Abstract: The present invention provides a pharmaceutical composition for use as art NPY Y5 receptor antagonist comprising a compound or the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Abstract: This application discloses a novel process for the synthesis of himbacine analogs, as well as the compounds produced thereby. The synthesis proceeds by alternative routes including the cyclic ketal amide route, the chiral carbamate amide route, and the chiral carbamate ester route. The compounds produced thereby are useful as thrombin receptor antagonists.

Abstract: It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO2F2) in the presence of an organic base or in the presence of an organic base and “a salt or complex comprising an organic base and hydrogen fluoride”. According to the present production process, it is not necessary to use perfluoroalkanesulfonyl fluoride, which is not preferable in industrial use, and it is possible to advantageously produce optically-active fluoro derivatives, which are important intermediates of medicines, agricultural chemicals and optical materials, specifically 4-fluoroproline derivatives, 2?-deoxy-2?-fluorouridine derivatives, optically-active ?-fluorocarboxylate derivatives, and the like, even in a large scale.

Abstract: The present invention relates to a process for preparing a compound of the formula: wherein R1 is lower alkyl, R4 is hydrogen or lower alkyl, and Z is optionally substituted lower alkyl, optionally substituted lower alkenly, optionally substituted amino, optionally substituted lower alkoxy, optionally substituted carbocyclyl or optionally substituted heterocyclyl.

Abstract: The present invention relates to Compounds of general formula (I), wherein R is hydrogen and R1 is hydroxy or acyloxy, or R is acyl and R1 is hydroxy or acyloxy, X is sulphur, oxygen or NR10, wherein R10 is hydrogen or (C1-4)alkyl; Y is sulphur or oxygen; R2 is hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry; R4 is hydrogen or (C1-4)alkyl; R5 is hydrogen or (C1-4)alkyl; R3 and R3? are hydrogen, deuterium, or halogen; R6, R7 and R8 are hydrogen, halogen or deuterium; m is a number selected from 0 to 4, n is a number selected from 0 to 10, and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. These Compounds are usefül as pharmaceuticals, particularly as antimicrobials.

Abstract: The instant invention constitutes an unique subject matter as a whole which has four individual aspects: (1) a class of chiral, non-racemic, synthetic carnitinoid analog carrier molecules which constitute biocompatible transport compounds not found in nature; (2) a subsequently formed, mitochondria-targeting, coupled antioxidant-carrier complex comprising an antioxidant reversibly attached to and releasable from the synthetic carrier molecule; (3) a method for introducing a biologically active antioxidant into the interior of mitochondria of a living cell for subsequent reaction with such reactive oxygen species may then be present; and (4) a system for delivering a biologically active antioxidant to the interior of mitochondria within a living cell.

Abstract: The present invention provides a process for obtaining highly pure crystalline form of oseltamivir free base, thus, for example, suspending or dissolving impure or non-crystalline oseltamivir free base in a hydrocarbon solvent and then isolating crystals to obtain oseltamivir free base in well defined crystalline form. The present invention also provides a process for preparation of oseltamivir phosphate in high purity.

Abstract: Allyl 1 {[(?-isobutanoyloxyethoxy)carbonyl]aminomethyl}-1-cyclohexane acetate can be prepared by combining allyl 1-aminomethyl-1-cyclohexane acetate hydrochloride, a polar organic solvent, chloroethyl chloroformate, and an amine base or an inorganic base selected from a group consisting of carbonate and bicarbonate to provide a reaction mixture; and adding isobutyric acid to the reaction mixture. The product can be purified and/or converted to gabapentin enacarbil.

Abstract: The present invention provides a process for obtaining highly pure crystalline form of oseltamivir free base, thus, for example, suspending or dissolving impure or non-crystalline oseltamivir free base in a hydrocarbon solvent and then isolating crystals to obtain oseltamivir free base in well defined crystalline form. The present invention also provides a process for preparation of oseltamivir phosphate in high purity.

