Abstract: The present invention relates to novel anticancer agents, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The present invention more particularly relates to novel derivatives of andrographolide, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, and their pharmaceutically acceptable solvates. The novel derivatives of andrographolide have the general formula (I).

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 invention relates to modified benzylidene-&ggr;-butyrolactones, to a process for their preparation and to the use as UV absorber, for example in pharmaceutical and cosmetic compositions, sunscreens, daycare and haircare products, for improving industrial products, such as paints, surface coatings, plastics, textiles, packaging materials and rubbers.

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

Abstract: Provided by the invention is a chemical-amplification positive-working photoresist composition used in the fine photolithographic patterning in the manufacturing process of semiconductor devices, which is suitable for the patterning light exposure with ArF excimer laser beams of very short wavelength by virtue of absence of aromatic structure in the ingredients of the composition. The composition comprises, as the film-forming resinous ingredient, an acrylic resin having unique monomeric units represented by the general formula &Brketopenst;CH2—CR1(—CO—O—CR2R3R4)&Brketclosest;, in which R1 is a hydrogen atom or a methyl group, R2 and R3 are each, independently from the other, an alkyl group having 1 to 4 carbon atoms and R4 is an alkoxycarbonyl group or a group derived from a molecule of a lactone compound or ketone compound by removing a hydrogen atom bonded to the carbon atom.

Abstract: A process for removing impurities from 3-(2′-acetoxyethyl)-dihydro-2(3H)-furanone (I), which comprises initially preparing the 3-(2′-acetoxyethyl)-dihydro-2(3H)-furanone containing the undesirable impurities in a manner known per se by acetylating 3-(2′-hydroxylethyl)-dihydro-2(3H)-furanone, subsequently treating it with strong mineral acids and finally removing the decomposition products of the undesirable impurities from I.

Abstract: The present invention relates to derivatives of the formula the process for their preparation, and to their uses in therapeutics, especially as drugs with anti-inflammatory, analgesic and chemopreventive properties.

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: The invention encompasses compounds of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I ##STR1## e.g. (5R)-3-(3,4-difluorophenyl)-5-ethyl-5-methyl-4-[4-(methylsulfonyl)phenyl]- 2,5-dihydro-2-furanone.

Abstract: The invention provides substituted furanone antiarthritic and analgesic pharmaceutical agents defined by Formula I, ##STR1## wherein: R.sup.1 is selected from the group consisting of(a) S(O).sub.2 CH.sub.3,(b) S(O).sub.2 NH.sub.2,(c) S(O).sub.2 NHC(O)CF.sub.3,(d) S(O)(NH)CH.sub.3,(e) S(O)(NH)NH.sub.2,(f) S(O)(NH)NHC(O)CF.sub.3,(g) P(O)(CH.sub.3)OH, and(h) P(O)(CH.sub.3)NH.sub.2 ;R.sup.2 and R.sup.3 independently are selected from(1) hydrogen,(2) halo,(3) C.sub.1 -C.sub.6 alkyl,(4) C.sub.1 -C.sub.6 alkoxy, and(5) C.sub.1 -C.sub.6 alkylthio;n is an integer from 1 to 3;m is an integor from 1 to 3;or a pharmaceutically acceptable salt thereof.

Abstract: There are described N-aminopyridone derivatives of the formula I: ##STR1## where the substituents R.sup.1 to R.sup.12 have the meanings given in claim 1, a process for their preparation, and their use for controlling undesirable vegetation.

Abstract: Described are racemic and enantiomerically pure chiral phenyldihydrofuranones, their preparation and their use in drugs (selective inhibition of the cAMP-specific phosphodiesterase IV).

Abstract: Novel nonpeptide antagonists of endothelin (I) are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prostatic hyperplasia (BPH), and diabetes.

Abstract: A vitamin D.sub.3 derivative represented by the following formula: wherein, R is, independently, a hydrogen atom, tri(C.sub.1 to C.sub.7 hydrocarbon)silyl group, C.sub.2 to C.sub.8 acyl group, or group forming an acetal bond together with an oxygen atom of a hydroxyl group, A is ##STR1## where, R.sup.1 is a methyl group or methylene group, and when R.sup.1 is a methylene group, the bond between the R.sup.1 and the 3-position of the lactone ring is a double bond, R.sup.2 is a hydrogen atom or C.sub.1 to C.sub.3 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together indicate a substitutable single methylene group.

