Abstract: The invention relates to benzopyranol derivatives which are intermediates in a process for stereoselectively forming N-substituted dihydro-2,3 benzodiazopines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: Branched, substantially non-antigenic polymers are disclosed. Conjugates prepared with the polymers and biologically active molecules such as proteins and peptides demonstrate extended circulating life in vivo. Substantially fewer sites on the biologically active material are used as attachment sites. Methods of forming the polymer, conjugating the polymers with biologically active moieties and methods of using the conjugates are also disclosed.

Abstract: Antineoplastic cyclolignan derivatives are of formula (I): ##STR1## in which Ar is a 3,4,5-trialkoxyphenyl or 4-hydroxy-3,5-dialkoxyphenyl; X is an oxygen, sulphur or nitrogen atom, a methine group .dbd.CH-- or an alkylmethine group .dbd.C(alkyl)--; Y is a hydrogen atom or an alkyl, alkenyl, (poly)haloalkyl, aryl, hydroxy, alkoxy, amino, monoalkylamino, dialkylamino, (poly)haloalkylamino, arylamino, acyl or acetamido group, or the group Y is absent; Z is an alkyl, hydroxyalkyl, acyl, carboxy, alkoxycarbonyl or aryloxycarbonyl group; and the dotted lines indicate one double bond located at position .DELTA..sup.7-8 or .DELTA..sup.8-8'.

Abstract: The present invention relates to a plant growth regulator comprising as an active ingredient an epoxycyclohexane derivative represented by general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom, a C.sub.1 -C.sub.6, alkyl group or C.sub.3 -C.sub.6 cycloalkyl group, and R.sup.2 and R.sup.3 are independently C.sub.1 -C.sub.6 alkyl groups or are combined to form a C.sub.2 -C.sub.3 polymethylene group which may be substituted with a C.sub.1 -C.sub.6, alkyl group, as well as to a plant growth regulator comprising the epoxycyclohexane derivative and a brassinosteroid as active ingredients. The epoxycyclohexane derivatives exhibit a potent plant growth regulating action which is equivalent to or higher than that of abscisic acid, and are useful as plant growth regulators such as a plant growth accelerator, a germination growth accelerator, a transpiration and wilting inhibitor, a cold resistance enhancer, an accelerator for growing, thickening or maturing fruits, roots, stems or bulbs, etc..

Abstract: Provided herein are novel syntheses of the phosphate-based inositol derivatives 1-O-?(+)-menthoxycarbonyl!-6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inos itol (D4P), D-myo-inositol 1,4,5-trisphosphate (D-IP.sub.3), 6-O-benzyl-2,3:4,5-di-O-isopropylidene-myo-inositol H-phosphonate ((-)-3-HP) and L-myo-inositol 1,4,5-trisphosphate (L-IP.sub.3). These syntheses employ fewer column chromatography steps for the isolation of intermediates than do prior art syntheses, and hence, are more convenient, economical and efficient than are the previously known synthetic methods.

Abstract: Antineoplastic cyclolignan derivatives are of formula (I): ##STR1## in which Ar is a 3,4,5-trialkoxyphenyl or 4-hydroxy-3,5-dialkoxyphenyl; X is an oxygen, sulphur or nitrogen atom, a methine group .dbd.CH-- or an alkylmethine group .dbd.C(alkyl)--; Y is a hydrogen atom or an alkyl, alkenyl, (poly)haloalkyl, aryl, hydroxy, alkoxy, amino, monoalkylamino, dialkylamino, (poly)haloalkylamino, arylamino, acyl or acetamido group, or the group Y is absent; Z is an alkyl, hydroxyalkyl, acyl, carboxy, alkoxycarbonyl or aryloxycarbonyl group; and the dotted lines indicate one double bond located at position .DELTA..sup.7-8 or .DELTA..sup.8-8'.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: ##STR1## wherein R.sub.1 and R.sub.2 are independently chosen from hydrogen, C.sub.1 -C.sub.8 alkyl, OCH.sub.3, OH, OSO.sub.2 CF.sub.3, OSO.sub.2 CH.sub.3, SOR.sub.5, CO.sub.2 R.sub.5, CONH.sub.2, CONR.sub.5 R.sub.6, COR.sub.5, CN, SO.sub.2 NH.sub.2, SO.sub.2 NR.sub.5 R.sub.6, SO.sub.2 R.sub.5, --OCO--(C.sub.1 -C.sub.6 alkyl), --NCO--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 O--(C.sub.1 -C.sub.6 alkyl), --CH.sub.2 OH, --CO-Aryl, --NHSO.sub.2 -Aryl, --NHSO.sub.2 --(C.sub.1 -C.sub.6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R.sub.1 and R.sub.2 together form --O(CH.sub.2).sub.1-2 O-- or --(CH.sub.2).sub.3-6 -- (except that only one of R.sub.1 and R.sub.2 can be hydrogen or OH in any such compound); R.sub.3 and R.sub.4 are independently chosen from C.sub.2 -C.sub.4 alkenyl, C.sub.3 -C.sub.8 alkynyl, C.sub.3 -C.sub.

