Abstract: Polymeric articles containing at least one polymeric material and a sufficient amount of at least one novel hindered amine light stabilizers to inhibit at least one of photo- or thermal degradation. The hindered amine light stabilizer may be a monomeric or an oligomeric hindered amine light stabilizer.

Abstract: A crystalline salt according to formula (1): or the opposite enantiomer thereof, wherein X+ is a cation. Such salts are useful in preparing chiral scaffolds, in particular of formulae (a)-(d).

Abstract: Drugs or reagents containing as the active ingredient N-acyloxylated cycloalkyl compounds represented by general formula (I): wherein A is optionally substituted C4 or C5 cycloalkyl which may have one double bond in the ring; and R is C1-C3 alkyl or phenyl). The above compounds are hydroxyamine derivatives functioning as spin trapping agents and can rapidly react with free radicals or active oxygen in an objective organ in spite of their being excellent in stability during the preparation or administration thereof.

Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.

Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereosomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: The present invention relates to a process for the preparation of compounds of formula I 1

Abstract: The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive &pgr;-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples of catalysts for nucleophilic additions that comprise a main-group metal and a tri- or tetra-dentate ligand.

Abstract: The present invention relates to selected 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,3,6 trimethyl piperidine derivatives which are substituted in the 4 position by an oxygen or nitrogen atom; a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) said piperidine derivatives. Further aspects of the present invention are a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-2,2 diethyl-6,6 dimethyl piperidine and 1-alkoxy-2,6 diethyl-2,6 dimethyl piperidine derivatives which are substituted in the 4 position by an oxygen or nitrogen atom for controlled polymerization. The intermediate N-oxyl derivatives, a composition of the N-oxyl derivatives with ethylenically unsaturated monomers and a free radical initiator, as well as a process for polymerization are also subjects of the present invention.

Abstract: The present invention relates to a photo-stabilizer of the general formula (I): 1

Abstract: The present invention provides a process for the preparation of amine oxide by reacting a tertiary or a secondary amine with hydrogen peroxide as an oxidant in the presence of a recyclable heterogeneous catalyst comprising a layered double hydroxide exchanged with an anion in the presence of an additive selected from the group consisting of benzonitrile, propionitrile, isobutyronitrile, benzamide and isobutyraride.

Abstract: This invention relates to (2R,3S,4R,5R)-2-amino-5-methylpiperidine-3,4-diol or a (2S,3S,4R,5R)-2-N-substituted-2-amino-5-methylpiperidine-3,4-diol represented by the general formula (I): wherein R1 and R2 each are a hydrogen atom, or R1 is a hydrogen atom and R2 is a lower alkanoyl group or a lower &ohgr;-trihaloalkanoyl group, or R1 and R2 together denote phthaloyl group, and a pharmaceutically acceptable salt thereof. Said compound can be prepared from a (2S,3S,4R)-5-N-protected-2,3,4-O-tri-protected-5-aminopentane-1,2,3,4-tetraol by multi-steps of reactions.

Abstract: Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: &agr;,&bgr;,&bgr;-Trifluorostyrene and derivatives thereof synthesized in two steps from 1,1,1,2-tetrafluoroethylene. In the first step, 1,1,1,2-tetrafluoroethylene is reacted with a base, a metal salt such as zinc chloride and an optionally amine to form a trifluorovinyl metal complex. In the second step, the trifluorostyrene or derivative is obtained by reacting the trifluorovinyl metal complex with an aryl transfer agent such as, for example, an aryl triflate or an aryl halide, in the presence of a metal catalyst and optionally a coordinating ligand. Both steps may be carried out in one reactor.

Abstract: The present application describes novel lactams and derivatives thereof of formula I: 1

Abstract: A process is provided for the preparation of cyclic lactams of formula (II): 1

Abstract: The invention relates to a method for producing cyclic lactams of formula (II) by reacting a compound (I) of formula (I) with water in the presence of an organic, liquid dilution agent in the liquid phase. In formula (II), n and m respectively can have the values 0, 1, 2, 3, 4, 5, 6, 7, 8 and 9 and the sum of n+m is at least 3, preferably at least 4 and R1 and R2 represent C1-C6 alkyl, C5-C7 cycloalkyl or C6-C12 aryl groups. In formula (I), R1, R2, m and n are defined as above and R represents nitrile, carboxylic acid amide and carboxylic acid groups. The inventive method is characterized in that a) compound (I) is reacted with water in the liquid phase in the presence of an organic, liquid dilution agent (III) to form a mixture (IV) containing a lactam (II) and said mixture (IV) is subjected to an aqueous treatment to obtain a two-phase system.

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: Potent inhibitors of fatty acid amide hydrolase (FAAH) are constructed having K1's below 200 pM and activities 102-103 times more potent than the corresponding trifluoromethyl ketones. The potent inhibitors combine several features, viz.: 1.) an &agr;a-keto heterocylic head group; 2.) a hydrocarbon linkage unit employing an optimal C12-C8 chain length; and 3.) a phenyl or other &pgr;-unsaturation corresponding to the arachidonyl &Dgr;8,9/&Dgr;11,12 and/or oleyl &Dgr;9,10 positions. A preferred &agr;-keto heterocylic head group is &agr;-keto N4 oxazolopyridine, with incorporation of a second weakly basic nitrogen. Fatty acid amide hydrolase is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors).

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

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. In particular, the present invention relates to chemical compounds of formula (I) wherein: R1 may be the same or different and are independently selected from hydrogen, alkoyl, alkoxy, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor, R2 may be the same or different and are independently selected from alkyl groups; n is an integer 1, 2 or 3; or a salt thereof.

Abstract: A general, efficient, and environmentally friendly method is provided for producing mostly &bgr;-epoxides of &Dgr;5-unsaturated steroids using certain ketones as the catalyst along with an oxidizing agent, or by using certain dioxiranes. In another aspect of the invention, a method is provided for producing mostly 5&bgr;,6&bgr;-epoxides of steroids from &Dgr;5-unsaturated steroids having a substituent at the 3&agr;-position by an epoxidation reaction using a ketone along with an oxidizing agent under conditions effective to generate epoxides, or using a dioxirane under conditions effective to generate epoxides. A whole range of &Dgr;5-unsaturated steroids, bearing different functional groups such as hydroxy, carbonyl, acetyl or ketal group as well as different side chains, were conveniently converted to the corresponding synthetically and biologically interesting 5&bgr;,6&bgr;-epoxides with excellent &bgr;-selectivities and high yields.

Abstract: The present invention relates to N-alkylpiperidine derivatives represented by general formula (1) or (2); wherein R1 represents optionally fluorinated lower alkyl; R2 represents lower alkyl; and R3 represents alkenyl substituted at the 1-position with hydroxy, lower alkoxy, lower alkoxyalkyloxy, lower alkoxyalkyloxyalkyloxy, or lower alkanoyloxy and substituted at the end with radioactive iodine, or alkenyloxymethyl substituted at the end with a radioactive iodine reagent containing the same for assaying central local AchE activity; a method for assaying the central local AchE activity; and labeled precursors of the above compounds. After easily passing through the blood-brain barrier, these compounds are hydrolyzed specifically by AchE in the brain into alcohols, which are then captured by the brain. In contrast, alcohols formed outside the brain do not migrate into the brain. The compounds of the invention emit &ggr;-rays at an appropriate energy level.

Abstract: Compounds of formula (I) wherein R4 is an ester or thioester group and R, R1, R2 and R3 are as defined in the specification, inhibit proliferation of tumor cells.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: Compounds and methods of preparing compounds of the formula: RZ—CO—CRaRb—(CRcRd)n—NH—(Y)m—CO—A  (I) wherein n is an integer from 1 to 15, m is either 0 or 1; Ra, Rb, Rc, and Rd are each a hydrogen or a hydrocarbyl group; Y is CO—(CReRf)p, wherein Re and Rf are each a hydrogen or hydrocarbyl group and p is zero or an integer from 1 to 20 or CO—C6H4—, wherein the substitution pattern on the phenylene group is an ortho, meta, or para substitution pattern and one or more of the hydrogens of the phenylene group may be substituted by a hydrocarbyl group or a functional group; Z is —O— or —NG—, wherein G is H, C1-C12 alkyl or the radical R; wherein R is wherein R1 is hydrogen, C1-C18 alkyl, O, OH, CH2CN, C1-C18 alkoxy, C1-C18 hydroxyalkoxy, C5-C12 cycloalkoxy, C5-C12 hydroxycycloalkoxy, C3-C6 alkenyl, C1-C18 alkynyl, C7-C9 phenylalkyl, unsubstituted or substituted on the phenyl with 1, 2 or 3 C1-C4 alkyl