Abstract: The present invention provides a catalyst which exhibits a high catalytic activity and allows asymmetric reaction in a high asymmetric yield to obtain a reaction product having a high optical purity. The present invention also provides a process for the preparation of an optically active 4-methyl-2-oxetanone having a high optical purity useful as starting material of polymer in a high yield in a short period in the presence of the foregoing catalyst. A novel ruthenium-iodo-optically active phosphine complex is provided, represented by the following general formula (1):Ru--I.sub.2 --(R.sup.1 -BINAP) (1)wherein R.sup.1 -BINAP represents an optically active tertiary phosphine represented by the following general formula (2): ##STR1## wherein R.sup.1 represents an aryl group which may have a substituent selected from the group consisting of a C.sub.1-4 lower alkyl group, a C.sub.1-4 lower alkoxy group, a C.sub.1-4 lower alkylamino group, and a halogen atom or a C.sub.3-8 cycloalkyl group.

Abstract: A compound of formula I, ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' are independently the same or different and each represent hydrogen, hydroxy, or lower alkoxy, or any vicinal two of R.sub.1, R.sub.2, R.sub.3, R.sub.1 ', R.sub.2 ', and R.sub.3 ' combined together represent --O--(CH.sub.2).sub.n --O--, wherein n=1 or 2; R.sub.4 represents methylene or halomethyl; and X.sub.1, X.sub.2, X.sub.3, and X.sub.4 are independently the same or different and each represent hydrogen or halogen; or a pharmaceutically acceptable salt thereof. Also disclosed are a pharmaceutical composition that contains an effective amount of a compound of formula I together with a pharmaceutically acceptable excipient, and a method of treating cancer that involves the administration of an effective amount of the compound of formula I to a patient in need thereof.

Abstract: A process for the preparation of butyrolactones of the formula I ##STR1## where the substituents R.sup.1 and R.sup.2 are hydrogen, alkyl or hydroxyalkyl groups, or aryl and trialkylsilyl groups, if appropriate carrying inert: substituents, is described in which an alkyne of the formula IIR.sup.1 --C.tbd.C--R.sup.2 IIwhere the substituents have the meanings indicated above, is reacted under reducing conditions at elevated pressure and elevated temperature with carbon monoxide CO and hydrogen in the presence of a transition metal catalyst or with carbon monoxide and water in the presence of a transition metal catalyst.

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: Conformationally constrained diacylglycerol analogues, pharmaceutical compositions comprising such analogues, and methods of using such analogues as agonists and antagonists of protein kinase C.

Abstract: An optically active compound represented by the formula R.sub.1 --A.sub.1 --A.sub.2 --X.sub.1 --A.sub.3 --(CH.sub.2).sub.p --L--A.sub.4 --R.sub.2, in which R.sub.1 is F, CN or straight chain, branched or cyclic alkyl and R.sub.2 is H, F, CH or straight chain or branched alkyl; A.sub.3 is 1,4-phenylene, pyridine-2,5-diyl, pyrimidine-2,5-diyl, pyrazine-2,5-diyl, pyridazine-3,6-diyl, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, 1,3-ditiane-2,5-diyl, thiophene-2,5-diyl, thiazole-2,5-diyl, thiaziazole-2,5-diyl, benzoxazole-2,5-diyl, benzoxazole-2,6-diyl, benzothiazole-2,5-diyl, benzothiazole-2,6-diyl, benzofuran-2,5-diyl, benzofuran-2,6-diyl, quinoxaline-2,6-diyl, quinoline-2,6-diyl, 2,6-naphthylene, indane-2,5-diyl, 2-alkylindane-2,5-diyl, indanone-2,6-diyl, 2-alkylindane-2,6-diyl, coumarane-2,5-diyl and 2-alkylcoumarane-2,5-diyl; A.sub.1, A.sub.2 and A.sub.4 are single bond or A.sub.3 ; X.sub.1 ' is a single bond, --COO--, --OCO--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.tbd.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of inflammation and other cyclooxygenase-2 mediated diseases.

