Abstract: The invention relates to methods for the parenteral administration of aspirin, pharmaceutical compositions of aspirin prepared using the methods, and kits that may be used in the method. The method of the invention comprises the steps of: mixing a first vial comprising aspirin and optionally at least one excipient with a second vial comprising an aqueous solution comprising meglumine, sodium citrate, or mixtures thereof, optionally at least one surfactant, tonicity adjusting agent, or mixtures thereof, optionally at least one monosaccharide, disaccharide, sugar alcohol, or mixtures thereof, and optionally at least one non-aqueous co-solvent; to obtain an aqueous aspirin composition; and parenterally administering the aqueous aspirin composition to the subject in need thereof.

Abstract: A polymer comprising: In this embodiment, R? and R?, can be independently selected from the group consisting of: a halogen, a substituted alkyl, an unsubstituted alkyl, a substituted aryl, and an unsubstituted aryl. Additionally, X1 and X2 can be independently selected from the group consisting of: O, S, Se, N—R, and Si—R—R. Lastly, Ar and Ar? can be identical or different and can be independently selected from the group consisting of: a substituted aryl, and an unsubstituted aryl.

Abstract: A digital water intrusion notification system comprising a water intrusion detection device, a digital data transmission device, and a software interface is disclosed. The digital water intrusion notification system preferably comprises a deployable moisture collection device to cover an area, a digital data transmission device to provide internal monitoring, relay to a computer system, and cellular connectivity, and a software interface to provide instant notification of alerts and automated dispatch of a service technician. Such a system can detect water intrusion in roofing applications or other large areas requiring sufficient leak detection coverage, and may be assembled in various orientations and compositions to suit the relevant application.

Abstract: The present invention relates to analogs of bexarotene and methods of use thereof.

Abstract: The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II, and methods for treating or preventing or modulating moderate to severe pain in a disease may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.

Abstract: Photoactive additives are disclosed. The additive includes a benzophenone having at least one substituent that comprises a divalent linker and a linking group, wherein the linking group is a carboxyl group, ester group, or acid halide group. The additive can be a polymer, an oligomer, or a compound. When added to a base polymeric resin, the photoactive additive permits crosslinking upon exposure to ultraviolet light.

Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.

Abstract: The present invention relates to water-soluble formulations comprising the active agent dexketoprofen and to a process for production of said formulations. The present invention also relates to pharmaceutical formulations comprising dexketoprofen which is used in symptomatic treatment of mild to moderate pains such as musculoskeletal pains, dysmenorrhoea, toothache, post-operative pains. The formulations are characterized in being in effervescent form.

Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.

Abstract: The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.

Abstract: There is provided compounds of formula I, wherein Y, ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.

Abstract: The present invention relates to an improved process for the preparation of choline salt of fenofibric acid corresponding to formula (I). The present invention also provides crystalline polymorphic form of choline salt of fenofibric acid corresponding to formula (I) designated as form A.

Abstract: (R) and (S) 2-Aryl-propionic acids, and pharmaceutical compositions that contain them, are useful in inhibiting chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The acids are used for the prevention and treatment of pathologies deriving from said activation. In particular, the (R) enantiomers of said acids are lacking cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrofil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bollous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.

Abstract: There is described a process for the manufacture of a racemic 2-aryl propionic acid compound, or a pharmaceutically acceptable salt thereof, which comprises reacting the S- or R-enantiomer of the corresponding 2-aryl propionic acid compound with a base.

Abstract: The invention particularly discloses a process for preparing aryl alkyl carboxylic acid salts by preparing aqueous alkali solution, adding aryl alkyl carboxylic acid to said alkali solution at a temperature ranging from 4° to 121° C. for obtaining a clear solution, preferably by heating and/or stirring and concentrating and cooling to obtain aryl alkyl carboxylic acid salt The invention therefore discloses solid oral dosage forms and compositions of aryl alkyl carboxylic acid salts which are free of organic solvent/so. The solid oral dose compositions of aryl alkyl carboxylic acid salts of the invention are prepared in situ from aryl alkyl carboxylic acids and bases to obtain aryl acid alkyl carboxylic acid sails in crystalline/powder form with or without the use of pharmaceutical excipients.

Abstract: The invention provides polymers that include a biologically active molecule and methods for their use.

Abstract: Pharmaceutical agents characterized by containing benzophenone derivatives represented by the general formula: wherein the each substituent is as defined in the specification, or salts thereof have suppressive effect on RANKL production, suppressive effect on OPG reduction and inhibitory effects on differentiation/activation of osteoclasts, and are extremely useful for treating, for example therapy and/or prevention, of various diseases in which differentiation/activation of osteoclast are involved, such as osteoporosis.