Abstract: The present invention relates to the use of persistent free radicals, in particular persistent free radicals having a carbon-based .pi.-bonded electronic system available for delocalization of the unpaired electrons as image enhancing agents in magnetic resonance imaging (MRI), in particular electron spin resonance enhanced magnetic resonance imaging (ESREMRI). The invention also relates to contrast media containing such radicals and to the use of such radicals and their non-radical precursors in the manufacture of MRI and ESREMRI contrast media.

Abstract: The present invention is directed to methods of preparing high purity polyalkylene oxide carboxylic acids. The methods include reacting a polyalkylene oxide such as polyethylene glycol with a t-butyl haloacetate in the presence of a base followed by treatment with an acid such as trifluoroacetic acid. The resultant polymer carboxylic acids are of sufficient purity so that expensive and time containing purification steps required for pharmaceutical grade polymers are avoided.

Abstract: An immunosuppressant compound is produced having the structure: ##STR1## or a mirror image thereof, wherein X.sub.1 is 2,2-dimethylvinyl and X.sub.2 and X.sub.3 together are .dbd.CH.sub.2 ; or X.sub.1 is 2,2-dimethyloxiranyl, and X.sub.2 and X.sub.3 together are --0--CH.sub.2 --; or X.sub.1 is 1,2-dihydroxy-2-methyl-propyl, X.sub.2 is --CH.sub.2 OH, and X.sub.3 is OH; or X.sub.1 is 2-hydroxy-2-methylpropyl, X.sub.2 is H, and X.sub.3 is CH.sub.2 OH; or X.sub.1 is COOR, and X.sub.2 and X.sub.3 together are .dbd.O, where R is a lower alkyl, phenyl, or benzyl group; or X.sub.1 is 2-methylpropyl, X.sub.2 is H, and X.sub.3 is CH.sub.3. The compound can be produced by culturing Fusarium subglutinans f. sp. tripterygii ATCC 74358 isolated from the stems of Tripterygium wilfordii. A pharmaceutical composition for immunosuppression therapy is prepared containing the compound and a pharmaceutically acceptable vehicle.

Abstract: Described herein is a process for the preparation of (1S,2R)-1,2-epoxy-1,2,3,4-tetrahydronaphthalene having the Formula (I): ##STR1## which comprises the steps of (a) hydrogenating the compound of Formula (II) to form cis-(1R, 2S)-1,2-dihydroxy-1,2,3,4-tetrahydronaphthalene having the Formula (V): ##STR2## (b) reacting the dihydroxy compound of Formula (V) with a sulphonyl halide of formula R.sup.1 SO.sub.2 Z wherein R.sup.1 is methyl, ethyl, trifluoromethyl, phenyl or p-tolyl, and Z is fluorine, chlorine, bromine or iodine to give a bis-sulphonyl ester of formula (X): ##STR3## and (c) treating the bis-sulphonyl ester (X) with an alkali metal carbonate or alkali metal hydroxide to give the compound of Formula (I).

Abstract: There are described novel biocatalytic and chemical processes for the synthesis of various oxygenated compounds. Particularly, there are described processes for the synthesis of a useful synthon 12 made by reacting a protected diol (acetonide) with permaganate under appropriate conditions. Such synthon is useful of the synthesis of various pharmaceutically important compounds such as D-chiro-inositol and D-chiro-3-inosose. Also, there are disclosed novel compounds, including specifically the synthon 12 and compounds derived therefrom.

Abstract: A radical compound of formula Ia.C(Ar.sup.12).sub.3 (Ia)wherein:each Ar.sup.12, which may be the same or different, represents a 6-membered carbocyclic, at least one group Ar.sup.12 being a group Ar.sup.1 ;each group Ar.sup.1 represents a 6-membered ring optionally substituted at the or any ortho carbon by a group R.sup.1, R.sup.2, R.sup.3 or R.sup.4, at the or any meta carbon by a group R.sup.2 or R.sup.3, and at any para carbon by a group R.sup.1, R.sup.2, R.sup.3 or R.sup.4,with the proviso that no more than two ring carbons are unsubstituted;each of R.sup.1, R.sup.2, R.sup.3 or R.sup.4, which may be the same or different, independently represents a group of formula --M, --XM, --XAr.sup.2 or --Ar.sup.2 ;M represents a water solubilizing group, each group X, which may be the same or different, represents an oxygen or sulphur atom or a NH or CH.sub.2 group.

