Abstract: The invention relates to a method for preparation of (meth)acrylic acid esters from (meth)acrylic acid anhydrides. Wherein the method for preparation of the (meth)acrylic acid ester, comprises at least step (a) as follows: (a) reacting a (meth)acrylic acid anhydride of Formula (I): wherein R1 is a hydrogen atom or a methyl group; with a substrate in the presence of a first catalyst to form a product mixture comprising the (meth)acrylic acid ester; and wherein: the substrate is selected from the group consisting of: primary alcohols; secondary alcohols; tertiary alcohols; and phenols; and the first catalyst comprises a salt of magnesium or of a rare earth element.

Abstract: A polymerizable compound represented by formula (1). In formula (1), one of eight hydrogen atoms is substituted by a (meth)acryloyloxy group, and the rest seven hydrogen atoms are independently non-substituted or substituted by a saturated hydrocarbon group having 1 to 10 carbons.

Abstract: The invention relates to compounds of Formula I, wherein the variables are as defined in the claims, which are useful in the treatment and/or prevention of bacterial infections in a subject. The invention further relates to the use of a compound of Formula I in the manufacture of a medicament, and medical devices when used in a method of treating or preventing a bacterial infection in a subject, and related aspects.

Abstract: This disclosure describes biosynthesized compounds including anhydromevalonolactone and ?-methyl-?-valerolactone. This disclosure further describes biosynthetic methods for making these compounds. In some embodiments, the biosynthetic methods can include a combination of biosynthesis and chemical steps to produce ?-methyl-?-valerolactone. Finally, this disclosure described recombinant cells useful for the biosynthesis of these compounds.

Abstract: This disclosure describes biosynthesized compounds including anhydromevalonolactone and ?-methyl-?-valerolactone. This disclosure further describes biosynthetic methods for making these compounds. In some embodiments, the biosynthetic methods can include a combination of biosynthesis and chemical steps to produce ?-methyl-?-valerolactone. Finally, this disclosure described recombinant cells useful for the biosynthesis of these compounds.

Abstract: The invention relates to compounds of Formula (I), wherein the variables are as defined in the claims, which are useful in the treatment and/or prevention of bacterial infections in a subject. The invention further relates to the use of a compound of Formula (I) in the manufacture of a medicament, and medical devices when used in a method of treating or preventing a bacterial infection in a subject, and related aspects.

Abstract: The invention relates to a method for producing lactones from a strain of Aureobasidium pullulans that are produced from a pre-culture of the Aureobasidium pullulans strain CBS 771.97, obtained from CBS-KNAW Fungal Biodiversity Center, Uppsalalaan 8, 3584 CT Utrecht, Netherlands, or related strains; from an inoculum obtained from the pre-culture; a culture is produced by fermentation at a temperature between 20° C. and 40° C. over a period of at least 3 days so as to produce metabolites, in a sterilized aqueous production medium containing: a carbon source; a nitrogen source; a mineral salt solution; and a calcium source, at a concentration between 2 and 100 mM; and following the fermentation period, converting the metabolites produced into a lactone mixture comprising (R)-5,6-dihydro-6-pentyl-2H-pyran-2-one (or (R)-(?)-massoia lactone) and/or (4R,6R)-4-hydroxy-6-pentyl-tetrahydro-2H-pyran-2-one.

Abstract: Organohalides (e.g., organofluorides) represent a rapidly expanding proportion of molecules used in pharmaceuticals, diagnostics, agrochemicals, and materials. The present invention exploits the naturally occurring acetate condensation pathway as a means of introducing halogenated building blocks into natural product scaffolds. In an exemplary embodiment, the invention provides a pathway involving at least one polyketide synthase system and utilizes haloacetate or a haloacetate synthon (e.g., halomalonate) to incorporate an organohalide into the polyketide backbone in vitro. In an exemplary embodiment, the invention provides an analogous method for site-selective introduction of haloacetate or a synthon into polyketide products in vivo. The present invention expands the scope of existing chemical methods for producing halogenated natural product scaffolds such as complex halogenated natural products.

Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.

Abstract: In one aspect, the present invention provides catalysts for the carbonylation of heterocycles. The inventive catalysts feature metal-ligand complexes having cationic functional groups tethered to the ligand, wherein the tethered cationic groups are associated with anionic metal carbonyl species. The invention also provides methods of using the inventive catalysts to affect the ring opening carbonylation of epoxides.