Abstract: Novel hindered amine light stabilizers of the formula wherein R1 is C1 to C8 alkyl, alkoxy, alkylphenyl, hydroxy alkyl, allyl, acyl, or cycloalkyl; R2 is hydrogen or methyl; R3 is vinyl or C1-4 alkyl vinyl; R4 is hydrogen, C1-4 alkyl or alkyl phenyl; R5 is hydrogen or C1-4 alkyl; and X is O, NH, C1-8 linear or branched chain or alkylamino, are prepared from the corresponding 1-unsubstituted, 4-XH-substituted piperidines by first reaction with a carbonyl compound and subsequent reaction with a vinyl group-containing acyl chloride.

Abstract: The present invention is concerned with an improved process for the manufacture of mixed anhydrides. The process comprises adding an adjuvant base to a mixture of acid and reactive acid derivative. It is especially suitable for use in the synthesis of peptides and/or for the manufacture of pharmaceutically active substances or corresponding intermediates.

Abstract: An improved process for preparing sulfonylcarboxamide derivatives of the formula I 1

Abstract: A process for the preparation of 1,5-dideoxy-1,5-imino hexitols of a hexose sugars from novel hydroxyl protected oxime intermediates. The process includes formation of a lactam which is reduced to the hexitol. The hexitols are useful as drugs.

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. For example, the present invention relates to chemical compounds of the formula: wherein R1 may be the same or different and are independently selected from hydrogen, alkoyl, alkoxy, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups and groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may the same or different and are independently selected from alkyl groups; n is an integer 1, 2 or 3; or a salt thereof.

Abstract: A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): The compounds are potentially useful as glycosidase inhibitors. The synthetic schemes comprise reacting a cyclic sulfate with a 5-membered ring sugar containing a heteroatom (X). The heteroatom preferably comprises sulfur, selenium, or nitrogen. The cyclic sulfate and ring sugar reagents may be readily prepared from carbohydrate precursors, such as D-glucose, L-glucose, D-xylose and L-xylose. The target compounds are prepared by opening of the cyclic sulfates by nucleophilic attack of the heteroatoms on the 5-membered ring sugars. The resulting heterocyclic compounds have a stable, inner salt structure comprising a heteroatom cation and a sulfate anion. The synthetic schemes yield various stereoisomers of the target compounds in moderate to good yields with limited side-reactions.

Abstract: The invention relates to a process for the preparation of 1,2,3,6-tetrahydro 2,2,6,6-tetramethylpyridine N-oxide by the catalytic oxidation of 1,2,3,6-tetrahydro-2,2,6,6-tetramethylpyridine, wherein 1,2,3,6-tetrahydro-2,2,6,6-tetramethylpyridine is oxidized with hydrogen peroxide in an aqueous medium in the presence of an alkaline earth metal salt or hydroxide as catalyst. The product is a polymerization inhibitor for monomers.

Abstract: A process for the synthesis of 2,2,6,6-tetramethyl-4-oxopiperidine is disclosed wherein the process comprises reacting in a liquid phase reaction mixture:

Abstract: The present invention relates to chemical compounds comprising a nitric oxide (NO) donor and a superoxide ion (O2−) scavenger, their preparation and their use in the treatment of conditions associated with oxidative stress or endothelial dysfunction. For example, the present invention relates to chemical compounds of the formula: wherein R1 may be the same or different and are independently selected from hydrogen, alkoyl, alkoxy, carboxy, hydroxy, amino, amido, cyano, nitro, thio, sulphonyl, sulphoxide alkyl groups and groups comprising an NO-donor, provided that at least one R1 is a group comprising an NO-donor; R2 may the same or different and are independently selected from alkyl groups; n is an integer 1, 2 or 3; or a salt thereof.