Abstract: There are described novel biocatalytic and chemical processes for the synthesis of various oxygenated compounds. Particularly, there are described processes for the synthesis of a useful synthon 12 made by reacting a protected diol (acetonide) with permaganate under appropriate conditions. Such synthon is useful of the synthesis of various pharmaceutically important compounds such as D-chiro-inositol and D-chiro-3-inosose. Also, there are disclosed novel compounds, including specifically the synthon 12 and compounds derived therefrom.

Abstract: There are described novel biocatalytic and chemical processes for the synthesis of various oxygenated compounds. Particularly, there are described processes for the synthesis of a useful synthon 12 made by reacting a protected diol (acetonide) with permaganate under appropriate conditions. Such synthon is useful of the synthesis of various pharmaceutically important compounds such as D-chiro-inositol and D-chiro-3-inosose. Also, there are disclosed novel compounds, including specifically the synthon 12 and compounds derived therefrom.

Abstract: The invention provides novel persistent free radicals useful in Overhauser MRI being triarylmethyl radicals having as at least one aryl group a group of formula ##STR1## (wherein each X which may be the same or different is an oxygen or sulphur atom or a group CO or S(O).sub.n, (where n is 1 to 3) with the proviso that at least one group X is a sulphur atom or a S(O).sub.n group; R.sup.1 is a hydrogen atom or group of formula --M, --XM, --X--Ar.sup.2, or --Ar.sup.2 where M is a water solubilizing group, and Ar.sup.2 represents a 5-10 membered aromatic ring optionally substituted by a water solubilizing group M; and each of the groups R.sup.7, which may be the same or different, is a hydrogen atom, or a hydrocarbon group or a water solubilizing group M, or two groups R.sup.

Abstract: The invention is antiobesity/antidiabetic/beta-3 agonists of the formula ##STR1## wherein the substituents R.sub.o, R.sub.1, R.sub.4, R.sub.4 ', R.sub.5, R.sub.6 or n are as defined in the specification.

Abstract: A compound of the general formula I: ##STR1## is disclosed as a potent anticonvulsant drug. Pharmaceutical compositions and methods of treatment are also disclosed.

Abstract: Provided by the present invention is a process for the biocatalytic synthesis of optically pure sphingosines from achiral starting material. The stereoisomers of sphingosine are prepared from chiral arene diols using stereospecific reaction techniques to obtain the desired sphingosine or derivative thereof.

Abstract: Provided by the present invention is a process for the biocatalytic synthesis of optically pure sphingosines from achiral starting material. The stereoisomers of sphingosine are prepared from chiral arene diols using stereospecific reaction techniques to obtain the desired sphingosine or derivative thereof.

Abstract: A process for producing chlorosulfate and sulfamate esters of 2,3:4,5-bis-O-(1-methylethylidene)-.beta.-D-fructopyranose and (1-methylcyclohexyl)methanol is disclosed. The process involves a two step procedure involving in the first step reacting of an alcohol with sulfuryl chloride in the presence of a tertiary or heterocyclic amine base in a solvent selected from the group consisting of toluene, t-butyl methyl ether or tetrahydrofuran to produce a chlorosulfate intermediate, which is preferably stabilized by an aqueous wash and/or treatment with a base, and in the second step reacting of the resulting intermediate with an amine in a solvent selected from the group consisting of t-butyl methyl ether, tetrahydrofuran and lower alkanol.

Abstract: Optically active or racemic compounds represented by the formula ##STR1## where R.sub.2 is OA and R.sub.3 is selected from the group consisting of H and OA; where A is H or is selected from the group consisting of hydrocarbyl radicals comprising between 1 and 3 carbon atoms, as well as ##STR2## with the proviso that when R.sub.3 is OA, then R.sub.2 and R.sub.3 may be bonded together to form the group R.sub.4 is selected from the group consisting of alkyl and aromatic residues having from 1 to 20, preferably from 1 to 12, carbon atoms, for example, alkyl, optionally substituted with aromatic residues, and aromatic residues optionally substituted with alkyl radicals; n is an integer from 1 to 4; R.sub.5 is an unbranched alkyl chain comprising from 1 and 3 carbon atoms or a cyclopropylmethyl radical; R.sub.1 is alkoxy, cycloalkoxy and a cyclic ether of the formula ##STR3## where m is an integer from 3 to 5; with the proviso that when R.sub.1 is alkoxy, then R.sub.

Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.

Abstract: Aryloxy- and heteroaryloxy-alkylene derivatives of amines of formula ##STR1## wherein each of A and B is a group of formula (i) to (iii): ##STR2## wherein Y is --O--, --S-- or --NR-- in which R is hydrogen or C.sub.1 -C.sub.6 alkyl; each of R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is independently:a) hydrogen, halogen, hydroxy, cyano or nitro;b) C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by halogen,c) C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio;d) C.sub.1 -C.sub.6 alkyl-sulfonyl;e) a substituted amine group --NR.sub.7 R.sub.8 ;f) a --COR.sub.12 group; org) two adjacent groups of R.sub.3, R.sub.4, R.sub.5 and R.sub.6, taken together, form a C.sub.1 -C.sub.4 alkylenedioxy group;each of R.sub.1 and R.sub.2 independently is hydrogen, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkenyl or C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl; or R.sub.1 and R.sub.

Abstract: Processes for the preparation of a series of tetracyclic amines useful in the treatment and/or prevention of cerebrovascular disorders are disclosed.

Abstract: Optically active mono-esters of dicarboxylic acid of the formula III: ##STR1## being useful as intermediates for preparing optically active natural products or medicines; asymmetric synthesis process for preparing thereof being characterized by the reaction of an acid anhydride with an (R)- or (S)-arylacetic acid derivative; and the key substances therefor are also claimed.

Abstract: 6-Fluoroshikimic acid derivatives of the formula (I): ##STR1## wherein R.sup.1 is hydroxy or a moiety biotransformable thereto and R.sup.2 is hydrogen or --P(O)(OH).sub.2 have antibacterial, antifungal and herbicidal activity. Their preparation and use are described as are pharmaceutical compositions containing them.

Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.

Abstract: There are disclosed intermediates which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.

Abstract: The invention concerns heterocyclic nitromethane derivatives of the formula 1 as defined hereinafter (and their non-toxic salts) wherein the heterocyclic moiety Q is thienyl, benzothienyl or dibenzothienyl and may bear a wide variety of optional substituents, together with pharmaceutical compositions containing them. The nitromethane derivatives are inhibitors of the enzyme aldose reductase and are of value in the treatment of certain complications of diabetes and galactosemia.

Abstract: Castanospermine is prepared by starting from 5-(t-BOC)amino-5-deoxy-1,2-O-isopropylidene-.alpha.-D-glucuronolactone. Two additional carbons are added to the starting material using ethyl acetate and a strong base and the resulting cyclic hemiketal is subjected to a series of reductions, with intervening removal of protecting groups, to give the castanospermine. A substituted hydroxypyrrolidinone and a substituted hydroxypyrrolidine serve as intermediates in the process.

Abstract: Naphthalene derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkoxycarbonyl andR.sup.2 is a lower alkoxycarbonyl, or R.sup.1 and R.sup.2 are combined together to form a group of the formula: ##STR2## each of R.sup.3 and R.sup.4 is a lower alkoxy, or one of R.sup.3 and R.sup.4 is hydrogen atom and the other is a lower alkoxy, andRing A is a substituted or unsubstituted benzene ring, and a pharmaceutically acceptable salt thereof are disclosed. Said naphthalene derivative (I) and its salt have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.

Abstract: Aromatic carbonyl compounds, in particular arylene ether ketones, are prepared by reacting an appropriate reagent system in the presence of free Lewis acid and a complex between a Lewis acid, for example, aluminum trichloride, and an inorganic salt controlling agent, for example, lithium chloride, and, optionally, a diluent, such as methylene chloride. The process is particularly advantageous for the preparation of substantially or all para-linked arylene ether ketones as the presence of the Lewis acid/Lewis base complex markedly reduces alkylation and ensures the substantial absence of ortho substitution.

Abstract: Castanospermine is prepared by starting from 5-(t-BOC)amino-5-deoxy-1,2-O-isopropylidene-.alpha.-D-glucuronolactone. Two additional carbons are added to the starting material using ethyl acetate and a strong base and the resulting cyclic hemiketal is subjected to a series of reductions, with intervening removal of protecting groups, to give the castanospermine. A substituted hydroxypyrrolidinone and a substituted hydroxypyrrolidine serve as intermediates in the process.

Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

Abstract: Compounds of the formula ##STR1## in which Ar is substituted or unsubstituted phenyl, naphthyl, or thienyl; and Ar.sup.1 is 3-phenoxyphenyl, 4-fluoro-3-phenoxyphenyl, 2-methyl[1-1'-biphenyl]-3-yl, or 6-phenoxy-2-pyridyl, exhibit pyrethroid-like insecticidal and acaricidal activity and are relatively nontoxic to fish.