Abstract: The use of statins as antiepileptic, anticonvulsant, neuroprotector and antioxidant compounds, potentially useful for the prevention and/or treatment of epilepsy, epileptic seizures, convulsions, neurodegenerative diseases, or diseases associated with undesired oxidation, is described.

Abstract: The object of the invention is to provide a technique of suppressing tumorigenesis in IPS cells and inducing differentiation into target differentiated cells. In use of a statin and a differentiation inducer, iPS cells are differentiated into target differentiated cells, whereby iPS cells can be differentiated into differentiated cells in which tumorigenesis is suppressed.

Abstract: A transformant is prepared to insert at least a gene expression cassette comprising a gene involved in the synthesis of 2-deoxy-scyllo-inosose into E. coli as host cells. A 2-deoxy-scyllo-inosose is synthesized from D-glucose, oligosaccharide, polysaccharide, starch and rice bran, using the transformant. A culture solution containing the 2-deoxy-scyllo-inosose is treated with a mixed bed or double bed type column comprising a hydrogen form of strong acidic cation exchange resin and an organic ion form of basic anion exchange resin. The 2-deoxy-scyllo-inosose as purified is reacted with trimethoxymethane to convert into 2-deoxy-scyllo-inosose dimethylketal, and the dimethylketal is crystallized and purified. Then, DOI is highly purified through hydrolyzing the dimethylketal in the presence of acid.

Abstract: Disclosed herein are novel compounds of formula (I), and uses thereof. The compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds of Formula (I) for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g.

Abstract: A method for preparing a statin compound by lactonization is disclosed, which comprises the following step: lactonizing a compound of formula II into the compound of formula I in the presence of a strong acid catalyst and a dehydrant in a first solvent, wherein Z represents H, ammonium, or a metal cations; R1 is H or C1-C6 alkyl, preferably H or CH3, R2 is CH3, OH, CH2OH, CH2OC(O)R3, CH2OR3, or COOR4, preferably CH3 or OH, R3 and R4 are independently selected from the group consisting of H and C1-C6 alkyl.

Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.

Abstract: There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Ra represents an alkyl group, such as a C1-16 alkyl group, and preferably an isopropyl group; Rb represents an aryl group, preferably a 4-fluorophenyl group; Rc represents hydrogen, a protecting group or an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO2Re group where Re is an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group.

Abstract: This invention provides a skin-whitening agent, a tyrosinase activity inhibitor, and melanin production inhibitor comprising, as an active ingredient, a compound exhibiting excellent solubility in various solvents. Such skin-whitening agent, tyrosinase activity inhibitor, and melanin production inhibitor comprise 3-hydroxy-2-pyrone.

Abstract: The present invention relates to a polyketide molecule of the following formula (I): or a pharmaceutically acceptable salt thereof, where R1 is a hydrogen atom or a (C1-C7) alkyl group, as well as the method of preparation and use thereof, in particular as an anticancer agent.

Abstract: A method for determining if a subject with cancer or precancerous lesions or a benign tumor, will respond to treatment with an inhibitor selected from the group comprising an inhibitor of one or more enzymes in the mevalonate pathway, an inhibitor of geranylgeranyl transferase, an inhibitor of farnesyl transferase or an inhibitor of squalene synthase, by (i) obtaining a sample of the cancer cells, precancerous cells or benign tumor cells from the subject, (ii) assaying the cells in the sample for the presence of a mutated p53 gene or a mutant form of p53 protein or a biologically active fragment thereof, and (iii) if the cells have the mutated p53 gene or mutant form of the p53 protein, then determining that the subject will respond to treatment with the inhibitor or combinations thereof. Some embodiments are directed to treatment with the inhibitors.

Abstract: The present invention relates to the use of compounds of the formula (I) for the care, preservation or improvement of the general condition or appearance of the skin or hair, and to preparations comprising compounds of the formula (I).

Abstract: Therapeutic conjugates containing a statin or a modified statin (collectively “statin”) linked to a therapeutic agent (also referred to as a drug herein) are targeted to the liver by the statin or modified statin and thereby deliver the therapeutic agent to liver cells

Abstract: Fluorinated prodrug compounds as can be used for selective streptococcal mevalonate pathway inhibition.

Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.

