Abstract: The present Invention relates to pharmaceutical compositions of (3S,11aR)—N-[(2,4-difluorophenyhmethyl]-2,3,5,7,11,11a-hexahydro-6-hydroxy-3-methyl-5,7-dioxo-oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide, useful in the treatment or prevention of Human Immunodeficiency Virus (HIV) infections.

Abstract: Object of the present invention is an improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts.

Abstract: The present invention relates to a solid dispersion characterized in that it comprises carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester as an active ingredient and a water-soluble polymer having a glass transition temperature lower than the melting point of the active ingredient as a carrier, and it is prepared via melt extrusion. The solid dispersion of the present invention remarkably increases the solubility and dissolution rate of the active ingredient which is an insoluble drug to efficiently improve the bioavailability when it is orally administered.

Abstract: The present invention relates to a solid dispersion characterized in that it comprises carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester as an active ingredient and a water-soluble polymer having a glass transition temperature lower than the melting point of the active ingredient as a carrier, and it is prepared via melt extrusion. The solid dispersion of the present invention remarkably increases the solubility and dissolution rate of the active ingredient which is an insoluble drug to efficiently improve the bioavailability when it is orally administered.

Abstract: The present invention relates to a solid dispersion characterized in that it comprises carbamic acid 3-(4-benzyloxy-phenyl)-isoxazol-5-ylmethyl ester as an active ingredient and a water-soluble polymer having a glass transition temperature lower than the melting point of the active ingredient as a carrier, and it is prepared via melt extrusion. The solid dispersion of the present invention remarkably increases the solubility and dissolution rate of the active ingredient which is an insoluble drug to efficiently improve the bioavailability when it is orally administered.

Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

Abstract: [PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.

Abstract: A method to produce and manufacture cocrystals and salts is disclosed wherein crystalline solids and other components were combined in the desired proportions into a mixing chamber and mixed at high intensity to afford a cocrystalline product. No grinding media were required. The mixing system consists of a resonant acoustic vibratory system capable of supplying a large amount of energy to the mixture and is tunable to a desired resonance frequency and amplitude. The use of resonant acoustic mixing to assist cocrystallization is novel. This discovery enables the manufacture of cocrystals and salt forms, simplifying their manufacture and scale-up, and avoiding the use of grinding methods or grinding media. The present invention affords the manufacture of cocrystals and salts on kilogram to multi-ton scale and is adaptable to continuous manufacturing through the use of resonant mixing methods.

Abstract: The invention relates to a process for the asymmetric transfer hydrogenation of a ketone substrate to produce as chiral secondary alcohol with an ee of greater than 85% in which an enantio-enriched chiral catalyst containing ruthenium or rhodium is used with a hydrogen donor and in which an anion exchange resin is used as a base.

Abstract: The present invention provides a novel process for the preparation of 10-oxo-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxamide, commonly known as oxcarbazepine, which is a medicament and a useful intermediate in the preparation of eslicarbazepine acetate. The present invention further provides a process for the preparation and purification of eslicarbazepine acetate.

Abstract: A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition.

Abstract: The invention provides a drug selected from eslicarbazepine acetate and eslicarbazepine, for use in treating or preventing a disorder selected from epilepsy, affective disorders, schizoaffective disorders, bipolar disorders, neuropathic pain and neuropathic pain related disorders, attention disorders, anxiety disorders, sensorimotor disorders, vestibular disorders, and fibromyalgia, in a patient suffering from or susceptible to absence seizures.

Abstract: The present disclosure relates to the treatment of various diseases and conditions with eslicarbazepine acetate. The present disclosure also relates to the use of eslicarbazepine acetate in a method for reducing or decreasing epileptic seizures in a patient. The present disclosure also relates to a method for increasing the exposure to eslicarbazepine in a patient. The present disclosure also relates to a method of preparing a pharmaceutical composition comprising eslicarbazepine acetate.

Abstract: The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R1, R6-R8, R16, R18, R19, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.