Abstract: Compounds of the Formula (I) wherein x is an integer from 1-4; p is an integer from 1-3; q is an integer from 0-3; Ar is phenyl, naphthyl, anthryl or phenanthryl each of which optionally is substituted by one or more Cl, CN, OR5, C3-C5alkenyl or C1-C6alkyl which optionally is substituted by one or more OR6, COOR or halogen; R1 if x is 1, is ORS, O—X+, NR8R9, C1-C20alkyl optionally substituted by one or more COOR10, or is C2-C20alkyl interrupted by one ore more O, or is C2-C5alkenyl or phenyl-C1-C4alkyl; R1 if x is 2, is for example C1-C20alkylene; R1 if x is 3, is for example a tri-valent radical; R1if x is 4, is for example a tetravalent radical; R2and R3are hydrogen or C1-C8alkyl, or R2and R3 together are O, C1-C3alkylene or CH?CH; R4 is C1-C4alkyl; R5, R6, R7, R8, R9 and R10 are for example hydrogen or C1-C4alkyl; and X is a x-valent cationic counter ion; are in particular suitable as photoinitiators for the curing with UV-A light (320-450 nm).

Abstract: Disclosed is a method for producing pulverized particles of a crystalline organic compound which is poorly water-soluble. Also disclosed is a pulverized organic compound particle produced by such a method. Specifically disclosed is a method for producing a poor water solubility organic compound particle for medical use, which is characterized in that a poor water solubility organic compound for medical use is mixed with a physiologically acceptable salt and a physiologically acceptable polyol, and subjected to wet milling. Also specifically disclosed is a poor water solubility organic compound particle for medical use, which is produced by such a production method.

Abstract: Disclosed herein is a metal enolate initiator for polymerizing isocyanates and a method for polymerizing isocyanates by anionic polymerization using the same, in which the initiator forms a cluster upon the initiation and protects stability of terminal anions at the end of the chain to cause controlled polymerization, thus preventing depolymerizaton and improving reaction time and efficiency without the use of a separate additive.

Abstract: The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, R1, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with ?-secretase activity, including Alzheimer's disease.

Abstract: The invention relates to pharmaceutical compositions of alkylammonium salts of 2-aryipropionic acids, including ketoprofen, ibuprofen, naproxen and tiaprofenic acid. The compositions are suitable for parenteral administration arid, due to buffering at pH 8 to 9, cause less pain upon injection than previously known composition.

Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).

Abstract: This invention relates to the compositions and processes for preparing 2,3,3?,4?-tetramethylbenzophenone and asymmetrical dianhydrides such as 2,3,3?,4? benzophenone dianhydride (a-BTDA), and 3,4?-(hexafluoroisopropylidene)diphthalic anhydride (a-6FDA). a-BTDA is prepared by Suzuki coupling with catalysts from a mixed anhydride of 3,4-dimethylbenzoic acid and 2,3-dimethylbenzoic acid with a respective 2,3-dimethylphenylboronic acid and 3,4-dimethyl phenylboronic acid to form 2,3,3?,4?-tetramethylbenzophenone which is oxidized to 2,3,3?,4?-benzophenonetetracarboxylic acid followed by cyclodehydration to obtain a-BTDA. The a-6FDA was prepared by nucleophilic trifluoromethylation of 2,3,3?,4?-tetramethylbenzophenone with trifluoromethyltrimethylsilane to form 3,4?-(trifluoromethylmethanol) bis(o-xylene) which is converted to 3,4?-(hexafluoroisopropylidene-bis(o-xylene). The 3,4?-(hexafluoroisopropylidene)-bis(o-xylene) is oxidized to the corresponding tetraacid followed by cyclodehydration to yield a-6FDA.

Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):

Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid is crystallized as an anhydrous, stoichiometric 1.5 HCl salt and a scaleable crystallization method is disclosed. The salt form was characterized and the absolute configuration of the chiral center was confirmed as “S”. (2S,5Z)-2-amino-7-(ethanimidoylamino)-2-methylhept-5-enoic acid was high melting and appears acceptably non-hygroscopic for use in a pharmaceutical composition.

Abstract: A process for producing compounds of formula (VIIa) and (VIIb) wherein X is a leaving group; Y and Y1 are idependently Cl or Br; and Z is Cl, Br or a haloalkyl group which process comprises a) reacting a compound of formula (VII) wherein X, Y, Y1 and Z are as defined for compounds (VIIa) and (VIIb) with a substantially optically pure chiral amine in a solvent to form a diastereoisomeric salt; b) separating the diastereomeric salt of each enantiomer; c) converting the diastereomeric salt of each anantiomer separately to compounds of formulae (VIIa) and (VIIb) respectively by acid or base hydrolysis, the use of the compounds in making pyrethroid insecticides and novel intermediates.

