Abstract: Tetrahydrothiophene derivatives of the formula (I) R1—X—(A1—M1)a—(A2—M2)b—A3—Y—T—Z—R2  (I) where the symbols and indices have the following meanings, for example: T is undirected and is tetrahydrothiophene-2,5-diyl or tetrahydrothiophene-2,4-diyl R1 is hydrogen or a straight-chain or branched C1-20-alkyl or C2-20-alkenyl radical (with or without asymmetric carbon atoms), R2 is hydrogen or a straight-chain or branched alkyl radical (with or without asymmetric carbon atoms) having 1 to 20 carbon atoms, X is a single bond, —O—, OC(═O)—, —C(═O)O— or —OC(═O)O— Y is —OC(═O)—, —SC(═O)—, —OCH2— or —CH2CH2— Z is a single bond or —O— A1, A2 and A3 are undirected different and are each, independently of one another phenylene-1,4-diyl, M1 and M2 are undirected and are each, independently of one another —OC(&boxH

Abstract: A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions.

Abstract: A compound expressed by chemical structural formula: having the characteristic of specifically inhibiting the activity of &agr;-glucosidase (an enzyme that breaks down disaccharides, etc.) at the intestinal level. The compound is obtained by extraction and fractionation from Salacia prinoides and/or Salacia oblonga, which are used as natural drugs. A highly safe antidiabetic agent and dieting agent are produced using the compound as a base.

Abstract: The present invention relates to ureido and thioureido derivatives of 4-amino-2(5H)-furanones and 4-amino-2(5H0-thiophenones for the treatment of tumors.

Abstract: The present invention provides compounds of the formula where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocylic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or —C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.

Abstract: Urocanic acid derivatives useful as antiallergic agents represented by the following formula (I) or a pharmacologically acceptable salt thereof: wherein R2 denotes hydrogen or lower alkyl, R3 denotes nitro, amino, cyano or COOR2, wherein R2 in said COOR2 is as defined above, and Q denotes carbon or nitrogen.

Abstract: The present invention is directed to double prodrugs containing polymeric-based transport forms.

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor &agr;, nuclear factor &kgr;B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovis replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-heteroarylalk(en)yl derivatives as ocular hypotensives.

Abstract: Pharmaceutical compositions which are useful for the treatment of cancer or illnesses which arise due to an abnormally elevated cell proliferation comprise acyl derivatives of aromatic aldehydes, especially arylidene diesters and .alpha.-alkoxyarylidene esters of general formula (I).

Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: The present invention provides a herbicidal compound of formula I, methods for the preparation thereof and intermediates useful therefor. ##STR1## wherein X and Y are each independently O or S; Z is N or CR.sub.4.

Abstract: This invention relates to compositions, compounds and methods for lightening skin, using active compounds having the structure: ##STR1## wherein: (i) each X is, independently, selected from the group consisting of halo, alkyl, substituted alkyl, aryl, OR, OCOR, COR, CONRR COOR, CN, SR, SOR, SO.sub.2 R, SO.sub.3 R and NRR, wherein X is other than hydroxy, amino and thio, if this X is attached ortho to the phenol hydroxy;(ii) m is an integer from 0 to 4;(iii) each R' and each R" is, independently, selected from the group consisting of hydrogen, halo, alkyl, substituted alkyl, aryl, OR, OCOR, OCRROR, COR, CR(OR)OR, CONRR, COOR, CRROR, CN, SR, and NRR; wherein halo, when it appears, is other than geminal to a hydroxy, NH.sub.

Abstract: A compound of the general formula I ##STR1## where the indices and the substituents have the following meanings: R.sup.1 is C(CO.sub.2 CH.sub.3).dbd.CHOCH.sub.3, C(CO.sub.2 CH.sub.3).dbd.NOCH.sub.3, N(OCH.sub.3)CO.sub.2 CH.sub.3 and C(CONHCH.sub.3).dbd.NOCH.sub.3 ;R.sup.2 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl and C.sub.1 -C.sub.4 -alkoxy;m is 0 or 1;R.sup.3 is cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl and C.sub.1 -C.sub.4 -alkoxy;n is 0, 1, 2 or 3, it being possible for the substituents R.sup.3 to be different from each other when n is 2 or 3;R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl and phenyl;X and Y are C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino or a C.sub.1 -C.sub.

Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: The invention relates to thiophenes bearing (.omega.-sulfonate)alkoxy or (.omega.-sulfonic acid)alkoxy groups and water-soluble polythiophenes bearing (.omega.-sulfonic acid)-alkoxy side-chains prepared therefrom. The invention also relates to methods for the preparation of these compounds and to antistatic coatings and EMI shieldings comprising the polythiophenes.

Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, and Z are as defined. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.

