Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Nitrogen Of The Tricyclo Ring System Patents (Class 540/589)
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Patent number: 11224597Abstract: 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.Type: GrantFiled: October 13, 2016Date of Patent: January 18, 2022Assignee: ViiV Healthcare CompanyInventors: Deepak B. Mundhra, Rennan Pan
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Patent number: 9845293Abstract: Object of the present invention is an improved process for the preparation of Elsicarbazepine and Eslicarbazepine acetate by means of chiral Ruthenium catalysts.Type: GrantFiled: February 23, 2016Date of Patent: December 19, 2017Assignee: F.I.S.—FABBRICA ITALIANA SINTETICI S.P.A.Inventors: Simone Zaramella, Emiliano Rossi, Ottorino De Lucchi, Siro Serafini
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Patent number: 9724335Abstract: 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.Type: GrantFiled: December 29, 2016Date of Patent: August 8, 2017Assignee: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Myoung Ki Baek, Augustin Pegan
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Patent number: 9566268Abstract: 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.Type: GrantFiled: August 8, 2016Date of Patent: February 14, 2017Assignee: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Myoung Ki Baek, Augustin Pegan
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Patent number: 9439970Abstract: 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.Type: GrantFiled: November 7, 2013Date of Patent: September 13, 2016Assignee: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Myoung Ki Baek, Augustin Pegan
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Patent number: 9206135Abstract: 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.Type: GrantFiled: October 15, 2012Date of Patent: December 8, 2015Assignee: Bial-Portela & CA, S.A.Inventors: David Alexander Learmonth, Gabriela Alexandra Grasa, Antonio Zanotti-Gerosa
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Patent number: 8987253Abstract: [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.Type: GrantFiled: May 31, 2013Date of Patent: March 24, 2015Assignee: National University Corporation Chiba UniversityInventors: Kazuei Igarashi, Hiromitsu Takayama
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Publication number: 20150080567Abstract: 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.Type: ApplicationFiled: August 28, 2014Publication date: March 19, 2015Applicant: Nalas Engineering Services Inc.Inventors: Jerry Salan, Stephen R. Anderson, David J. am Ende
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Patent number: 8975396Abstract: 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.Type: GrantFiled: April 14, 2011Date of Patent: March 10, 2015Assignee: Euticals GmbHInventors: Richard Wisdom, Joerg Jung, Andreas Meudt
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Publication number: 20150065704Abstract: 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.Type: ApplicationFiled: July 11, 2012Publication date: March 5, 2015Inventors: Ketan Hirpara, Chandra Has Khanduri, Mukesh Kumar Sharma
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Publication number: 20140343043Abstract: 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.Type: ApplicationFiled: December 17, 2013Publication date: November 20, 2014Applicant: BIAL - PORTELA & C.A., S.A.Inventors: Teófilo Cardoso de Vasconcelos, Ricardo Jorge dos Santos Lima, Rui Cerdeira de Campos Costa
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Publication number: 20140315821Abstract: 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.Type: ApplicationFiled: August 24, 2012Publication date: October 23, 2014Applicant: BIAL - PORTELA & Ca, S.A.Inventor: Patricio Manuel Vieira Araujo Soares Da Silva
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Publication number: 20140288058Abstract: 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.Type: ApplicationFiled: February 21, 2014Publication date: September 25, 2014Applicant: Bial-Portela & CA. S.A.Inventors: Jose' Luis de Almeida, Patricio Manuel Vieria Arauj Soares da Silva
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Publication number: 20140113890Abstract: 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.Type: ApplicationFiled: December 23, 2013Publication date: April 24, 2014Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Avinash Phadke, Dawei Chen, Venkat Gadhachanda, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Atul Agarwal, Ha Young Kim, Shuoming Li, Cuixian Liu, Suoming Zhang, Milind Deshpande
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Publication number: 20130345198Abstract: 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.Type: ApplicationFiled: March 6, 2012Publication date: December 26, 2013Applicant: JUBILANT LIFE SCIENCES LIMITEDInventors: Sujay Biswas, Shailendra Kumar Dubey, Vikas Bansal, Mukesh Masand, Dharam Vir
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Patent number: 8563713Abstract: 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.Type: GrantFiled: March 22, 2011Date of Patent: October 22, 2013Assignee: Guangzhou Kingmed Center for Clinical LaboratoryInventors: Liuming Yu, Yaoming Liang, Hongbo Li
