Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.

Abstract: The present invention relates to the new impurities of Fesoterodine, Fesoterodine symmetric dimer impurity and asymmetric dimer impurity, process for preparing and isolating thereof. The invention also deals with analytical standards and analytical methods used for the control of the production process and final quality of Fesoterodine.

Abstract: The invention relates to a method for continuous production of reaction products by addition reactions based on a Michael reaction, wherein at least one compound (B) having at least one nucleophilic functional group is added to at least one compound (A) having at least one activated alkene or activated alkyne carbon-carbon multiple bond, wherein the reaction takes place in a reaction mixing pump.

Abstract: This invention features betulinic acid derivatives having the formula: wherein the variables are defined herein. The invention also provides related compounds and intermediates thereof, as well as pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Treatment methods and methods of manufacture are also provided.

Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.

Abstract: Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

Abstract: Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided.

Abstract: The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.

Abstract: The present invention relates to a method for the synthesis of an ? amino acetal, comprising (i) oxidizing a tertiary amine in the presence of a copper catalyst, at least one oxidant and a solvent, or (ii) reacting a secondary amine and an aliphatic aldehyde in the presence of a copper catalyst, at least one oxidant and a solvent.

Abstract: Disclosed is a process for the preparation of (R)-2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)-phenol isobutyrate (Fesoterodine) or a pharmaceutically acceptable salt thereof having a low content of impurities such as tolterodine and tolterodine isobutyrate.

Abstract: Provided herein, inter alia, are prodrugs of bimatoprost, methods of using the same and compositions including the same.

Abstract: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.

Abstract: The invention relates to a process for obtaining 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, comprising a chemoselective reduction of the acid group against the ester group in compounds of general formula (V), wherein R1 is C1-C8 alkyl; and R3 and R4, independently of one another, represent H or C1-C8 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound. The invention also relates to the compounds of formula (V), as well as their enantiomers, solvates and salts.

Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.

Abstract: The present invention provides compounds produced by the reaction of glycidyl ethers and glycidyl esters with ether compounds including N,N,N?-trimethyl-bis-(aminoethyl)ether. N,N,N?-trimethyl-bis-(aminoethyl)ether and its derivatives can be used as polyurethane catalysts.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: A novel compound is a highly-sensitive photopolymerization initiator with excellent stability, low sublimability, excellent developability, and high transmittance in the visible region. It efficiently absorbs, and is activated by, near-ultraviolet rays such as at 365 nm. Also provided are a photopolymerization initiator and a photosensitive composition using such compound. An oxime ester compound is represented by the following general formula (I), a photopolymerization initiator containing the same, and a photosensitive composition containing the photopolymerization initiator and a polymerizable compound having an ethylenically unsaturated bond: R1 and R2 each represent R11, COR11, CONR12R13, CN, etc.; R11, R12, and R13 each represent a C1-20 alkyl group, etc.; R3 and R4 each represent R11, OR11, COR11, CONR12R13, OCOR11, CN, a halogen atom, etc.; a and b each represent an integer 0-4; X represents an oxygen atom, a sulfur atom, etc.

Abstract: A process for the preparation of phenolic monoesters of 2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol by converting (±)6-halo-4-phenylchroman-2-one to (±)4-halo-2-(3-hydroxy-1-phenylpropyl)phenol. The two hydroxyl groups are protected and the protected compound is reacted with diisopropylamine to give (±)[3-(2-benzyloxy-5-halophenyl)-3-phenylpropyl]diisopropylamine. The halo substituent on the benzene ring is converted to corresponding benzyl alcohol and then the protection is removed to give racemic 5-HMT. Racemic 5-HMT is converted R enantiomer and then it is esterified.

Abstract: New solid forms of fesoterodine fumarate are described. In particular, amorphous fesoterodine fumarate, characterized by a powder X-ray diffraction spectrum as shown in FIG. 1 and by an IR spectrum as shown in FIG. 2 is described. Also fesoterodine fumarate in crystalline form I, characterized by a powder X-ray diffraction spectrum as shown in FIG. 3, by a DSC profile as shown in FIG. 4, by an IR spectrum as shown in FIG. 5, by a solid state 13C-NMR spectrum as shown in FIG. 6 and by a Raman spectrum as shown in FIGS. 7, 8 and 9 is described.

Abstract: The invention provides a novel compound useful as a highly-sensitive photopolymerization initiator that has excellent stability, low sublimability, excellent developability, and high transmittance in the visible region and that efficiently absorbs, and is activated by, near-ultraviolet rays such as at 365 nm. Also provided are a photopolymerization initiator and a photosensitive composition using the above-described compound. Specifically, the invention provides an oxime ester compound represented by the following general formula (I), a photopolymerization initiator containing the same, and a photosensitive composition containing the photopolymerization initiator and a polymerizable compound having an ethylenically unsaturated bond: wherein, R1 and R2 each represent R11, COR11, CONR12R13, CN, etc.; R11, R12, and R13 each represent a C1-20 alkyl group, etc.; R3 and R4 each represent R11, OR11, COR11, CONR12R13, OCOR11, CN, a halogen atom, etc.

