Abstract: The present invention relates to novel dihydropyrones of Formula I wherein X is NH or NR8, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.

Abstract: The present invention relates to a processing method for preparing lovastatin and simvastatin which comprises the steps of (1) performing lactonization of mevinic acid and its homologous compounds in the presence of a mixed organic solvent without an acid catalyst through nitrogen sweep; and (2) making crystals. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced remarkably. Therefore, the processing method of the present invention can be convenient and economical.

Abstract: The present invention relates to novel phenyl-substituted 5,6-dihydro-pyrone derivatives of the formula (I) in which W, X, Y, Z, G, A, B, Q1 and Q2 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.

Abstract: Compounds which mimic the chemical and/or biological activity of discodermolide are provided and intermediates useful in their preparation.

Abstract: Compounds or their salts having general formulas (I) and (II): wherein s is an integer equal to 1 or 2, A is the radical of a drug that satisfies certain pharmacological tests, C and C1 are bivalent radicals, and precursors of the radicals B and B1 satisfy certain pharmacological tests.

Abstract: The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

Abstract: Disclosed are compounds useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.

Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis.

Abstract: The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid.

Abstract: There is disclosed, a process for lactonization to produce highly pure simvastatin of Formula I which comprises lactonization of a compound of Formula II where Z is H or NH4 in a mixture of acetonitrile and glacial acetic acid under anhydrous conditions at a temperature of 65-70° C.

Abstract: A process for the isolation and purification of HMG-CoA reductase inhibitors from a mycelium biomass is described, which process comprises: clarifying a mycelium broth and concentrating the clarified broth to a lower volume, acidifying of the concentrate to a pH value in the range of 4.5 to 7.5, followed by extracting the HMG-CoA reductase inhibitor with ethyl acetate, crystallization of the HMG-CoA reductase inhibitor from a water-miscible or water-soluble organic solvent, and crystallization of the HMG-CoA reductase inhibitor from an organic solvent having limited miscibility or solubility with water. The crystallization steps may also be reverse. The concept of a combination of the specified crystallization steps can also be used for the purification of a crude HMG-CoA reductase inhibitor.

Abstract: In a process for preparing mevinolin by fermentation of a biomass in a fermentation liquor, which includes dissolving mevinolin from the biomass into the fermentation liquor, and separating the biomass from the fermentation liquor to obtain a separated fermentation liquor, separating the mevinolin from the separated fermentation liquor, and recovering the end product, the improvement which comprises carrying out the dissolving at a pH between 7.5 and about 10, and the separating of the mevinolin is carried out at a pH between about 4.5 and about 1.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: There is disclosed a process for the manufacture of simvastatin of Formula I which comprises heating a compound, namely acid or ammonium salt of compound of Formula II, where Z is H or NH4 in an organic solvent at a temperature of 130-140° C.

Abstract: Processes for preparing a calcium salt of a statin from an ester derivative or protected ester derivative of the statin by using calcium hydroxide are provided. The ester or protected ester derivative is contacted with calcium hydroxide to obtain the calcium salt. Preferred statins are rosuvastatin, pitavastatin and atorvastatin, simvastatin and lovastatin. In processes beginning with a protected statin ester derivative, the protecting group is hydrolyzed during salt formation by contact with calcium hydroxide, or is contacted with an acid catalyst followed by contact with calcium hydroxide.

Abstract: Processes for preparing a calcium salt of a statin from an ester derivative or protected ester derivative of the statin by using calcium hydroxide are provided. The ester or protected ester derivative is contacted with calcium hydroxide to obtain the calcium salt. Preferred statins are rosuvastatin, pitavastatin and atorvastatin, simvastatin and lovastatin. In processes beginning with a protected statin ester derivative, the protecting group is hydrolyzed during salt formation by contact with calcium hydroxide, or is contacted with an acid catalyst followed by contact with calcium hydroxide.

Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: using an acyl halide of the formula: wherein R1, R2 R3 and X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&dgr;-lactone.

Abstract: The present invention relates to novel phenyl-substituted 5,6-dihydro-pyrone derivatives of the formula (I) 1

Abstract: There is disclosed, a process for lactonization to produce highly pure simvastatin of Formula I 1

Abstract: The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid.

Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The present invention relates to novel sulfide and disulfide compounds, compositions comprising sulfide and disulfide compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: The present invention relates to novel ketone compounds, compositions comprising ketone compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising a ketone compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.

Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as and antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergilus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicilium genus, some are obtained by treating the fermentation products using the method of chemical synthesis or they are the products of total chemical synthesis. The purity of the active ingredient is an important factor for manufacturing the safe and effective pharmaceutical, especially if the pharmaceutical product must be taken on a longer term basis in the treatment or prevention of high plasma cholesterol. The accumulation of the impurities from the pharmaceuticals of lower purity may cause many side effects during the medical treatment.

Abstract: A composition comprising pravastatin sodium substantially free of pravastatin lactone is described.

Abstract: A process of the present invention produces a hydroxylactone by subjecting an unsaturated carboxylic acid having a double bond not conjugated to a carboxyl group or an ester thereof to (i) a reaction with hydrogen peroxide in the presence of a metallic compound containing a metallic element selected from W, Mo, V and Mn or (ii) a reaction with a peroxide containing the metallic element to thereby yield a corresponding hydroxylactone having a hydroxyl group combined with one of carbon atoms constituting the double bond and being cyclized at the other carbon atom position. The metallic compound may be one selected from oxides, oxoacids and salts thereof. The unsaturated carboxylic acid includes, for example, &bgr;,&ggr;-unsaturated carboxylic acids, &ggr;,&dgr;-unsaturated carboxylic acids, and &dgr;,&egr;-unsaturated carboxylic acids. The process can produce hydroxylactones in high yields at low cost.

Abstract: There is disclosed a process for the manufacture of simvastatin of Formula I 1

Abstract: This invention relates to preparation of enantio-enriched compounds, and more particularly to enantio-enriched kavalactone compounds and derivatives thereof. The methods provide compounds that are useful as reagents, or building blocks, in the construction of other enantio-enriched compounds.

Abstract: This invention features a 5,6-dihydro-2-pyrone compound of formula (I), wherein R1 is H, OH, or C2˜C5 alkoxyl; and R2 is 2-phenyl ethyl, 2-phenyl ethenyl, 2-heteroaryl ethyl, or 2-heteroaryl ethenyl; in which the phenyl or the heteroaryl is optionally mono-, di-, or tri-substituted with R3, R4, or R5; each of R3, R4, and R5, independently, is Cl, F, Br, I, CN, C1˜C5 alkyl, C1˜C5 alkoxyl, C3˜C5 alkenyloxy, C4˜C6 cycloalkoxyl, C4˜C8 cycloalkyl alkoxyl, C3˜C5 alkoxy alkoxyl, or C1˜C4 alkoxy carbonyl.

Abstract: Compounds of formula (I) and salts thereof: Wherein R1 represents methyl, ethyl, isopropyl or s-butyl; and R2 represents hydrogen or alkyl. R3 represents hydrogen, optionally substituted alkanoyl, optionally substituted alkenoyl, optionally substituted alkynoyl, alkylsulfonyl, or alkoxycarbonyl, or R2 and R3 together with the nitrogen atom to which they are attached form a saturated, optionally substituted 4- to 6-membered heterocyclic ring group. The moiety -a- together with the carbon atom to which it is attached forms a 3- to 6-membered cycloalkyl group. These compounds have anthelmintic, acaricidal and insecticidal activity.

Abstract: The present invention relates to a process for preparing lovastatin and simvastatin which comprises (1) performing step of a lactonization of mevinic acid and analog thereof compounds in the presence of a dehydrating agent and without an acid catalyst under nitrogen sweep; and then (2) making step of crystals at a high temperature. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced in an amount remarkably. Therefore, the process of the present invention is convenient and economical.

Abstract: The present invention relates to novel biphenyl-substituted cyclic ketoenols of the formula (I) in which W represents hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, Z represents hydrogen, halogen, alkyl, alkoxy, halogenoalkyl or halogenoalkoxy, CKE represents one of the groups  in which A, B, D, L, M, Q1, Q2, Q3, Q4, Q5 and Q6 are as defined in the description, to preparation and to their use as pesticides and herbicides.

Abstract: (Meth)acrylic acid is reacted with a fatty acid anhydride and the resultant reaction mixture is neutralized and washed with an aqueous alkaline solution having a pH of 7.5 to 13.5. Thus, high-purity (meth)acrylic anhydride can be industrially advantageously produced while avoiding polymerization. This (meth)acrylic anhydride is reacted with a secondary or tertiary alcohol in the presence of a basic compound which in 25° C. water has an acidity (pKa) of 11 or lower. Thus, a high-purity (meth)acrylic ester can be produced in high yield.

