Abstract: A process for the preparation of compounds of formula (I) wherein R is a C1 to C12 alkyl group and R1 is a protecting group or H which process comprises (a) converting the diol lactone of formula (II) to the protected diol lactone of formula (IIa) wherein R1 is a protecting group (b) acylating the protected diol lactone (IIa) to give compound (I) wherein R1 is a protecting group, (c) optionally removing the protecting group R1 to give compound (I) wherein R1 is H; and wherein steps (a) and/or (b) are carried out in the presence of N-methylimidazole.

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

Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: The present invention is a process for the preparation of a compound of the formula: where R3, R4 and n are defined in the specification which comprises hydrogenating a compound of the formula: the E-geometrical isomer thereof or a mixture of the Z- and E-isomers in the presence of catalyst containing Rh, a chiral ligand with at least one phosphorous atom where the hydrogenation is conducted in the presence of a base.

Abstract: A compound selected from the group consisting of a 5,6-dihydro-&agr;-pyrone of formula (I): wherein bond a is oriented either or ; X is O or NH; R1 is selected from the group consisting of: a group R3(O)C— wherein R3 is selected from the group consisting of: (i) a group of formula R4—CH═CH— wherein R4 is C1-C20 alkyl, C2-C20 alkenyl, an aryl group, or a 5- or 6-membered unsaturated heterocyclic ring containing one or two O, N or S atoms, (ii) C2-C20 alkyl; and (iii) an aryl group or a substituent which is a fused ring system of formula (1) or (2):  wherein each of R′ and R″, which are the same or different and may occupy any position on ring a or ring b of said fused ring system, is H or C1-C6 alkyl; a group ArCH2— wherein Ar is an aryl group; and a group R5O—CH2— wherein R5 is C1-C6 alkyl optionally interrupted by one or two O atoms; and R2 is CH3 or, when R1 is a group of formula (A) as defined below, R2 i

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: The present invention relates to cyclic ketones represented by the following formula and to drugs in which an effective component is such a cyclic ketone or a pharmacologically acceptable salt thereof. The cyclic ketones of the present invention encourage the production of blood platelets, leukocytes and erythrocytes, and can be employed in the prevention or treatment of cytopaenia brought about by cancer chemotherapy, radiotherapy or drug therapy, or by immunological abnormality, anaemia and the like.

Abstract: A method for treating or preventing type II diabetes mellitus comprising administering an effective amount of a gastrointestinal lipase inhibitor, such as, tetrahydrolipstatin.

Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.

Abstract: Novel analogs of compounds from the marine sponge Discodermia dissoluta have been prepared. These compounds have been shown to have activity against mammalian cancer cells, and can be used in treating human patients which host cancer cells, including leukemia, melanoma, breast, colon, CNS, renal, ovarian, prostate, and lung tumors.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: Compositions comprising hydroxy-substituted monolactones, a process for reacting olefinic compounds with certain carboxylic reactants and products prepared by the process. The compositions containing the hydroxy-substituted lactones and the products of the process are useful as intermediates for the preparation of additives for lubricants and fuels.

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) ##STR1## in which Het represents one of the groups ##STR2## in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.

Abstract: This invention provides processes for preparing lactone intermediates useful for the preparation of pharmaceutical compounds such as tetrahydrolipstatin and cryptophycin compounds.

Abstract: A process for the production of simvastatin and its analogues that is efficient, economical and convenient involves the use of hydroxyl protected intermediates of formula (III) or (VII). These intermediates allow for direct alkylation of the butyrate side chain followed by deprotection and reformation of the lactone ring. R.sup.1 is hydrogen or methyl; R.sup.2 represents a straight or branched chain alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, or an aralkyl group having 1 to 6 carbon atoms in the alkyl chain; R.sup.3 and R.sup.4 each independently represent an alkyl group, an ether group, a thioether group, an aryl group, an aralkyl group, an alkenyl group, a cyclic ether group, or a cyclic thioether group; and R.sup.5 and R.sup.6 each independently represent hydrogen, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, or an ether group.

Abstract: Synthetic methods for lactone-containing compounds such as the discodermolides are provided, as are compounds which mimic the chemical and/or biological activity thereof, and methods and intermediates useful in their preparation.

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

Abstract: Disclosed is a novel process and novel intermediates to prepare [R-(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propy l-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide (XIX) ##STR1## which is a protease inhibitor useful in treating humans infected with the HIV virus.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: Compositions comprising hydroxy-substituted monolactones, a process for reacting olefinic compounds with certain carboxylic reactants and products prepared by the process. The compositions containing the hydroxy-substituted lactones and the products of the process are useful as intermediates for the preparation of additives for lubricants and fuels.

Abstract: An acylation process using a sulfonic acid, a salt of the sulfonic acid, or a mixture thereof, as a catalyst. Compound 6 is prepared by protecting the 4-hydroxyl group on the pyranone ring of the 8'-hydroxy compound 2 to form a .beta.-protected compound 3, acylating the 8-hydroxy group on the polyhydronaphthyl ring of compound 3 to give protected ester, compound 4, then removing the protecting group, where the compounds 6, 2, 3 and 4 are as described in the specification.

Abstract: The process for preparing compound 2 by reacting the compound 1, each as described in the specification hereof, with a tetraalkyl ammonium hydroxide having the formula R.sub.1 R.sub.2 R.sub.3 R.sub.4 N.sup.+ OH.sup.-, wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently a C.sub.1 -C.sub.10 alkyl group or a (C.sub.6 -C.sub.10) aryl (C.sub.1 -C.sub.10) alkyl group, to obtain an triol carboxylate thereof, acidifying the triol carboxylate, then lactonizing the product to obtain diol lactone, a key intermediate for production of antihypercholesterolemia agents.

Abstract: The invention provides a simple and selective method for the deacylation of 4-acylated statins during the preparation of statins from a fermentation broth, more specifically a reduction of impurities from the process, by increasing the pH of the fermentation broth.

Abstract: The present invention provides convergent processes for preparing myxopyronins and corallopyronins, compounds useful as antibacterial therapeutics. The present invention also provides novel compositions of matter which are useful for the preparation of pyronin antibiotics.

Abstract: The invention relates to novel 3-aryl-5-halogeno-pyrone derivatives of the formula (I) ##STR1## in which A, D, G, X, Y, Z and n are each as defined in the description,to a plurality of processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: Heterocyclic compounds IR.sup.1 --X--L (I)whereL is a cyclic carbamate residue, a lactonoxy residue or a lactam residue,X is an oxygen-containing group ##STR1## where A is a linker, and R.sup.1 is an organic radical or a group L,are used as activators for inorganic peroxy compounds, in particular as cold bleach activators or optical brighteners in detergents, cleaners and bleaches and in disinfectants.

Abstract: A novel process of lactonizaton in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises dissolving the open ring hydroxy acid form of the statins in an organic solvent by heating at a temperature, which ranges from ambient to reflux of the solvent, under anhydrous conditions to produce a solution, treating the solution with a mild catalyst at a temperature from about ambient to 50.degree. C., and adding water to the solution to cause the statins in lactone form to crystalize from the reaction mixture. The mild catalyst used in the reaction is a salt of an organic base with an organic or inorganic acid, such as pyridine hydrobromide, pyridine hydrochloride, or pyridinium, p-toluene sulfonate. The organic solvent comprises a lower alkanol, a non-alcoholic polar solvent, or a mixture of the two.

Abstract: An improved process of lactonization in the preparation of statins (e.g., the HMG--CoA reductase inhibitors lovastatin and simvastatin) employs very mild reaction conditions. The improved process comprises treating the open ring hydroxy acid form of the statins with an excess of acetic acid and in the absence of a strong acid catalyst under mild heating conditions (e.g., ambient to 55.degree. C.), and adding an anti-solvent to the reaction mixture, thereby causing the statins in lactone form to crystalize from the reaction mixture. The acetic acid serves as both a solvent and a catalyst for the lactonization reaction.

Abstract: The present invention relates to compounds of formulae (I) and (II) which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl?b!pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R.sub.10 and R.sub.20 taken together are formulae (III) and (IV).

Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.

Abstract: Novel lactone compounds from the marine sponge Discodermia dissoluta have been isolated. These compounds and their analogs have been shown to have activity against mammalian cancer cells, and can be used in treating human patients which host cancer cells, including leukemia, melanoma, and breast, colon, CNS, and lung tumors.

Abstract: This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions.The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 represents a group of formula (II) or (III): ##STR2## R.sup.2 is alkyl, alkenyl or alkynyl; R.sup.3 and R.sup.4 are each hydrogen, alkyl, alkenyl or alkynyl; R.sup.5 is hydrogen or a carboxy-protecting group; R.sup.a is a group of formula --OR.sup.6 ; R.sup.6 is hydrogen; R.sup.6a and R.sup.6b are each hydrogen, a hydroxy-protecting group, alkyl, alkanesulfonyl, halogenated alkanesulfonyl or arysulfonyl, and their salts and esters. Such compounds inhibit the synthesis of cholesterol, and can be used for the treatment and prophylaxis of hypercholesterolemia and of various cardiac disorders.

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

Abstract: The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.

Abstract: A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.

Abstract: The invention concerns new bishipidine derivatives, processes for their production and pharmaceutical agents containing these compounds. The new methylene-bishispidine derivatives can be used for the prophylaxis and therapy of late diabetic damage as well as for the prophylaxis and therapy of atherosclerosis and arteriosclerosis.

Abstract: Cysteine protease inhibitors which deactivate the protease by covalently bonding to the cysteine protease and releasing the enolate of a 1,3-dicarbonyl (or its enolic form). The cysteine protease inhibitors of the present invention accordingly comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a .beta.-dicarbonyl enol ether leaving group.

Abstract: Novel lactone compounds from the marine sponge Discodermia dissoluta have been isolated. These compounds and their analogs have been shown to have activity against mammalian cancer cells, and can be used in treating human patients which host cancer cells, including leukemia, melanoma, and breast, colon, CNS, and lung tumors.

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: A process for the separation of at least one isomer from a mixture of isomers of a tetrahydropyran-2-one, having at least two chiral centres which comprises selective reaction of at least one isomer with a reagent catalysed by a hydrolase enzyme whereby at least one isomer is preferentially converted into a distinct chemical species from the other isomers so that it is susceptible of separation by an appropriate chemical or physical separation process in which the tetrahydropyran-2-one is of Formula (1): ##STR1## wherein: Z is --H or a protecting group susceptible of reaction with the reagent under the influence of the enzyme; andY is formyl or protected formyl.

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: A process is described for the removal of a silyl protecting group from the 4-hydroxy group of a tetrahydro-pyran-2-one moiety.

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

Abstract: Enzymatic hydrolysis and esterification processes for the preparation of compounds useful as HMG-CoA reductase inhibitors and/or as intermediates in the preparation of HMG-CoA reductase inhibitors.

Abstract: A lactone compound, useful as an osteogenetic accelerator, having the formula (I): ##STR1## wherein n is zero or 1 and m is zero or 1, provided that both n and m are not zero at the same time, or a stereoisomer thereof at the 23- and/or 25-positions or any mixture thereof and a production process thereof.

Abstract: A 4-fluorobiphenyl derivative of formula (I), which is useful as a cholesterol lowering agent or a lipid lowering agent because of its strong inhibitory effect on HMG-CoA reductase), and which is also useful as an intermediate for producing the above-mentioned cholesterol lowering agent or lipid lowering agent: ##STR1## wherein A is a .omega.-oxycarbonyldihydroxybutyl group, a tetrahydropyranyl group, a .omega.-oxycarbonyl-3-oxobutyl group, a formyl group, or a cyano group; R.sup.1 is a halogen atom, an alkyl group, or a group represented by R.sup.5 O--, wherein R.sup.5 is a hydrogen atom, or an alkyl group; R.sup.2 is a hydrogen atom, an alkyl group; R.sup.3 is a hydrogen atom, or an alkyl group; R.sup.5 and R.sup.2 may form a five-membered ring or a six-membered ring in combination with the oxygen atoms to which R.sup.5 and R.sup.2 are respectively bonded, and R.sup.5 and R.sup.3 may form a five-membered ring or a six-membered ring in combination with the oxygen atom to which R.sup.5 is bonded.

Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##

Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formula (II): ##STR1##