Abstract: The present invention relates to the therapeutic use of non-amine tropane analogues that bind to the SERT to treat neuropsychiatric disorders.

Abstract: The present invention provides a compound which is highly safe in terms of toxicity and has a stronger antiallergic action, and particularly has an action of inhibiting both immediate and delayed type allergic reactions. A benzopyran derivative represented by the general formula (I): wherein R1 is an alkyl group having 1-10 carbon atoms or an alkenyl group having 2-10 carbon atoms, and one of R2, R3, R4, and R5 is an alkoxy group substituted with a hydroxy group or an alkoxy group substituted with a carboxy group, and the others are hydrogen atoms or physiologically acceptable salts thereof are superior as the active ingredient of an antiallergic agent.

Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

Abstract: The present invention is a method for producing warfarin sodium from warfarin sodium 2-propanol clathrate by thermal, nondestructive solvent expulsion. The solvent expulsion is conducted under conditions of controlled heat transfer whereby the 2-propanol is expelled from the warfarin sodium 2-propanol clathrate without decomposition of warfarin sodium or the clathrate. Heating is conducted the clathrate at a temperature from about 100° C. to about 170° C. in an active oven under air or in an inert atmosphere and at partial pressures ranging from that of a relative vacuum to atmospheric pressure. The invention also relates to pure warfarin sodium prepared according to the method of the invention and pharmaceutical compositions containing warfarin sodium.

Abstract: Compounds of formula (I); wherein R1=alkyl, alkenyl or alkynyl, O-alkyl, O-alkenyl or optionally substituted, optionally interrupted O-alkynyl; R2=hydrogen or halogen; R3=hydrogen, alkyl or halogen; R4=NHR′ or NHOR″, R′ or R″ are identical or different and represent hydrogen, alkyl, alkenyl or alkynyl, aryl; R5=hydrogen or O-alkyl; R6=alkyl or CH2—O-alkyl; R7=hydrogen or alkyl or R6 et R7 form a cycle together with the carbon carrying them in addition to the addition salts thereof with bases. The compounds of formula (I) have antibiotic properties.

Abstract: The present invention relates to a novel flavone derivative, pharmaceutically acceptable salt, hydrate, solvate and isomer thereof which is useful as an inhibitor against Cyclin Dependent Kinase (CDK), a process for preparation thereof, and a composition of anti-cancer agent or agent for treating neurodegenerative disease comprising this compound as an active ingredient.

Abstract: The present invention is to obtain novel FT-0554 substance which is useful for treatment of helminthiasis. The present invention comprising the steps of culturing the microorganism belonging to fungi having producing activity of FT-0554 substance represented by the following formula [I] subjected ho accumulation of FT-0554 substance in the cultured medium, and isolating FT-0554 substance from the said cultured mass. The medicament useful for treatment of parasitic infection, specifically helminthiasis can be obtained.

Abstract: The invention relates to a flavonoid ester. This flavonoid ester results from the reaction product of at least one flavonoid selected from the group consisting of a flavonoid with a ketone group in the 4-position, a salt, ester or ether of such a flavonoid, and a C-heteroside and/or O-heteroside derivative of such a flavonoid, with the proviso that this flavonoid contains at least one free alcohol group, with an organic monoacid having from 3 to 30 carbon atoms. These flavonoid esters constitute useful active principles for the manufacture of cosmetic, dermopharmaceutical, pharmaceutical, dietetic or agri-foodstuff compositions.

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: The present invention provides a novel &bgr;-diketone compound represented by formula (3): [wherein X represents (CH2)n; n represents an integer of 2-20; and the CH2 of X may be replaced by an oxygen atom, a hetero ring, or an aromatic ring, but oxygen atoms are not sequentially arranged in X], and a metal-coordinated &bgr;-diketone compound in which a metal is coordinated with the &bgr;-diketone compound. The compound of the present invention can be easily synthesized, and serves as a catalyst for asymmetric synthesis which can provide high asymmetric yield and chemical yield.