Abstract: A rust inhibitor usable for metal surface coating includes, as an effective component, a compound containing a chelate group, and a long chain alkyl group and/or a cyclic alkyl group, which are bonded by an ester bond or other bonds.

Abstract: A process is described for preparing fesoterodine and/or fesoterodine fumarate comprising the esterification of (R)-feso deacyl with isobutyric acid or a precursor thereof, such as an isobutyryl halide or the isobutyric acid anhydride to give fesoterodine, in a mixture of water at alkaline pH and/or at least one organic solvent. This process allows obtaining products with high yields and purities, and in particular a product having a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-isobutyroyloxymethyl-phenyl isobutyrate less than 1% by mole and a content of (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol less than 0.05% by mole.

Abstract: This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate, polymorph, stereoisomer, metabolite or prodrug thereof; wherein R3, R4 and R5 are defined herein. Compounds of formula (I) and formula (II) are known to be useful in treating arrhythmias.

Abstract: The present invention relates to a process for the cosmetic treatment of wrinkled skin, comprising the topical application to the said skin of a composition comprising, in a physiologically acceptable medium, at least one ester of ((dialkylamino)alkoxy)ethanol of formula (I): It also relates to novel compounds belonging to the formula (I) and corresponding to the formulae (II) and (III): and to the cosmetic compositions comprising them.

Abstract: The present invention relates to a process for the preparation of a peroxyester which can be used in particular in polymerizations, such as the polymerization of vinyl chloride, or in the thermosetting of polyester resins. This process comprises the reaction of a hydroxyhydroperoxide salt with an acid halide or an acid anhydride under the following conditions: the molar ratio Rb of the hydroxyhydroperoxide corresponding to the hydroxyhydroperoxide salt to the acid halide is between 0.5 and 1.5; or alternatively the molar ratio Rb? of the hydroxyhydroperoxide corresponding to the hydroxyhydroperoxide salt to the acid anhydride is between 1.0 and 3.0; the hydroxyhydroperoxide salt was prepared beforehand by reaction of the corresponding hydroxyhydroperoxide with a base according to a molar ratio Ra of the base to the hydroxyhydroperoxide of between 0.5 and 1.5; and this process is carried out in aqueous media.

Abstract: The present invention provides carbohydrate analogs of the formula: wherein X is CH2, O, or NH, and R1-8 are independently H, a short hydrocarbon, a substituted amine, an alcohol, a substituted ether, a substituted amide, a substituted ketone, a substituted carboxylic acid, a short peptide, or a short oligosaccharide, Y is H, a short hydrocarbon, a short peptide, or a short oligosaccharide, and R9 is H, a short hydrocarbon, a substituted amine, an alcohol, a substituted ether, a substituted amide, a substituted ketone, a carboxylic acid, a short peptide, or a short oligosaccharide.

Abstract: Substituted C-cyclohexylmethylamine derivatives, methods for the production thereof, pharmaceuticals containing said compounds, the use of substituted C-cyclohexylmethylamine derivatives for producing pharmaceuticals, and method of pain treatment using the pharmaceuticals.

Abstract: The invention relates to the compound of the formula 1 and to its physiologically acceptable salts. The compound is suitable, for example, as a hypolipidemic.

Abstract: The present invention relates to compositions which comprise mixtures of open-chain and cyclic molecules of the sugar alcohols D-sorbitol and D-mannitol which have been esterified with at least one carboxylic acid, processes for preparing these compositions and the use of this composition as lubricant or hydraulic liquid.

Abstract: Benzhydryl derivatives of the formula I, where the index and the variables are as defined below: X is oxygen or sulfur; R1, R3 are halogen, cyano, nitro, hydroxyl, mercapto, amino, alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, alkylcarbonyloxy, formyloxy, alkylthio, alkenylthio, alkynylthio, alkylamino, dialkylamino, alkylcarbonyl or formyl, where the carbon atoms in the radicals mentioned may be partially or fully halogenated; R2 is halogen, cyano, nitro, hydroxyl, mercapto, amino, alkyl, alkoxy, haloalkyl or haloalkoxy, where the groups R2 may be different if n=2; R4 is alkyl, alkenyl or alkynyl, where the carbon atoms in these radicals may be unsubstituted or partially or fully halogenated; R5, R6 are hydroxyl, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, alkenyloxy, haloalkoxy, haloalkenyloxy, cycloalkyl, cycloalkylalkyl, cycloalkoxy or cycloalkylalkoxy; n is 0, 1 or 2; processes for preparing the compounds I, compositions comprising them and their use for con

Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.

Abstract: Water-soluble or water-dispersible branched or unbranched cationic epoxy compounds comprise a backbone having covalently attached thereto two or more epoxy moieties and one or more of the same or different organoonium moieties. The backbone comprises at least 25 weight % oxygen.

