Abstract: R.sup.6 is H, halogen, alkyl, alkoxy, alkylthio, cyano, or nitro;R.sup.10 is phenylthio, dialkylamino, alkylthio, alkoxycarbonyl, N-morpholinyl, or N-piperidinyl;R.sup.11 is hydrogen or alkyl;Q is alkoxy, alkenyloxy, alkynyloxy, alkylthio, alkenylthio, alkynylthio, alkoxycarbonyl, alkoxyiminomethyl, or Y--Ar;Y is --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S--, or --CH.sub.2 SO.sub.2 --;Ar is a substituted or unsubstituted phenyl or aromatic heterocyclic group,useful for the inhibition of the replication of HIV-1, in vitro and in vivo.

Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.10 alkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, furanyl, pyridinyl or thienyl, and Ar.sup.1 is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; and Ar is phenyl, napthyl, furanyl, pyridinyl or thienyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH.

Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.

Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.

Abstract: A compound which consists of a proactive alkylating moiety containing an electron-withdrawing group, a bioreductive moiety containing at least two double bonds, and a linker joining the proactive alkylating moiety and the bioreductive moiety.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: Disclosed herein are substituted benzylurea derivatives represented by the following general formula (1): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, a halogen atom, or an alkyl or alkoxyl group, R.sup.3 is a phenyl or heterocyclic group which may be substituted, n is an integer of 1-6, and R.sup.4 is a phenyl group which may be substituted, or salts thereof, and medicines comprising such a derivative as an active ingredient. The derivatives or salts thereof strongly inhibit only ACAT in macrophages and are hence useful as prophylactic and therapeutic agents for arteriosclerosis.

Abstract: The invention relates to 7-?5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)! heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: The present invention provides a method for producing N-acyl carbamate in high yield. The method of the present invention comprises the step of reacting an unsaturated acid halide with a carbamate in the presence of a hindered amine. Another method of the present invention comprises the step of reacting a N,N-diacyl carbamate with an active hydrogen compound.

Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.

Abstract: A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,R.sup.3 is hydrogen, hydroxy or C.sub.1-4 alkoxy, andR.sup.4 is fluoro, trifluoromethyl, nitro, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkylthio, heteroaryl, optionally substituted aryl, optionally substituted aryl C.sub.1-6 alkyl, optionally substituted aryl C.sub.2-6 alkenyl, optionally substituted aryl C.sub.2-6 alkynyl, optionally substituted aryloxy, optionally substituted aryl C.sub.1-6 alkoxy, optionally substituted arylthio, optionally substituted aryl C.sub.1-6 alkylthio or --CONR"R'", --SO.sub.2 NR"R"", --NR"R'", --OCONR"R"' or --SONR"R'" where R" and R'" are each hydrogen, C.sub.1-6 alkyl or aryl C.sub.

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 relates to matrix metalloproteinase (MMP) inhibiting compounds of the formula: ##STR1## where R.sup.1 is C.sub.1 -C.sub.12 alkyl, straight or branched and optionally substituted by halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, amino, carboxyl, C.sub.1 -C.sub.6 alkoxycarbonyl, carboxamido, nitrile, mono- or di-(C.sub.1 -C.sub.6)alkylamino, thio, C.sub.1 -C.sub.6 alkylthio, aryl, --Oaryl or --OCH.sub.2 aryl where aryl is optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, carboxy, halogen, cyano, nitro, carboxamido, or hydroxy; and C.sub.1 -C.sub.6 alkanesulfonyloxy. R.sup.2 is .alpha.-OH or .beta.-OH and R.sup.6 is H or R.sup.2 and R.sup.6 together are carbonyl; the chemical intermediates; and processes for the preparation of these compounds and the intermediates thereto.Matrix metalloproteinases (MMP) are a family of zinc-containing calcium dependent proteinases, including stromelysins, collagenases, and gelatinases.

Abstract: Imide compounds having a propioloyl group or pharmaceutically acceptable salts thereof which exhibit potent activities to inhibit the production of Interleukin 1-.beta. and also the production of Tumor Necrosis Factor .alpha.. These imide compounds are useful as a prophylactic or therapeutic agent for inhibiting the production of Interleukin 1-.beta. and the production of Tumor Necrosis Factor .alpha., typically for such diseases as chronic rheumatism, sepsis, ulcerative colitis, Crohn's disease and many other related diseases in which Interleukin 1-.beta. and/or Tumor Necrosis Factor .alpha. would participate.

Abstract: Peptidomimetic compounds useful in the treatment of Ras-associated human cancers, and other conditions mediated by farnesylated or geranylgeranylated proteins; and synthetic intermediates thereof.

Abstract: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Abstract: The invention relates to chiral compounds containing at least one divalent or polyvalent chiral group, at least one polymerizable group, at least one spacer and at least one mesogenic group, and to their use as polymerizable, chiral dopes for the preparation of cholesteric networks. The novel compounds are suitable for use in electro-optical displays or as chiral dopes for nematic or cholesteric liquid crystals in order to produce layers which reflect in colors.

Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --Co.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.

Abstract: Heteroaromatic compounds of the formulae IA and IB ##STR1## where the dashed line is a double bond between the carbon atom and a Z atom, and the index and the substituents have the following meanings:R.sup.1 alkyl, alkoxy, alkylaminoR.sup.2 alkyl;A a direct bond; alkylene, alkenylene, alkynylene; O, S, S-oxides, N and alkylene derivatives or oxime radicals thereofB hydrogen, halogen, alkyl, alkenyl, alkynyl; cycloalkyl, cycloalkenyl, cycloalkynyl, heterocyclyl, aryl, hetarylU CH.sub.2, CHCl, CHR.sup.2 or NOR.sup.2 ;X hydrogen, cyano, nitro, halogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, hetaryl; oxi- and thio derivatives thereof, carbonyl derivatives thereof, carbonyloxy derivatives thereof, amino derivatives thereof, oxime derivatives thereof, amino which may bear one or two of the abovementioned groups;m 1 or 2,Y oxygen or sulfur;Z.sup.1 -Z.sup.2, Z.sub.3 -Z.sub.

Abstract: The present invention relates to novel 3,3-(disubstituted)cyclohexan-1-ol dimers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: Peptidyl derivatives are disclosed that are orally active metalloproteinase inhibitors. The peptidyl derivatives have a selective gelatinase action, have a long duration of action, and are useful in the prophylaxis or treatment of diseases or disorders in which stromelysis, collagenase or gelatinase have a role, for example, in the treatment of cancer to control the development of tumor metastases.

Abstract: 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. It has been determined that 5-lipoxygenase activity, oral availability, and stability in vivo (for example, glucuronidation rate) can vary significantly among the optical isomers of the disclosed compounds.

Abstract: This invention relates to a novel class of immunosuppressive compounds having an affinity for the FK-506 binding protein (FKBP). Once bound to this protein, the immunosuppressive compounds inhibit the prolyl peptidyl cis-trans isomerase (rotamase) activity of the FKBP and inhibit T cell activation. As such, the compounds of this invention can be used as immunosuppressive drugs to prevent or significantly reduce graft rejection in bone marrow and organ transplantations and for use in the treatment of a wide variety of autoimmune diseases in humans and other mammals.

Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.

Abstract: A process for preparing a chiral tetracyclic compound of formula: ##STR1## wherein R is hydrogen or a C.sub.1 -C.sub.6 -alkyl group and Z is oxygen, sulfur or --CH.dbd.CH--, the compounds having uses as dopamine agonists. The process involves reacting a chiral starting material and subsequent chiral intermediates in a series of chirality-preserving synthetic reactions.

Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl or hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group; have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.

Abstract: Compounds of the formula ##STR1## which have retinoid-like biological activity.

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: The present invention provides a process for producing a variety of unsaturated carbamic acid derivatives from corresponding unsaturated carbamates by substitution reaction. The present invention provides a process for producing unsaturated carbamic acid derivatives, comprising reacting an unsaturated carbamate represented by ##STR1## wherein R represents a hydrogen atom or an alkyl group having 1 to 8 carbon atoms, R.sup.1 represents a residue of an alcohol from which an OH group is removed,with an alcohol, a primary or secondary amine or an oxime at a temperature of 80.degree. to 150.degree. C. to substitute the --OR.sup.1 group in the formula (A).

Abstract: A polycyclic aromatic compound having the formula ##STR1## and its salts have useful therapeutic and cosmetic action particularly in psoriasis. In the formula,X represents --CH.dbd.CH--, O or S,R.sub.1 represents hydrogen, branched alkyl having 3-15 carbon atoms, alkoxy having 1-6 carbon atoms or 1-adamantyl, R.sub.2 represents hydroxy, hydrogen, linear or branched alkyl having 1-15 carbon atoms Or alkoxy having 1-6 carbon atoms, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, or R.sub.1 and R.sub.2 together with the adjacent carbon atoms of the naphthalene ring form a 5 or 6 chain ring optionally substituted by at least one lower alkyl radical, or interrupted by an oxygen atom,R.sub.3 represents --CH.sub.2 OH or --COR.sub.4, or --CH.sub.3 when R.sub.1 and R.sub.2 taken together form a 5 or 6 chain ring,R.sub.4 represents --OR.sub.5 or ##STR2## R.sub.

Abstract: Methylene compounds are preferably prepared by reducing an aluminum halide complex of the formula ##STR1## in which R.sup.1 represents a C.sub.6 -C.sub.10 -aryl radical which is optionally substituted by 1 to 4 C.sub.1 -C.sub.4 -alkyl radicals, 1 to 4 fluorine, chlorine and/or bromine atoms, one C.sub.1 -C.sub.8 -alkoxy group and/or one acetoxy group, or represents a heteroaryl radical which is optionally substituted by one C.sub.1 -C.sub.4 -alkyl radical and/or one fluorine, chlorine or bromine atom and contains 5 to 10 C atoms and one O or S atom andR.sup.2 represents a C.sub.1 -C.sub.12 -alkyl radical which is optionally substituted by 1 to 5 fluorine, chlorine and/or bromine atoms, independently of R.sup.1 represents a radical as defined for R.sup.1 and, in the case where R.sup.1 =a C.sub.6 -C.sub.

Abstract: A process for preparing a compound of the structure I ##STR1## where A is oxygen and sulfur and R.sup.1 is selected from the group consisting of hydrogen, halogen, alkyl of one to six carbon atoms, alkoxy of one to six carbon atoms, and trifluoromethyl, and R.sup.2 is alkyl of one to four carbon atoms, comprising coupling a compound of formula II: ##STR2## where X is bromine or iodine, with an N-hydroxyurea compound of formula III: ##STR3## in the presence of a palladium catalyst followed by reaction of the product thus formed with an alkali metal isocyante.The compounds of formula I are inhibitors of the enzyme 5-lipoxygenase and are thus useful as therapeutic agents for the treatment of allergic and inflammatory disease conditions.

Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is alkyl,A is unsubstituted or substituted C.sub.3 -, C.sub.5 - or C.sub.6 -alkylene or C.sub.3 -, C.sub.5 - or C.sub.6 -alkenylene,X is NO.sub.2, CN, halogen, alkyl, alkoxy, phenoxy, alkylthio, haloalkyl, haloalkoxy, carboxyl, alkoxycarbonyl, unsubstituted or substituted benzyloxycarbonyl and/or unsubstituted or substituted phenyl,n is 0-3 or 1-5 where X is halogen,R.sup.

Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.

Abstract: Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.

Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK.sub.3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.

Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.

Abstract: The invention concerns a method for treating depression or senile dementia using a compound which acts selectively as an agonist of gamma aminobutyric acid (GABA) at GABA autoreceptors with the proviso that the compound is not fengabine and progabide.

Abstract: The invention provides compounds of the formulas ##STR1## which are useful as intermediates for the preparation of 6-demethyl-6-deotetracycline antibiotic agents.

Abstract: The invention provides a process for the production of compounds of the formula: ##STR1## wherein R, R.sup.3, R.sup.4 and W are defined in the specification in which a compound of the following formula: ##STR2## is reacted with a nucleophile of the formula WH in an inert atmosphere in the presence of a polar aprotic solvent. The resulting compounds are useful as antibiotics.

Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.

Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.

Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl 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. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes 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, to a patient in need of such therapy.

Abstract: The invention relates to novel intermediates for the preparation of a certain group of novel phenylsulfonylurea herbicides, which herbicides are particularly advantageous for use in crop protection. The novel intermediate compounds are of the formula II ##STR1## and of the formula VI, ##STR2## as defined in the specification and claims. The intermediate compounds may be used to prepare herbicidal and plant growth regulating compounds of the formula I or salts thereof: ##STR3## as defined in the specification. The herbicides so obtained are particularly suitable for selectively controlling weeds.

Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.

Abstract: The invention provides compounds of the formula: ##STR1## wherein R, and R.sup.1 and W are defined in the specification. These compounds are useful as antibiotic agents.

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: The present invention provides a manufacturing method for unsaturated carbamic acid esters by allowing an unsaturated amide compound to react with a metallic base in an inert solvent, followed by a reaction with a halogenated formic acid ester.The invention also provides a manufacturing method of unsaturated carbamic acid esters by allowing an urethane derivative to react with a metallic base in an inert solvent, followed by a reaction with an unsaturated acid halide.

Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Abstract: Unsaturated cyclohexenone oxime ethers I ##STR1## (Q=H, alkylcarbonyl, benzoyl, alkali metal or alkaline earth metal ion, substituted or unsubstituted ammonium ion, phosphonium ion, sulfonium ion, sulfoxonium ion, an equivalent of a transition metal cation;W=--C.tbd.C-- or --CH.dbd.CH--;R.sup.1 =substituted or unsubstituted cycloalkyl, cycloalkenyl or 6-membered heterocyclic group which has 1-2 oxygen and/or sulfur atoms and can be saturated or partially unsaturated; substituted or unsubstituted 5-membered saturated heterocycle with 1-2 oxygen and/or sulfur atoms; substituted or unsubstituted 5-membered heteroaromatic group with 1-2 nitrogen atoms and/or 1 oxygen or sulfur atom; substituted or unsubstituted phenyl, pyridyl or R.sup.9 --X-substituted alkyl with X=O, S, --SO--, --SO.sub.2 -- andR.sup.9 =alkyl, phenyl, 5/6-membered hetaryl with 1-3 hetero atoms;R.sup.2 =alkyl;R.sup.3 =H, alkyl;R.sup.4 =H, halogen, alkyl;R.sup.5 =H, alkyl;or R.sup.3 +R.sup.4, R.sup.3 +R.sup.5 or R.sup.4 +R.sup.5 together form C.