Abstract: Method for preparing compounds of the formula (III) by reacting compounds of the formula (II) with a) an alcoholate or b) an alcohol R1-OH and a base in the presence of a Cu-containing catalyst and of a ligand, where X1-5 are independently of one another either carbon or nitrogen, or in each case two adjacent X1R1, with i=1?6, linked by a formal double bond together O, S, NRH or Nrl. The ligands preferably employed are acyclic and/or cyclic oligo- and polyglycols, oligo- and polyamides or oligo- and polyamine glycols of the general formula (IV) k is an integer >0 and n is an integer >1; X and Y are independently of one another O, NH or NR1.

Abstract: Novel 2-halofuryl/thienyl-3-carboxamides of the formula (I) in which A, Hal, R, M and Z are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.

Abstract: This invention describes protected 5,7-dihydroxy-4,4-dimethyl-3-oxoheptanoic acid ester and 5,7-dihydroxy-2-alkyl-4,4-dimethyl-3-oxoheptanoic acid ester for the synthesis of epothilones and epothilone derivatives and process for the production of these esters.

Abstract: Novel ester compounds having formulae (1) to (4) wherein A1 is a polymerizable functional group having a carbon-carbon double bond, A2 is oxygen, methylene or ethylene, R1 is a monovalent hydrocarbon group, R2 is H or a monovalent hydrocarbon group, any pair of R1 and/or R2 may form an aliphatic hydrocarbon ring, R3 is a monovalent hydrocarbon group, and n is 0 to 6 are polymerizable into polymers. Resist compositions comprising the polymers as a base resin are thermally stable and sensitive to high-energy radiation, have excellent sensitivity and resolution, and lend themselves to micropatterning with electron beam or deep-UV.

Abstract: Inhibitors of HIV reverse transcriptase which are useful for the treatment of HIV infection. Exemplars of the invention are compounds of the formula wherein the substituents are as defined in the following table R1 R2 R4 R5 R8a F CF3 Me H —OH F CF3 Cl H —OH F CF3 Me H —O—CH2CO2H Cl CN Cl H —OH.

Abstract: A process for preparing (S)-(?)-N-[4-[4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxy]phenyl]methanesulfonamide hemifumarate salt, which comprises reacting N-[4-[(2S)-tetrahydro-5-hydroxy-2-furanyl]phenyl]methanesulfonamide(IIa) with fluoroamine (III) in the presence of triacetoxyborohydride and ethyl acetate to provide [4-[-4-[ethyl(6-fluoro-6-methylheptyl)amino]-1-hydroxylphenyl]methanesulfonamide (I) and then converting I into the hemifumarate salt Ia. A process for preparing IIa is also claimed as well as intermediates IIa-IId.

Abstract: A compound represented by the following formula (I) wherein R1 is a lower alkyl group, R2 is a hydrogen, a halogen, a cyano group, a lower alkyl group or a lower alkoxy group, and n is 0 or 1, which has a calpain inhibitory activity, is provided.

Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

Abstract: An acrylate compound of formula (4): is produced by allowing an acrylic acid compound of formula (1): to react with an unsaturated compound of formula (2) or (3): In formulae (1) through (4), R1 and R2 are H or F, R3 is H, F, or an alkyl, alkenyl, fluoroalkyl or fluoroalkenyl group, R4 and R5 are H, halogen, or an alkyl, alkenyl, halogenated alkyl or halogenated alkenyl group; and X and Y are an unsubstituted or substituted hydrocarbon group, and dashed line - - - means that X and Y may be bonded together to form a cyclic structure.

Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.

Abstract: Compounds of general formula (I): wherein R1, R2, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.

Abstract: The invention concerns a method for purifying a composition containing at least a product for internal dehydration of a hydrogenated sugar. The invention is characterised in that it comprises: (a) an optional step whereby said composition is treated, whether after re-dissolving or not, with at least a discoloration means; (b) a subsequent step whereby the composition, optionally treated with discoloration means, is treated with at least ion-exchanging means; (c) a subsequent step whereby the resulting composition is treated with at least discoloration means. Said method is in particular applicable to isohexide compositions, in particular isosorbide or isomannide. The resulting compositions, which exhibit particular characteristics in terms of purity and proportion of some impurities, constitute novel products for use in chemical, pharmaceutical, cosmetology and food industries.

Abstract: An adamantanetricarboxylic acid derivative is represented by following Formula (1): wherein X is a hydrogen atom or a hydrocarbon group; and R1, R2 and R3 may be the same as or different from one another and are each a carboxyl group which may be protected by a protecting group, or a carbonyl halide group, wherein at least one of R1, R2 and R3 is a carboxyl group which is protected by a protecting group, or a carbonyl halide group.

