, which comprises reacting an isoleucine derivative having a specific skeletal with a compound having a carbazolyl group in the presence of dichloromethane and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride to obtain an isoleucine derivative having a carbazolyl group.

Abstract: Carbazoles of formula (I) with R2=hydroxyfunctional amide (hydroxamic or esters) are disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: The invention concerns a process for the preparation of N-aryl-aza-heterocycles of the general formula I by reaction of aza-heterocycles with activated aryl halides with use of caesium carbonate without addition of further catalysts at room temperature.

Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.

Abstract: There are described tetrahydrocarbazoles of formula (1) or (2). The compounds are suitable as antimicrobial active ingredients.

Abstract: Carbazoles of formula (I) with R2=hydroxyfunctional amide (hydroxamic or esters) are disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 and R5 are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1&bgr; secretion.

Abstract: This invention relates to a novel organophotoreceptor that includes: (a) a charge transport composition comprising molecules having the formula 1

Abstract: Fluoro substituted cycloalkanoindole derivatives are antagonists of prostaglandins, and as such are useful for the treatment of prostaglandin mediated diseases.

Abstract: A novel compound with anthraquinone structure and having the following foluma (I): 1

Abstract: Substituted arylcycloalkanes, compositions containing them and use thereof. The present invention relates especially to substituted arylcycloalkanes with therapeutic activity, which may be used such as in oncology.

Abstract: An improved process for the preparation of cis-1,3-diols is described where a beta hydroxy ketone is treated with a trialkylborane or dialkylalkoxyborane or a mixture of a trialkylborane and a dialkylalkoxyborane followed by recovery and reuse of the alkylborane species to convert additional beta hydroxy ketone to the cis-1,3-diol.

Abstract: A class of novel indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock

Abstract: The invention relates to a method of producing heterocyclic carbamates of the general formula (I) by reacting aza-heterocyclic compounds with alkyl- or aryl-halides in the presence of carbon dioxide and alkali carbonate, and to new compounds of the general formula (I).

Abstract: The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein tyrosine kinases using indolinone compounds and methods of treating diseases by modulating the function of protein tyrosine kinases and related signal transduction pathways.

Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.

Abstract: Novel substituted amino acids of formula are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.

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 describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: A compound having the formula wherein R1 is COOR8 wherein R8 is alkyl having from 1 to 10 carbon atoms or aralkyl, the aralkyl having from one to four carbon atoms in the alkyl portion and a carbocyclic or heterocyclic group in the aryl portion; R2 is H, alkyl having from 1 to 10 carbon atoms, or COOR7 wherein R7 is alkyl having from 1 to 10 carbon atoms; R3 is H, alkyl having from 1 to 10 carbon atoms, or COOR8; R4 is H, alkyl having from 1 to 10 carbon atoms, or COOR8; R5 is H, alkyl having from 1 to 10 carbon atoms, aralkyl having from 1 to 4 carbon atoms in the alkyl portion, aryl having from 1 to 10 carbon atoms, acyl having from 1 to 10 carbon atoms, or COOCH3; and R6 is H or COOCH3; and thereof.

Abstract: Compounds having a .beta.-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R.sup.1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R.sup.2 represents hydrogen, hydroxymethyl, NHR.sup.3, SO.sub.2 NR.sup.4 R.sup.4', or nitro; R.sup.6 represents hydrogen or lower alkyl; and X represents nitrogen, R.sup.9 represents hydrogen, one of R.sup.7 and R.sup.8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.

Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: ##STR2## represents an aromatic or alicyclic ring; R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1 and R.sub.2 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, or --COR'" where R'" is C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.

Abstract: A compound of formula (I): ##STR1## wherein Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are each hydrogen, halogen, nitro, cyano, hydroxyl, thiol, amino, alkyl, haloalkyl, alkylthio, a protected or unprotected carboxyl, a protected or unprotected sulfonamide, or tetrazol; one of R.sup.1 and R.sup.2 is hydrogen, alkyl, aryl, aralkyl, oxazolyl, or a protected or unprotected carboxyl and the other of R.sup.1 and R.sup.2 is hydrogen, alkyl, aryl or aralkyl; and R.sup.3 is hydrogen or an amino protecting group, and pharmaceutically acceptable salts or esters thereof. The compounds are effective for treating dementia, Alzheimer's disease and delirium and are effective as sedatives.

