Abstract: This invention concerns a compound for detecting the presence or absence of at least one microorganism. The invention also concerns the use of a compound in a detection and/or diagnostic test. The said invention further concerns a method for detecting nitroaryl reductase activity in a bacteria culture medium. Finally, the invention concerns the use of such a compound, methods for isolating and detecting microorganisms or a group of microorganisms in a sample likely to contain them, and various applications thereof.

Abstract: Method for identifying a drug lead compound that inhibits binding of target bioogical molecules (TBM) by contacting TBM with members of a library of candidate cross-linked target binding fragments (CXBF), each CXBF having at least two candidate target bindig fragments (CTBF), which are inhibitors of binding, linked to a cross-linker, and selecting CXBF that inhibit the binding of the TBM to a greater extent than either of the individual CTBF linked to said cross-linker, wherein the library of CXBF is produced by: (a) screening a population of CTBF capable of being chemically cross-linked by a cross-linker to identify a subpopulation of the CTBF that inhibit binding of the TBM; and (b) chemically cross-linking members of the subpopulation of CTBF or structurally related analogs thereof with a cross-linker to provide a library of CXBF, wherein at least one linking group comprises an oxime ether linking group.

Abstract: The present invention is directed to novel methods for identifying small molecule ligands that are capable of binding with high affinity to a biological target molecule of interest. High affinity binding ligands identified by the described methods find use, for example, as small molecule lead compounds that may they themselves be, or may give rise to, novel therapeutic drugs. More specifically, the subject invention is directed to methods for identifying a ligand that binds to a target biological molecule of interest, wherein a population of small organic compounds are selected and then “pre-screened” to identify those that are capable of binding to the molecular target.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Methods are provided for treatment of eye disorders and injury, including methods for treatment of reduced flow of blood or other nutrients to retinal tissue and/or optic nerve, methods for treatment of retinal ischemia and trauma and methods for treatment for optic nerve injury/damage.

Abstract: This invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutical compositions of such compounds and a method of treatment to inhibit aggregation of platelets.

Abstract: Compounds of the formula ##STR1## where one of Z and Y is CO and the other is C--W--R.sup.2 and the dotted line indicates a double bond is present where necessary to meet valency requirements, W is O, S(O).sub.n, N(R.sup.3), N(R.sup.3)(R.sup.4), N(R.sup.3)O or ON(R.sup.3); R.sup.1 is hydrogen, or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or heterocyclyl group; R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, are as defined above for R.sup.1, or are acyl, or R.sup.2 and R.sup.3 or R.sup.2 and R.sup.4 or R.sup.3 and R.sup.4 together with the nitrogen or oxygen to which they are attached form an optionally substituted ring which may contain other hetero atoms; each X, which may be the same as or different from any other X, is halogen, CN, NO.sub.2, SF.sub.5, B(OH).sub.2, triakylsilyl or a group E, OE or S(O).sub.n E where E is a group as defined hereinbefore for R.sup.

Abstract: The present invention relates to novel flavone/flavanone compounds or their pharmaceutically acceptable salts and process for preparation thereof for protecting gastrointestinal tracts against gastritis, ulcers and inflammatory bowel disease.

Abstract: Good yields and selectivities are achieved in a process for preparing an isochroman-3-one of the formula (I) ##STR1## by reacting a 1,3-dihydroisobenzofuran of the formula (II) ##STR2## with carbon monoxide at a CO pressure of from 0.1 to 20 MPa in the presence of an ionic halide, a palladium catalyst and a dipolar aprotic solvent.

Abstract: Compounds of formula (XXIII): ##STR1## wherein p is 0 or 1, and processes for making such compounds.

Abstract: The present invention relates to new coumarin derivatives represented by the general formula I ##STR1## wherein R.sup.1 =NH.sub.2 or --NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =F,R.sup.1 =R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H,R.sup.1 =H or OH, R.sup.3 =NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2, R.sup.2 =R.sup.4 =R.sup.5 =H,R.sup.1 =OH, R.sup.2 =R.sup.3 =R.sup.4 =H, R.sup.5 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2,R.sup.1 =R.sup.3 =R.sup.5 =H, R.sup.2 =CH.sub.3 or CF.sub.3, R.sup.4 =--NHCH.dbd.C(CO.sub.2 C.sub.2 H.sub.5).sub.2,processes for the preparation thereof and their use as intermediates for the synthesis of new coumarin derivatives with potential biological action.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: The invention relates to benzopyran compounds of formula (I) possessing pharmacological activity, as well as to pharmaceutical compositions containing the compounds of formula (I) and processes for the preparation thereof.

Abstract: The present invention describes 7-aminocoumarin dyes that are substituted one or more times at the 3-, 6- and/or 8-positions by a sulfonic acid or a salt of a sulfonic acid, said dyes being useful as fluorescent probes or in the preparation of enzyme substrates, caged probes, or adducts with reducing sugars. The dyes of the invention optionally possess a reactive group useful for preparing fluorescent conjugates, which conjugates and methods for their preparation are described herein.

Abstract: The subject invention provides for novel compounds for inactivating viruses. These compounds include 6-nitroso-1,2-benzopyrone, 3-nitrosobenzamide, 5-nitroso-1(2H)-isoquinolinone, 7-nitroso-1(2H)-isoquinolinone, 8-nitroso-1(2H)-isoquinolinone. The invention also provides for compositions containing one or more of the compounds, and for methods of treating viral infections, cancer, infectious virus concentration with the subject compounds and compositions.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Unsubstituted or substituted 5-iodo-6-amino-1,2-benopyrones and their metabolites are potent, selective and non-toxic inhibitors and suppressants of cancer growth and viral infections in a mammalian host. The compounds are particularly useful for treatment and suppression of tumors and viruses associated with AIDS, herpetic episodes and cytomegaloviral infections. The methods of treatment of tumorigenic and viral diseases by 5-iodo-6-amino-1,2-benzopyrones and/or its metabolites are described.

Abstract: The invention relates to hydrosoluble coumarin derivatives. These derivatives comply with the formula: ##STR1## in which R.sup.1 represents ##STR2## with m=1 to 30 and in which R.sup.7 can be a hydrogen atom or various groups, R.sup.2 to R.sup.6 can be different substituents, particularly substituents making it possible to introduce into the derivative an appropriate group as the enzyme substrate or for the synthesis of enzyme substrates.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.sup.o stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Abstract: Coumarin deviatives of the formula ##STR1## in which R.sup.1 denotes cyano,R.sup.2 represents phenyl or thiazolyl bonded in the 2-, 4-, or 5-position,R.sup.3 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.4 -alkyl andR.sup.4 represents hydrogen, C.sub.1 -C.sub.4 -alkyl or phenylsulphonyl, where C.sub.1 -C.sub.4 -alkyl can be substituted by hydroxyl, amino, carboxyl or C.sub.1 -C.sub.4 -alkoxy-carbonyl and phenyl can be monosubstituted or disubstituted by chlorine, bromine or C.sub.1 -C.sub.4 -alkyl, where furthermore R.sup.3 and R.sup.4, together with the N atom which they substitute, can denote a morpholine ring, a piperazine ring or a triazole ring which can carry one or two substituents from the group comprising methyl, ethyl and phenyl, andwhere furthermore one of the radicals R.sup.2, R.sup.3 and R.sup.4 denotes or carries a primary or secondary amino group, the hydroxyl group, the carboxyl group or the C.sub.1 -C.sub.

Abstract: A process for the preparation of a substituted guanidine by reacting a substituted cyanamide with ammonia or a substituted amine in the presence of a Lewis acid catalyst. Also disclosed is a process for the preparation of a tri-substituted guanidine by reacting a mono-substituted cyanamide with a di-substituted amine.

Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

Abstract: Fluorescent compounds useful in the determination of chloramphenicol acetyltransferase (CAT) enzyme activity are described. The compounds are fluorescent derivatives related in structure to chloramphenicol comprising a base, ##STR1## substituted at one to five aromatic ring positions by substituents, which may be the same or different, that are alkyl-, hydroxy-, alkoxy-, aryl-, halo-, nitro-, amino-, alkylamido-, or arylamido-; and a fluorescent moiety linked to the base at --NH-- by an aliphatic chain of 1-12 atoms other than hydrogen, where such atoms are carbon, nitrogen, oxygen, or sulfur, or combinations thereof. The substrate compounds are acylated in the presence of CAT to produce fluorescent mono- and diacylated products, which are then physically separated from the reaction mixture and quantitated by means of their fluorescence and/or absorbance.

Abstract: A photochemotherapeutic compound of the formula ##STR1## wherein (i) n is zero, W is a (C.sub.1-16) alkyl, alkenyl, or alkynyl linear or branched chain hydrocarbon, having no more than four O, N, or S atoms in or attached to the chain; or(ii) n is 1, W is CR or CR.sub.2, and R, R', and R" are independently H or CH.sub.3 ; or(iii) N is 2, W is CR or CR.sub.2, and R, R', and R" are independently H or CH.sub.3 ; andA, B, C, and D are independently selected from hydrogen, alkyl, aryl, halogen, amino, aminoalkyl, nitro, alkoxy, aryloxy, hydroxy, carboxy, haloalkyl, or haloalkoxy, particularly compounds of the foregoing structure in which W is a charged substiuent and n=0 or 1.

Abstract: A novel heterocyclic amine derivative of the general formula: ##STR1## wherein a ring A and a ring B stand independently for an optionally substituted benzene ring, Z.degree. stands for O or S or ##STR2## stands for --CH.sub.2 --, X stands for O, S or NR.sup.1 wherein R.sup.1 stands for hydrogen atom or an alkyl group, Y stands for NH, O or (CH.sub.2).sub.n wherein n denotes 0 to 2, and R.sup.2 stands for an optionally substituted hydrocarbon group, or their salts.

Abstract: .alpha.-Homojirimycin and 6-dpi-homojirimycin are each synthesized from 2-azido-2-deoxy-3,4:6,7-di-O- isopropylidene-D-glydero-D-talo-heptono-1,5-lactone in which the side chain acetonide is hydrolyzed to give the corresponding diol which is then protected with a silyl protecting agent to form a silyl ether. The latter compound is used as a divergent intermediate in which the piperidine ring is formed by joining the nitrogen function at C-2 to C-6 (A) with inversion of configuration at C-6 to form 6-epi-homomannojirimycin or (B) with retention of configuration at C-6 to form .alpha.-homomannojirimycin.

Abstract: Solid particle dispersions of dyes according to the formula: ##STR1## are disclosed as filter dyes for photograhic elements. In this formula,m is 0 or 1.R.sub.1 and R.sub.2 are each independently substituted or unsubstituted alkyl or substituted or unsubstituted aryl, or together with R.sub.3 and R.sub.4 form a heterocyclic ring.R.sub.3 and R.sub.4 are each H or together with R.sub.1 and R.sub.2 form a heterocyclic ring.A is a ketomethylene residue.X represents a carboxyphenyl or sulfonamidophenyl, or a carboxy or sulfonamido substituent that is appended to an aryl ring that is part of A.

Abstract: This invention provides a process for producing 2H-1-benzopyran-2-ones (coumarins) from optionally-substituted o-halocinnamic acids or esters under polyester-forming conditions. When the coumarins contain appropriately reactive functional groups, and desired monomers are present, a colored or UV-absorbing coumarin/polyester copolymer is provided in one step.

Abstract: Isocoumarins with cationic substituents, their use in inhibiting serine proteases with trypsin-like, chymotrypsin-like and elastase-like specificity and their roles as anticoagulant agents, and anti-inflammatory agents.

Abstract: A fluorogenic substrate for tryptophanase useful for identifying an unknown microorganism is a fluorescent dye linked to an amino acid by a carbamate or thiocarbamate group. In preferred substrates, the dye is fluorescein or 7-amino-4-methyl coumarin and the amino acid linked thereto is cysteine, threonine or serine.

Abstract: Optical indicator chalcogen (selenide or sulfide) compounds responsive to oxidants, e.g., hydrogen peroxide, and methods for preparing and using such indicators. Upon oxidation the resulting intermediate undergoes spontaneous elimination of the chalcogen residue to yield a signal compound which provides an optical signal such as fluorescence. Preferred fluorogenic indicator compounds are 3-chalcogen-3,4-dihydrocoumarin derivatives and 3-chalcogen-3,4-dihydro-2-quinolone derivatives. Such indicator compounds provide highly fluorescent products upon oxidation by hydrogen peroxide and are useful in analytical systems which generate hydrogen peroxide in response to the analyte under determination.

Abstract: A novel compound having the formula (I): ##STR1## or a reactive derivative or functional equivalent thereof, wherein m is an integer from 1 to 4, and R.sub.1 and R.sub.2 are same or different and selected from hydrogen and 1-4C alkyl; a fluorescent conjugate having the formula (III): ##STR2## wherein m R.sub.1 and R.sub.2 have the meaning given in claim 1, and R.sub.4 is a substituent attached to the keto group of formula (III) by a covalen bond. The new compounds and conjugates are usefual as fluorescent labelling agents.

Abstract: Chromogenic or fluorogenic silanes are formed in which a reactive organosilane is coupled to a chromogenic or fluorogenic nucleus of the coumarin class of compounds, by an ether, urethane or urea linkage. The preferred compounds have the general formula.X.sub.y R'.sub.z Si(CH.sub.2).sub.n L-Couwherein X is a displaceable or hydrolyzable group which allows the silanes to derivatize protic materials; R' is an aliphatic or aromatic hydrocarbon group; L is an ether (O), urethene (NCO) or urea (NCN) linkage; Cou is a coumarin derivative; n=1 to 8; y=1 to 3 and Z=0 to 2, such that y plus z equal 3. The ether linked silanes may be formed by hydrosilylation of an alkenyl ether of the coumarin compound, while the urethane or urea linked silanes may be formed by the direct reaction of a reactive silylisocyanate with a hydroxyl- or amine-substituted coumarin compound. The silanes are useful in derivatizing protic materials to provide the protic materials with chromogenic or fluorogenic properties.

Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.

Abstract: Substituted isocoumarins, their preparation, their use in inhibiting serine proteases with trypsin-like, chymotrypsin-like and elastase-like specificity and their roles as anticoagulant agents, and anti-inflammatory agents.

Abstract: Fluorogenic indicator compounds responsive to the presence of hydrogen peroxide and methods and test compositions for determining hydrogen peroxide in a test sample. Preferred indicator compounds are 3,4-dihydrocoumarin derivatives and 3,4-dihydro-2-quinolone derivatives, especially those having a dialkylamino group at the 7-position. Such particularly preferred compounds are of the formula: ##STR1## wherein R.sup.1 is hydrogen, cyano, or --COOR.sup.6, --CONHR.sup.6 or --CON(R.sup.6).sub.2 where R.sup.6 is hydrogen, alkyl, alkenyl, or aryl; R.sup.3 and R.sup.4 are lower alkyl; and Y is .dbd.0 or .dbd.N--R.sup.5 where R.sup.5 is hydrogen or lower alkyl. The indicator compounds yield highly fluorescent products upon oxidation by hydrogen peroxide in the presence of a peroxidatively active substance and are useful in analytical systems which generate hydrogen peroxide in response to an analyte under determination in a test sample.

Abstract: 7-Phenylacetic acid-4-alkyl-coumarinyl amides having the formula ##STR1## wherein R is alkyl having 1 to 4, in particular 1 to 2 carbon atoms, optionally substituted by one or more halogen atoms, in particular fluorine atoms, especially methyl or trifluoromethyl, are suitable substances for the fluorometric determination of the activity of hydrolases, in particular of penicillin G-acylase, since by the enzymatic reaction they provide cleavage products which in regard to their fluorescence properties differ drastically from those of the substrate. They can be used in processes for the fluorometric determination of the activity of hydrolases, in particular of penicillin G-acylase.

Abstract: Compounds of the formula ##STR1## wherein Y is ##STR2## M is hydrogen, or an alkali metal or ammonium ion, X is --O-- or an amino group,R is H, Cl, Br, CN or carbamoyl,R.sup.1 is H or --SO.sub.3 H, andA is one of several particular organic radicals,are especially useful in the photometric or fluorimetric determination of phosphatase or sulphatase activity in a liquid sample.

Abstract: There are described novel dyes of the formulae ##STR1## in which R.sub.1 and R.sub.2 independently of one another are each hydrogen, unsubstituted or substituted alkyl, cycloalkyl, aralkyl or aryl, and R.sub.1 and R.sub.2 together with the nitrogen atom, and optionally with the inclusion of further hetero atoms, can also form a 5- to 7-membered heterocycle, or one of the radicals R.sub.1 or R.sub.2 can be linked with the carbon atom, in the o-position with respect to the amino group, of the ring A to form a fused-on, saturated, unsubstituted or substituted 5- or 6-membered ring,X is .dbd.NR.sub.3, .dbd.NCOR.sub.4, ##STR2## .dbd.NH or .dbd.O, wherein R.sub.3 is alkyl or unsubstituted or substituted phenyl,R.sub.4 is unsubstituted or substituted alkyl, aralkyl, aryl, vinyl, alkoxy, phenoxy or amino, andR.sub.5 is cyano, carbalkoxy, or unsubstituted or substituted carbonamide, andR.sub.

Abstract: This invention relates to a novel N-acyl acidic amino acid diamide derivative represented by the general formula or a salt thereof: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, represents a hydrogen atom or a substituted or unsubstituted alkyl, cycloalkyl, alkenyl or aralkyl group, or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, when taken together with the respective adjacent nitrogen atoms, form a substituted or unsubstituted heterocyclic group; R.sup.5 represents a substituted or unsubstituted cycloalkyl, acyl or heterocyclic group; A represents a bond or a substituted or unsubstituted alkylene, alkenylene or alkadienylene group; and n is 1, 2 or 3. Said compound has an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such a compound, to a process for the production thereof and to an anti-ulcer agent containing the same.

Abstract: This invention is a process for cyclizing an ortho-alkenyl arenol, wherein the double bond of the alkenyl moiety is one or two carbons removed from the aromatic ring, with carbon monoxide, wherein the process comprises contacting an ortho-alkenyl arenol with carbon monoxide in the presence of a catalytic amount of a catalyst comprising (1) a rhodium-carbonyl complex and (2) an amine with a pK.sub.a of 6 or greater, arsine, phosphine, stibine or mixture thereof, under conditions such that a lactone-fused aromatic compound is prepared.

Abstract: 1-R.sub.1 -3-amino-5-(3-R'-4-R"-phenyl)-6-R-2(1H)-pyridinones or salts thereof, which are useful as cardiotonics, where R.sub.1 is hydrogen, lower-alkyl, or lower-hydroxyalkyl, R is hydrogen or lower-alkyl, and, R' and R" are each hydrogen, hydroxy or amino at least one of R' or R" being other than hydrogen, are prepared by reacting the corresponding 3-carbamyl compound with a reagent capable of converting carbamyl to amino or by first reacting the corresponding 3-carbamyl compound where R' and R" are each hydrogen, nitro or lower-alkoxy at least one of R' and R" being other than hydrogen with a reagent capable of converting carbamyl to amino and then reacting the resulting 3-amino compound where R' and/or R" are/is lower-alkoxy and/or nitro with a reagent capable of converting lower-alkoxy to hydroxy and/or with a reagent capable of converting nitro to amino. Preparation of the corresponding 3-carbamyl and 3-cyano compounds is shown, the latter including cardiotonically active novel 1-R.sub.

Abstract: A light-collecting system, characterized in that it contains a coumarin derivative of the formula ##STR1## in which T denotes O or NR.sub.4, in whichR.sub.4 represents hydrogen, optionally substituted aryl, optionally substituted cycloalkyl or optionally substituted aralkyl,R.sub.1 denotes a carbocyclic or heterocyclic 5-membered or 6-membered ring bonded via a C atom, or a 5-membered or 6-membered heterocyclic ring which is bonded via a N atom and is rotationally asymmetrical to an axis placed through the coumarin/N-heterocyclic bond, it being possible for the said 5-membered or 6-membered rings to carry non-ionic substituents and for an optionally substituted benzene ring or an optionally substituted naphthalene ring to be fused to the said rings;X signifies ##STR2## or --OR.sub.2 ', in which R.sub.2 represents hydrogen, alkyl, cycloalkyl, aralkyl or aryl, it being possible for the said hydrocarbon radicals to be substituted, and R.sub.3, in addition to having the definitions given for R.sub.

Abstract: Novel substituted lactones of amino acids in all their possible stereoisomeric forms or mixtures thereof of the formula ##STR1## wherein A is a hydrocarbon chain of 1 to 10 chain members containing one or more heteroatoms and one or more unsaturations and the chain members being a mono- or polycyclic system or comprises a system of spiro or endo type and may contain one or more chiral atoms or the lactone copula can present a supplementary chirality due to the asymetric spatial configuration of the molecule make up and R is selected from the group consisting of ##STR2## wherein Z is the organic remainder of an amino acid of the formula ##STR3## Y is derived from a primary, secondary or tertiary alcohol of the formula Y--OH and B is the remainder of a heterocyclic amino acid of 3 to 6 carbon atoms of the formula ##STR4## and their preparation and their use for the resolution of amino acids.

Abstract: The present invention is directed to novel amino-substituted 2-cumaryl-3'-chromenylium salts of the general formula ##STR1## wherein R.sup.3 and R.sup.7 are a dialkyl or cycloalkyl disubstituted amino group, hydrogen, or hydroxy group, provided that at least one of R.sup.3 and R.sup.7 is an amino group, R.sup.1, R.sup.2, R.sup.4, R.sup.5, R.sup.6, and R.sup.8 are hydrogen, an alkoxy group, or two of these substituents together form an aromatic ring, provided that R.sup.1, R.sup.2 and R.sup.4 may be the same or different, and R.sup.5, R.sup.6 and R.sup.8 may be the same or different, and Y.sup.- is an acidic anion and to the process for their preparation.

Abstract: A method is disclosed for determining the presence of an enzyme in a biological fluid, which includes the steps of contacting the fluid with a synthetic chromogenic substrate, which is an amino acid derivative of 7-amino-4-trifluoromethylcoumarin; incubating the substrate-containing fluid to effect enzymatic hydrolysis; and fluorometrically determining the presence of the free 7-amino-4-trifluoromethylcoumarin chromophore in the hydrolyzate.

Abstract: Synthetic substrates are provided which may be represented as A-D. The A moiety thereof includes an amino acid, polypeptide, or derivative thereof. The D moiety thereof includes 7-amino coumarin derivatives having an electron withdrawing substituent group at the 3 position carbon or fused between the 3 and 4 position carbons.