Abstract: The present invention describes a compound of formula (I) its hydroxy acid form, the pharmaceutically acceptable salts of said hydroxy acid and pharmaceutically acceptable prodrugs and solvates of the compound and of its hydroxy acid form and, in particular, said compound, its hydroxy acid form, salts, etc. for use in the prevention of: neurodegenerative diseases, cognitive impairment, diseases associated with undesired oxidation, age-associated pathological processes and progeria, cardiovascular diseases such as atherosclerosis, atrial fibrillation, dyslipidemia, hypercholesterolemia, hyperlipidemia, and hypertriglyceridemia, inflammation or inflammatory processes, or epilepsy, epileptic seizures and convulsions.

Abstract: The present invention relates to a novel carbohydrate lactone, functionalized aliphatic polyesters and copolymers formed therefrom, and processes for the preparation thereof from renewable resources.

Abstract: What is described is an implant that comprises a coating, at least in areas, in the implanted state in the surface areas that are at least directly in contact with skin and/or soft tissue. The implant is preferably characterized in that the coating comprises both a statin, such as simvastatin, in the hydrolyzed or unhydrolyzed form, or pharmaceutically compatible salts thereof, as well as at least one other component selected from the group consisting of branched or linear, substituted or unsubstituted, saturated or partially unsaturated C10-C30 alkyl, alkenyl, alkylaryl, aryl, cycloalkyl, alkylcycloalkyl, alkylcycloaryl amines or mixtures thereof and/or at least one water-soluble ionic polymer component. A method for production such an implant is also described as well as a composition that can be used in such a method.

Abstract: A polymer includes a repeating unit shown by a general formula (1). R1 represents a hydrogen atom, a methyl group, a fluorine atom, or a trifluoromethyl group. R2 represents a substituted or unsubstituted aryl group having 6 to 22 carbon atoms. Y represents a carbon atom. X represents —X1Z1X2— which is an atomic group which forms a cyclic structure including a heteroatom together with Y. Z1 represents —O—, —S—, —CO—, —COO—, —SO—, or —SO2—. Each of X1 and X2 individually represents a single bond, a methylene group, or an alkylene group having 2 to 25 carbon atoms. Each of X1 and X2 is unsubstituted or substituted with a substituent, and optionally a carbon atom included in X1 and a carbon atom included in X2 are bonded via a divalent group.

Abstract: The present invention describes dental adhesive compositions used for bonding dental biomaterials to hard tissue comprising a polymerizable blend of one or more newly synthesized low shrinkage, stable, multifunctional compounds, where the compounds are acidic-methacrylate derivatives, having excellent properties of bonding the hard tooth substance (enamel or dentin) to dental restorative materials, and present high quality marginal sealing between the tooth and the material thus bond and improved storage stability

Abstract: There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Ra represents an alkyl group, such as a C1-16 alkyl group, and preferably an isopropyl group; Rb represents an aryl group, preferably a 4-fluorophenyl group; Rc represents hydrogen, a protecting group or an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO2Re group where Re is an alkyl group, such as a C1-16 alkyl group, and preferably a methyl group.

Abstract: A method for preparing a statin compound by lactonization is disclosed, which comprises the following step: lactonizing a compound of formula II into the compound of formula I in the presence of a strong acid catalyst and a dehydrant in a first solvent, wherein Z represents H, ammonium, or a metal cations; R1 is H or C1-C6 alkyl, preferably H or CH3, R2 is CH3, OH, CH2OH, CH2OC(O)R3, CH2OR3, or COOR4, preferably CH3 or OH, R3 and R4 are independently selected from the group consisting of H and C1-C6 alkyl.

Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.

Abstract: The object of this invention was to probe the reactivity of lovastatin, simvastatin, pravastatin, and mevastatin in the solid-state without radical initiators in order to determine the antioxidant that provided the best stability for the statin. Phenolic antioxidants were evaluated.

Abstract: Provided is a method of preparing a (6R)-3-hexyl-4-hydroxy-6-undecyl-5,6-dihydropyran-2-one, and a (5R)-2-hexyl-5-hydroxy-3-iminohexadecanoate derivative used in said method as an intermediate.

Abstract: Antitumoral compounds obtained from a porifera, of the family Raspailiidae, genus Lithoplocamia, species lithistoides, and derivatives thereof are provided.