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Patent number: 8530647Abstract: 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.Type: GrantFiled: May 6, 2009Date of Patent: September 10, 2013Assignee: Mylan Laboratories LimitedInventors: Nageswara Rao Karusala, Uma Sankara Sastry Tummalapally, Appi Reddy Talatala, Debashish Datta
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Patent number: 8513236Abstract: 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.Type: GrantFiled: July 30, 2010Date of Patent: August 20, 2013Assignee: Laurus Labs Private LimitedInventors: Nathan C. Schultheiss, Sarah J. Bethune
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Patent number: 8476258Abstract: 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.Type: GrantFiled: April 26, 2007Date of Patent: July 2, 2013Assignee: National University Corporation Chiba UniversityInventors: Kazuei Igarashi, Hiromitsu Takayama
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Publication number: 20130123490Abstract: 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.Type: ApplicationFiled: April 14, 2011Publication date: May 16, 2013Applicant: Euticals GmbHInventors: Richard Wisdom, Joeng Jung, Andress Meudt
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Publication number: 20130041146Abstract: 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.Type: ApplicationFiled: October 15, 2012Publication date: February 14, 2013Applicant: BIAL - PORTELA & C.A., S.A.Inventor: BIAL - PORTELA & C.A., S.A.
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Patent number: 8367821Abstract: 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.Type: GrantFiled: April 11, 2007Date of Patent: February 5, 2013Assignee: BIAL—Portela & C.A., S.A.Inventors: Bing Yu, Wenge Li, David Alexander Learmonth
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Patent number: 8288532Abstract: 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.Type: GrantFiled: April 21, 2006Date of Patent: October 16, 2012Assignee: Bial-Portela & CA., S.A.Inventors: David Alexander Learmonth, Gabriela Alexandra Grasa, Antonio Zanotti-Gerosa
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Publication number: 20120244546Abstract: 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.Type: ApplicationFiled: March 22, 2011Publication date: September 27, 2012Applicant: Guangzhou Kingmed Center for Clinical LaboratoryInventors: Liuming YU, Yaoming Liang, Hongbo Li
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Publication number: 20120197005Abstract: 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.Type: ApplicationFiled: January 30, 2012Publication date: August 2, 2012Applicant: UCHICAGO ARGONNE, LLCInventors: Chris J. Benmore, Johann R. Weber
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Publication number: 20120022047Abstract: 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.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: GLENMARK GENERICS LTDInventors: Joseph Prabahar Koilpillai, Pravin Bhalchandra Kulkarni, Sachin Bapurao Sawant, Nagesh Devidasrao Limbekar
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Patent number: 7999100Abstract: 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).Type: GrantFiled: July 13, 2005Date of Patent: August 16, 2011Assignee: Bial-Portela CA & S.A.Inventors: David Alexander Learmonth, Günter Weingaertner, Matthias Kraemer
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Patent number: 7982032Abstract: 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).Type: GrantFiled: March 10, 2005Date of Patent: July 19, 2011Assignee: Sun Pharmaceutical Industries LimitedInventors: Mandakini Muthukumaran, Muthukumaran Natarajan, Rajamannar Thennati
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Publication number: 20110112291Abstract: 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.Type: ApplicationFiled: November 26, 2008Publication date: May 12, 2011Inventors: Eva Hoess, Rene Blind, Gerhard Fink, Hans-Joachim Kytzia
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Publication number: 20110086818Abstract: 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.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
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Publication number: 20110065917Abstract: 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.Type: ApplicationFiled: May 6, 2009Publication date: March 17, 2011Applicant: MATRIX LABORATORIES LTDInventors: Nageswara Rao Karusala, Uma Sankara Sastry Tummalapally, Appi Reddy Talatala, Debashish Datta
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Process for the preparation of (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz (b,f)azepine-5-carboxamide
Patent number: 7858780Abstract: (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.Type: GrantFiled: November 15, 2005Date of Patent: December 28, 2010Assignee: Farchemia S.R.L.Inventors: Mauro Panunzio, Eileen Campana, Sabatino Pulcini, Gabriele Breviglieri -