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

Abstract: Preparation of 4-hydroxy substituted butyrolactones is described. A process for the preparation of 3-hydroxybutyrolactone, 1,2,4-trihydroxybutane and 3,4-dihydroxy acid methyl ester from malic acid is particularly described. The preparation of 4-hydroxymethyl-4-hydroxybutyric acid -1-methyl ester and 4-hydroxymethyl butyrolactone is particularly described. The compounds are intermediates to various pharmaceutical and agricultural products.

Abstract: Seco-D steroid derivatives having the formula ##STR1## wherein R, R.sup.1, R.sup.2 and R.sup.3 have the meanings specified in the specification, useful as cardiovascular agents and pharmaceutical compositions containing same, are disclosed.

Abstract: A vitamin D.sub.3 derivative represented by the following formula: ##STR1## wherein, R is, independently, a hydrogen atom, tri(C.sub.1 to C.sub.7 hydrocarbon)silyl group, C.sub.2 to C.sub.8 acyl group, or group forming an acetal bond together with an oxygen atom of a hydroxyl group, A is ##STR2## where, R.sup.1 is a methyl group or methylene group, and when R.sup.1 is a methylene group, the bond between the R.sup.1 and the 3-position of the lactone ring is a double bond, R.sup.2 is a hydrogen atom or C.sub.1 to C.sub.3 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together indicate a substitutable single methylene group.

Abstract: Novel acetogenins isolated from Asimina triloba and Goniothalamus giganteus of the family Annonaceae and derivatives of those and other acetogenins are described. Bioactive cyclic formaldehyde acetal derivatives are prepared from Annonaceous acetogenins having 1,2-, 1,4- or 1,5-diols. A non-adjacent bis-tetrahydrofuran (THF) acetogenin is prepared from an unsaturated mono-THF acetogenin earlier isolated from Goniothalamus giganteus. The substantially pure acetogenins and acetogenin derivatives of the invention exhibit cytotoxicity to human solid tumor cell lines equipotent to adriamycin or orders of magnitude more potent than adriamycin, and they exhibit effective pesticidal activities.

Abstract: Described is a process for preparing cyclopentadecanolide defined according to the structure: ##STR1## using as a starting material the dicarboxylic acid having the structure: ##STR2## according to the reaction sequence: ##STR3## Also described is a process for using the resultant cyclopentadecanolide for augmenting, enhancing or imparting aromas in or to perfume compositions, colognes and perfumed articles including but not limited to solid or liquid anionic, cationic, nonionic or zwitterionic detergents, perfumed polymers, fabric softener compositions, fabric softener articles, cosmetic powders and hair preparations.

Abstract: The present invention relates to a process for producing lactones starting from cyclic ketones which comprises an oxidation reaction which is performed in the presence of an optionally substituted cycloaliphatic peracid or of an optionally substituted aliphatic peracid that is immiscible with water. The process allows to obtain high selectivity, does not entail the use of dangerous reagents, and allows excellent economic advantages.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is free or esterified carboxy, hydroxymethyl or formyl,R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radicals andR.sub.3 is azido, or amino that is aliphatically or araliphatically substituted and/or protected by an amino-protecting group,and the salts thereof, are valuable intermediates in the preparation of medicinal active ingredients, for example of compounds of formula II ##STR2## wherein R.sub.A is an aromatic or heteroaromatic radical,R.sub.2 and R.sub.4 are each independently of the other aliphatic, cycloaliphatic, cycloaliphaticaliphatic or araliphatic radicals,R.sub.3 is unsubstituted or N-mono- or N,N-di-lower alkylated or N-lower alkanoylated amino, andR.sub.B is an aliphatically, cycloaliphatically or heteroaromatically-aliphatically substituted amino group,and the salts thereof, which can be used, for example, as antihypertensives.

Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.