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: The various embodiments of the present invention are directed to methods and compositions for treatment, inhibition or reduction of metastasis in cancers. In particular, the invention is related to compositions and methods affecting connective tissue growth factor (CTGF). An aspect of the present invention comprises a method for interfering with the activity of connective tissue growth factor, comprising, administering to a subject an effective amount of a composition that inhibits production of or activity of connective tissue growth factor (CTGF), wherein the composition interferes with the activity of CTGF or prevents the transcription of CTGF genes or translation of CTGF mRNA. For example, the composition can comprises at least one HMG-CoA reductase inhibitor compound, such as a statin.

Abstract: The present invention describes a compound of formula (I) its hydroxy acid form, the pharmaceutically acceptable salts of said hydroxy acid and pharmaceutically acceptable prodrugs and solvates of the compound and of its hydroxy acid form and, in particular, said compound, its hydroxy acid form, salts, etc. for its use in the prevention of: neurodegenerative diseases, cognitive deterioration, diseases associated with undesired oxidation, age-associated pathological processes and progeria, epilepsy, epileptic seizures and convulsions, cardiovascular diseases such as atherosclerosis, atrial fibrillation, dyslipemia, hypercholesterolemia, hyperlipidemia, and hypertriglyceridemia, or fungal or viral infections.

Abstract: Compositions which modulate mitochondrial functions treat diseases associated with cells that are hyperactively using their endoplasmic reticulum. Screening assays identify agents which modulate mitochondrial functions.

Abstract: HIF-1 inhibitors and methods of use thereof are provided.

Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.

Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.

Abstract: This invention relates to an improved process for preparing substantially pure simvastatin (I), chemically known as (1S,3R,7S,8S,8aR)-8-[2-[(2R,4R)-4-hydroxy-6-oxotetrahydro-2-H-pyran-2-yl]ethyl]-3 ,7-dimeth-yl-1,2,3,7,8,8a-Hexahydronaphthalen-1-yl2,2-dimethyl butanoate, which comprises of: a) treating lovastatin (II) with an alkali metal hydroxide in a chosen suitable alcoholic solvent followed by relactonization to obtain the diol lactone intermediate (III) in a single vessel. b) selective silylation of 4-hydroxy group of diol lactone intermediate (III) with a chosen suitable silylating reagent to obtain mono silylated intermediate diol lactone (IV).

Abstract: The present invention relates to a complex made up of at least one molecule of statin or a derivative thereof, covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one 2-methyl-buta-2-ene unit, to nanoparticles of such a complex, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least one complex and/or nanoparticles such as previously defined. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of hyperlipemia and hypercholesterolemia.

Abstract: The invention relates to the preparation of 2-(6-substituted-1,3-dioxane-4-yl)acetic acid derivatives of formula (1), where X stands for a leaving group, and R1, R2, and R3 each independently stand for an alkyl group with 1-3 carbon atoms from 4-hydroxy-6-X-substituted-methyl-tetrahydropyran-2-one compounds, where X is as defined above, with the aid of an acetalization agent, in the presence of an acid catalyst. The invention also relates to the novel compounds of formula (1) as well as salts and acids to be prepared from these, with the OR3 group in formula (1) being replaced by an OY group, where X, R1 and R2 have the meanings defined above and where Y stands for an alkaline (earth) metal or a substituted or unsubstituted ammonium group or stands for hydrogen, and to the novel compounds of formula (2). The products concerned are, after conversion into the t-butyl ester of 2-(6-hydroxymethyl-1,3-dioxane-4-yl)acetic acid, important as intermediary products in the preparation of statins.

Abstract: Intermediates in the preparation of epothilones and epothilone analogs are provided along with synthetic methods useful in the synthesis of epothilone compounds.

Abstract: The present invention provides zebrafish based methods for the identification of compounds potentially useful in the treatment of motor neuron degenerative diseases (MNDDs), compounds identified by these methods and compositions, methods and medicaments for treating MNDDs.

Abstract: The use of statins as antiepileptic, anticonvulsant, neuroprotector and antioxidant compounds, potentially useful for the prevention and/or treatment of epilepsy, epileptic seizures, convulsions, neurodegenerative diseases, or diseases associated with undesired oxidation, is described.

Abstract: Compounds and related methods as can be used for selective mevalonate pathway inhibitors.

Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.