Abstract: The present invention relates to novel hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids of the general formulae I, II, III and IV: wherein R1=R2=4-hydroxycoumarin; R1=R2=4,7-dihydroxycoumarin; R1=R2=4,5,7-trihydroxycoumarin; R1=4-hydroxycoumarin, R2=—CH(OH)CH3. An object of the invention are also processes for the preparation of hydroxy and polyhydroxy derivatives of coumarin fused with dialdehydes and aldehyde acids, and the antiviral action thereof. Novel hydroxy and polyhydroxy derivatives of coumarin according to the present invention exhibit antiviral action against HIV-1 virus.

Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.

Abstract: The invention relates to a flavonoid ester. This flavonoid ester results from the reaction product of at least one flavonoid selected from the group consisting of a flavonoid with a ketone group in the 4-position, a salt, ester or ether of such a flavonoid, and a C-heteroside and/or O-heteroside derivative of such a flavonoid, with the proviso that this flavonoid contains at least one free alcohol group, with an organic monoacid having from 3 to 30 carbon atoms. These flavonoid esters constitute useful active principles for the manufacture of cosmetic, dermopharmaceutical, pharmaceutical, dietetic or agri-foodstuff compositions.

Abstract: The present inventor has discovered chemical compounds which inhibit the first-pass effect of orally administered drugs in humans; that phototoxic low molecular weight furocoumarins and certain ether-substituted furocoumarins that are naturally present in citrus extracts, juices, byproducts, etc. may be removed therefrom or reduced in concentration without destroying the first-pass effect inhibiting compounds therein, and a method for preparing citrus-based compositions using only FDA or USP acceptable reagents.

Abstract: The present invention provides an aminomethylene derivative represented by general formula (I): ##STR1## wherein A is a cyclic oxo group selected from the group consisting of following general formulae (a), (b), (c), (d) and (e): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent H, an alkyl group or the like; R.sup.6, R.sup.7 and R.sup.8 each independently represent an alkyl group or the like; R.sup.1 and R.sup.2 or R.sup.7 and R.sup.8 may combine with each other to form a tetramethylene group or the like; R represents an alkyl group optionally containing OH or O; and n is an integer of 0 to 4, a process for the same, and the use thereof. The derivatives have an excellent ultraviolet absorption ability and a high optical stability.

Abstract: A sulphamate compound suitable for use as an inhibitor of both oestrone sulphatase activity and aromatase activity. The compound can have the general formula (II) wherein F represents a phenolic ring structure (the first ring structure), J represents the third ring structure; I represents a phenolic ring structure (the second ring structure), G is an optional double bond, H is a link joining the second ring structure to the third ring structure, and Y represents a suitable second group; wherein any one of ring structures F, J and I has bound thereto a sulphamate group.

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: Compounds of the formula The compounds are useful in the treatment of bacterial infections.

Abstract: Liquid petroleum products and industrial liquids are marked with highly soluble silent fluorescent markers having the formula: ##STR1## where R is selected from a linear or branched C.sub.1 -C.sub.18 alkylcarboxy radical.

Abstract: The present invention offers a safe and effective drug for heart diseases and a safe and effective method for treating heart diseases such as ischemic heart disease and cardiac arrhythmia. The method comprises administering a pathologically effective amount of a benzopyran derivative expressed by the following general formula (I): ##STR1## wherein R.sup.1 is an alkyl group or an alkenyl group, R.sup.2 is a hydrogen atom, an alkyl group, an alkyl group having at least one hydroxyl group, an alkenyl group, an acyl group or a glycosyl group; or physiologically acceptable salts thereof.

Abstract: New purine retinoid compounds according to the formula: ##STR1## wherein R is a purine derivative, and pharmaceutical compositions thereof, are provided which exhibit cancer-inhibiting activity.