Abstract: Novel acetogenins isolated from Asimina triloba and Goniothalamus giganteus of the family Annonaceae and derivatives of those and other acetogenins are described. Bioactive cyclic formaldehyde acetal derivatives are prepared from Annonaceous acetogenins having 1,2-, 1,4- or 1,5-diols. A non-adjacent bis-tetrahydrofuran(THF) acetogenin is prepared from an unsaturated mono-THF acetogenin earlier isolated from Goniothalamus giganteus. The substantially pure acetogenins and acetogenin derivatives of the invention exhibit cytotoxicity to human solid tumor cell lines equipotent to adriamycin or orders of magnitude more potent than adriamycin, and they exhibit effective pesticidal activities.

Abstract: 5-Oxaspiro[2.4]heptan-6-one: ##STR1## is obtained from [3-(hydroxymethyl)oxetan-3-yl]acetonitrile by reaction with hydrogen bromide and then cyclizing the intermediate product 4,4-bis(bromomethyl)dihydro-2-furanone with zinc. 5-Oxaspiro[2.4]heptan-6-one is an intermediate product for the production of leukotriene antagonists.

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: A process for the preparation of 3-(2'-acyloxyethyl)-dihydro-2(3H)furanones of the general formula I ##STR1## in which R.sup.1 denotes C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.12 aralkyl, or C.sub.7 -C.sub.12 alkylaryl, in which a 3-(2'-oxyethyl)-dihydro-2(3H)furanone of the general formula II ##STR2## in which R.sup.2 denotes C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.12 aralkyl, or C.sub.7 -C.sub.12 alkylaryl is caused to react with a carboxylic acid, a carboxylic anhydride, and/or an acyl halide in the presence of an acid catalyst at temperatures of from 50.degree. to 250.degree. C. and pressures of from 0.1 to 100 bar.

Abstract: A process for preparing 5-membered ring heterocycles of the general formula I ##STR1## where R.sup.1 is methyl or hydroxyethyl,R.sup.2,R.sup.3,R.sup.4,R.sup.5 and R.sup.6 are hydrogen, C.sub.1 - to C.sub.12 -alkyl, C.sub.2 - to C.sub.12 -alkenyl, aryl, C.sub.3 - to C.sub.8 -cycloalkyl, C.sub.1 - to C.sub.12 -alkoxy, halogen, C.sub.2 - to C.sub.20 -alkoxycarbonylalkyl, C.sub.2 - to C.sub.20 -alkylcarbonyloxy, formyl, C.sub.2 - to C.sub.20 -formylalkyl, benzoyl or --CH(OR.sup.3)(OR.sup.5), or R.sup.3 and R.sup.5 together are a C.sub.2 - to C.sub.7 -alkylene chain which is unsubstituted or monosubstituted to pentasubstituted by R.sup.4 or a .dbd.CH--CH.dbd.CH--CH.dbd. unit which is unsubstituted or monosubstituted to tetrasubstituted by R.sup.4,X is oxygen or N--R.sup.4by reacting 5-membered ring heterocycles of the general formula II ##STR2## where R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and X have the abovementioned meanings and Y is hydrogen, acetyl or C.sub.2 - to C.sub.

Abstract: Novel anti-inflammatory furanone compounds have the following formula: ##STR1## where R.sub.1 independently is H, or alkyl of 1 to 9 carbons and n is an integer having the values of 1 or 2, and where when n is 1 the R.sub.1 group is attached to the 5 position of the 2-furanone, when n is 2 then R.sub.1 is attached to both the 3 and 5 positions, with the proviso that when n is 1 then R.sub.1 is not H; Y.sub.1 is H, alkyl of 1 to 20 carbons, phenyl C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkenyl containing one or more olefinic bonds, where R.sub.3 is H, C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkenyl containing one or more olefinic bonds, phenyl, halogen substituted phenyl or C.sub.1 -C.sub.6 alkyl substituted phenyl, with the proviso that when Y.sub.1 is CO--OR.sub.3 or CONHR.sub.3 then R.sub.3 is not hydrogen; Y.sub.2 is H, an alkyl group of 1 to 25 carbons, or phenyl.

