A Ring Or Polycyclo Ring System In A Substituent E Is Attached Indirectly To The Carboxamide Nitrogen Or To An Amino Nitrogen In Substituent E By Acyclic Nonionic Bonding Patents (Class 564/219)
  • Patent number: 9409857
    Abstract: The present invention relates to an Agomelatine sulfuric acid complex in formula (I) and the preparation method thereof (HX=H2SO4, RSO3H (R?CH3, Ph, 4-CH3Ph)). The solubility of the Agomelatine sulfuric acid complex obtained by the method of the present invention is significantly improved compared with Agomelatine, has good stability and higher purity, and is suitable for application in finished-product medicinal preparations. The preparation process is quite simple, and a product with high purity can be obtained without special operations.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: August 9, 2016
    Assignee: SHANGHAI RIGHTHAND PHARMTECH, CO., LTD.
    Inventors: Haiping Wang, Cheng Chi, Zhengming Chi, Jin Wang, Guanyu Xu
  • Publication number: 20150148419
    Abstract: Isolated metabolites of (1R-trans)-N-[[2-(2,3-dihydro-4-benzofuranyl)cyclopropyl]-methyl]propanamide, methods for their use, and compositions containing the metabolites.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 28, 2015
    Inventors: Marlene Michelle Dressman, Deepak Phadke
  • Publication number: 20150141519
    Abstract: The present invention relates to an Agomelatine sulfuric acid complex in formula (I) and the preparation method thereof (HX=H2SO4, RSO3H (R=CH3, Ph, 4-CH3Ph)). The solubility of the Agomelatine sulfuric acid complex obtained by the method of the present invention is significantly improved compared with Agomelatine, has good stability and higher purity, and is suitable for application in finished-product medicinal preparations. The preparation process is quite simple, and a product with high purity can be obtained without special operations.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Inventors: Haiping Wang, Cheng Chi, Zhengming Chi, Jin Wang, Guanyu Xu
  • Patent number: 9024068
    Abstract: The invention concerns a new process for the preparation of crystalline form of agomelatine from a solution of agomelatine in a solvent, characterized in that the agomelatine is crystallized by instantaneous precipitation from said solution, at a temperature equal to or below ?10° C.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: May 5, 2015
    Assignee: Laboratorio Chimico Internazionale S.p.A.
    Inventors: Bruno De Angelis, Faris Garis, Salvatore De Gennaro, Giorgio Bertolini
  • Patent number: 8927771
    Abstract: The present invention relates to novel solid forms of agomelatine (I), specifically novel phaamaceutically acceptable cocrystals thereof, as well as to methods of preparing them. Three pharmaceutically acceptable cocrystals of (I) that have physico-chemical properties acceptable for pharmaceutical development were obtained.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: January 6, 2015
    Assignee: Zentiva k.s.
    Inventors: Gary James Miller, Ludek Ridvan, Jindrich Richter, Ondrej Dammer, Tomas Chvojka, Tomas Pekarek, Winfried Heyse, Norbert Nagel
  • Publication number: 20150004110
    Abstract: The 1-aryl-2-aryloxyethane compounds of Formula 1 in which n and m are zero or equal to 1, provided that n+m=1, R1 and R2 in particular representing hydrogen atoms, R3 and R4 in particular representing hydrogen atoms, halogen atoms, hydroxy or alkoxy groups, and R5 in particular representing hydrogen atoms, hydroxy, alkyl, alkoxy, amino or nitro groups, in cosmetic compositions intended for anti-ageing and/or depigmenting and/or anti-inflammatory and/or wound-healing care.
    Type: Application
    Filed: December 18, 2012
    Publication date: January 1, 2015
    Applicant: DIVERCHIM
    Inventors: Natacha Frison, Benoit Folleas, Jean-Louis Brayer, Florence Wafflart
  • Patent number: 8871975
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: October 28, 2014
    Assignee: Les Laboratories Servier
    Inventors: Samir Zard, Béatrice Sire, Mehdi Boumediene
  • Publication number: 20140221690
    Abstract: The invention concerns a new process for the preparation of two crystalline forms of agomelatine, in particular a process for preparation of form I and a new form of agomelatine, here called form VII.
    Type: Application
    Filed: December 29, 2011
    Publication date: August 7, 2014
    Applicant: LABORATORIO CHIMICO
    Inventors: Bruno De Angelis, Faris Garis, Salvatore De Gennaro, Giorgio Bertolini
  • Patent number: 8779199
    Abstract: The present invention relates to the intermediate compounds for preparation of agomelatine, as well as the preparation methods thereof The intermediate of the present invention for preparation of agomelatine is compound A as shown in the following formula. Also provided are two novel intermediate compounds. When we use these new intermediate compounds to prepare agomelatine, it is simple to manipulate, well-controlled and with high purity, without complicated operations such as rectification and column chromatography separation, and suitable for industrial production. Meanwhile, the preparation methods of the two new intermediates themselves is simple and high yield, only using the most commonly-used 7-methoxy-tetralone as original starting material and undergoing one step of reaction to obtain the intermediates, followed by one more step of converting the intermediate compounds to desired product agomelatine.