Abstract: Fluorinated five-membered ring compounds of the formula (I) R1—X—(A1—M1)a—(A2—M2)b—A3—Y—E ??(I) where E is a radical T—Z—R2 containing a five-membered ring and, for example, T is undirected and is 4-fluorothiophene-2,5-diyl, 3-fluorothiophene-2,5-diyl, 3-fluorothiophene-2,4-diyl, 5-fluorothiophene-2,4-diyl, furan-2,5-diyl, furan-2,4-diyl, isoxazole-3,5-diyl, thiazole-2,5-diyl, thiazole-2,4-diyl, cyclopentane-1,3-diyl or cyclopentene-1,3-diyl, R1 and R2 are hydrogen, X is a single bond, —O—, OC(?O)—, —C(?O)O— or —OC(?O)O—, Y is —OC(?O)—, —OCH2—, —CH2CH2—, Z is a single bond or —O—, A1, A2, A3 are each, independently of one another, phenylene-1,4-diyl, M1, M2 are undirected and are each, independently of one another, —OC(?O)—, —OCH2—, —CH2CH2—, —OC(?O)CH2CH2—, —OCH2CH2CH2—, —C?C—, —CH2CH2CH2CH2— or a single bond, a, b are each, independently of one another, 0 or 1, are used in FLC mixtures.

Abstract: This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions containing such compounds and their use as anti-proliferative agents, especially tumor growth inhibitors and anti-cancer agents, antibiotics and/or antiviral agents.

Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).

Abstract: A dihydrofuran-containing nonlinear optical chromophore having a ?-electron donor group conjugated to the dihydrofuran group through a ?-electron conjugated bridge group. The nonlinear optical chromophore is a hyperpolarizable chromophore that can be used as an electro-optic modulator in electro-optic devices.

Abstract: HIV protease inhibitors are among the most powerful drugs in suppressing HIV in human patients. However, HIV developed resistance to all protease inhibitor drugs so far marketed or used in clinical trials. HIV generates resistance by mutating its protease. The strains of HIV containing mutant proteases less vulnerable to inhibitor drug are able to replicate better and maintain the infection. No effective principle exists for the design of resistance-proof HIV protease inhibitors (HIVPr). A new inhibitor has been developed based on a new concept for designing resistance invulnerable HIVPr inhibitors. In vitro data have shown that this inhibitor is effective against many known HIVPr mutants resistant to other HIVPr inhibitor drugs. The new concept is, therefore, generally applicable for the design of other resistance invulnerable HIVPr inhibitor drugs.

Abstract: The present invention relates compounds that are NK-1 antagonists and that are of use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: Provided are processes and chemical intermediates useful for preparing a compound of the formula I wherein X is selected from the group consisting of C1-C6 trihalomethyl; C1-C6 alkyl; and an optionally substituted or di-substituted phenyl group of formula II: Y and Z are independently selected from the group consisting of substituted and unsubstiotuted aryl

Abstract: For the preparation of an 11-oxaprostaglandin such as [2R,(1E,3R),3S,(4Z),4R)]-7-{tetrahydro-2-[4-(3-chlorophenoxy)-3-hydroxy-1-butenyl]-4-hydroxy-3-furanyl}-4-heptenoic acid and its ester derivatives, a novel process uses a novel enantiomerically enriched compound for formula (1) wherein the bond between carbon atoms y and z is either a single or double bond; R1 is selected from vinyl, trialkylsilylethynyl, a formyl group protected as an acetal, or a protected hydroxymethyl group; R2 is C1-5 alkyl, optionally substituted at the terminus with an aryloxy or alkoxy group; and R3-R6 are independently selected from C1-6 alkyl and C6-10 aryl

Abstract: The present invention provides certain [3.1.0] bicyclic oxazolidinone derivatives of Formulea I and II, described herein, or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: The present invention relates to novel covalent derivatives of alkanolamides of monocarboxylic and dicarboxylic acids with aminoalcohols of general formula (I) which can usefully be used as agonists of the CB2 cannabinoid receptor and hence as drugs active in pathological conditions which can be controlled by stimulation and/or costimulation of this receptor

Abstract: Compounds of formula (I) wherein R1is selected from H, C(?O)R?, P(?O)R?R?, S(?O)R?R?, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, or substituted or unsubstituted aryl; or R1 together with R2 forms a saturated or unsaturated heterocyclic ring; R2 and R3 are each, independently, selected from H, C(?O)R?, P(?O)R?R?, S(?O)R?R?, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, or substituted or unsubstituted aryl; or one of R2 or R3 together with R1 forms a saturated or unsaturated heterocyclic ring; or R2 and R3 together form a saturated or unsaturated heterocyclic ring; R4 is selected from H, C(?O)R?, P(?O)R?R?, S(?O)R?R?, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18, alkynyl, or substituted or unsubstituted aryl, wherein R? is selected from the group consisting of

Abstract: There are disclosed novel neuropeptide Y ligands having the general formula I Wherein the symbols W, A, D, R1, R2, R3, R4 are further defined in the description. Compounds of formula I are agonists and antagonists of neuropeptide Y, and are therefore useful as regulators.