Abstract: Novel radical ion salts of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently of one another are each hydrogen, methyl, ethyl, phenyl, methoxy, ethoxy, fluorine, chlorine or bromine, or R.sup.1 or R.sup.1 and R.sup.3 may furthermore be tert-butyl and/or R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4 together may in each case form a radical of the formula ##STR2## where z is 0, 1, 2 or 3, and the fused aromatic rings are unsubstituted or monosubstituted or disubstituted by chlorine, bromine, methyl and/or methoxy, M.sup.m.sym. is an m-valent alkali metal, alkaline earth metal, transition metal, tin, lead, thallium, ammonium, phosphonium, arsonium or stibonium ion, k is from 1 to 5, l is from 0.1 to 4, m is from 1 to 3, n is from 0.1 to 4, x is from 0 to 2 and y is from 0 to 6, and k, l, n, x and y may furthermore be non-integral numbers and (l+x)=n.m, are electrically conductive in the crystalline state. A number of the salts are stable at 300.degree. C. and above.

Abstract: The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.

Abstract: The present invention is directed to novel taxols useful as a chemotherapeutic agent. Moreover, the present invention is directed to the process of preparing taxols and various intermediates in said process. A key intermediate is this process is 2,5-dihydroxy-2-patchoulenes. Therefore the present invention is also related to said intermediate and the process for its preparation.

Abstract: A compound of formula II: ArCHR.sub.1 CO.sub.2 CHDR.sub.2in which formula:Ar represents a phenyl or naphthyl group optionally substituted by one or more halogen, alkoxy, haloalkoxy, methylenedioxy, C.sub.1 -C.sub.6 alkyl or haloalkyl groups;R.sub.1 represents the group --CH(CF.sub.3)CH.sub.3 or --C(CF.sub.3).dbd.CH.sub.2R.sub.2 represents the residue of an alcohol R.sub.2 CHDOH in which D is hydrogen or cyano and of which the [1R, cis]2,2-dimethyl-3-(2,2-dibromovinyl)cyclopropane carboxylic ester is significantly insecticidal.

Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodoplyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)-alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

Abstract: There are disclosed intermediate which can be converted into podophyllotoxin and related compounds, which are known antineoplastic agents. There are also disclosed processes for the preparation of such intermediates, and processes for the conversion of the intermediates into known intermediates which are readily converted into podophyllotoxin and related compounds.

Abstract: Naphthalenes of the formula: ##STR1## wherein: m is 1 or 2;n is 1, 2, or 3;R.sup.1 is alkyl of one to seven carbon atoms or an optionally substituted phenyl;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl, optionally substituted phenyl-lower-alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, hydroxy, or lower alkylthio are useful in relieving psoriasis.

Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.

Abstract: There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.

Abstract: Pesticidal compounds of formula IR.sub.A CR.sub.3 .dbd.CR.sub.4 CHDR.sub.B Iin which formula:R.sub.A represents a group ArCR.sub.1 R.sub.2 --in which Ar represents a phenyl or naphthyl group optionally substituted by one or more halogen, alkoxy, haloalkoxy, methylenedioxy, C.sub.1 -C.sub.6 alkyl or haloalkyl groups;R.sub.1 and R.sub.2 together with the carbon to which they are attached represent a C.sub.3 -C.sub.6 cycloalkyl group optionally substituted by one or more halogen atoms or C.sub.1 -C.sub.6 alkyl groups.R.sub.3 and R.sub.4 which may be identical or differ, represent hydrogen halogen or C.sub.1 -C.sub.6 alkyl groups andR.sub.B represents the residue of an alcohol R.sub.B CHDOH in which D is hydrogen or cyano and of which the [1R, cis]2,2-dimethyl-3-(2,2-dibromovinyl) cyclopropane carboxylic ester is significantly insecticidal,the configuration of R.sub.A and CHDR.sub.

Abstract: Naphthalene derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom or a lower alkoxycarbonyl andR.sup.2 is a lower alkoxycarbonyl, or R.sup.1 and R.sup.2 are combined together to form a group of the formula: ##STR2## each of R.sup.3 and R.sup.4 is a lower alkoxy, or one of R.sup.3 and R.sup.4 is hydrogen atom and the other is a lower alkoxy, andRing A is a substituted or unsubstituted benzene ring, and a pharmaceutically acceptable salt thereof are disclosed. Said naphthalene derivative (I) and its salt have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.

Abstract: The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.