Abstract: The invention relates to pyrrolidine monomeric units and to oligomers which are joined via phosphate linkages, including phosphorothioate, phosphodiester and phosphoramidate linkages.

Abstract: Substituted 1,2,3,4-tetrahydrocarbazoles of the formula ##STR1## having the meaning for R.sup.1 to R.sup.8 indicated in the description, can be prepared by catalytically hydrogenating a substituted phenol of the formula ##STR2## reacting the hydrogenation solution with a phenylhydrazine of the formula ##STR3## to give the hydrazone and cyclizing the hydrazone under acidic conditions.

Abstract: 1-amino-2-cyclohexene compounds represented by the following formula (I): ##STR1## wherein the substituents are as defined in the specification, a process for preparing the compounds and their use as intermediates in the production of medicinal and agricultural agents is disclosed.

Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.

Abstract: Novel pyrrolidine monomers bearing various functional groups are used to prepare oligomeric structures. The pyrrolidine monomers can be joined via standard phosphate linkages including phosphodiester and phosphorothioate linkages. Useful functional groups include nucleobases as well as polar groups, hydrophobic groups, ionic groups, aromatic groups and/or groups that participate in hydrogen-bonding.

Abstract: The present invention provides novel compound of the formulas (Ia) or (I): ##STR1## wherein Q is one or two amino acid residues which may be substituted; R.sup.3 is a carboxyl group which may be esterified or an acyl group; A is an alkylene group; B is hydrogen or an alkyl group which may be substituted or an acyl group; or a salt thereof; ##STR2## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a hydrocarbon residue which may be substituted; R.sup.3, A and B have the same definitions as those shown above; m and n each is 0 or 1; provided that where both m and n are both equal to 0, R.sup.3 is a carboxyl group which may be esterified or an acyl group having not less than 7 carbon atoms; or a salt thereof.The compound (Ia) or (I) shows cathepsin L inhibitory and bone resorption inhibitory activities and are useful as a prophylactic/therapeutic agent for osteoporosis.

Abstract: A two stage interpolation system provides greater bandwidth for signals compressed and expanded by interpolation, for example video signals displayed in a zoom or enlarged mode. A finite impulse response filter generates from a first signal of digital samples a second signal of digital samples representing signal points between the samples of the first signal. The first signal is delayed, but otherwise substantially unmodified. The second signal and the delayed first signal are interleaved, for example by a multiplexer, to produce a third signal of digital values having a sample density twice that of the first signal. A compensated variable interpolator derives from the third signal a fourth signal of digital samples in which the frequency content of information represented by the first signal has been changed.

Abstract: An intermediate compound of Formula (V): ##STR1## wherein G is COQ.sub.1 and Q.sub.1 represents chloro, bromo, C.sub.1-4 alkoxy, PhO--, Cl.sub.5 C.sub.6 O--, Cl.sub.3 CO--, succinimidyloxy or imidazolyloxy; the remainder of the terms R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and Y are defined in the specification. The intermediates of Formula V are useful for preparing 1-(2,3-dihydro-1-carboxamide final products wherein said final products possess 5-HT M-receptor antagonist activity.

Abstract: New cycloalkano[b]dihydroindoles and -indolesulphonamides, substituted by heterocycles, of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different andrepresent hydrogen, nitro, cyano, halogen, trifluoromethyl, carboxyl, hydroxyl or trifluoromethoxy, orrepresent a group of the formula --S(O).sub.w R.sup.5, in whichR.sup.5 denotes alkyl or optionally substituted aryl,w denotes the number 0, 1 or 2, orrepresents alkoxy or alkoxycarbonyl, or benzyloxy, orrepresents a group of the formula --NR.sup.6 R.sup.7, in whichR.sup.6 and R.sup.7 are identical or different anddenote hydrogen, alkyl or acyl ordenote aryl, ordenote a group of the formula --S(O).sub.w R.sup.5, in which R.sup.

Abstract: A method of decreasing the melanin content in mammalian skin and hair by administering to a mammal a composition comprising an effective amount of one or more derivatives of 5,6-dihydroxyindole, the derivatives having one or more substituents which are capable of being removed enzymatically, in admixture with a pharmaceutically acceptable carrier, the amount being 0.5% to 20% wt/wt based on the composition.