Abstract: The present invention provides a novel process for the preparation of substituted optically pure (S)-(+)- or (R)-(?)-10-hydroxy-dihydrodibenz[b,f]azepines or derivatives thereof, starting from 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepines using boronate esters or their derivatives. The present invention also provides use of thus prepared (S)-(+)- or (R)-(?)-10-hydroxy-dihydrodibenz[b,f]azepines for the preparation of their ester such as (S)-(?)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide or (R)-(+)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide. The present invention also provides novel solid state crystalline forms J1, J2, J3, J4 and amorphous form of eslicarbazepine and the process for the preparation thereof. Also, the present invention provides novel solid state crystalline form and amorphous form of eslicarbazepine acetate and the process for the preparation thereof.

Abstract: The present disclosure is directed to antibodies specific to carbamazepine, immunogens used to produce the antibodies, and immunoassay kits and methods for using the antibodies.

Abstract: The present invention relates to an improved process for the preparation of 10-oxo-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide (Oxcarbazepine) by reacting 10-methoxy-5H-dibenz[b,f]azepine (10-methoxyiminostilbene) and alkali metal cyanate in presence of ?-hydroxy acids, and also relates to the process for the preparation of carbamazepine from iminostilbene. Further the present invention is directed to the novel crystalline form of 10-methoxy carbamazepine.

Abstract: Cocrystals of pterostilbene are disclosed, including: pterostilbene:caffeine cocrystal, pterostilbene:carbamazepine cocrystal, pterostilbene:glutaric acid cocrystal, and pterostilbene:piperazine cocrystal. The pterostilbene:caffeine cocrystal is polymorphic. Forms I and II of the pterostilbene:caffeine cocrystal are disclosed. The therapeutic uses of the pterostilbene cocrystals and of pharmaceutical/nutraceutical compositions containing them are also disclosed. The disclosure sets out various methods of making and characterizing the pterostilbene cocrystals.

Abstract: A novel compound having NMDA receptor channel blocking activity, is provided. A pharmaceutical agent comprising the compound is also provided. The pharmaceutical agent can be used for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, and can comprise a compound having NMDA receptor channel blocking activity and represented by the formula (1), or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to a process for the asymmetric transfer hydrogenation of a ketone substrate to produce as chiral secondary alcohol with an ee of greater than 85% in which an enantio-enriched chiral catalyst containing ruthenium or rhodium is used with a hydrogen donor and in which an anion exchange resin is used as a base.

Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

Abstract: A process for preparing a compound of the formula IA or IB: wherein R is alkyl, aminoalkyl, halogenalkyl, aralkyl, cycloalkyl, cycloalkylalkyl, alkoxy, phenyl or substituted phenyl or pyridyl group; the term alkyl means carbon chain, straight or branched, containing from 1 to 18 carbon atoms; the term halogen represents fluorine, chlorine, bromine or iodine; the term cycloalkyl represents a saturated alicyclic group with 3 to 6 carbon atoms; the term aryl represents unsubstituted phenyl group or phenyl substituted by alkoxy, halogen or nitro group, the process comprising asymmetric hydrogenation of a compound of the formula II: wherein R has the same meanings as above, using a chiral catalyst and a source of hydrogen.

Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

Abstract: The present disclosure is directed to antibodies specific to carbamazepine, immunogens used to produce the antibodies, and immunoassay kits and methods for using the antibodies.

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: The present invention relates to the purification and particle size of eslicarbazepine acetate. The present invention also relates to the physical characteristics of solid state eslicarbazepine acetate, and pharmaceutical compositions containing the same.

Abstract: A method for chiral inversion of optically pure or optically enriched mixtures of (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (I) and (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II).

Abstract: A process for preparing 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide, compound of formula (I), said process comprising a. reacting compound of formula (Ivb) with alkali metal methoxide to yield compound of formula (II); and b. converting compound of formula (II) to compound of formula (I).