    Type: Grant
    Filed: June 8, 2011
    Date of Patent: July 15, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Peng Zhang, Yu Huang, Zhedong Yuan, Hanbin Shan, Xiong Yu
  • Patent number: 8729132
    Abstract: The present invention relates to an agomelatine hydrobromide hydrate of formula I wherein X is Br, preparation and use thereof, and to pharmaceutical compositions containing it. The agomelatine hydrobromide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: May 20, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Hanbin Shan, Zhedong Yuan, Xueyan Zhu, Peng Zhang, Hongjuan Pan, Xiong Yu
  • Patent number: 8729131
    Abstract: The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: May 20, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Hanbin Shan, Zhedong Yuan, Xueyan Zhu, Peng Zhang, Hongjuan Pan, Xiong Yu
  • Patent number: 8722929
    Abstract: This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: May 13, 2014
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Jianlan Song, Huanming Chen, Zhi Hong
  • Patent number: 8716508
    Abstract: The present disclosure relates to a method for preparing a metal catalyst comprising at least one ligand that is coordinated to the metal through at least one phosphorous (P) atom and at least one nitrogen (N) atom, the method comprising reacting a metal pre-cursor complex with an acid addition salt of an aminophosphine, diaminophosphine, aminodiphosphine or diaminodiphosphine, in the presence of a base.
    Type: Grant
    Filed: October 8, 2009
    Date of Patent: May 6, 2014
    Assignee: Kanata Chemical Technologies Inc.
    Inventors: Kamaluddin Abdur-Rashid, Dino Amoroso, Xuanhua Chen, Rongwei Guo, Shuiming Lu, Chi-Wing Tsang
  • Patent number: 8710101
    Abstract: New co-crystal of agomelatine composed of: agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I) and an organic acid. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: April 29, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Philippe Letellier, Michael Lynch, Jean-Manuel Pean
  • Publication number: 20140051887
    Abstract: The present invention relates to novel solid forms of agomelatine (I), specifically novel phaamaceutically acceptable cocrystals thereof, as well as to methods of preparing them. Three pharmaceutically acceptable cocrystals of (I) that have physico-chemical properties acceptable for pharmaceutical development were obtained.
    Type: Application
    Filed: April 25, 2012
    Publication date: February 20, 2014
    Inventors: Gary James Miller, Ludek Ridvan, Jindrich Richter, Ondrej Dammer, Tomas Chvojka, Tomas Pekarek, Winfried Heyse, Norbert Nagel
  • Publication number: 20140011883
    Abstract: The present invention provides a new crystalline form VII of agomelatine, its method of preparation, application and pharmaceutical composition. This new crystalline form offers high purity, a stable crystalline structure and good reproducibility, while its method of production lends itself well to large scale production. In terms of stability and purity, it is superior to the numerous crystalline forms which have hitherto been reported. As a result, the crystalline form VII of the present invention possesses advantages in pharmaceutical preparation.
    Type: Application
    Filed: March 22, 2012
    Publication date: January 9, 2014
    Applicants: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, LES LABORATOIRES SERVIER
    Inventors: Yu Huang, Ling Tong, Xueyan Zhu, Hanbin Shan, Zhedong Yuan, Xiong Yu
  • Publication number: 20130289125
    Abstract: Methods and compositions for pest control, and more particularly for control of ants, e.g., of the subfamily Myrmicinae, using tyramides.
    Type: Application
    Filed: November 3, 2011
    Publication date: October 31, 2013
    Inventors: Tappey H. Jones, Robert Kenneth Vander Meer
  • Publication number: 20130289308
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Application
    Filed: January 4, 2012
    Publication date: October 31, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Samir Zard, Béatrice Sire, Mehdi Boumediene
  • Publication number: 20130281664
    Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.
    Type: Application
    Filed: October 11, 2011
    Publication date: October 24, 2013
    Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
  • Publication number: 20130267738
    Abstract: The present invention relates to the intermediate compounds for preparation of agomelatine, as well as the preparation methods thereof. The intermediate of the present invention for preparation of agomelatine is compound A as shown in the following formula. Also provided are two novel intermediate compounds. When we use these new intermediate compounds to prepare agomelatine, it is simple to manipulate, well-controlled and with high purity, without complicated operations such as rectification and column chromatography separation, and suitable for industrial production. Meanwhile, the preparation methods of the two new intermediates themselves is simple and high yield, only using the most commonly-used 7-methoxy-tetralone as original starting material and undergoing one step of reaction to obtain the intermediates, followed by one more step of converting the intermediate compounds to desired product agomelatine.