Abstract: Carbazole compounds represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, R.sup.2 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkanoyl group having 2 to 6 carbon atoms or a benzoyl group, R.sup.3 and R.sup.4 are the same or different, and are each hydrogen atom, an alkyl group having 1 to 7 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkyl group having 1 to 3 carbon atoms substituted by a phenyl group, or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are attached form a morpholino group, a piperidino group, a pyrrolidino group or a piperazino group, and n is an integer from 1 to 3, and salts thereof have strong antipsychotic activity.

Abstract: A process for the preparation of aromatic carboxylic acids or their salts comprises heating carboxyl-free aromatic compounds and aromatic carboxylic acid salts whose basic structures differ from those of the aromatic compounds, or heating polycyclic aromatic compounds with three or more rings and monocyclic or bicyclic aromatic carboxylic acid salts, under carbon dioxide pressure in the presence of one or more metal compounds selected from group (a) of compounds of zinc, cadmium, and thallium and one or more compounds selected from group (b) of compounds of cesium, Group II metals, And Group IIIa metals to effect the intermolecular transfer of the carboxyl groups.

Abstract: Novel fungicidally active compounds of the formula ##STR1## in which R represents alkyl, cyanoalkyl or in each case optionally substituted alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl or phenylalkyl,R.sup.1 represents the --OR.sup.2 or --NR.sup.3 R.sup.4 groups, andR.sup.3 and R.sup.4 have special special definitions.

Abstract: Compounds of the formula: ##STR1## wherein R1 is hydrogen, C1 to C4 alkyl, C2 to C4 alkenyl, or NR2R3, wherein R2 and R3 are independently selected from hydrogen, C1 to C4 alkyl and hydroxyl, but R2 and R3 are not simultaneously hydroxyl;X is oxygen, sulfur, CO2, or NR4, wherein R4 is hydrogen, C1 to C6 alkyl, C1 to C6 alkoyl or aroyl;A is selected from C1 to C6 alkylene and C2 to C6 alkenylene;Y is selected independently at each occurrence from hydrogen, halogen, hydroxy, cyano, nitro, halosubstituted alkyl, C1 to C12 alkyl, C2 to C12 alkenyl, C1 to C12 alkoxy, C3 to C8 cycloalkyl, aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, C1 to C12 arylthicalkoxy, and substituted derivatives of aryl, aryloxy, aroyl, C1 to C12 arylalkyl, C2 to C12 arylalkenyl, C1 to C12 arylalkoxy, or C1 to C12 arylthioalkoxy, wherein C12 alkyl, alkoxy, and halosubstituted alkyl; n is a number having the values 0-4; when n=0 then Y=hydrogen;and M is hydrogen, a pharmaceutically acceptable cation,

Abstract: A composition comprising an aromatic copolyestercarbonate having flexural modulus, flexural yield and secondary transition temperature improvement over a corresponding aromatic polycarbonate effective amount of ester units of the structure ##STR1## or mixtures of the above two structures wherein R.sub.1 and R.sub.2 are the same or different and are alkyl of one to six carbon atoms, inclusive, cycloalkyl of four to seven carbon atoms, inclusive, phenyl, one to three alkyl substituted phenyl each alkyl having one to three carbon atoms, inclusive, and R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached form a ring of four to six carbon atoms, inclusive, or carbazole.

Abstract: Carbazolylmethane compounds of the formula ##STR1## wherein one of Y.sub.1, Y.sub.2 and Q represents a 3-carbazolyl radical of the formula ##STR2## and each of the other two independently represents an amino-substituted phenyl radical of the formula ##STR3## a 3-indolyl radical of the formula ##STR4## These compounds are particularly suitable for use as color formers in pressure-sensitive or heat-sensitive recording material.

Abstract: To prepare basic dyestuffs of the general formula ##STR1## in which A and B independently of one another represent a hetero-aromatic radical or a radical of the general formula ##STR2## compounds of the general formulaA--CH.sub.2 --BA and B have the abovementioned meaning,are oxidized with oxygen in the presence of a nucleophilic compound of the general formulaD--Hand in the presence of catalytic amounts of benzoquinones substituted by halogen or cyano or of phenanthrenequinones substituted by nitro, and in the presence of catalytic amounts of nitrogen oxides--with the exception of dinitrogen monoxide--or of substances which produce such nitrogen oxides under the reaction conditions.