Abstract: A process for the co-production of a diol product (e.g. butane-1,4-diol) and a cyclic ether (e.g. tetrahydrofuran) by hydrogenation of an aliphatic diester or lactone feedstock (e.g. dimethyl or diethyl maleate), which contains a minor amount of acidic material, such as the corresponding monoester. The process utilizes a plurality of hydrogenation zones connected in series, each containing a charge of a granular ester hydrogenation catalyst. The catalyst in the first hydrogenation zone is tolerant of a minor amount of acidic material, while the catalyst in the second hydrogenation zone provides enhanced yields of cyclic ethers compared to the catalyst of the first hydrogenation zone. The catalyst in a third hydrogenation zone exhibits low selectivity towards conversion of the diester to at least one by product (e.g. 2-4?-hydroxybutoxy-tetrahydrofuran).

Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.

Abstract: An acrylate compound of formula (4): is produced by allowing an acrylic acid compound of formula (1): to react with an unsaturated compound of formula (2) or (3): In formulae (1) through (4), R1 and R2 are H or F, R3 is H, F, or an alkyl, alkenyl, fluoroalkyl or fluoroalkenyl group, R4 and R5 are H, halogen, or an alkyl, alkenyl, halogenated alkyl or halogenated alkenyl group; and X and Y are an unsubstituted or substituted hydrocarbon group, and dashed line - - - means that X and Y may be bonded together to form a cyclic structure.

Abstract: A compound represented by the following formula (I) or a salt thereof and a medicament such as an angiogenesis inhibitor and an antitumor agent which comprises said compound or a physiologically acceptable salt thereof as an active ingredient.

Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.

Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I:

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: The invention relates to a method of detecting and/or assaying nucleoside hydrolases or nucleoside phosphorylases using a chromogenic substrate. Preferred chromogenic substrates have formula (I) where X is OH, or H, and Y is the residue of Y—OH where Y—OH is a chromophore or a compound readily converted to a chromophore and the substrates are hydrolyzed by the nucleoside hydrolase to yield ribose or 2-deoxyribose plus Y—OH. Alternatively, those substrates may be phosphorylysed by nucleoside phosphorylase to yield ribose-1-phosphate plus Y—OH. The methods may be used to detect and/or assay parasites in biological samples.

Abstract: The invention concerns a method for purifying a composition containing at least a product for internal dehydration of a hydrogenated sugar. The invention is characterised in that it comprises: (a) an optional step whereby said composition is treated, whether after re-dissolving or not, with at least a discoloration means; (b) a subsequent step whereby the composition, optionally treated with discoloration means, is treated with at least ion-exchanging means; (c) a subsequent step whereby the resulting composition is treated with at least discoloration means. Said method is in particular applicable to isohexide compositions, in particular isosorbide or isomannide. The resulting compositions, which exhibit particular characteristics in terms of purity and proportion of some impurities, constitute novel products for use in chemical, pharmaceutical, cosmetology and food industries.

Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Abstract: Compounds of Formula (I): wherein R1, R2, R3, X, Y, Z and Q are as defined in the specification which compounds are inhibitors of Ras farnesyl-protein transferase enzyme (FPTase), and useful in treating ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid and processes for the preparation of said compounds of Formula (I).

Abstract: Compounds of formula (I): 1

Abstract: Primary intermediates for hair coloring compositions for oxidative dyeing of hair are compounds of the formula (1): wherein R is hydrogen, hydroxy, nitro, amino, halogen, C1 to C5 alkyl or haloalkyl, C1 to C5 alkoxy or cyclic alkoxy, C1 to C5 hydroxyalkyl and C1 to C5 hydroxyalkoxy; Ar is an aromatic group, preferably an aromatic group selected from a furanyl, thienyl, pyridinyl, phenyl, 2,3-dihydro-benzo[1,4]dioxin-5 or -6-yl or benzo[1,3]dioxol-4 or -5-yl group; and y=1 to 3.

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.

Abstract: The present invention relates compounds of the formula (1): wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.

Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.

Abstract: The present invention relates to a 2-fluoro-2-(3-oxobicyclopentyl)acetate derivative represented by the formula (1): 1

Abstract: Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.

Abstract: A new, more efficient and highly stereospecific process is described for the preparation of compounds with general formula (R)-(I) and of absolute configuration (R), where the groups M, W, Q and Q1 are as defined in the description, starting from compounds of absolute configuration (S) by hydrolysis, in the presence of acids, of the corresponding esterified derivatives. The (R)-(I) products obtained with the process described herein are chiral synthons useful for the production of enanthiomerically pure drugs. The preparation of (R)-carnitine is also provided.

Abstract: The invention relates to a compound of formula Ia, Ib or Ic 1

Abstract: P51084 The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.