Abstract: The present invention relates to pharmaceutical compositions of a non-steroidal anti-inflammatory drug (NSAIDs) such as, aspirin, diclofenac, ibuprofen, ketoprofen, or naproxen, or any pharmaceutically acceptable salts, solvates, or prodrugs thereof, and the medical use of these compositions. The compositions, which can be formulated for topical administration, can provide extended release of the NSAIDs. The compositions of the invention are useful, for example, in the prophylactic treatment or treatment and/or reduction of pain, in the prophylactic treatment or treatment of headaches such as migraine headaches and symptoms of migraine headaches, and in the treatment of temporomandibular disorders (TMD).

Abstract: A radiation-sensitive resin composition includes an acid-dissociable group-containing resin, and a compound shown by the following general formula (1). wherein Z? represents a monovalent anion shown by a general formula (2), M+ represents a monovalent onium cation, R1 represents a linear or branched alkyl group having 1 to 12 carbon atoms substituted or unsubstantiated with a fluorine atom, or a linear or branched alkoxy group having 1 to 12 carbon atoms, and n is 1 or 2.

Abstract: The invention relates to fatty acid acylated salicylate derivatives; compositions comprising an effective amount of a fatty acid acylated salicylate derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a fatty acid acylated salicylate derivative.

Abstract: A means of directing nucleation and crystal growth has been developed in which these stages of crystallization are influenced by surface energy modifications to amorphous substrates. The surface energy of a substrate can affect the contact angle, line tension, wettability and energetics of the interaction with a supersaturated solution, and these factors are important in crystallization. The use of amorphous substrates creates an opportunity to modify their surface to create useful ranges of surface energies that enhance or inhibit, as may be advantageous, the thermodynamic, kinetic, or a combination of both, factors in nucleation, crystal growth, or crystallization from a supersaturated solution.

Abstract: The invention relates to Fatty Acid Acetylated Salicylate Derivatives; compositions comprising an effective amount of a Fatty Acid Acetylated Salicylate Derivative; and methods for treating or preventing an inflammatory disorder comprising the administration of an effective amount of a Fatty Acid Acetylated Salicylate Derivative.

Abstract: A detergent including one or more neutral or overbased alkaline earth metal C10 to C40 hydrocarbyl substituted hydroxybenzoates, in which: (i) the one or more neutral or overbased alkaline earth metal C10 to C40 hydrocarbyl substituted hydroxybenzoates is or includes one or more C10 to C40 hydrocarb-1-yl substituted hydroxybenzoates; or, (ii) greater than 50 mole % of the one or more neutral or overbased alkaline earth metal C10 to C40 hydrocarbyl substituted hydroxybenzoates, based on the total number of moles of said C10 to C40 hydrocarbyl substituted hydroxybenzoates, is or includes one or more C10 to C40 hydrocarb-2-yl substituted hydroxybenzoates.

Abstract: A method of reducing asphaltene precipitation or ‘black paint’ in an engine is disclosed. The method includes the step of lubricating the engine with a lubricating oil composition comprising: an oil of lubricating viscosity in a major amount; and, a salicylate detergent system in a minor amount comprising one or more neutral or overbased alkaline earth metal C22 hydrocarbyl substituted salicylates.

Abstract: The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent, a method for using the dentinal drug delivery to provide a dental treatment, and a method for identifying anti-inflammatory agents capable of diffusing through dentin.

Abstract: The present invention provides stable non-crystalline aspirin that does not crystallize at room temperature during storage for prolonged periods of time and processes for obtaining the stable non-crystalline aspirin.

Abstract: Novel betaine salts of acetylsalicylic acid, namely 4-trimethylammoniobutanoate acetylsalicylic acid addition salt (gamma-butyrobetaine acetylsalicylate), L-carnitine acetylsalicylic acid addition salt and 3-(trimethylammonioamino)propanoate (meldonium) acetylsalicylic acid addition salt. Use of meldonium acetylsalicylate as antiplatelet agent for treating various pathologies induced by platelet aggregation, anti-inflammatory and antihyperlipidemic agent.

Abstract: There is described a pharmaceutical composition for controlled release of an active compound wherein the active compound is selected from the group comprising tramadol, resveratrol, acetaminophen, xorphanol, cinfenoac, furcloprofen, bismuth subsalicylate, enofelast, triflusal, ketorfanol, indriline, furofenac, cizolirtine, dacemazine, demelverine, and fenethazine, and derivatives and/or combinations thereof for the treatment or alleviation of depression. More particularly, there is described an abuse resistant pharmaceutical composition for the treatment of inter alia, depression and controlled release pharmaceutical compositions of related thereto.

Abstract: The present invention relates to salts of Memantine and COX-INHIBITORs, their crystal form, the processes for preparation of the same and their uses for the treatment of various disorders, including pain.

Abstract: Methods and compositions are provided for the reduction of fouling of objects present in marine environments. The methods and compositions include anticoagulants, such as, for example, glycosaminoglycans, coumarin-type molecules, metal chelators, plasminogen activators and platelet inhibitors. The methods include reducing marine fouling, comprising incorporating an anticoagulant compound into a marine coating. In addition, the methods include identifying compounds useful for reducing marine fouling, comprising measuring either blood coagulation or barnacle cement polymerization in the presence and absence of the compound, wherein a reduction in the blood coagulation or the barnacle cement polymerization in the presence of the compound identifies the compound as useful for reducing marine fouling. The coagulation or the polymerization can be measured by a serine protease activity or a transglutaminase activity.

Abstract: The present application relates to perfume raw materials, perfume systems and consumer products comprising such perfume raw materials and/or such perfume systems, as well as processes for making and using such, perfume systems and consumer products. The perfume compositions, including the delivery systems, disclosed herein expand the perfume communities' options as such perfume raw materials can provide variations on character and such compositions can provide desired odor profiles.

Abstract: The present invention relates to a new combination of an antithrombotic and aspirin and to pharmaceutical compositions comprising them.

Abstract: Pharmaceutically active salts and esters of 1-dimethylamino-3-(3-methoxyphenyl)-2-methylpentan-3-ol and 3-(3-dimethylamino-1-ethyl-1-hydroxy-2-methylpropyl)-phenol, and methods of using the same for treating or inhibiting increased urinary urgency or urinary incontinence and/or pain.

Abstract: The present invention provides stable non-crystalline aspirin that does not crystallize at room temperature during storage for prolonged periods of time and processes for obtaining the stable non-crystalline aspirin.

Abstract: Compounds of the present invention of the formula are thyromimetic agents which can be used to prevent and/or treat diseases associated with an imbalance of thyroid hormones, such as hypo- and hyper-thyroidism, obesity, osteoporosis and depression. The compounds of the invention are, in particular, hypolipedemic agents which enhance the clearance of cholesterol from circulation, particularly the clearance of cholesterol in the form of low density lipoproteins (LDL). The compounds are useful for reducing total cholesterol plasma levels in mammals, in particular for reducing levels of LDL-cholesterol. Furthermore, such compounds also lower elevated lipoprotein (a) [Lp(a)] levels, an independent cardiovascular risk factor, in mammals.

Abstract: The invention provides vitamin K-dependent polypeptides with enhanced membrane binding affinity. These polypeptides can be used to modulate clot formation in mammals. Methods of modulating clot formation in mammals are also described.

Abstract: Compounds of the formula in which W is O, S, S(O) or S(O)2; X is —SR4, —S(O)R4, or —S(O)2R4, —S(O)2NR5R6; or X is —C(O)NR5R6 provided that —C(O)NR5R6 is located at the 3′, 4′ or 5′ position; Y is O or H2; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogen, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted alkoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or —NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S(O), S(O)2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring;

Abstract: The present invention provides a fast, high yield method for preparing salicylamide intermediates. The method comprises reacting a C4 or higher alkyl ester of salicylic acid or derivative thereof with at least one amine selected from the group consisting of monoalkylamines, dialkylamines, ammonia, and any combination of any of the foregoing in alcohol to yield the sali-cylamide. The C4 or higher alkyl ester of salicylic acid or a derivative thereof is preferably prepared by reacting salicylic acid or a derivative thereof with a C4 or higher alcohol in presence of at least one of sulfuric acid, a sulfonic acid, and a mineral acid. This process for preparing salicylamide intermediates from salicylic acid or derivative thereof generally has a cycle time of about 2 days, and yields about 95% of a 99% pure material. In comparison, when a C3 or lower alkyl ester is used in lieu of the C4 or higher alkyl ester, the process generally has a cycle time of 7-9 days and yields about 60% of a 95% pure material.

Abstract: Compounds of the formula in which W is O, S, S(O) or S(O)2; X is —SR4, —S(O)R4, or —S(O)2R4, —S(O)2NR5R6; or X is —C(O)NR5R6 provided that —C(O)NR5R6 is located at the 3′, 4′ or 5′ position; Y is O or H2; Z is hydrogen, halogen, hydroxy, optionally substituted alkoxy, aralkoxy, acyloxy or alkoxycarbonyloxy; R is hydrogen, halogen, trifluoromethyl, lower alkyl or cycloalkyl; R1 is hydroxy, optionally substituted alkoxy, aryloxy, heteroaryloxy, aralkyloxy, cycloalkoxy, heteroaralkoxy or —NR5R6; R2 is hydrogen, halogen or alkyl; R3 is halogen or alkyl; R4 is optionally substituted alkyl, aryl, aralkyl, heteroaralkyl or heteroaryl; R5, R6 and R7 are independently hydrogen, optionally substituted alkyl, cycloalkyl, aryl, aralkyl, heteroaryl, or heteroaralkyl; or R5 and R6 combined are alkylene optionally interrupted by O, S, S(O), S(O)2 or NR7 which together with the nitrogen atom to which they are attached form a 5- to 7-membered ring;

Abstract: Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.

Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

Abstract: The invention describes a method for the synthesis of nitroxymethylphenyl esters of aspirin derivatives.

Abstract: The invention relates to a process for purifying and decolorizing a phenyl ester salt. The process combines a phenyl ester salt with a solvent to form a mixture and then stirs the mixture to form a slurry. The phenyl ester salt is substantially insoluble in this solvent. The process then collects the phenyl ester salt from the slurry. The collected phenyl ester salt may then be optionally dried or recrystallized. The collected phenyl ester salt is dissolved in a solvent to form a solution. The solution is decolorized and then spray dried to form a powder of the phenyl ester salt. As a result of the process the phenyl ester salt powder has a higher purity and an improved color as compared to the starting phenyl ester salt.

Abstract: Ibuprofen-aspirin compounds useful in treating aspirin or ibuprofen-treatable conditions and hydroxymethylacylfulvene analogs useful as antitumor drugs.

Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

Abstract: The present invention provides a method for the synthesis of acetyl salicylic acid comprising mixing acetic anhydride and salicylic acid in approximately or exactly stoichiometric proportions and calcium oxide or zinc oxide, obtaining a yield of a mixture of acetyl salicylic acid and calcium acetate or zinc acetate with 2% maximum of free salicylic acid content. The reaction is fast, exothermic, one-pot, non-pollutant of the environment due to the fact that it doesn't require elimination of acid residues nor requires the use of any type of organic solvent (other than such solvent activity provided by the reactants themselves), and doesn't require recrystallization since it yields a dense product which can be mixed with the common excipients for acetyl salicylic acid and compressed into tablets immediately after the synthesis process.

Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.

Abstract: The present invention relates to carboxylic acid esters of 2-hydroxy-5-isoalkyl-beta-methylstyrenes wherein the said isoalkyl substituent comprises 8-18 carbon atoms.

Abstract: The present invention relates to a biodegradable plastic made from a combination of at least one synthetic plastic polymer, at least one natural polymer and a natural polymer attacking agent and articles made therefrom.The present invention further relates to a method of eliminating hydrocarbon contaminating a region subjected to extreme temperatures by contacting the region with hydrocarbon-degrading microorganisms and adjusting the temperature of the region for optimum growth.The present invention also relates to a method of treating aspirin-treatable conditions comprising administering to a patient in need of such treatment a compound of Formula I ##STR1## In addition, the present invention relates to a method of protecting a philatelic item bearing a mark identifying an expert or owner of the item and possibly an additional distinguishable mark specific to the philatelic item from alteration.

Abstract: Medicinal products for the selective control of tumor tissue and a method for control of such tumor tissue by administration of such product to a host. The products comprise: (a) two different compounds having a pH below 7 when the compounds are present in a protonated form, such compounds having the formula set forth below and (b) a pharmaceutically acceptable inert medicinal product carrier. The compounds have the following ##STR1## wherein R.sub.1 is hydrogen or a moiety which completes an ester group or an ether group, R.sub.2 is independently selected from the group consisting of an amino group, hydroxyl, an ester group, an ether group and a halogen, and n is an integer of 1 to 4.

Abstract: The present invention is directed to a polymeric vehicle, the formulated coating composition and a coating binder made from the polymeric vehicle and a method for making the polymeric vehicle where the polymeric vehicle includes a phenolic urethane reactive diluent. The phenolic urethane reactive diluent may be made from a phenolic ester alcohol having at least one aliphatic hydroxyl group.

Abstract: The present invention also relates to a method of treating aspirin-treatable conditions comprising administering to a patient in need of such treatment a compound of Formula I ##STR1##

Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: The present invention provides a salicylate analogue having the structure ##STR1## wherein R is selected from the group consisting of hydrogen, methyl, ethyl, n-propyl, i-propyl, n-butyl, i-butyl; pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, phenyl, naphthyl and cyclohexyl; wherein R1 is selected from the group consisting of hydrogen, a C1-C12 alkyl group, F, Cl, Br, I, CO.sub.2 H, CONHR, CONR.sub.2, CO.sub.2 R, C.tbd.N, CHO, COR, SO.sub.3, SO.sub.2 NHR, SO.sub.2 NR.sub.2, OH, OR, OCOR, SH, SR, OCONHR, OCONR.sub.2, SCOR, SCONHR, SCONR.sub.2 and NH2, NHR, NHCOR and NR2; and wherein R1 is in the 3-, 4-, 5- or 6-position, or a combination thereof. Also provided are various pharmaceutical compositions of the novel compounds of the present invention.

Abstract: Chemical compounds which interact inside the central water cavity of hemoglobin and bridge between the two .alpha. subunits can be used to allosterically modify hemoglobin towards tense and relaxed states. The functional groups employed are aldehydes and carboxylic acids, wherein the aldehydes form covalent bonds (schiff base) with amino acid residues of hemoglobin and the carboxylic acids form ionic bonds with amino acid residues of hemoglobin. Particularly useful compounds within the practice of this invention bond to the n-terminal valine of one .alpha. subunit of hemoglobin, and the lysine 99 and/or arginine 141 of the other .alpha. subunit.

Abstract: Compositions degrading by hydrolysis to release a bioactive compound having carboxylic acid moieties, which are organic acid anhydrides having the following formula: ##STR1## wherein R' is a residue of a therapeutic bioactive compound, for example, a non-steroidal anti-inflammatory agent; a penicillin or cephalosporin antibiotic; or bioactive compounds for non-therapeutic use, for example, herbicides, insecticides, fungicides, antimicrobials, pesticides, pheromones, and fertilizers; m is an integer of between 1 and 3; and R is a carrier. The resulting mixed anhydrides are characterized by having between one and three drug molecules attached to a single carrier molecule. The prodrugs are highly susceptibility to hydrolytic degradation in a predictable and controlled fashion, have variable solubilities in water and lipids, with increased biomembrane transport, elicit a bio-affecting/pharmacological response, and are less irritating to topical and gastric or intestinal mucosal membranes.

Abstract: A novel process for the acetylation of a mono-substituted phenol or a mono-substituted naphthol is disclosed which comprises reacting the said mono-substituted phenol or the said mono-substituted naphthol respectively with vinyl acetate at a temperature of not more than 160.degree. C.

Abstract: Bis(salicyl) diesters useful as cross-linking agents for hemoglobin are prepared in high yield and purity by reacting salicylic acid or a derivative thereof with a lower aliphatic dicarboxylic acid halide in a lower aliphatic ketone or nitrile solvent in the presence of a pyridine derivative. The desired diester is recovered from the resulting insoluble pyridine derivative salt.

Abstract: A process for the preparation of 7-(2-diethylaminoethyl)-theophylline acetylsalicylate and use of the product obtained. The process comprises prior filtering of a solution of the reactants through a layer of diatomaceous earth and activated carbon, cooling and treatment with a source of high frequency ultrasounds. The product is used in the manufacture of anti-agglutination and anti-thrombotic agents.The process provides products having a high level of purity.

Abstract: The hydrated complex of magnesium acetylsalicylate and urea of formula ##STR1## possesses exceptional analgesic and antipyretic properties. It may be crystallized from a solution obtained by reacting acetylsalicylic acid with magnesium carbonate in the presence of urea.

Abstract: The invention is drawn to a compound of the formula ##STR1## which can be prepared by the reaction of acetylsalicylic acid with potassium carbonate or potassium bicarbonate in the presence of minor amounts of water. The compound is a substantially stable solid which readily dissolves in water with the formation of a neutral solution of an aspirin salt, i.e., potassium acetylsalicylate.

Abstract: The hydrated complex of magnesium acetylsalicylate and urea of formula ##STR1## possesses exceptional analgesic and antipyretic properties. It may be crystallized from a solution obtained by reacting acetylsalicylic acid with magnesium carbonate in the presence of urea.

Abstract: The present invention provides combination of materials for strengthening the antithrombotic action of acetylsalicylic acid. It covers a composition which contains diltiazem or a pharmaceutically acceptable acid-addition salt thereof in combination with acetylsalicylic acid. It also forms the new compound diltiazem acetysalicylate. It also covers compositions containing the above and methods for using the compositions or compound.

Abstract: Acyloxy aromatic carboxylic acids, e.g., 4-acetoxybenzoic acid, are prepared by oxidizing with oxygen an acyloxy aromatic ketone, e.g., 4-acetoxyacetophenone in the presence of manganese cations and a lower-carboxylic acid anhydride as catalyst and a co-reductant or promoter. The acyloxy aromatic ketone may be prepared by acylating a hydroxy aromatic ketone, e.g., 4-hydroxyacetophenone, which has the effect of "masking" the hydroxyl group of the ketone in a manner necessary to effect the subsequent transition-metal catalyzed oxidation of the ketone to the acyloxy aromatic carboxylic acid.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a member selected from the group consisting of a hydrogen atom, lower alkyl groups and lower alkoxy groups, R.sub.2 is a member selected from the group consisting of a hydrogen atom, halogen atoms, lower alkyl groups, a hydroxyl group and a trifluoromethyl group, R.sub.3 is a member selected from the group consisting of a hydrogen atom, halogen atoms, lower alkyl groups, lower alkoxy groups, an acetyl group, a carbamoyl group and lower alkyl carboxylate groups, and R.sub.4 represents a hydrogen atom or a halogen atom, a pharmaceutical composition comprising such a phenylguanidine acetylsalicylate compound as an active ingredient; and a process for production of aforesaid compound.

Abstract: A process for the preparation of aryl carboxylates is provided in which an arylmetallo carboxylate is contacted with an aryliodoso carboxylate in liquid medium to form the desired aryl carboxylate. Promoters can be employed to increase the rate of reaction and improve selectivity to the aryl carboxylate.

Abstract: A process for the catalytic preparation of aryl carboxylates is provided in which an arylmetallo carboxylate is contacted in liquid medium with an organic peracid in the presence of a catalytic amount of an aryl iodide, to form the desired aryl carboxylate.