Abstract: Compounds of formula I are hepatitis C virus (HCV) RNA-dependent RNA polymerase (RdRp) inhibitors, and are useful in therapeutic and prophylactic treatment of persons infected with hepatitis C virus.

Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): 1

Abstract: The invention concerns compounds of formula (I) wherein: A represents R1 or (O)R1 where R1 represents an alkyl group comprising 1 to 30 carbon atoms, linear or branched, saturated or unsaturated, capable of being partly or totally substituted by Hal where Hal represents —Cl,—Br, or —F, and of being interrupted by one or several units selected among —O—,—S—,—C(O)—,—NR3C(O)—, —Ph(R4)n— and —CH2—CH2—O)n′—, wherein R3 represents or —CH2)n″—CH where n″=0 to 17; R4 represents, —CH3,—CH2H5,—C3H7 and n=0 to 4 and n′=1, 2, or 3, or R1 represents a cyclanic radical with diterpene or triterpene root; and R2 represents a C1−C11 linear or branched alkyl group.

Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1

Abstract: The present invention related to novel dihydropyrones possessing 3-position nitrogen atom, which inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS.

Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1

Abstract: The present invention relates to a novel process for producing a &dgr;-lactone of the formula: 1

Abstract: The present invention relates to certain substituted polyketides of formula I, 1

Abstract: The present invention provides a novel process for the synthesis of Simvastatin of formula II. The process comprises converting Lovastatin to the corresponding amide intermediate using a secondary amine. The C-8 2-methylbutyrate side chain of the amide intermediate is subsequently methylated by reaction with a suitable base, followed by treatment with a methylating agent. The 2,2-dimethylbutyrate intermediate is further transformed to the final product, Simvastatin, by hydrolysis, followed by lactonization. In another aspect, the present invention provides intermediates of formula IIb and IIc useful for the preparation of Simvastatin: wherein R1 and R2 are as defined herein.

Abstract: The present invention relates to new compounds of the formula (I) 1

Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): wherein R1 represents a hydrogen atom or an alkyl group of 1 to 5 carbons; R2 represents hydrogen, —CO—R5 or —SO2R6; R3 represents hydrogen, an alkyl group of 1 to 5 carbons, etc.; and R4 is a substituent attached to the 4-carbon, 5-carbon, 6-carbon or 7 carbon of the benzofuran ring; and their salts. The compounds are useful as therapeutic agent for hypertriglyceridemia, lipid metabolism enhancers, or prophylactic and/or therapeutic agents for arteriosclerosis.

Abstract: Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis.

Abstract: The present invention relates to a processing method for preparing lovastatin and simvastatin which comprises the steps of (1) performing lactonization of mevinic acid and its homologous compounds in the presence of a mixed organic solvent without an acid catalyst through nitrogen sweep; and (2) making crystals. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced remarkably. Therefore, the processing method of the present invention can be convenient and economical.

Abstract: The invention relates to novel oxymethoxy-3-aryl-pyrone derivatives of the formula (I) in which A, D, R1, R2, X, Y, Z and n have the meanings specified in the description, a process for their preparation and their use as pesticides, fungicides and herbicides.

Abstract: The present invention relates to a process for producing Simvastatin comprising acylating 6(R)-[2-(8′(S)-hydroxy-2′(S), 6′(R)-dimethyl-1′, 2′, 6′, 7′, 8′, 8′a(R)-hexahydronaphthyl-1′(S)ethyl-4(R)-t-butyldimethylsilyloxy-3,4,5,6-tetrahydro-2H-pyran-2-on with the carboxylic acid compound of formula (VI): wherein R is methyl, ethyl, propyl, n-butyl, t-butyl or phenyl, and hydroxylating the resulting compound.

Abstract: This invention describes the synthesis of simvastatin from lovastatin by converting the lovastatin to lova amide using a secondary amine and subsequent reaction with a metal amide base generated from n-butyl lithium and pyrrolidine and followed by treatment with methyl iodide to give desired C-methylated intermediate. This intermediate was further transformed to the final product, simvastatin. This method of production consumes lesser quantities of metal amide, gives fewer side reactions and a lowered overall cost of manufacture of simvastatin than other procedures reported.

Abstract: Lactonization of statins can be achieved using a lactonization agent that forms a hydrated complex with the produced water that is insoluble in the reaction solvent. By binding the produced water in an insoluble complex, the reaction is pulled to the lactone side, using mild conditions in short reactions times and with reduced risk of impurities.