Abstract: Tertiary amines of the formula wherein A1, A2, A3, A4, M, p, T and Q are as defined herein, and acid addition salts thereof, have antimycotic and cholesterol-lowering activity.

Abstract: Compounds of the formula: 1

Abstract: A new process is described for the preparation of a compound of the formula I wherein R1, R2, R3 and R4, independently of each other, are C1-C8alkyl or C1-C5hydroxyalkyl, or R1 and R2 together with the carbon atom they are attached to are C5-C12cycloalkyl or R3 and R4 together with the carbon atom they are attached to are C5-C12cycloalkyl; R5, R6, R7, R8 and R9, independently of each other, are H, C1-C8alkyl, C2-C8alkenyl, C5-C12aryl, C1-C4haloalkyl, an electron withdrawing group, or C1-C12aryl which is substituted by a residue selected from C1-C4alkyl, C1-C4alkoxy, halogen; and R7 and R8 together may also form a chemical bond; and R is an organic linking group containing 2-500 carbon atoms and forming, together with the carbon atoms it is directly connected to and the nitrogen atom, a substituted, 5-, 6 or 7-membered cyclic ring structure; characterized in that a compound of the formula II is oxidized.

Abstract: Hindered amines substituted on the N-atom with an —O—E—OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal —O—E moieties.

Abstract: Pulps or papers, especially chemimechanical or thermomechanical pulps or papers, which still contain lignin, have enhanced resistance to yellowing when they contain an effective stabilizing amount of a N,N-dialkylhydroxylamine, an ester, amide or thio substituted N,N-dialkylhydroxylamine or N,N-dibenzylhydroxylamine or an amminium salt thereof. This performance is often further enhanced by the presence of one or more coadditives selected from the group consisting of the UV absorbers, the polymeric inhibitors, the nitrones, the fluorescent whitening agents and metal chelating agents. Combinations of hydroxylamines or their salts, benzotriazole or benzophenone UV absorbers and a metal chelating agent are particularly effective. N,N-Diethylhydroxylamine and N,N-dibenzylhydroxylamine and their acid salts are surprisingly effective for this purpose.

Abstract: 1

Abstract: Hindered amines substituted on the N-atom with an -O-E-OH moiety are particularly effective in stabilizing polyolefin and automotive coating compositions against the deleterious effects of oxidative, thermal and actinic radiation where the presence of the OH group on the compounds adds important properties not attainable by the use of normal -O-E moieties.

Abstract: The invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one sulfamic acid or salt thereof to inhibit bacterial adhesion to the submergible surface. The invention also relates to a method for controlling biofouling of an aqueous system. This method adds an effective amount of at least one sulfamic acid or salt thereof to inhibit bacteria from adhering to a submerged surface within the aqueous system. This method effectively controls biofouling without substantially killing the fouling organisms. The sulfamic acid used in the method of the invention has the formula R1R2NS(O)2(OH). In this formula, R1 and R2 are independently a hydrogen, a C4-C20 alkyl group or a cyclohexyl group. However, R1 and R 2 are not both hydrogen.

Abstract: Novel methods for the treatment and/or prophylaxis of diseases caused by tissue-adhering bacteria are disclosed. By interacting with periplasmic molecular chaperones it is achieved that the assembly of pili is prevented or inhibited and thereby the infectivity of the bacteria is diminished. Also disclosed are methods for screening for drugs as well as methods for the de novo design of such drugs, methods which rely on novel computer drug modelling methods involving an approximative calculation of binding free energy between macromolecules. Finally, novel pyranosides which are believed to be capable of interacting with periplasmic molecular chaperones are also disclosed.

Abstract: The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.

Abstract: Disclosed are novel N-oxyl compounds of the following formula (1). wherein n is an integer of 1 to 18; R1 and R2 are each hydrogen or methyl, but at least one of them is hydrogen; R3, R4, R5 and R6 are each a straight-chain or branched alkyl group; and R7 is hydrogen or (meth)acryloyl. When these compounds are added to vinyl monomers such as &agr;,&bgr;-unsaturated carboxylic acids and esters thereof, they exhibit a satisfactory polymerization-inhibiting effect even at low contents and even at elevated temperatures.