Abstract: A process for producing coumarin and substituted coumarins starting from substituted hexahydrocoumarins or from substituted dihydrocoumarins. The process includes dehydrogenation in the presence of catalysts based on metals of Group VIII of the periodic table of the elements and in the presence of at least one easily reducible organic compound. The invention allows to achieve exceptionally high yields that do not require the recycling of the hexahydrocoumarin or of the dihydrocoumarin that are present at the end of the reaction, and also allows to achieve high selectivity and easy purification.

Abstract: Viral and bacterial contaminants present in biological solutions are inactivated by mixing one of a novel class of photosensitizer with said solution and irradiating the mixture.

Abstract: The present invention provides novel antiviral naphthoquinone compounds, which may be isolated from plants of the genus Conospermum or synthesized chemically, in accordance with the present inventive methods. The antiviral naphthoquionone compounds, derivatives thereof, and prodrugs thereof, may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2, in the treatment or prevention of viral infection.

Abstract: A process for preparing compounds useful as intermediates used for preparing lubricant and fuel additives. The intermediates include the products prepared by the process and dilactones.

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: The present invention comprises 6,8-difluoro-7-hydroxycoumarins and derivatives of 6,8-difluoro-7-hydroxycoumarins, including reactive dyes, dye-conjugates and enzyme substrates. These fluorine-substituted fluorescent dyes typically possess greater photostability and lower pH sensitivity in the physiological pH range than their nonfluorinated analogs, exhibit less fluorescence quenching when conjugated to a substance, possess absorption and emission spectra that closely match those of their nonfluorinated analogs, and also exhibit higher quantum yields than their nonfluorinated analogs.

Abstract: There are provided methods to control mono-cotyledenous weed species in the presence of crops and particularly in the presence of cereal crops. Also provided are 4-(2,6-disubstituted-phenoxy)coumarin derivatives useful as herbicidal agents and methods to prepare same.

Abstract: Viral and bacterial contaminants present in biological solutions are inactivated by mixing one of a novel class of photosensitizer with said solution and irradiating the mixture.

Abstract: A process for preparing compounds useful as intermediates used for preparing lubricant and fuel additives. The intermediates include the products prepared by the process and dilactones.

Abstract: The dicarboxylic acid derivatives according to the invention have the following structure ##STR1## wherein X denotes O, S, (CF.sub.2).sub.m, C(CF.sub.3).sub.2 or CF.sub.2 --CF(CF.sub.3) (m=1 to 10), and R stems from the following compounds: fluoro- or trifluoromethyl- and nitro- or cyanophenols, thiophenols or -aminobenzenes, 4-hydroxy-, 4-mercapto- or 4-aminocoumarins, N-hydroxysuccinimides or N-hydroxymaleimides, 2-hydroxy- or 2-mercaptobenzoxazoles or -benzothiazoles and 1-hydroxy- or 1-mercaptobenzotriazoles.

Abstract: A process for preparing compounds useful as intermediates used for preparing lubricant and fuel additives. The intermediates include the products prepared by the process and dilactones.

Abstract: New retinoid compounds, as coumarin retinoids and/or purine retinoids and compositions thereof, are provided which exhibit therapeutic and/or biological activity on cancer or precancer cells, as well as to methods of use of same.

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 present invention provides processes which are flexible, cost effective, and commercially viable methods of manufacturing or producing products from 2-hydroxyacetophenone (2-HAP).Of particular interest of the available products are 4-hydroxycoumarin, warfarin-alkali salt, preferably warfarin sodium and warfarin-alkali salt-isopropyl alcohol (2-propanol) complex, more preferably warfarin-sodium-isopropyl alcohol complex.As is known, these compounds are useful as vitamin K dependent anticoagulants in the treatment of humans and animals. In different doses, they are also useful as rodenticide.The inventive process involves contacting 2-HAP, carbonate ester and effective base followed by treatment with an unsaturated ketone and phase transfer catalyst to ultimately yield product.