Abstract: The present invention discloses a composition containing a conjugate comprising two moieties covalently linked by a thiourea linker and thiourea or a derivative thereof in free form. It also relates to a method for stabilizing a conjugate comprising two moieties covalently linked by a thiourea linker is described the method comprising the steps of providing the conjugate, adding thereto thiourea or a derivative thereof in free form and thereby stabilizing the conjugate and to the use of a composition containing a conjugate comprising two moieties covalently linked by a thiourea linker and thiourea or a derivative thereof in free form.

Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.

Abstract: The present invention relates to an improved process for the preparation of 10-oxo-10,11-dihydiO-5H-dibenz[b,fjazepine-5-carboxamide (Oxcarbazepine) by reacting 10-methoxy-5H-dibenz[b,f]azepine (10-methoxyiminostilbene) and alkali metal cyanate in presence of ?-hydroxy acids, and also relates to the process for the preparation of carbamazepine from iminostilbene. Further the present invention is directed to the novel crystalline form of 10-methoxy carbamazepine.

Abstract: A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxyamide by hydrolysis of 5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine with peroxy compounds in alkali medium and in the presence of solvents.

Abstract: Process for preparing oxcarbazepine according to the steps of chlorocarbonylating (a), ammonolysis (b), and deprotecting (c). The invention is characterized by the use of triphosgene as chlorocarbonylating agent in step a).

Abstract: (S)-(+)-10,11-Dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxyamide is prepared starting from racemic 5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine by phthaloylation, separation of the diastereomeric salts of the phthaloyl derivative with (S)-phenylethylamine, hydrolysis of the (S, S) salt to (S)-(+)-5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine and hydrolysis of the nitrile group of the latter to amido group, by treatment with peroxy compounds in alkali medium.

Abstract: A process for the preparation of 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (1) by ring opening of 11a,10b-dihydro-6H-dibenz/b,f/oxireno[d]azepine-6-carboxamide (5), characterised in that the ring opening is carried out under conditions of elevated pressure.

Abstract: An efficient and high-yielding method for the preparation of optically pure (S)-(+)-10,11 -dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide and (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide by resolution of racemic (±)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide using a tartaric acid anhydride.

Abstract: The present invention relates to compounds and compositions useful for reducing the risk of epileptic occurrences and/or for alleviating epileptic phenomena in patients. In accordance with the invention, the compounds and compositions have at least the following two components: a) vitamin B6-based component selected from pyridoxal, pyridoxamine, pyridoxine, their pharmaceutically acceptable functional derivatives and salts; and b) at least one antiepileptic drug (AED) or anticonvulsive, neuro-protective drug or nootrope compound or moiety. The invention further relates to methods for preventing epileptic episodes and for alleviating epileptic episodes, as well as methods for reducing side effects of antiepileptic drugs.

Abstract: The present invention provides a method of preparing a 5H-dibenz[b,f]azepine-5-carboxamide of formula (1) wherein R1, R2, R3, and R4 are independently selected from the group consisting of hydrogen, halogen, nitro, cyano, carboxyl, A, —CO(A), —OCO(A), —O(A), —N(A)2, —CON(A)2, and —COO(A), wherein A is selected from the group consisting of C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C5-C10 cycloalkenyl, C2-C10 alkynyl, and C6-C20 aryl, wherein the two A groups of —N(A)2 and —CON(A)2 can be the same or different, and wherein R2 and R3 can together form a bond; comprising reacting a 5H-dibenz[b,f]azepine of formula (2) with a) a cyanate salt selected from the group consisting of alkali metal cyanate salts and alkaline-earth metal cyanate salts, and b) a salt of an amino compound having no N—H bonds, wherein the salt has a Ka (25° C.) of at least about 10×10?11.

