Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: Methods and compositions for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of systemic mastocytosis are disclosed. The compositions contain a mast cell stabilizing disulfide derivative as an active ingredient.

Abstract: Compounds of formula (I) 1

Abstract: A compound represented by the following general formula (1); wherein X represents R1(R2)(R3)C— where R1 represents a C3-C8 cycloalkyl group, an optionally substituted C6-C14 aryl group, an optionally substituted heterocyclic residue, an optionally substituted C6-C14 aryloxy group, or an optionally substituted C7-C15 arylmethyl group; R2 and R3 independently represent hydrogen atom or a C1-C5 alkyl group, or R2 and R3 may combine to represent a C2-C7 alkylene group; or X represents R7—A— wherein R7 represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or —N—R8 where R8 represents hydrogen atom or a C1-C5 alkyl group, Y represents an oxygen atom or a sulfur atom, R4 and R

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: The present invention is directed to nitrile-oxide precursor compounds, and their preparation and use as an irreversible cross-linking agent in polymers having appropriate functionality, i.e., alkenes, alkynes nitriles, and isocyanates. The present invention is also directed to the use of nitrile oxide compound in filled or unfilled applications such as pressure sensitive adhesives, reactive hot melts, polyurethane dispersions, thermosetting adhesives, thermoplastic adhesives or coatings.

Abstract: The present invention relates to a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for male hormone therapy such as oral testosterone replacement therapy, treating prostate cancer, imaging prostate cancer.

Abstract: Novel brain targeted low molecular weight, hydrophobic antioxidants and use of antioxidants in treatment of central nervous system neurodegenerative disorders such as Parkinson's, Alzheimer's and Creutzfeldt-Jakob's diseases and in treatment of conditions of peripheral tissues, such as acute respiratory distress syndrome, amyotrophic lateral sclerosis, atheroscierotic cardiovascular disease and multiple organ dysfunction, in which oxidants are overproduced.

Abstract: A novel process for the preparation of N,N′-bis[2,3-dihydroxypropyl]-5-[(hydroxyacetyl) methylamino]-2,4,6-triiodo-1, 3-benzenedi carboxamide of formula (I), commonly known as lomeprol, a novel non-ionic contrast agent which shows very good safety and contrast effectiveness.

Abstract: Disclosed are cathepsin S reversible inhibitory compounds of the formulas (I),(Ia) and (II),(IIa) as defined herein. The compounds are useful for treating autoimmune diseases. Also disclosed are processes for making such novel compounds.

Abstract: This invention relates to a method of preparing a compound type where at least one of R′ or R″ is a carboxyl group (I) by treating a compound of formula (II) with a Group I(a) or Group II(a) metal halide, with an aprotic dipolar amide-based solvent and water.

Abstract: Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula 1

Abstract: Novel perfluoroalkyl-substituted mono-, di- and poly-amide compounds which are reaction products of a mono-, di- or polyamine of 60 to 2000 molecular weight with a perfluoroalkyl substituted unsaturated acid or its corresponding lower alkyl ester and optionally a non-fluorinated amino-reactive compound such as an acid, ester, anhydride, epichlorohydrin, isocyanate or urea, are useful as internally or externally applied paper sizes to impart oil and grease resistance to paper, and as oil proofing coatings on textiles, wood, masonry and the like, or as high-performance surface active agents.

Abstract: A mono-, bi- and/or polyfunctional amide of the formulae (Ia) and/or (Ib),

Abstract: Method for preparing a combinatorial chemistry library of compounds of the formula R1—C(═O)—NH—R2, wherein R1 and R2 are as defined in the specification, which comprises acylating a combinatorial chemistry intermediate of the formula 1A wherein Y1, Y2, X, n, R1 and R2 are as defined in the specification to produce a compound of the formula wherein Y1, R1, R2 and X are as defined in the specification, followed by acidolytic cleavage of the resin bound linker to release the compound of the formula R1—C(═O)—NH—R2.

Abstract: Amphoteric derivatives of aliphatic polyamines, such as diethylenetriamine or bis (hexamethylene) triamine reacted with long chain fatty acids, esters or triglycerides from various natural or synthetic sources are effective in the softening/texture modification of substrates such as paper, textiles, human skin surfaces and hair tresses, as well as in applications for metal working and lubrication. The polyamines are first reacted with fatty acids, esters or triglycerides derived from various animal, vegetable or synthetic sources ranging in molecular distribution from butyric through erucic acids (e.g. milkfat, soy bean oil, rapeseed oil) to form amidoamines or imidazolines; and are then further reacted with unsaturated or carboxylated epoxy compounds (e.g. acrylic acid, itaconic acid, verndic) to form the various amphoteric structures.