Abstract: The present invention relates to a process for preparing bromoisophthalic acid compounds, particularly 5-bromoisophthalic acid compounds and 4,5-dibromoisophthalic acid compounds comprising brominating an isophthalic acid compound of the general formula (1) wherein R1 and R2 independently of one another are hydrogen atom or C1-6 alkyl, with bromine in a solvent containing sulfur trioxide. The object of the invention is to provide a process for preparing bromoisophthalic acid compounds, particularly 5-bromoisophthalic acid compounds and 4,5-dibromoisophthalic acid compounds in a highly selective manner by using bromine that is industrially inexpensive.

Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.

Abstract: Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.

Abstract: A method of producing a compound of the formula: and its pharmaceutically acceptable salts, wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic group; comprising: (1) reacting a compound of the formula: wherein Ar is as described above, with N2CHCOOR, wherein R is alkyl, in the presence of a catalytic amount of a Bronsted acid or Lewis acid to form a compound of the formula: wherein Ar and R are as described above; and (2) reacting the compound of formula (II) with a reducing agent in the presence of an alkyl amine to form a compound of the formula: wherein Ar and R are as described above.

Abstract: The present invention relates to a process for preparing bromoisophthalic acid compounds, particularly 5-bromoisophthalic acid compounds and 4,5-dibromoisophthalic acid compounds comprising brominating an isophthalic acid compound of the general formula (1) 1

Abstract: Compounds and pharmaceutical compositions useful as plasminogen activator inhibitor (PAI) antagonists are provided. In particular, methods of antagonizing PAI with substituted and unsubstituted aryl and heteroaryl ethers and thioethers, benzils, benzyl ethers, benzoate esters, sulfones and benzophenones are provided.

Abstract: A method for transferring amino acid into ketone acid (ester) may obtain ketone acid (ester) at low cost. The method uses sodium hypochlorous acid as oxidizing agent and proceeds oxidation reaction with amino acid or its derivatives so as to obtain ketone acid and its derivatives. The sodium hypochlorous acid is easily to get with low cost and the conditions of the reaction are mild so that the method meets the needs of the industry.

Abstract: Novel glucocorticoid and thyroid receptor ligands as provided which have the general formula (I): in which R1 is an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano, or a pharmaceutically acceptable salt thereof. R2 and R3 are the same or different, and are hydrogen, halogen, alkyl of 1 to 4 carbons, or cycloalkyl of 3 to 5 carbons, at least one of R2 and R3 being other than hydrogen. X is carbonyl or methylene. R4 is an aliphatic, aromatic or heteroaromatic. Y is hydroxyl, methoxy, amino, or alkyl amino. n is an integer from 0 to 4. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid or thyroid receptor gene such as diabetes, hypercholesterolemia, or obesity using these compounds is also disclosed.

Abstract: This invention relates to a process for the preparation of compounds of the formula: 1

Abstract: Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.

Abstract: Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N′,N′-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.

Abstract: Biaromatic compounds connected by a propynylene or ailenylene bond, corresponding to the formula (I).

Abstract: A tetrahydrofluorene, which is represented by the following formula (I) wherein R1 to R6 each independently represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R1 and R2 are combined together to represent ═O, ═N or ═S, R7 and R8 each independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, a hydroxyl group or a carboxyl group, is subjected to a hydrogen transfer reaction in the presence of a hydrogen acceptor and a catalyst, whereby a fluorene and a hydride of the hydrogen acceptor are formed at the same time.

Abstract: A series of phloroglucide derivatives are synthesized, which possess potent antibacterial activities. They include unsymmetrical phloroglucide analogs, phloroglucides attached to cephalosporins at the C-3′ position, and 7-(phloroglucidamido)cephalosporins.

Abstract: Disclosed are novel compounds of formula I wherein R1, R2, R3, L, X and Y are as defined in the specification. These compounds are useful in the treatment of conditions mediated by nuclear receptors, in particular the Retinoid X Receptor (RXR) and the Peroxisome Proliferator-Activated Receptor (PPAR) families. Such conditions include diabetes and obesity.

Abstract: Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.

Abstract: Compounds of the formula where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.

Abstract: A phloroglucide derivative having the following formula: ##STR1## wherein Q is halogen; X is CH.sub.2 or C.dbd.O; Y is cephalosporin having a formula of ##STR2## wherein Ph is phenyl, Ac is acetoxy, or pharmaceutically acceptable salts thereof, and an antibacterial pharmaceutical composition derived thereof.

Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinois antagonist or retinoid inverse agonist type biological activity.