Abstract: The present invention provides an improved and commercially viable process for the preparation of oseltamivir phosphate. Thus, for example, ethyl (3R,4R,5S)-4-amino-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate is acetylated with acetic anhydride in methylene chloride in the presence of triethyl amine in the absence of water to give ethyl (3R,4R,5S)-4-(acetylamino)-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate.

Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Abstract: The present invention provides an improved and commercially viable process for the preparation of oseltamivir phosphate. Thus, for example, ethyl (3R,4R,5S)-4-amino-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate is acetylated with acetic anhydride in methylene chloride in the presence of triethyl amine in the absence of water to give ethyl (3R,4R,5S)-4-(acetylamino)-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate.

Abstract: The invention relates to a plurality of processes for the preparation of novel cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives of the formula (I) in which A, G, X and Y are as defined in the disclosure.

Abstract: A pleuromutilin derivative compound of general formula (I)

Abstract: Gabapentin prodrugs and intermediates thereof are described.

Abstract: The present invention relates to Compounds of general formula (I), wherein R is hydrogen and R1 is hydroxy or acyloxy, or R is acyl and R1 is hydroxy or acyloxy, X is sulphur, oxygen or NR10, wherein R10 is hydrogen or (C1-4)alkyl; Y is sulphur or oxygen; R2 is hydrogen or one or more substituents, e.g. including substituents such as conventional in organic, e.g. (pleuro)mutilin, chemistry; R4 is hydrogen or (C1-4)alkyl; R5 is hydrogen or (C1-4)alkyl; R3 and R3? are hydrogen, deuterium, or halogen; R6, R7 and R8 are hydrogen, halogen or deuterium; m is a number selected from 0 to 4, n is a number selected from 0 to 10, and p is a number selected from 0 to 10; with the proviso that n plus p are at least 1. These Compounds are usefül as pharmaceuticals, particularly as antimicrobials.

Abstract: The present invention relates to thioester compounds and the incorporation and use of the new chemical entities as flavor and fragrance chemicals.

Abstract: The invention described herein relates to certain pyridazinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.

Abstract: The invention relates to compounds embodying amino group-terminal viscosifiers, the resultant products thereof, and the uses thereof. The inventive viscosifiers are provided with formula (I), wherein R1 represents a divalent radical of a carboxyl group-terminal butadiene/acrylonitrile copolymer after removing the terminal carboxyl groups. The disclosed compounds increase the viscosity of the compositions formulated therewith. Compounds containing glycidyl groups are particularly important as resultant products thereof which can be used in thermosetting single-component epoxy resin adhesives.

Abstract: Described are merocyanine derivatives of formula wherein R2 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; a cyano group; or R1 and R2 together with the nitrogen atom linking them form a —(CH2)m— ring which is optionally interrupted by —O— or by —NR7—; R4 is a cyano group; or -Q1-R5; Q1 is —COO—; —CONH—; —CO—; —SO2—; or —CONR6—; R5 is C1-C22alkyl; cyclo-C3-C8alkyl; or unsubstituted or C1-C6alkyl-substituted C6-C20aryl; R6 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; R7 is hydrogen; C1-C22alkyl; cyclo-C3-C8alkyl; unsubstituted or C1-C6alkyl- or C1-C6alkoxy-substituted C6-C20aryl; the cyclohexene radical C is not substituted or substituted by one or more C1-C5alkyl; m is from 3 to 7; n is from 2 to 4; and o is from 2 to 4.

Abstract: This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; ?wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.

Abstract: A process for the preparation of Compound (I) comprising reacting Compound (II) with a base in an aprotic solvent, which is represented by the following scheme: wherein R1 and R2 are each independently lower alkyl.

Abstract: The present invention provides a process for obtaining highly pure crystalline form of oseltamivir free base, thus, for example, suspending or dissolving impure or non-crystalline oseltamivir free base in a hydrocarbon solvent and then isolating crystals to obtain oseltamivir free base in well defined crystalline form. The present invention also provides a process for preparation of oseltamivir phosphate in high purity.

Abstract: The invention provides a new process for the conversion of shikimic acid to oseltamivir (I), and optionally to an acid addition salt, via the intermediate phosphoramide VII.