Abstract: All possible stereoisomeric forms and mixtures thereof of a compound of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, alkyl, alkenyl and alkynyl of up to 4 carbon atoms, --CN and aralkynyl of up to 10 carbon atoms, Y is selected from the group consisting of halogen, --CH.sub.2 F, --CHF.sub.2, and --CF.sub.3, A is selected from the group consisting of ##STR2## having pesticidal properties.

Abstract: A convenient stereoselective process for the preparation of .alpha.-alkylidene-substituted-.gamma.-butyrolactones and .delta.-valerolactones is provided. The process involves reacting an .alpha.-acyl lactone, an aldehyde, and an alkali metal hydroxide in an inert diluent at an elevated temperature while removing water.

Abstract: The present invention provides sulphonamides of the general formula: ##STR1## wherein R.sup.1 and R.sup.2, which can be the same or different, are hydrogen or halogen atoms or C.sub.1 -C.sub.6 -alkyl, trifluoro-methyl, cyano, carboxyl, alkoxycarbonyl, aminocarbonyl, N-alkylaminocarbonyl or N,N-dialkylaminocarbonyl radicals or, when R.sup.1 and R.sup.2 are alkyl radicals ortho to one another, R.sup.1 and R.sup.2 together with the carbon atoms to which they are attached, form a saturated or unsaturated C.sub.5-C.sub.7 -alkylene ring, R.sup.3 is a hydrogen atom, an alkyl radical containing up to 6 carbon atoms, an acyl radical, a phenylalkyl or phenylalkenyl radical, the phenyl moiety of which can be substituted by halogen, alkyl or trifluoromethyl, C is a --(CH.sub.2).sub.m --radical, in which m is 0, 1, 2 or 3, or a branched C.sub.2 -C.sub.5 -alkylene radical, whereby a methylene radical --CH.sub.

Abstract: Liquid crystalline compounds having an optically active .gamma.-lactone ring of the general formula (A): ##STR1## wherein R.sup.1 is a group selected from the class consisting of ##STR2## n and e are each independently 0 or 1, R.sup.3 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 15 carbon atoms, said alkyl and alkenyl groups having each optionally one or more asymmetric carbon atoms, X and Y are each hydrogen atom, a halogen atom or a cyano group, R.sup.2 is an alkyl group having 1 to 15 carbon atoms or an alkenyl group having 2 to 15 carbon atoms, said alkyl and alkenyl groups having each optionally one or more asymmetric carbon atoms, and * means an asymmetric carbon atom, a liquid crystal composition containing the same and an element for opto-electronics devices comprising the liquid crystal composition.

Abstract: A process for preparing 3-(2'-oxyethyl)dihydro-2(3H)furanones of the general formula I ##STR1## where R.sup.1 is hydrogen or acetyl, by reacting ethylene oxide with acetoacetic acid esters of the general formula II ##STR2## where R.sup.2 is C.sub.1 -C.sub.4 -alkyl, which comprises carrying out the reaction in alcoholic solutions in the presence of alkali metal alkoxides at from 20.degree. to 100.degree. C. and from 1 to 20 bar, is described.

Abstract: A process is disclosed for the preparation of a compound of the Formula (VI) ##STR1## wherein X is a hydrogen atom, or OH,Y is a hydrogen atom, OH or a methyl group,R.sup.2 is a CH--COOR group, or a group of the formula (XI) ##STR2## and R is a C.sub.1 to C.sub.2 alkyl group, which comprises the step of: reacting a condensed salt of the Formula (IV) ##STR3## wherein Me is Na.sup.+ or K.sup.+, with a reactive derivative of trifluoromethane-sulfonic acid of the Formula (V)F.sub.3 C--SO.sub.2 OH.The compounds of the Formula (VI) are intermediates in the preparation of penicillins and cephalosporins with antibiotic activity.