Abstract: Triazine, benzotriazole and benzophenone derivatives which are substituted or bridged with polyoxyalkylene groups, according to claim 1, and their use as UV absorbers, especially in photographic materials, in inks, including inkjet inks and printing inks, in transfer prints, in paints and varnishes, organic polymeric materials, plastics, rubber, glass, packaging materials, in sunscreens of cosmetic preparations and in skin protection compositions.

Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Abstract: The present invention is directed to nitrile-oxide precursor compounds, and their preparation and use as an irreversible cross-linking agent in polymers having appropriate functionality, i.e., alkenes, alkynes nitrites, and isocyanates. The present invention is also directed to the use of nitrile oxide compound in filled or unfilled applications such as pressure sensitive adhesives, reactive hot melts, polyurethane dispersions, thermosetting adhesives, thermoplastic adhesives or coatings.

Abstract: A urethanized &bgr;-hydroxyalkylamide compound, a process for its preparation, and powder coating materials containing them.

Abstract: Substituted polycarboxylic ligand molecules and corresponding metal complexes of said ligands, preferably paramagnetic metals complexes for generating responses in the field of magnetic resonance imaging (MRI). The paramagnetic complexes of the polycarboxylic ligands possess advantageous tensioactive properties and are useful as MRI contrast media in formulations for investigating the blood pool.

Abstract: Compounds of Formula I are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or &agr;-hydroxyamide group and Z is an acyl or &agr;-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.

Abstract: Compounds of formula I wherein R1, R1-R3, R4′, R4″ and R5 are as defined in the description, have valuable pharmaceutical properties and are effective especially as NK1 and NK2 antagonists. They are prepared in a manner known per se.

Abstract: The present invention is directed to a process for the preparation of a compound of formula (X-a): or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted with 0-5 R1a, —(CH2)r—C3-10 cycloalkyl substituted with 0-5 R1a, and —(CH2)r-aryl substituted with 0-5 R1a. Compounds of Formula (X-a) are macrocyclic molecules containing anti-succinate residues which inhibit metalloproteinases such as aggrecanase, and the production of tumor necrosis factor (TNF). The anti-succinates are formed by an Ireland Claisen rearrangement of a silyl ketene acetal which proceeds with high stereoselectivity.

Abstract: There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.

Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: This invention features methods of biphasic synthesis for synthesizing combinatorial libraries and combinatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.

Abstract: The invention relates to a process for preparing a &bgr;-hydroxyalkylamide, in which alkyl esters are reacted with &bgr;-aminoalcohols in the absence of solvents and in the presence of basic catalysts, where, to improve the selectivity, the ratio of equivalents of ester to equivalents of amine is 1:1.001 to 8.

Abstract: Disclosed are a crystalline polypropylene resin composition comprising a crystalline polyproplylene resin and a &bgr;-nucleating agent, and a method of increasing the proportion of &bgr;-form crystals in a crystalline polypropylene resin molding comprising molding the composition, the &bgr;-nucleating agent being a diamide compound.

Abstract: The present invention relates to the composition, process of preparation, and use of novel derivatives prepared from 1,5-bis-(4′-carbomethoxyphenyl)-1,4-pentadien-3-one. These novel compositions can act as crosslinkers with polyfunctional monomeric, oligomeric, and/or polymeric anhydrides, esters, carboxylic acids, isocyantes, epoxies, carbonates, acetoacetates, and alkoxylated melamines.

Abstract: This invention features a template for synthesizing combinatorial libraries, methods of synthesizing combiatorial libraries of chemical compounds utilizing the template, and combinatorial libraries of chemical compounds formed by the methods of this invention.

Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.

Abstract: This invention is directed to a process for preparing a pseudotetrapeptide of formula I or a salt or prodrug thereof wherein is optionally nitrogen protected azaheterocyclyl; is a single or double bond; q is 1-5; B is alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl, or alkylaralkyl; Q2 is H or a carboxylic acid protecting group; J is —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, substituted aryl, aralkyl, substituted aralkyl; L is OR1, or NR1R2, where R1 and R2 are independently —H, alkyl, cycloalkyl, cycloalkylalkyl, alkylcycloalkyl, alkylcycloalkylalkyl, aryl, aralkyl, alkylaryl or alkylaralkyl; and p is 1 or 2 which comprises the coupling of two dipeptides or psuedopeptides.

Abstract: Disclosed are compounds which inhibit .beta.-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits .beta.-amyloid peptide release and/or its synthesis as well as methods for treating Alheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.

Abstract: The present invention relates to oligopeptidic compounds having the general formula (I):K--[--A--].sub.z --[--B--].sub.w --L (I)The compounds having general formula (I) are antifungals for agricultural purposes.

Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.

Abstract: Disclosed is a new process for the crystallization of (S)-N,N'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)a mino]-2,4,6-triiodo-1,3-benzendicarboxamide (I), using a linear or branched (C5-C6) alcohol or their mixtures.

Abstract: The present invention relates to a process for the preparation of compounds of the formula 1 ##STR1## by reacting a secondary acid amide of the formula 2 ##STR2## with an acid chloride of the formula 3 ##STR3## in the presence of N,N-diisopropyl-N-ethylamine. R.sup.1, R.sup.2 and R.sup.3 are alkyl or alkenyl radicals, if required also aryl radicals. The compounds of the formula 1 are suitable for use as insecticides or bleach activators.

Abstract: The following description concerns a therapeutic method for the treatment of diseases connected with the modulation of the cannabinoid peripheral receptor, comprising administering amidic derivatives of mono and bicarboxylic acids with aminoalcohols or arninoethers selectively active on said receptor.

Abstract: A logically ordered array of 10,240 different compounds, each compound prepared from the reaction product of an oxazolone, aldehyde and amine.

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated salts of inorganic and organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: The invention relates to novel substituted amino acid amides, to a process for their preparation and to their use as pesticides.

Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.

Abstract: The present invention relates to derivatives of 2,2,3,3-tetramethylcyclopropane carboxylic acid (TMCA) of general formula (I), ##STR1## wherein R is lower alkyl group (C.sub.1 -C.sub.6), an aryl group, an aralkyl group or an amide of general formula (II), ##STR2## where R.sub.1 and R.sub.2 are the same or different and may be hydrogen, a alkyl group (C.sub.1 -C.sub.6), an aryl group or an aralkyl group, and n=0-3, to their racemic mixtures and the D and L enantiomers. The invention also relates to processes for the preparation of said compounds and for pharmaceutical preparations comprising the same. The new compounds show improved activity against epilepsy.

Abstract: A cyclopropane-1,1-dicarboxylic acid compound is prepared by reacting a malonic acid compound and a 1,2-dihalogeno compound with an alcoholate as a condensation agent which is gradually added to a mixture of said malonic acid compound and said 1,2-chloro compound as a solution or suspension is an alcohol.

Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.

Abstract: Imide compounds having a propioloyl group or pharmaceutically acceptable salts thereof which exhibit potent activities to inhibit the production of Interleukin 1-.beta. and also the production of Tumor Necrosis Factor .alpha.. These imide compounds are useful as a prophylactic or therapeutic agent for inhibiting the production of Interleukin 1-.beta. and the production of Tumor Necrosis Factor .alpha., typically for such diseases as chronic rheumatism, sepsis, ulcerative colitis, Crohn's disease and many other related diseases in which Interleukin 1-.beta. and/or Tumor Necrosis Factor .alpha. would participate.

Abstract: The present invention relates to benzamidoxime derivatives represented by the formula ?I!; ##STR1## wherein R.sup.1 is unsubstituted or substituted C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted C.sub.2 -C.sub.4 alkenyl or unsubstituted or substituted C.sub.2 -C.sub.4 alkynyl, R.sup.2 is phenyl optionally having substituents or heterocycle optionally having substituents, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are each independently hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylthio or the like, and r.sub.1 and r.sub.2 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl or the like, having excellent fungicidal activity and being useful as a fungicide for agricultural and horticultural use, and methods for preparation thereof.

Abstract: A process for purifying Iopamidol which uses a butanol as solvent is described. Iopamidol is obtained with high yields, also starting from aqueous solutions of the same and has characteristics in accordance with those required by pharmacopoeia.