Abstract: A compound of formula (I) wherein n is 0 to 4; R is ethyl or vinyl; R1 is hydrogen or (C1-6)alkyl, R2 is hydrogen or cycloalkyl including (C3-6)cycloalkyl, or unsubstituted (C1-6)alkyl, or (C1-6)alkyl substituted by one or more of hydroxy; preferably one or two, halogen, (C3-6)cycloalkyl, or R1 is hydroxy and R2 is formyl.

Abstract: A method of conferring a cooling effect on the skin or mucous membranes by applying thereto at least one compound of the Formula I: (a) wherein B is selected from H, CH3, C2H5, OCH3, OC2H5; and OH; and (b) wherein A is a moiety of the formula —CO-D, wherein D is selected from the following moieties: (i) —NR1R2, wherein R1 and R2 are independently selected from H and C1-C8 straight or branched-chain aliphatic, alkoxyalkyl, hydroxyalkyl, araliphatic and cycloalkyl groups, or R1 and R2 together with the nitrogen atom to which they are attached form part of an optionally-substituted, five- or six-membered heterocyclic ring; (ii) —NHCH2COOCH2CH3, —NHCH2CONH2, —NHCH2CH2OCH3, —NHCH2CH2OH, —NHCH2CH(OH)CH2OH and (iii) a moiety selected from the group consisting of: The compounds are useful for providing cooling effects in a variety of products, such as foodstuffs, confectionery, tobacco products, beverages, cosmetics, dentifrices, medicinal preparations, mouthwashes and toiletries.

Abstract: The invention provides a new process for the conversion of shikimic acid to oseltamivir (I), and optionally to an acid addition salt, via the intermediate phosphoramide VII.

Abstract: Novel compounds having an average isocyanate functionality of greater than 2 are synthesized by the reaction of a (poly)isocyanate having an average functionality of greater than 2, with a compound X comprising a function B(H)n or B?(H)n? where n is equal to 1 or 2, n? is equal to 1, 2 or 3, H is a labile hydrogen atom and B is O, S, N, N being a primary or secondary nitrogen atom, —C(?O)—O, —C(?O)—N, or else the groups O?P(O)2; O?P(O)OR1; O?P(O)3; O?P(O)2OR1; O—P(O)—OR1, and B? is —SiR2R3R4, such reaction being carried out with a compound X/[compound X+(poly)isocyanate] weight ratio of at most 50%; compositions comprised thereof are of the hardener type and can be formulated into coatings of the paint or varnish type.

Abstract: An agent for suppressing the production of various cytokines (IL-8 and the like) and inflammatory mediators, an agent for suppressing the expression of COX-II and the like, or an inhibitor of various phosphorylation enzymes (ATF2 and the like), which contains a TLR signaling inhibitory substance, preferably a compound represented by the formula (I) or the formula (II) wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.

Abstract: The present invention provides an improved and commercially viable process for the preparation of oseltamivir phosphate. Thus, for example, ethyl (3R,4R,5S)-4-amino-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate is acetylated with acetic anhydride in methylene chloride in the presence of triethyl amine in the absence of water to give ethyl (3R,4R,5S)-4-(acetylamino)-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate.

Abstract: The present invention provides a compound of formula I processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and pharmaceutical compositions containing them.

Abstract: The present application describes deuterium-enriched oseltamivir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention relates to compounds selected from the group consisting of 14-0-[((Mono- or dialkylamino)-cycloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[((Cycloalkyl- or heterocyclylamino)-cy-cloalkylsulfanyl- or -cycloalkyl-oxy)-acetyl, -thioaceyl or -imino-oxy]-mutilins, 14-O-[((Heterocyc-N-yl-cycloalkyl)-sulfanyl- or -oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Mono- or dialkylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, 14-O-[(((Cycloalkyl- or heterocyclylamino)-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and 14-O-[((Heterocyc-N-yl-cycloalkyl)-alkylsulfanyl- or -alkyl-oxy)-acetyl, -thioacetyl or -imino-oxy]-mutilins, and their use as pharmaceuticals.