Abstract: The present invention relates to the use of a mixture of the enantiomers of a compound of formula I or of pharmaceutically acceptable salts of said enantiomers consisting of at least 55% of the R-enantiomer, most preferably of at least 98% of the R-enantiomer, and not more than 45% of the S-enantiomer, most preferably not more than 2% of the S-enantiomer, for the manufacture of a pharmaceutical composition for the treatment of neuropathic pain; to a method for the treatment of neuropathic pain; and to a pharmaceutical composition comprising as active agent a mixture of the enantiomers of the compound of formula I or pharmaceutically acceptable salts of said enantiomers consisting of at least 55% of the R-enantiomer and not more than 45% of the S-enantiomer.

Abstract: This invention relates to the use of 5H-dibenz/b,f/azepine-5-carboxamide derivatives in the manufacture of various medicaments for treating neuropathic pain and for treating neurological disorders which involve both motor impairment and neuropathic pain.

Abstract: A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX2(L)]2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R1 is chosen from C1-6 alkoxy and C1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R1 can be the same or different, and R2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR3R4R5 and formic acid, [R3R4R5NH][OOCH] and optionally formic acid, or [M][OOCH]x and formic acid, wherein R3, R4 and R5 are C1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.

Abstract: The present invention relates to dosage forms of oxcarbazepine for oral administration that contain oxcarbazepine having a median particle size of from about 14 ?m to about 30 ?m and to processes for the preparation of such dosage forms. The dosage form may be a solid or a liquid dosage form. The solid dosage form may be in the form of a tablet, a capsule, or a granulate. The liquid dosage form may be in the form of a solution or a suspension.

Abstract: The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical compositions which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating central nervous system disorders, obesity, and metabolic disorders.

Abstract: To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. A pharmaceutical agent for the treatment or prevention of a disease caused by overexcitation of an NMDA receptor, which comprises a compound having NMDA receptor channel blocking activity and represented by the formula (1), a salt thereof, or a hydrate of the compound or the salt.

Abstract: (S)-(+)-10,11-Dihydro-10-hydroxy-5H-dibenz[b,f]azepine-5-carboxyamide is prepared starting from racemic 5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine by phthaloylation, separation of the diastereomeric salts of the phthaloyl derivative with (S)-phenylethylamine, hydrolysis of the (S, S) salt to (S)-(+)-5-cyano-10,11-dihydro-10-hydroxy-5H-dibenz[b,f]azepine and hydrolysis of the nitrile group of the latter to amido group, by treatment with peroxy compounds in alkali medium.

Abstract: The present application describes deuterium-enriched oxcarbazepine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: A compound of formula (I) or tautomers, or stereoisomers, or solvates, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, T, L, W, X, Y and A are as defined herein for the for treatment of conditions mediated by the blockade of an epithelial sodium channel, particularly an inflammatory or allergic condition.

Abstract: A process for preparing 5H-dibenz[b,f]azepine-5-carboxamide of the general formula: wherein R1, R2, R3 and R4 are the same or different and can be hydrogen, halogen, nitro, cyano, carboxyl, R, —CO(R), —OCO(R), —O(R), —N(R)2, —CON(R)2, and —COO(R), wherein R is selected from the group consisting of C1-C10 alkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C5-C10 cycloalkenyl, C2-C10 alkynyl, and C6-C20 aryl, wherein the two A groups of —N(A)2 and —CON(A)2 can be the same or different, and wherein R2 and R3 can together form a bond is provided; the process comprising reacting 5H-dibenz[b,f]azepine of the general formula wherein R1, R2, R3 and R4 have the aforementioned meanings, with one or more alkali or alkaline-earth cyanates and in the presence of one or more unsaturated dicarboxylic acids.

Abstract: A method for chiral inversion of optically pure or optically enriched mixtures of (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (I) and (R)-(?)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide (II).

Abstract: A process for preparing 10,11-dihydro-10-oxo-5H-dibenz[b,f]azepine-5-carboxamide, compound of formula (I), said process comprising a. reacting compound of formula (Ivb) with alkali metal methoxide to yield compound of formula (II); and b. converting compound of formula (II) to compound of formula (I).