Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.

Abstract: The present invention relates to a process for the preparation of zeolitic catalysts comprising zeolite and oligomeric silica, which can be used in industrial reactors. The process consists in directly mixing the suspension, resulting from the synthesis of the zeolite, with an oligomeric silica sol, obtained from the hydrolysis of a tetra-alkyl ortho silicate in the presence of tetra-alkylammonium hydroxide, and in subjecting the mixture to rapid drying, by feeding to a spray-dry.

Abstract: Disclosed are retiferol derivatives of formula (I): wherein X is >C═CH2 or —CH2—; Y and Z are independently of each other hydrogen, fluorine or hydroxy; A is —O(CH2)3—, —(CH2)2-(1,2-C6H4)—, —CH═CH—(1,2-C6H4)—, —C═C—(1,2C6H4)—, —(CH2)2—CO—, —CH2—O—CO—, —CH2NHCO—, or —CH2NHCOCH2—; R1 is C1-C5-alkyl; R2 and R3 are independently of each other alkyl or perfluoroalkyl; and R4 is hydrogen, hydroxy, C1-C5-alkyl or C1-C5-alkyl or C1-C5-alkoxy; the use of such compounds to treat or present hyperproliferative skin diseases such as psoriasis, basal cell carcinomas, disorders of keratinization and keratosis; neoplastic diseases; disorders of the sebaceous glands such as acne and seborrhoic dermatitis; the use of these compounds in reversing the conditions associated with photodamage, particularly for the oral or topical treatment of the skin damaged through sun exposur

Abstract: Methods are disclosed of producing and purifying at least one amide. In accordance with one of the methods disclosed herein, the at least one amide is produced by providing an organic liquid comprising at least one oxime, providing at least one catalyst, adding the at least one catalyst to the organic liquid to form a rearrangement mass, wherein the rearrangement mass comprises at least one amide, at least one impurity, and the at least one catalyst, and heating the rearrangement mass to a temperature of at least about 115° C. for a period of time in order to sulfonate, break down and/or reduce the concentration of some of the at least one impurity in the rearrangement mass.

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: A biodegradable, novel cationic lipopolymer comprising a branched polyethylenimine(PEI), a cholesterol derived lipid anchor, and a biodegradable linker which covalently links the branched PEI and cholesterol derived lipid anchor. One example of such a novel lipolymer is poly{(ethylene imine)-co-[N-2-aminoehtyl)ethylene imine]-co-[N-(N-cholesteryloxycabonyl-(2-aminoethyl))ethylene imine]} (“PEACE”). The cationic lipopolymers in the present invention can be used in drug delivery and are especially useful for delivery of a nucleic acid or any anionic bioactive agent to various organs and tissues after local or systemic administration. Methods of preparing and using the cationic lipopolymer gene carriers of the present invention to efficiently transfect cells, both in vitro and in vivo, are disclosed.

Abstract: The present invention relates to compounds of formula (I) wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: The invention relates to a compound comprising a reaction product of (A) an isocyanate functional compound of which at least 40 wt. %, relative to the total amount of (A), has a molecular weight of at least about 500, and (B) a nitrogen-containing compound capable of reacting with said isocyanate functional compound (A). The reaction product has a molecular weight of less then about 20,000 and comprises an effective amount of groups that are able to form reversible intermolecular physical interactions such that a resulting compound shows polymeric mechanical properties at a temperature below a transition temperature. The nitrogen-containing compound is, for instance, melamine, urea, acetoguanamine, benzoguanamine, cyanamide, dicyanamide, thiourea, isocytosine, pyrimidone or aminopyridine. The supramolecular compound comprising a suitable amount of the reaction products exhibits a relatively high elongation at break.

Abstract: This invention relates to colorants comprising a chromophore having a single azo acetoacetanilide moiety, wherein said moiety each have at least one poly(oxyalkylene) chain. Such colorants exhibit extremely good base stability and lightfastness, particularly when incoporated within certain media and/or on the surface of certain substrates. These poly(oxyalkylene) chains provide solubility in different solvents or resins thereby permitting the introduction of such excellent coloring chromophores within diverse media and/or or diverse substrates. Compositions and articles comprising such colorants are provided as are methods for producing such inventive colorants.

Abstract: The present invention relates to a process for the preparation of N-phosphonomethylglycine by reacting a hexahydrotriazine derivative with a triacyl phosphite. The process gives N-phosphonomethylglycine in high yield and in a simple and inexpensive manner.

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: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: Compounds of the formula R2.[(AO)n.R3]m, where R2 is a residue of a group having at least m active hydrogen atoms derived from hydroxyl and/or amino and/or amido groups, AO is alkyleneoxy, n is 2 to 200; R3 includes residue(s) of alkenyl succinic acids and optionally other acids, and m is 2 to 10, but when m is 2 there are other restrictions in the definitions, are disclosed as useful thickeners and/or dispersants in aqueous systems. The use of such materials as thickeners is also disclosed.

Abstract: The invention relates to trifluoromethyl sulfonyl and trifluoromethyl sulfonamido compounds and the physiologically acceptable salts and the prodrugs thereof. These compounds are expected to modulate the activity of protein tyrosine enzymes which are related to cellular signal transduction, in particular, protein tyrosine phosphatase, and therefore are expected to be useful in the prevention and treatment of disorders associated with abnormal protein tyrosine enzyme related cellular signal transduction such as cancer, diabetes, immuno-modulation, neurologic degenerative diseases, osteoporosis and infectious diseases. The invention also relates to the use of compounds containing fluoromethyl sulfonyl groups as phosphate mimics. These mimics may be used to inhibit, regulate or modulate the activity of a phosphate binding protein in a cell.

Abstract: Methods for producing amide derivatives of the formula [XV] are described. These derivatives are useful as HIV protease inhibitors. wherein R4 is an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted aralkyl or an optionally substituted heteroarylalkyl, R6 and R7 are the same or different and each is a hydrogen atom, an optionally substituted alkyl, an optionally substituted aryl, an optionally substituted heteroaryl or an optionally substituted aralkyl, or R6 and R7 combinedly form, together with the adjacent nitrogen atom, a hetero ring, said hetero ring being optionally substituted by halogen atom, alkyl, alkenyl, alkoxy, amino, alkoxycarbonyl, carboxamide or alkyl-substituted carbamoyl, and R8 is a hydrogen atom, an alkyl, an optionally substituted aryl or an optionally substituted aralkyl, or an enantiomer thereof.

Abstract: The present invention relates to a process for the preparation of zeolitic catalysts of the MFI type in spheroidal form.

Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an &agr;,&bgr;-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an &agr;,&bgr;-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.

Abstract: The present invention relates to blocked polyisocyanate cross-linking agents and their use in one-component stoving lacquers, in particular in solvent-containing or predominantly water-based plastics coatings having a soft-feel effect.

Abstract: The invention is to provide a process for effectively removing impurities contained in an amide compound-containing solution by making an amide compound-containing solution, particularly an amide compound-containing solution produced by a hydration reaction of a nitrile compound by using a microorganism fungus body containing nitrile hydratase or a processed product of the microorganism fungus body, in contact with activated carbon under acidic conditions.

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.

Abstract: This invention relates generally to bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.

Abstract: Disclosed is an improved method for preparing an activated carboxylic acid in the form of a pentafluorophenyl ester, an improved method for making a carboxamide from a pentaflourophenyl ester, and a carboxamide and carboxamide library prepared using both of these methods.

Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.

Abstract: The invention relates to novel amino- and amido-diphenyl ethers, processes for their preparation and their use in pharmaceuticals, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: The present invention relates to compounds of the formula I in which A1, A2, R2 and R3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular disorders such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance. The invention relates to the use of compounds of the formula I for the therapy and prophylaxis of the designated disease states and for the production of pharmaceuticals therefor, novel compounds of the formula I, pharmaceutical preparations comprising them and processes for their preparation.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: Disclosed are novel multibinding compounds (agents) which bind macromolecular structures including cellular, extracellular, and microbial components derived from vectors, viruses, fungi, yeasts, bacteria, and the like. The compounds of this invention comprise a plurality of ligands each of which can bind to such macromolecular structures thereby modulating the biological processes/functions thereof. Each of the ligands is covalently attached to a linker (framework) to provide for the multibinding compound. The linker is selected such that the multibinding compound so constructed demonstrates increased modulation or disruption of the biological processes/functions of cell as compared to the aggregate of the individual units of the ligand.

Abstract: The present invention provides a dye precursor for forming color through contact with a base and which is represented by either of the following formulas (1) and (2): wherein Ar represents an aromatic ring or a heterocyclic ring, each of which may have a substituent; Cp represents a coupler residue; L1 represents a protective group which can be eliminated by a base; and L2 represents an elimination group or a protective group which is eliminated after L1 is eliminated. Further, the present invention provides an image forming material and an image forming method, wherein the image forming material has an image forming layer on a support, the image forming layer containing at least one type of each of a photopolymerization initiator, a dye precursor which can form color through contact with a base, a base or a base precursor, and a polymerizable compound.

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst diols of the general formula (I) 1

Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.

Abstract: A process for preparing N-alkenyl-amides by reacting the corresponding NH-amides with acetylenes in the liquid phase in the presence of basic alkali metal compounds and of a cocatalyst comprises using as the cocatalyst compounds of the general formulae (Ia) and/or (Ib)

Abstract: The present invention relates to the formation of an amido ester having the formula: R1—CO—NR3—R2—COL or R1—NR3—CO—R2—COL wherein R1 is C1-C12 linear or branched alkyl, C6-C14 aryl, C7-C14 alkyl substituted aryl unit; R2 is C1-C14 alkylene, C6-C14 arylene, C7-C14 alkyl substituted arylene; R3 is hydrogen, C1-C10 alkyl, C6-C10 aryl, C7-C10 alkyl substituted aryl, L is a aryl leaving group having the formula: R4 comprises one or more anionic or cationic units, wherein said compound is formed using a spinning disc reactor.

Abstract: N,N diacyl O-substituted imide bleach activators and compositions employing them are provided. The activators have the general formula: wherein X is selected from O, NR16 and S; e is 0 or 1; f is 0 or 1; R16 is selected from H and C1-C4 linear or branched, saturated or unsaturated alkyl groups; and R1 is preferably phenyl or C7-C13 linear or branched chain, saturated or unsaturated alkyl; R2 is preferably C1-C10 branched or unbranched, saturated or unsaturated alkyl and R3 is preferably C1-C12 linear or branched chain, saturated or unsaturated alkyl. Bleach additive and bleaching compositions including the bleach activators and methods of cleaning fabrics are also provided.

Abstract: The invention relates to an oral drug delivery system which delivers biologically active substances to the mucosal tissue of the intestine utilizing novel polymerized liposomes. Novel polymerizable fatty acids having a polymerizable group, a surfactant group, and a functional group, and optionally coupled to ligands which target mucosal tissue in the intestine are disclosed. Novel negatively charged polymerizable lipids which have phosphatidyl inositol (PI), phosphatidyl glycerol (PG) or phosphatidyl serine (PS) groups on a polymerizable backbone are also described.

Abstract: Processes for oxidizing hydrocarbons using a new family of crystalline manganese phosphate compositions have been developed. These compositions have an extended network which network can be a one-, two-, or three-dimensional network. The composition has an empirical formula of: (Aa+)v(Mnb+)(Mc+)xPyOz where A is a structure directing agent such as an alkali metal, M is a metal such as Al, Fe3+ and “b” is the average manganese oxidation state and varies from greater than 2.0 to a maximum of 3.0. Specific oxidation processes are oxidative dehydrodimerization and oxidative dehydrogenation.

Abstract: D- and L- &agr;-amino acids and D- and L-&agr;-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant &bgr;-hydoxycarbamate is deprotected to yield the corresponding &bgr;-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant &bgr;-hydroxysulfonamide is deprotected to yield the corresponding &bgr;-hydroxyamine.

Abstract: A process for producing an amide compound of the following formula by reacting a nitrile compound of the formula with an acid to obtain an oxazolinone compound of the formula and reacting the oxazolinone compound with a carboxy compound of the formula in the presence of a base.

Abstract: The invention relates to an oral drug delivery system which delivers biologically active substances to the mucosal tissue of the intestine utilizing novel polymerized liposomes. Novel polymerizable fatty acids having a polymerizable group, a surfactant group, and a functional group, and optionally coupled to ligands which target mucosal tissue in the intestine are disclosed. Novel negatively charged polymerizable lipids which have phosphatidyl inositol (PI), phosphatidyl glycerol (PG) or phosphatidyl serine (PS) groups on a polymerizable backbone are also described.

Abstract: The present invention relates to peptide-like compounds, eg aminocarboxylic acid amide derivatives, and to methods of using same to stimulate cells of the immune system, bone marrow and other organs. The present compounds can be used to enhance vaccination, increase synthesis of and enhance function of blood cell components and enhance anti-neoplastic effects of various agents. The compounds of the invention can be used to produce a variety of further pharmacologic effects.

Abstract: The invention relates to a process for the preparation of carboxamides, in particular peptides, from an acid component in the form of a compound containing at least one carboxyl group and an amine component in the form of a compound containing at least one primary or secondary amino group, and its use.

Abstract: Disclosed are methods for treating or preventing inflammatory bowel disease (IBD) using amide and related compounds. Pharmaceutical compositions containing amide compounds which are useful for the treatment or prophylaxis of IBD are also disclosed.

Abstract: A solid acid-base catalyst contains vanadium pentoxide hydrate. Moreover, it is preferable that the vanadium pentoxide hydrate in the solid acid-base catalyst has a composition which is represented by the following general equation (1): V2O5.nH2O  (1) (n: 0.1-3). Creation of the vanadium pentoxide hydrate was confirmed by measuring X-ray diffraction spectrum shown in FIG. 1. In accordance with the above arrangement, the solid acid-base catalyst can sufficiently display catalytic activity under mild conditions, and it can be suitably applied to various reactions, such as the syntheses of olefins or ethers through dehydration reactions of alcohols, the syntheses of aldehydes or ketones through dehydrogenation reactions of alcohols, hydrations and isomerization reactions of olefins, alkylations, esterifications, amidations, acetalizations, aminations, hydrogen shift reactions, aldol condensation reactions and polymerization reactions.

Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanedlyl, Ar represents optionally substituted aryl, R1 represents optionally substituted alkyl and R2 represents hydrogen, halogen or alkyl, and to novel intermediates for this purpose and to processes for their preparation.

Abstract: The present invention relates to (2S)-enantiomers of 2-aminoindan derivatives of formula I: 1

Abstract: A method of preparing carboxylic acid derivatives comprising mixing a quaternary ammonium salt having a particular triazine ring in the molecules thereof, a carboxylic acid compound and a compound having a nucleophilic functional group, to condense the carboxylic acid with the compound having the nucleophilic functional group. The invention further provides a condensing agent comprising the quaternary ammonium salt. The condensation is conducted under mild conditions to form carboxylic acid derivatives and, particularly, amide compounds or ester compounds maintaining high yields.

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: The invention relates to novel cationic 2-acylaminophenols of formula (I) comprising at least one cationic group, to their use as couplers for the oxidation dyeing of keratin fibers, and in particular of human keratin fibers such as the hair, to oxidation dye compositions containing them in combination with at least one oxidation base, and to oxidation dyeing processes using them.

Abstract: The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.

Abstract: A compound, of the following formula: Also disclosed is a pharmaceutical composition containing a pharmaceutically effective amount of the compound.

Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.