Abstract: A process for the preparation of Compound (I) comprising reacting Compound (II) with a base in an aprotic solvent, which is represented by the following scheme: wherein R1 and R2 are each independently lower alkyl.

Abstract: The present invention provides compounds which are useful as safe substitutes for the organotin reagent used in coupling reaction for the oxymethylation of aromatic rings, such as alkoxymethylation or hydroxymethylation, with a palladium catalyst and which can dispense with chromatographic purification with silica gel in the production and are suitable for mass production; and compounds applicable even to the oxymethylation of aromatic ring substrates which do not permit coupling reaction by conventional technique or have low reactivity.

Abstract: The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino acid ester and N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough and/or asthma.

Abstract: The present invention relates to a diastereomeric mixture of Silacycle Compounds and methods for using the diastereomeric mixture of Silacycle Compounds for stereoselective synthesis.

Abstract: Metal chelators of formula (I) and formula (II) are disclosed or a farmaceutically acceptable salt thereof. Also disclosed are metal chelator-targeting moiety complexes, metal chelator-targeting moiety-metal conjugates, kits, and methods of their preparation and use in diagnosis and/or treatment of diseases and conditions, including, inter alia, cancer and thrombosis.

Abstract: The invention provides novel compounds of Formula (I), pharmaceutical compositions and methods of synthesis thereof.

Abstract: The invention concerns novel molecules, their preparation and their uses, in particular in the field of human and veterinary medicine and cosmetics. The inventive compounds are partly fatty acid derivatives and exhibit advantageous pharmacological and cosmetic properties. The invention also concerns various uses of said compounds, the pharmaceutical compositions containing them and methods for preparing them. The inventive compounds are useful in particular for preventing and/or treating dyslipidemiae, cardiovascular diseases, syndrome X, restenosis, diabetes, obesity, hypertension, certain cancers, dermatological diseases and in cosmetics, for fighting against skin aging and its effects notably against wrinkles and the like.

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.

Abstract: A process for the manufacture of ?-Difluoromethylornithine, analogs and derivatives is described from ornithine hydrochloride or from N?-phthaloyl ornithine hydrochloride, conversion to an alkyl ester, conversion to solid derivatives through the formation of Schiff bases, subsequent halomethylation using suitable bases and hydrolysis.

Abstract: Novel processes for the preparation of the anti-viral agent, Oseltamivir Phosphate and novel intermediates prepared in such processes. The novel processes use as starting materials D-glucose or D-xylose in the preparation of Oseltamivir Phosphate.

Abstract: A process for the preparation of Compound (I) comprising reacting Compound (II) with a base in an aprotic solvent, which is represented by the following scheme: wherein R1 and R2 are each independently lower alkyl.

Abstract: The present invention relates to optically active boronate derivatives which are useful as intermediates for the synthesis of HMG-CoA enzyme inhibitors such as atorvastatin, cerivastatin rosuvastatin, pitavastatin, and fluvastatin.

Abstract: Disclosed herein are high refractive index monomers that are curable by ultraviolet light. These monomers may be a component of curable compositions useful in the preparation of optical articles. Also disclosed is a method of synthesizing the monomers.

Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Abstract: Cyclic ?-(acylamino)acrylate derivatives were hydrogenated using Ru-chiral phosphine ligand catalysts and thereafter converted to the corresponding cyclic ?-aminoacids in high yield and enantioselectivity according to the reaction scheme:

Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A—(B)b0—(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R—T1—, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from anminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.

Abstract: The present invention provides, in one aspect, a substantially pure ethyl ester of N-[[5-methyl-2-(1-methylethyl)cyclohexyl]carbonyl]glycine. In another aspect, disclosed is a method for producing substantially pure ethyl ester of N-[[5-methyl-2-(1-methylethyl)cyclohexyl]carbonyl]glycine. In still another aspect, disclosed are various consumer products comprising the substantially pure ethyl ester of N-[[5-methyl-2-(1-methylethyl)cyclohexyl]carbonyl]glycine disclosed herein.