Abstract: Optically active lactones are described, such as an intermediate lactone having the formula ##STR1## where R and R.sup.2 are each independently alkyl with 1 to 6 carbon atoms, cycloalkyl with 6 to 10 carbon atoms, aryl with 6 to 10 carbon atoms, or arylalkyl with 7 to 19 carbon atoms, R.sup.4 is H or C.sub.1-6 alkyl, and Ar is a homo- or heteroaromatic ring with 5 or 6 ring atoms being optionally substituted by C.sub.1-6 alkyl or alkoxy groups, halogen atoms, cyano or nitro groups. Such optically active, intermediate lactones are prepared from L-aspartic acid, and can be readily converted to (+)-pilocarpine and its analogues by hydrolysis, reduction, and hydrogenation, such as to an optically active lactone having the formula ##STR2## which is (+)-pilocarpine when R is ethyl, R.sup.4 is H, and Ar is 1-methylimidazol-5-yl.

Abstract: Heterocyclic-alkylene quinoxalinyloxyphenoxypropanoate compounds exhibit unexpectedly desirable selective herbicidal activity. Also disclosed are compositions comprising such compounds as well as a method of controlling the growth of undesirable plants employing such compounds.

Abstract: Liquid crystalline compounds having an optionally active .gamma.-lactone ring of the formula: ##STR1## wherein R.sup.1 is a group selected from the group consisting of ##STR2## n and e are each independently 0 or 1; R.sup.3 is an alkyl group having 1 to 15 carbon atoms; R.sup.2 is a group of the formula: --(CO).sub.m --R.sup.4 ; m is 0 or 1; R.sup.4 is hydrogen atom or an alkyl having 1 to 15 carbon atoms; and the symbol * is an asymmetric carbon atom, and an intermediate thereof, and process for the production of the same.

Abstract: The invention provides a process for preparing 1,5-diaryl pyrazole anti-inflammatory agents. A 6-aryl-4,6-dioxohexanoic acid is treated with acetic anhydride or acetyl chloride to produce an enol lactone, which is added to methylhydroxylamine to generate the dione hydroxamic acid. This dione hydroxamic acid is then treated with 4-methoxyphenylhydrazine hydrochloride to yield the 1,5-diaryl pyrazole. Novel intermediate compounds in the synthetic pathway are also disclosed.

Abstract: The invention provides a novel process for the manufacture of enantiomerically-pure halolactones of the formula I which are useful for the production of certain 5-amino-4-hydroxyvaleric acid derivatives, themselves valuable intermediates in the production of compounds which are renin inhibitors. The process involves a diastereoselective alkylation of an oxazolidinone of the formula III, followed by a highly stereoselective and novel halolactonisation of an oxazolidinone of the formula II. Certain of the oxazolidinones of the formula II are novel and are provided as a further feature of the invention. The invention also provides a novel process for the production of the pharmaceutically-useful 5-amino-4-hydroxyvaleric acid derivatives of formula VI.

Abstract: Screening of crude extracts of the bark of Annona bullata Rich. (Annonaceae) showed cytotoxic and pesticidal activities. By monitoring with brine shrimp lethality, two novel extremely potent acetogenins, bullatacin (1) and bullatacinone (2), were isolated. Spectral and chemical methods identified bullatacin as a diastereomer of asimicin. Bullatacinone represents bullatacin with the lactone cleaved and reformed at the 4-OH. Unlike asimicin, which is more generally cytotoxic, 1 and 2 show some selective cytotoxicities in human tumor cell lines, and certain susceptible cells give ED.sub.50 values as low as 10.sup.-12 -10.sup.-15 mcg/ml. Bullatacin was pesticidal at concentration as low as 1 ppm, while bullatacinone lacked pesticidal activities.

Abstract: The present invention provides a process for preparing dihydrofuranone derivative of the formula (I): ##STR1## wherein R.sup.1 and R.sup.3 are individually lower alkyl, and R.sup.2 is hydrogen or lower alkyl, by reacting a dihydrofuranone derivative of the formula(I): ##STR2## wherein R.sup.1 is as defined above, with a malonic acid derivative of the formula (II): ##STR3## wherein R.sup.2 and R.sup.3 are as defined above, in the presence of an alkalimetal alkoxide and/or an alkalimetal hydroxide.

Abstract: Variously substituted 4-(biphen-2-ylmethylcarbamoyl)-3-hydroxybutyric acids and esters, also named as N-(biphen-2-yl)-3-hydroxyglutaramic acid derivatives, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.