Abstract: Cosmetic or pharmaceutical preparations comprising an oxalkylated polyglycerol ester of the formula (1) 1

Abstract: A base catalyst, obtained by formulating at least one alkali metal compound selected from the group consisting of alkoxides, hydroxides and oxides of alkali metals and an alkaline-earth metal oxide in a ratio of “the weight of alkaline metal compound/the weight of alkaline-earth metal oxide”=0.005 to 1, is used in a reaction of an aldehyde to produce a glycol monoester, thereby providing a base catalyst with an improved efficiency which can be applied to aldol reaction or the like and which has high activity to give target product in a high selectivity.

Abstract: The invention provides adjuvants, immunogenic compositions, and methods useful for polynucleotide-based vaccination and immune response. In particular, the invention provides an adjuvant of cytofectin:co-lipid mixture wherein cytofectin is GAP-DMORIE.

Abstract: An improved process for the manufacture of monoesters of polyhydroxyalcohols to high yields and high purities.

Abstract: The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells.

Abstract: Simvastatin is produced from lovastatin in high yield and in pharmaceutical purity by forming an amide of lovastatin and protecting the free hydroxyl groups of the lovastatin amide with hexamethyidisilazane (HMDS) to form a protected lovastatin amide. The &agr;-carbon of the 2-methylbutyrate secondary chain of the protected lovastatin amide may be methylated to form a protected simvastatin amide. The protecting groups may be removed therefrom by quenching the methylation reaction with water. The simvastatin amide which is obtained may be hydrolyzed to form simvastatin acid, followed by forming a simvastatin ammonium salt, lactonizing the salt to form simvastatin, and recrystallizing the thus formed crude Simvastatin to a high degree of purity. The HMDS protecting agent for the lactone hydroxyl groups of Lovastatin is selected so as to result in a reaction that does not produce acid so that a base, such as imidazole, is not required to neutralize the acidity of the reaction medium.

Abstract: The present invention relates to a process for the preparation of esters from alcohols using acetic acid as acetylating agent and clays as catalysts, which comprises the preparation of esters in a single step from the reaction of aliphatic, acyclic, cyclic, heterocyclic, &agr;,&bgr;-unsaturated and aromatic alcohols with carbon atoms in the range of C1 to C10 with acetic acid in a molar ratio of 1:3 to 11 using reusable natural montmorillonite/metal ion-exchanged clay catalysts in the solvent medium of aliphatic, aromatic, or chlorinated hydrocarbons at 30-140° C. for a period in the range of 0.02 to 3.0 hrs, and recovering the corresponding esters by simple work-up procedure.

Abstract: A topical medicament for the treatment of psoriasis comprises metallic iodine, virgin wax, a variety of oils of animal and plant origin, camphor, chlorophyll and benzoic acid in a pharmaceutically acceptable emollient excipient base.

Abstract: A process for producing (2R, 3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S, 3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S, 3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S, 3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S, 3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base. An intermediate for the production of an HIV protease inhibitor can be produced from L-phenylalanine.

Abstract: The present invention provides novel cationic amphiphiles containing novel N-hydroxyalkyl group and therapeutic formulations containing the said amphiphiles that are capable of facilitating transport of biologically active molecules into cells.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: The present invention relates to a process for the preparation of esters from alcohols using acetic acid as acetylating agent and clays as catalysts, which comprises the preparation of esters in a single step from the reaction of aliphatic, acyclic, cyclic, heterocyclic, &agr;,&bgr;-unsaturated and aromatic alcohols with carbon atoms in the range of C1 to C10 with acetic acid in a molar ratio of 1:3 to 11 using reusable natural montmorillonite/metal ion-exchanged clay catalysts in the solvent medium of aliphatic, aromatic, or chlorinated hydrocarbons at 30-140° C. for a period in the range of 0.02 to 3.0 hrs, and recovering the corresponding esters by simple work-up procedure.

Abstract: A process for the production of simvastatin and its analogues that is efficient, economical and convenient involves the use of hydroxyl protected intermediates of formula (III) or (VII). These intermediates allow for direct alkylation of the butyrate side chain followed by deprotection and reformation of the lactone ring. R1 is hydrogen or methyl; R2 represents a straight or branched chain alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, or an aralkyl group having 1 to 6 carbon atoms in the alkyl chain; R3 and R4 each independently represent an alkyl group, an ether group, a thioether group, an aryl group, an aralkyl group, an alkenyl group, a cyclic ether group, or a cyclic thioether group; and R5 and R6 each independently represent hydrogen, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, or an ether group.

Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: The invention concerns novel glyoxylic acid derivatives, a process for their preparation and their use as pesticides.

Abstract: The invention relates to a novel process for the preparation of hydroxyalkyl- and acyloxyalkyl-substituted cycloketones by free-radical addition of hydroxyalkenes and acyloxyalkenes respectively to cyclic ketones.

Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.