Abstract: The objects of the present invention are:novel organoselenium compounds: aromatic diselenides and selenosulphides;the use of said novel compounds as antioxidant agents;pharmaceutical compositions containing them;a method of preparation of said novel compounds.

Abstract: This invention relates to a novel 2-hydroxypropionic acid derivative and its manufacturing method. Based on its mechanism to inhibit the CPT I, 2-hydroxypropionic acid derivative of this invention has blood glucose lowering effects so that the derivative may be effectively used as an antidiabetic agent having remarkable antidiabetic activity and fewer side effects.

Abstract: Compounds of the formula (I) in which A is oxygen, sulphur or NH; B is a group of the formula (IIa) or (IIb); and the other variables have the meaning given in claim 1, may be used as inhibitors of the enzyme cyclooxygenase II ##STR1##

Abstract: The present invention relates to compounds of the formula: ##STR1## and their use in therapeutics, especially as medicaments with anti-inflammatory and analgesic properties.

Abstract: Novel .alpha.-pyrones are described. The .alpha.-pyrones are useful in a method for controlling .alpha.-pyrone responsive states in a mammal. The method includes administering to a mammal a therapeutically effective amount of an .alpha.-pyrone such that control of .alpha.-pyrone responsive states in a mammal occurs. .alpha.-Pyrone responsive states can be associated with undesirable cell proliferation such as bacteria or cancer. Packaged pharmaceuticals and pharmaceutical compositions including the novel .alpha.-pyrones are also described.

Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.

Abstract: The present invention relates to the derivatives of formula: ##STR1## and to their use in therapeutics, especially as drugs with anti-inflammatory and analgesic properties.

Abstract: The present invention relates to novel 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrothiophenone derivatives of the formula (I) ##STR1## in which A, B, G, S, X, Y, Z and n have the meaning given in the description, to processes for their preparation, to novel intermediates and to the use of the compounds of the formula (I) as agents for controlling pests.

Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.

Abstract: An ester compound represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represent a C.sub.1 -C.sub.6 alkyl group, or other specified groups, which may be optionally substituted with one or more halogen atoms; and R.sub.3 represents a pyrethroid acid residue (a group resulting from elimination of the carboxyl group from pyrethroid acid), and a pesticidal composition containing the ester compound as an active ingredient.

Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Abstract: The invention relates to the use of derivatives of F-type prostaglandins as ocular hypotensives. The PGF derivatives used in accordance with the invention are represented by the following formula I: ##STR1## wherein wavy line attachments indicate either the alpha (.alpha.) or beta (.beta.) configuration; hatched segments indicate .alpha. configuration, solid triangles are used to indicate .beta. configuration, dashed bonds represent a double bond, or a single bond, R is a substituted heteroaryl radical, R.sup.1 is hydrogen or a lower alkyl radical having up to six carbon atoms, X is selected from the group consisting of --OR.sup.1 and --N(R.sup.1).sub.2, Y is .dbd.O or represents 2 hydrogen radicals. Certain of the compounds represented by Formula I comprise another aspect of the present invention.

Abstract: Substituted N-phenyl- and N-heteroarylalkylcarbamates of formula (I), in which Q is a group (1), (2) or (3); R is halogen, trifluoromethyl, cyano, nitro or C.sub.1 -C.sub.3 haloalkoxy; Z is hydrogen or halogen; or Z and R together in the 2- and 3-position of the phenyl ring form a group --OCF.sub.2 O--; R.sub.1 is C.sub.1 -C.sub.5 alkyl; R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, methyl or ethyl; X is oxygen, sulfur, --SO-- or --SO.sub.2 --, Y is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or cyano; n is 0, 1 or 2; n.sub.1 is 0 or 1; and m is 0 or 1, with the proviso that m is 1 if Q is group (1) or (2); and the diastereomers and enantiomers thereof, exhibit pre- and post-emergence herbicidal properties. The preparation of these compounds and their use as herbicidally active ingredients are described.

Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: Disclosed is a benzoylethylene derivative represented by the following formula (I) or a salt thereof. ##STR1## R.sup.1 to R.sup.5 : a hydrogen atom, --OR.sup.9 (R.sup.9 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.), etc.,R.sup.6 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc.,R.sup.7 : a hydrogen atom, a cyano group, a C.sub.1 -C.sub.5 alkyl group, --SO.sub.q R.sup.15 (q: 0, 1, 2, R.sup.15 : a thienyl group, a phenyl group, etc.) etc.,R.sup.8 : a cyano group, --CR.sup.22 R.sup.23 X (R.sup.22, R.sup.23 : a hydrogen atom, a C.sub.1 -C.sub.5 alkyl group, etc., X: --NR.sup.24 R.sup.25 (R.sup.24, R.sup.25 : a C.sub.1 -C.sub.5 alkyl group, etc., an alkylene group by combining, etc.)), etc.The benzoylethylene derivative of the present invention has potent tyrosine kinase inhibiting activity and cancer cell growth inhibiting activity. The tyrosine kinase inhibitor of the present invention is useful as a carcinostatic agent.

Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an integral salt or their salts with organic or mineral acids wherein the substituents are as defined in the application and having antibacterial properties.

Abstract: There is described a process for preparing 3-(2-thienylthio)butyric acid by converting a compound having the formula (III): ##STR1## wherein R is a straight chain or branched C.sub.1 to C.sub.4 alkyl group, whereby the production of 3-(3-thienylthio)butyric acid as a by-product which is the position isomer can be controlled to at most 0.1 mol %. 3-(2-Thienylthio)butyric acid is a useful compound as an intermediate for a medicinal compound.

Abstract: The substituted thiophene derivative of the invention which is represented by the general formula (1) has a broad disease spectrum for a pathogenic fungus of various crops, exhibits an excellent controlling effect on disease such as gray mold, powdery mildew and rust in particular, and is also effective for a resistant fungus of conventional fungicides which has become a serious problem, and consequently is useful for an agricultural and horticultural fungicide.

Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.

Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.

Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.

Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof,which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the aides and pharmaceutical compositions containing them.

Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: This invention is concerned with an improved process for the synthesis of and intermediate en route to 5,6-dihydro-(s)-4-(ethylamino)-(s)-6-methyl-4h-thieno[2,3-b]thiopyran-2-su lfonamide 7,7-dioxide and related compounds. The instant process reduces the reaction time for the synthesis of the key intermediate from 3 to 4 days to from about 2 to about 4 hours while retaining the high enantiomeric purity of the product.

Abstract: Compounds of Formula 1 ##STR1## wherein X is S or O; R.sub.1 -R.sub.5, m, o, X, Y, A, B are as defined in the specification.

Abstract: 1. Leukotriene-B.sub.4 antagonists of formula I, ##STR1## are described, in whichX represents C.sub.1 -C.sub.4 -alkoxy or --S(O).sub.p --(C.sub.1 -C.sub.4)-alkyl,p represents 0, 1 or 2Y represents a hydrogen atom or the radical CO--A--COR.sub.2 with A meaning an alkylene group with 1-6 C atoms in the chain or a radical ##STR2## R.sub.1 and R.sub.2 represents the radical OH, --O--(C.sub.1 -C.sub.4)-alkyl, --O--(C.sub.3 -C.sub.6)-cycloalkyl, --O--(C.sub.7 -C.sub.12)-aralkyl or the radical NR.sub.3 R.sub.4 with R.sub.3 and R.sub.4 meaning hydrogen, (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.6 -C.sub.10)-aryl or (C.sub.7 -C.sub.12)-aralkyl as well as their salts with physiologically compatible bases and their cyclodextrin clathrates, process for their production and their use as pharmaceutical agents.

Abstract: This invention is directed to 1-alkoxy-2-(alkoxy- or cycloalkyloxy-)-4-(cyclothioalkyl- or cyclothioalkenyl-)benzene compounds that inhibit cyclic AMP phosphodiesterase or tumor necrosis factor (TNF) and are useful in treating patients suffering from disease state capable of being modulated by inhibiting production of cyclic AMP phosphodiesterase or TNF by administering the compound to the patient. The invention is also directed to the preparation of these compounds, pharmaceutical compositions containing these compounds and methods for their pharmaceutical use.

Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.

Abstract: The present invention provides a cyclic sulfide compound represented by a general formula (I) ##STR1## (where R.sup.1 represents --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --O--CH.sub.2 --, --CH.sub.2 --O--, or --CH.sub.2 --S--). According to this invention, a novel cyclic sulfide compound which gives high refractive index and high Abbe number can be obtained. The polymerizable compositions for manufacturing optical products with this compound as their main component can be readily molded into plastic lenses which give superhigh refractive indices and high Abbe numbers or those which give high refractive indices and high Abbe number with low sp.grs. in addition thereto. The castings obtained from said polymerizable compositions are useful as plastic lenses for glasses, manifesting optical uniformity and being excellent in processability, transparency, and thermal, impact and light resistance.

Abstract: Thioalkane .alpha.,.beta.-diketones have interesting organoleptic properties and are therefore suitable as aroma substances.

Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.

Abstract: A method for making a triarylsulfonium hexafluoro metal or metalloid salt is provided by effecting reaction between a diarylsulfoxide and an aromatic substrate, such as an arylalkylether in the presence of a solution of phosphorus pentoxide and methanesulfonic acid to produce a triarylsulfonium complex. A metathesis of the resulting triarylsulfonium complex is effected with an alkali metal hexafluoro metal or metalloid salt.