    Type: Application
    Filed: June 8, 2011
    Publication date: October 10, 2013
    Applicant: LES LABORATORIES SERVIER
    Inventors: Peng Zhang, Yu Huang, Zhedong Yuan, Hanbin Shan, Xiong Yu
  • Publication number: 20130245321
    Abstract: Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).
    Type: Application
    Filed: October 11, 2012
    Publication date: September 19, 2013
    Inventors: SARAH SPIEGEL, ROBERT ELLIOT ZIPKIN, JEFFREY KROLL ADAMS
  • Patent number: 8436208
    Abstract: A process for the preparation of a substituted 2,2?-dithiophene is described, which process comprises the steps (a), (c) and optional steps (b) and (d): a reaction of a compound of the formula: with a suitable lithium organic compound, preferably Li-alkyl or Li-alkylamide; b) optional exchange of lithium against another metal selected from Mg1 Zn and Cu; c) reaction of the metallated intermediate obtained in step (a) or (b) with a suitable electrophil, which is CO2 or an aldehyde (addition reaction), or a compound Y?—R17 or Y?—R18-Z (substitution reaction), where R17 and R18 are as defined in claim 1; and optionally d) modification of the product obtained in step (c), e.g. by introducing one or more conjugating moieties Y ring closure between suitable monovalent residues R17, exchange or extension of functional groups or substituents such as addition to carbonyl or substitution of carbonyl in R17 or R18.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: May 7, 2013
    Assignee: BASF SE
    Inventors: Hans Jürg Kirner, Frank Bienewald, Jean-Charles Flores, Olivier Frédéric Aebischer
  • Patent number: 8377990
    Abstract: A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: February 19, 2013
    Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan University
    Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
  • Publication number: 20130005820
    Abstract: The present invention relates to an agomelatine hydrochloride hydrate of formula I, preparation and use thereof, and to pharmaceutical composition containing it. The agomelatine hydrohalide hydrate obtained through the present method has significant increased solubility than agomelatine, and therefore is more suitable for manufacturing pharmaceutical formulations. In addition, the product enjoys higher stability and purity. Using the present method, product of high purity can be obtained through a simple process, free of any complicated steps. wherein X is Cl.
    Type: Application
    Filed: March 17, 2011
    Publication date: January 3, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Hanbin Shan, Zhedong Yuan, Xueyan Zhu, Peng Zhang, Hongjuan Pan, Xiong Yu
  • Publication number: 20120316245
    Abstract: New co-crystal of agomelatine composed of: agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide of formula (I) and an organic acid. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Application
    Filed: June 8, 2012
    Publication date: December 13, 2012
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Philippe Letellier, Michael Lynch, Jean-Manuel Pean
  • Publication number: 20120252901
    Abstract: Agomelatine crystal, which is a drug for treating depression, and pharmaceutical compositions thereof are provided. The X-ray powder diffraction spectra of such agomelatine crystal, which is irradiated by Cu-K? and showed by 2?(degree), has characteristic diffraction peaks at 12.84, 13.84, 16.14, 18.56, 19.12, 20.86, 21.20, 23.84; its IR absorption pattern has characteristic absorption peaks at about 3234, 3060, 2940, 1638, 1511, 1436, 1249, 1215, 1184, 1032, 908, 828, 755, 588 cm-1, and its DSC endothermic transition temperature is 97.6° C. The use of the agomelatine crystal as an active ingredient in preparing a medicament for the treatment of depression is also provided.
    Type: Application
    Filed: December 13, 2010
    Publication date: October 4, 2012
    Applicant: TIANJIN TAIPU PHARMACEUTICAL SCIENCE & TECHNOLOGY DEVELOPMENT CO., LTD
    Inventors: Jianqiang Zhu, Qingson Tian, Jian Zhao
  • Patent number: 8252957
    Abstract: Process for obtaining the crystalline form V of the compound of formula (I):
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: August 28, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Damien Martins, Gerard Coquerel, Julie Linol, Pascal Langlois
  • Publication number: 20120214785
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: August 17, 2011
    Publication date: August 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
  • Publication number: 20120214852
    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.
    Type: Application
    Filed: November 8, 2011
    Publication date: August 23, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Publication number: 20120209003
    Abstract: Methods for identifying MarR family inhibiting compounds are described. The methods include the use of computer aided rational based drug design programs and three dimensional structures of MarR family polypeptides.
    Type: Application
    Filed: September 9, 2011
    Publication date: August 16, 2012
    Applicant: Paratek Pharmaceuticals, Inc.
    Inventors: Michael N. Alekshun, Stuart B. Levy, Brent L. