Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: The present invention relates to novel carbamates, ureas, and pharmaceutically acceptable salts thereof, compositions comprising the carbamate, urea, or a pharmaceutically acceptable salt thereof, and methods for treating or preventing cancer, inflammation, or a viral infection comprising administering to a patient in need of such treatment or prevention a therapeutically effective amount of the carbamate, urea, or pharmaceutically acceptable salt thereof.

Abstract: Serine carbonates of formula I are precursors for organoleptic compounds, masking agents and antimicrobial agents. Further they are alternative substrates for malodor producing enzymes. The symbols in formula I are defined in claim 1.

Abstract: Disclosed are polyester-ether polyols and their use in urethane prepolymers, urethane foams and non-foam urethane coatings, adhesives, sealants and/or elastomers. Methods for producing such polyester-ether polyols are disclosed, along with methods for producing urethane prepolymers. The polyester-ether polyols of the instant invention are preferably the reaction product of phthalic anhydride, diethylene glycol, and propylene oxide. These polyester-ether polyols are useful as either the primary polyol in urethane compositions or in combination with conventional auxiliary polyester- and/or polyether-based polyols. The polyester-ether polyols impart greatly improved solubility and compatibility to mixtures of either polyether and/or polyester polyols. The polyester-ether polyols of the instant invention are desirably of lower viscosity than their precursor intermediate polyester polyols and are generally soluble in either polyester- and/or polyether-based polyols.

Abstract: Branched, substantially non-antigenic polymers are disclosed. Conjugates prepared with the polymers and biologically active molecules such as proteins and peptides demonstrate extended circulating life in vivo. Substantially fewer sites on the biologically active material are used as attachment sites. Methods of forming the polymer, conjugating the polymers with biologically active moieties and methods of using the conjugates are also disclosed.

Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: The present invention is for a new class of allyl urethane resin which can be cured with peroxide at high temperature alone or in combination with some accelerators. These allyl urethane resins can be sued alone or in combination with other free radically polymerizable materials such as allyl monomers and ligomers or (meth)acrylate monomers and oligomers. These new allyl urethane resins contain at least two allyl functional groups.

Abstract: Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.

Abstract: The invention relates to a method for making oligomeric isocyanates by reacting diisocyanates in the presence of a catalyst, wherein the catalyst comprises a saline compound prepared from a five-membered N-heterocycles and the N-heterocycle comprises at least one N-H function in the five-membered ring, to the products produced in this way and to polymers prepared from these products.

Abstract: The present invention relates to a dimeric urethane compounds derived from monohydric alcohols, generally fatty alcohols, and a diisocyanate according to the following reaction scheme: 1

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: The invention provides a process for preparing an allophanate-containing compound in the presence of a metal catalyst and a tertiary amine. In a preferred process, the tertiary amine compound also has a hydroxyl group. The hydroxyl group can react with the isocyanate functionality. Also disclosed is a process in which an allophanate-containing compound is prepared with copper acetate monohydrate as a catalyst. The allophanate-containing compound is used as a curing agent in coating compositions, particularly electrocoat coating compositions. The coating compositions are used to coat articles.

Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.

Abstract: A powder coating composition comprising a powdered solid ethylenically unsaturated material having a melting point from 60° to 120° C. obtained by reacting a polyisocyanate with an at least stochiometric amount of an alcoholic component comprising: at least a monovalent alcohol, a part of which bears an ethylenic unsaturation derived from acrylic acid or methacrylic acid, and optionally at least a monomeric polyol. This composition is useful for coating substrates.

Abstract: A purpose of the present invention is to provide TNF-&agr; production inhibitors being useful as therapeutic agents for autoimmune diseases such as rheumatoid arthritis.

Abstract: Fluorochemical urethane compositions comprising one or more compounds or oligomers having at least on fluorine-containing repeatable unit and at least one fluorine-containing terminal group are described. The compositions are useful as coatings or incorporated as melt additives. The fluorochemical compositions impart oil and water repellency to the substrate. In other aspects, this invention relates to processes for imparting oil and water repellency characteristics to substrates and articles.

Abstract: A low-monomer PU prepolymer containing free NCO groups which is obtained from polyhydric alcohols and diisocyanates differing in their reactivity and which is distinguished by the ratio of the NCO groups of the partly slower-reacting diisocyanate to the NCO groups of the faster-reacting diisocyanate. It is greater than 6:1. Nevertheless the prepolymer according to the invention cures more quickly than a known prepolymer predominantly containing fast-reacting NCO groups. In a preferred embodiment, TDI is used as the partly slower-reacting diisocyanate while MDI is used as the faster-reacting diisocyanate. The prepolymer is produced in two stages. The prepolymer according to the invention is suitable for bonding plastic articles, metals and paper, especially films. The accelerated absence of migration is particularly noticeable in this regard.

Abstract: A method of forming a methylol urea prepolymer and a particle coated in with the prepolymer. The method involves providing a source of methylol urea and a source of aldehyde and reacting the urea and the aldehyde in the presence of an excess of urea to form the methylol urea prepolymer. The coated particle is preferably a controlled-release fertilizer particle. The particle is a substrate coated with a substantially uniform coating comprising a total nitrogen content ranging from about 39N to about 42N. The coating includes a low molecular weight methylene urea compounds.

Abstract: Methods are disclosed for prophylactically and chronically preventing symptomatic depression, neuronal cell injury and cell death in systemic and neurological conditions, populations with cerebrovascular risk factors, and invasive vascular procedures, employing a glycine-site antagonist at the NMDA (N-methyl-D-aspartate) complex e.g., 2-phenyl-1,3-propanediol dicarbamate (felbamate).

Abstract: The invention relates to positional isomer diethyloctandioldicarbamates and diethyloctandioldiallophanates, to a method for the production thereof and to the use thereof as synthetic building blocks and constituents of adhesives, luting compounds and coating materials.

Abstract: This invention pertains generally to valency molecules, such as valency platform molecules which act as scaffolds to which one or more molecules may be covalently tethered to form a conjugate. More particularly, the present invention pertains to valency platform molecules which comprise a carbamate linkage (i.e., —O—C(═O)—N<). In one aspect, the present invention pertains to valency platforms comprising carbamate linkages, which molecules have the structure of any one of Formulae I, II, or III, shown in FIG. 1. In one aspect, the present invention pertains to valency platforms comprising carbamate linkages, which molecules have the structure of any one of Formulae IV, V, or VI, shown in FIG. 8. The present invention also pertains to methods of preparing such valency platform molecules, conjugates comprising such valency platform molecules, and methods of preparing such conjugates.

Abstract: The present invention relates to blocked fluorine-containing polyisocyanates which have a fluorine content, calculated as F=19, of 1.0 to 20.0 wt. %, preferably 4.0 to 10.0 wt. %, and are suitable for preparing stoving coatings having a water- and soil-repellent surface, wherein the fluorine-containing polyisocyanates are based on the reaction product of aliphatic polyisocyanates or polyisocyanate mixtures having an NCO content of 10 to 25 wt. % and a functionality of at least 2.5 with monofunctional isocyanate blocking agents and a fluorinated monoalcohols wherein i) 75 to 95 equivalent-% of the isocyanate groups are reacted with isocyanate blocking agents, ii) 5 to 25 equivalent-% of the isocyanate groups are reacted with fluorinated monoalcohols and iii) the equivalents of i) and ii) add up to 100%.

Abstract: Pigment dispersants prepared by reacting an isocyanate oligomer having an average functionality of at least three with a polyester or polyacrylate, a poly(ethylene glycol)alkyl ether, and a diamine having a primary amine and a tertiary amine have excellent stabilizing properties and offer a wide formulation latitude with a variety of solvent systems, including polar solvents and water, and are particularly useful as pigment dispersants for paints and coating applications.

Abstract: Helical oligomer and polymer compositions that form nanotubes are described. The compositions comprise a plurality of aromatic substituents linked by at least one amide group. The compositions have a curved backbone due to intramolecular hydrogen bonds that rigidify the amide linkage of each amide group to each aromatic substituent and due to an interaction between the aromatic substituents such that the curved backbone is stabilized. The helical compositions are formed by ridigifying the amide group, which is flanked on each side by the aromatic substituents, by introducing intramolecular hydrogen bonds into a linkage between the amide group and each aromatic substituent such that the compositions fold into a helical shape when the amide linkages are meta to each other.

Abstract: The present invention relates to novel felbamate derivatives and their use to treat neurological diseases such as epilepsy and to treat tissue damage resulting form ischemic events. The felbamate derivatives are modified to prevent the formation of metabolites that are believed responsible for the toxicity associated with felbamate therapy.

Abstract: This invention pertains generally to valency molecules, such as valency platform molecules which act as scaffolds to which one or more molecules may be covalently tethered to form a conjugate. More particularly, the present invention pertains to valency platform molecules which comprise a carbamate linkage (i.e., —O—C(═O)—N<). In one aspect, the present invention pertains to valency platforms comprising carbamate linkages, which molecules have the structure of any one of Formulae I, II, or III, shown in FIG. 1. In one aspect, the present invention pertains to valency platforms comprising carbamate linkages, which molecules have the structure of any one of Formulae IV, V, or VI, shown in FIG. 8. The present invention also pertains to methods of preparing such valency platform molecules, conjugates comprising such valency platform molecules, and methods of preparing such conjugates.

Abstract: Novel (hydroxyethyl)ureas are described. These compounds are effective inhibitors of certain aspartyl proteases, notably secretases involved in the enzymatic cleavage of amyloid precursor protein (APP) to yield amyloid-&bgr; peptide. Methods are provided for administering the novel compounds to treat &bgr;-amyloid-associated diseases, notably Alzheimer's disease.

Abstract: The present invention relates to water dispersible polyisocyanate mixtures prepared from aliphatic, cycloaliphatic, araliphatic and/or aromatic diisocyanates and having a) an average isocyanate functionality of at least 2.0, b) a content of 5.0 to 25.0 wt. %, based on resin solids, of isocyanate groups (calculated as NCO; molecular weight=42) and c) a content of 2 to 50 wt. %, based on resin solids, of ethylene oxide units calculated as C2H2O; molecular weight 44) incorporated within polyether chains containing an average of 5 to 35 ethylene oxide units, wherein at least 60 mole % of the polyether chains are connected via allophanate groups to two polyisocyanate molecules which are each prepared from at least two diisocyanate molecules. The present invention also relates to a process for the preparation of these water dispersible polyisocyanate.

Abstract: The present invention relates to polyisocyanate mixtures prepared from aliphatic and/or cycloaliphatic diisocyanates and having a) an average isocyanate functionality of at least 2.0, b) a content of isocyanate groups (calculated as NCO; molecular weight=42) of 4.0 to 28.0 wt. % and c) a content of alkoxy groups having up to 36 carbon atoms of 2.0 to 37.5 wt. %, wherein the alkoxy groups are constituents of allophanate groups or optionally urethane groups, provided that >50 mol % of the alkoxy groups are a constituent of allophanate groups that are connected to at least two polyisocyanate molecules which are each prepared from at least two diisocyanates. The present invention also relates to a process for preparing these polyisocyanate mixtures and to coating compositions, which are highly diluted or dilutable with non-polar solvents and contain these polyisocyanate mixtures and lacquer binders or binder components optionally containing isocyanate-reactive groups.

Abstract: Polyisocyanates are prepared by a process which comprises (i) preparation of an addition product (A) which contains one group which is reactive toward isocyanate and one isocyanate group by reacting (a) a diisocyanate I with (b) compounds containing two groups which are reactive toward isocyanate, where at least one of the components (a) or (b) has functional groups having differing reactivities toward the functional groups of the other component, (ii) if desired, intermolecular addition reaction of the addition product (A) to form a polyaddition product (P) which contains one group which is reactive toward isocyanate and one isocyanate group and (iii) reaction of the addition product (A) and/or the polyaddition product (P) with a diisocyanate or polyisocyanate II which is different from diisocyanate I.

Abstract: Low-monomer, NCO-containing prepolymers based on 1,4-diisocyanato-2,2,6-trimethylcyclohexane, a process for their preparation, and their use.

Abstract: Organic diurethanes and/or polyurethanes are prepared by reacting organic diamines and/or polyamines (a) with urea and/or alkyl cabamates (b) and alcohols (c) in the presence of soluble zirconium compounds, preferably zirconium alkoxides, zirconium acetate or zirconium acetylacetonate, as catalyst (d). They can be used for preparing diisocyanates and/or polyisocyanates by thermal dissociation.

Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of negatively charged polymers thereby facilitating cellular uptake of such polymers.

Abstract: The present invention relates to a dimeric urethane compounds derived from monohydric alcohols, generally fatty alcohols, and a diisocyanate according to the following reaction scheme: wherein R1 is selected from the group of saturated, unsaturated or halogen substituted linear, cyclic or branch-chained hydrocarbons and R2 is a linear, cyclic or branch-chained alkyl or aminoalkyl group ranging from two to 200 carbon atoms, preferably two to 50 carbons, more preferably 6 to 36 carbons, said urethane compound being substantially free from terminal hydroxyl groups.

Abstract: The present invention relates to a process for the production of polyisocyanates containing allophanate groups and having aliphatically and/or cycloaliphatically bound isocyanate groups by reacting organic compounds containing urethane groups with organic polyisocyanates containing aliphatically and/or cycloaliphatically bound isocyanate groups in the presence of tin compounds and to the use of these polyisocyanates, optionally blocked with blocking agents for isocyanate groups, as an isocyanate component in the production of polyurethanes, in particular polyurethane coatings.

Abstract: Fluorine-containing diols represented by the following formula are provided: wherein Rf represents a perfluoroalkyl or perfluoroalkenyl group having 1 to 20 carbon atoms; X represents a substituted or unsubstituted alkylene group having 1 to 10 carbon atoms, a substituted or unsubstituted alkenylene group represented by —CH═CH—(CH2)n— in which n is from 1 to 10, or in which n is from 0 to 6; Y represents a direct bond, —O—, —NH—, or —R0—NH— in which R0 is an alkylene group having 1 to 6 carbon atoms; Z represents a direct bond or —N(R′)R— in which R is an alkylene group having 1 to 20 carbon atoms and R′ is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R1 and R2 divalent organic groups; and R3 represents a residual group of diisocyanate. These diols are useful for polyurethanes.

Abstract: Trisubstituted N-protected guanidines and methods for use as guanidinylating reagents to yield N-protected guanidine derivatives.

Abstract: The invention includes colorless compounds having a central core and at least two arms extending from the core. The core can comprise one or more atoms. The at least two arms have the formula In such formula, Z is a segment of one or more atoms; j is an integer from 1 to about 300 and can be different at one of the at least two arms than at another of the at least two arms; Q is an alkyl or aryl group and can vary amongst different alkyl and aryl groups within the colorless compound; and n is an integer greater than 1 and can be different at one of the at least two arms than at another of the at least two arms. In other aspects, the invention encompasses phase change inks incorporating the above-described colorless compound as toughening agent, and methods of printing with such phase change inks.

Abstract: A low monomer 1:1-monoadduct from a diisocyanate and a hydroxy(meth)acrylate with a free diisocyanate content of less than 0.7% by weight and a free NCO content of 10.4-16.4% by weight can be used as a starting material for an acrylic or NCO functionalized crosslinker; a bonding agent for coatings and adhesives; and a linker for solid-phase synthesis of oligo-nucleotides, polynucleotides or peptides. The monoadduct is obtained by converting 5-20 mol diisocyanate with 1 mol hydroxy(meth)acrylate at a temperature of 40-120 ° C. in the presence of at least one inhibitor; subsequently separating a non-converted diisocyanate from a reaction product by short-path distillation at 80-220 ° C./0.1-10 mbar; feeding air, nitrogen monoxide or oxygen or a mixture containing (a) air, oxygen or nitrogen monoxide and (b) a proportion of 1-90% by volume of carbon dioxide, nitrogen, an inert gas or a mixture thereof through a reaction apparatus.

Abstract: Polyfunctional polymerizable urethane- or urea-containing oligomers allow the design, adjustment, and regulation of chemical and physical properties of the described oligomers. The invention discloses the formulas and compositions of these oligomers, methods of their synthesis, and methods of converting the described oligomers into useful polymeric products. The described oligomers can be used for many purposes, both directly and in combination with other chemicals in multiple applications such as adhesives, sealants, coatings, composites, etc., as well as in castable and moldable materials.

Abstract: The present invention relates to compounds containing modified hydrazide groups and corresponding to formula I wherein R represents the residue obtained by removing the isocyanate groups from a monomeric polyisocyanate, a polyisocyanate adduct or an NCO prepolymer, X represents OR′ or NHR′ and R′ represents a group which is inert to isocyanate groups under the conditions used to form the compound of formula I, R″ represents a divalent, linear or branched aliphatic group containing 2 to 10 carbon atoms, provided that there are at least two carbons between the oxygen atoms wherein the aliphatic group may optionally be substituted by heteroatoms to form ether or ester groups, and n is 2 to 6.

Abstract: The invention concerns an isocyanate composition at least partially masked, characterized in that it is masked by at least two agents, one of which at least has a non-carbon carboxylic function. The invention is applicable to organic synthesis.

Abstract: The present invention relates to aspartate-terminated urea/urethane prepolymers that are based on the reaction products of NCO prepolymers with compounds corresponding to the formula wherein X represents an organic group which has a valency of n and is inert towards isocyanate groups at a temperature of 100° C. or less, R1 and R2 may be identical or different and represent organic groups which are inert towards isocyanate groups at a temperature of 100° C. or less, R3 and R4 may be identical or different and represent hydrogen or organic groups which are inert towards isocyanate groups at a temperature of 100° C. or less and n represents an integer with a value of at least 2, at an equivalent ratio of aspartate groups to isocyanate groups of 1.5:1 to 20:1. The present invention also relates to coating compositions containing the aspartate-terminated urea/urethane prepolymers and a polyisocyanate.

Abstract: A polymeric furanone magenta colorant is disclosed that contains a furanone magenta chromophore having a furanone adduct, the adduct containing at least one alkoxylated phenyl radical, the chromophore further being derived from at least one aromatic aldehyde having a para-nitrogen and containing electron donating groups selected from the group consisting of alkyls, cycloalkyls, and oligomers or polymers derived from alkyleneoxy or aryleneoxy moieties. The colorant can be utilized in resins, waxes and inks.

Abstract: The present invention relates to a process for the preparation of diesters of poly (ethylene glycol) by reacting poly (oxyalkylene glycol) and amino acid hydrochloride in the presence of a condensing agent in a suitable solvent at a temperature in the range of 0° C. to room temperature for a period ranging between 1 hour to 24 hours. The reaction mixture is then filtered and the filtrate poured into another solvent, which is a nonsolvent for the products. The products precipitated thereby are then isolated.

Abstract: High-functionality polyisocyanates are prepared by a process which comprises

Abstract: The present invention relates to aspartate-terminated urea/urethane prepolymers that are based on the reaction products of NCO prepolymers with compounds corresponding to the formula 1

Abstract: A urea-urethane compound having one or more urea groups and one or more urethane groups in the molecular structure, the number of said urea groups (A) and the number of said urethane groups (B) satisfying the following numerical formula:

Abstract: Carbamate solutions are obtainable by reacting at least one alkanolamine with carbon dioxide in, as solvent, at least one organic compound having a molecular weight of from 60 to 600 and containing at least one hydroxyl group, wherein the carbamate contains at least 0.

Abstract: An adhesive paste, free of water, based on a reaction product of a polyisocyanate component and a co-reactant selected from the group consisting of a polyol, a monofunctional fatty derivative component and mixtures thereof, wherein the reaction product contains moisture reactive isocyanate groups.