Patent number: 7858778Abstract: 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.Type: GrantFiled: November 10, 2005Date of Patent: December 28, 2010Assignee: Farchemia S.R.L.Inventors: Mauro Panunzio, Eileen Campana, Gabriele Breviglieri
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Patent number: 7858779Abstract: 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).Type: GrantFiled: February 21, 2005Date of Patent: December 28, 2010Assignee: Archimica S.r.l.Inventors: Aldo Banfi, Deborah Bollini, Maurizio Serra, Gianluca Di Lernia
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Patent number: 7834177Abstract: 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.Type: GrantFiled: January 13, 2006Date of Patent: November 16, 2010Assignee: Bial - Portela & CA, S.A.Inventors: David Alexander Learmonth, Günter Weingärtner, Matthias Kraemer
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Patent number: 7820813Abstract: 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.Type: GrantFiled: September 25, 2006Date of Patent: October 26, 2010Assignee: Portela & C.A., S.A.Inventor: David Alexander Learmonth
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Patent number: 7745426Abstract: 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.Type: GrantFiled: August 12, 2004Date of Patent: June 29, 2010Assignees: D-Pharm Ltd., Advanced Neuroprotective Systems Ltd.Inventors: Svetlana Dolina, Vitaly Shteiman, Marina Vinnikova, Israel Shapiro
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Patent number: 7723514Abstract: 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.Type: GrantFiled: June 29, 2006Date of Patent: May 25, 2010Assignee: Taro Pharmaceuticals U.S.A., Inc.Inventors: Daniella Gutman, Wael Baidossi
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Publication number: 20100120746Abstract: 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.Type: ApplicationFiled: December 8, 2009Publication date: May 13, 2010Inventors: Alyson Fox, Stuart Bevan
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Publication number: 20090209517Abstract: 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.Type: ApplicationFiled: February 14, 2007Publication date: August 20, 2009Inventor: Patricio Manuel Vieira Araújo Soares Da Silva
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Publication number: 20090203902Abstract: 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.Type: ApplicationFiled: April 21, 2006Publication date: August 13, 2009Inventors: David Alexander Learmonth, Gabriela Alexandra Grasa, Antonio Zanotti-Gerosa
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Publication number: 20090196919Abstract: 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.Type: ApplicationFiled: October 24, 2005Publication date: August 6, 2009Inventors: Ajay Singla, Sachin Arora, Rahul Dabre
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Publication number: 20090143361Abstract: 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.Type: ApplicationFiled: November 25, 2008Publication date: June 4, 2009Applicants: ELBION GMBH, WYETHInventors: Michael S. Malamas, Yike Ni, James Joseph Erdei, Hans Stange, Rudolf Schindler, Norbert Hofgen, Ute Egerland, Barbara Langen
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Publication number: 20090105472Abstract: (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.Type: ApplicationFiled: November 15, 2005Publication date: April 23, 2009Inventors: Mauro Panunzio, Eileen Campana, Sabatino Pulcini, Gabriele Breviglieri
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Publication number: 20090105223Abstract: 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.Type: ApplicationFiled: April 26, 2007Publication date: April 23, 2009Applicant: NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITYInventors: Kazuei Igarashi, Hiromitsu Takayama
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Publication number: 20090082335Abstract: The present application describes deuterium-enriched oxcarbazepine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 19, 2008Publication date: March 26, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20080312212Abstract: 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.Type: ApplicationFiled: December 20, 2006Publication date: December 18, 2008Inventors: Stephen Paul Collingwood, Nichola Smith
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Patent number: 7459553Abstract: 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.Type: GrantFiled: March 11, 2005Date of Patent: December 2, 2008Assignee: Glenmark Generics Ltd.Inventors: Bobba Venkata Sivakumar, Shekhar Bhaskar Bhirud, Chandrasekhar Batchu, Sanjay Anantha Kale
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Publication number: 20080293934Abstract: 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).Type: ApplicationFiled: July 13, 2005Publication date: November 27, 2008Inventors: David Alexander Learmonth, Gunter Weingaertner, Matthias Kraemer
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Publication number: 20080269480Abstract: 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).Type: ApplicationFiled: March 10, 2005Publication date: October 30, 2008Inventors: Mandakini Muthukumaran, Muthukumaran Natarajan, Rajamannar Thennati