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: The present invention relates to new compounds of general formula having thrombin-inhibiting activity. Exemplary are: 1-Methyl-2-[4-(N-hydroxyamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-ethoxycarbonylethyl)-amide, and 1-Methyl-2-[4-(N-methoxycarbonylamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amide.

Abstract: A process for the preparation of taxanes comprising wherein R is a tert. butoxycarbonyl or benzoyl group; PMP is p-methoxyphenyl group; G1 is acetyl group; G2 is haloacetyl group comprising a) protecting the C-7 hydroxyl group of 10-deacetylbaccatin III with haloacetyl chlorides and then acetylating the C-10 hydroxyl group with acetyl chloride to obtain a protected 10-deacetylbaccatin III (1); b) subjecting the protected 10-deacetylbaccatin III (1) to coupling with an oxazolidine-5-caboxylic acid of formula 2 wherein R is tert. butoxycarbonyl or benzoyl; PMP is p-methoxyphenyl group in the presence of a condensation agent and an activating agent to obtain C-13 esters of formula 3; c) treating the coupled products 3 with weak acidic medium to open the oxazolidine ring to obtain intermediates of formula 4; wherein R is a tert.

Abstract: This invention features the use of the spirolaxine of formula (I) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the Type 2 insulin-resistant diabetes. This invention also features a pharmaceutical composition in which the spirolaxine of formula (I) acts as active principle in association with the all-trans retinoic acid of formula (II) for the treatment of those pathologies responding to the activation of the PPAR? receptor, such as the acute malignant haemopathies.

Abstract: The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obsructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

Abstract: The present invention provides a novel 4?-demethyl-4?-O-substituted-1-deoxypodophyllotoxin derivative, a geometric isomer thereof, a process for the preparation thereof, and an anticancer composition comprising the same.

Abstract: The present invention relates to an integrated process for the preparation in continuous of epoxides which comprises: (a) preparing an alcoholic or hydro-alcoholic solution of hydrogen peroxide in a concentration of over 3% by weight, using a gaseous stream containing hydrogen, oxygen and an inert gas, in the presence of a bimetallic catalyst based on palladium and platinum as active components; (b) putting the alcoholic or hydro-alcoholic solution of hydrogen peroxide obtained in step (a) in contact with an olefin and a buffering agent, in the presence of an epoxidation catalyst suspended in the reaction solvent, in order to obtain a reaction mixture containing the epoxide corresponding to the olefin, water and alcoholic solvent; (c) treating the alcoholic stream leaving step (b), after separation of the epoxide, in order to eliminate the nitrogenated compounds present; (d) feeding the alcoholic solvent obtained in (c) to step (a).

Abstract: Compounds of the formula where the variations have the meaning defined in the specification are capable of reducing serum glucose levels in diabetic mammals without the undesirable side effects of transiently increasing triglyceride levels and reducing serum thyroxine levels.

Abstract: Propylene oxide is formed by reaction of propylene with molecular oxygen in a high boiling solvent containing slurried solid catalyst, the light components are flashed and the remaining liquid containing slurried catalyst is recycled.

Abstract: Process for the preparation of a derivative or analog of baccatin III or 10-desacetyl baccatin III having a C9 substituent other than keto in which the C9 keto substituent of taxol, a taxol analog, baccatin III or 10-desacetyl baccatin III is selectively reduced to the corresponding hydroxy group.

Abstract: A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Abstract: Etoposide analogs such as 4?-O-demethyl-4?-[4?-(methyl-L-tyrosine-N-carbonyl)-anilino]-4-desoxy-podophyllotoxin (12) and 4?-O-demethyl-4?-[4?-(methyl-L-tryptophan-N-carbonyl)-anilino]-4-desoxypodophyllotoxin (13) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.

Abstract: A novel class of decalactones with the general formula (I) and their stereoisomers is disclosed. A method for the synthesis of the decalactones of general formula (I) and the use of the decalactones in pharmaceutical compositions is also described.

Abstract: Oxidation products are recovered from a mixture of the products in a dense phase or supercritical solvent by a liquid—liquid extraction at dense phase conditions.

Abstract: Propylene oxide is formed in a two step reaction wherein in a first step oxygen and hydrogen are reacted in the absence of propylene to form hydrogen peroxide and in a second step propylene is reacted with the formed hydrogen peroxide to form propylene oxide, the same solid noble metal on TS-1 catalyst being used to catalyze the reaction in each step.

Abstract: This invention is drawn to compounds which are more easily metabolized by the metabolic drug detoxification systems. Particularly, warfarin analogs which have been designed to include esters within the structure of the compounds are taught. The invention teaches methods of reducing the toxicity of drugs comprising the introduction of ester groups into drugs during the synthesis of the drug. This invention is also drawn to methods of treating coagulation disorders comprising the administration of compounds which have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester containing warfarin, analogs are also taught.

Abstract: Derivatives of UK-2A are provided.

Abstract: The epoxidation of cyclic, at least monounsaturated alkenes is conducted by a process, which comprises conducting the epoxidation of a cyclic, at least monounsaturated alkene in the presence of an oxidant in a reaction medium that contains at least 1% by weight of the saturated cyclic alkane corresponding to the cyclic, at least monounsaturated alkene. In a preferred embodiment the reaction medium contains at least 2.5% by weight of the saturated cyclic alkane corresponding to the cyclic, at least monounsaturated alkene.

Abstract: Biologically active crystalline solvates of paclitaxel are precipitated using polar, aprotic, organic solvents. A pharmaceutical composition is also disclosed, as well as the preparation of the novel solvates and their uses as anti-tumor agents.

Abstract: The present invention relates to a novel process for producing a ?-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)-?-lactone.