Abstract: The present invention provides a novel process for making compounds of formula 2a or 2b or pharmaceutically acceptable salts thereof, ##STR1## wherein R1 is selected from the group consisting of phenyl and phenyl substituted with at least one group selected from NO.sub.2 and halogen;R.sub.2 is H;R.sub.3 is selected from the group consisting of C.sub.1-4 alkyl, phenyl, and benzyl; and,R.sub.4 is selected from the group consisting of H and halogen;which comprises the steps of:a) oxidizing a racemate of formula 2 or a salt thereof to form a dehydro-compound of formula 3, ##STR2## wherein R.sub.5 is selected from the group consisting of H, CH.sub.3, benzyl, C.sub.2-8 acyl Na, Li and K; and,b) asymmetrically hydrogenating a compound of formula 3 in the presence of a chiral phosphine catalyst to form a compound of formula 2a or 2b.

Abstract: There are provided methods to control mono-cotyledenous weed species in the presence of crops and particularly in the presence of cereal crops. Also provided are 4-(2,6-disubstituted-phenoxy)coumarin derivatives useful as herbicidal agents and methods to prepare same.

Abstract: The invention relates to novel compositions comprising ene and free radical adducts of unsaturated and saturated hydrocarbons, and acyclic and cyclic vicinal polycarbonyl compounds such as diethyl ketomalonate and indantrione. The adducts are reacted with nucleophiles such as amines, electrophiles such as anhydrides and esters, and metal ions. Post-products are obtained via reaction of said products with capping reagents such as boric acid. Compositions containing said adducts, products and post-products include oleaginous substances such as fuels and lube oils.

Abstract: A compound of formula V: ##STR1## wherein all the R's groups are as defined in the specification, is useful in the treatment of bacterial infections.

Abstract: Photoactive indicator compounds of the formula ##STR1##

Abstract: There are provided methods to control monocotyledenous weed species in the presence of crops and particularly in the presence of cereal crops. Also provided are 4-(2,6-disubstituted-phenoxy)coumarin derivatives useful as herbicidal agents and methods to prepare same.

Abstract: The present invention relates to novel adducts of cyclic carbonyl monomers with substituted olefins, which also are useful as solution viscosifiers.

Abstract: The present invention relates to novel coumarin derivatives and related compounds which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The coumarin derivatives are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized coumarins and of related structures.

Abstract: Novel substituted cis-1,2-dihydroxy-cyclohexadiene compounds, useful as intermediates in the production of compounds for use as intermediates in the production of agrochemicals and pharmaceuticals, and a microbial process for the preparation thereof.

Abstract: A heterocyclic cyclohexanedione derivative represented by the general formula I!: ##STR1## wherein R.sup.1 is optionally substituted lower alkyl, optionally substituted cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic ring; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different from one another and each independently represents hydrogen or lower alkyl; R.sup.6 is hydrogen; R.sup.7 is OR.sup.8 wherein R.sup.8 is hydrogen, lower alkyl, aralkyl, lower acyl, alkylsulfonyl or arylsulfonyl; or R.sup.6 and R.sup.7 are combined together to represent a single bond; X is oxygen, sulfur or N--R.sup.9 wherein R.sup.9 is hydrogen, lower alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted phenyl or optionally substituted heterocyclic ring, a salts thereof, a process for producing the same, and a herbicides comprising the same.

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: A pharmaceutical composition comprising a compound of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, a saturated or unsaturated aliphatic acyl having 2 to 25 carbon atoms or benzoyl group and R.sup.3 is a hydrogen atom or alkyl group, and a pharmaceutically acceptable carrier is disclosed. Further, a novel compound of the general formula (I) wherein R.sup.1 and R.sup.2 are, independently, a hydrogen atom, pivaloyl, capryloyl, lauroyl, palmitoyl, stearoyl, linoleoyl, docosahexaenoyl, or benzoyl group, and R.sup.3 is a hydrogen atom or methyl group, is also disclosed.

Abstract: This invention relates to compounds having the following formula ##STR1## wherein Z is a lactone or a lactone which is fused to a benzene ring which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidines derivatives.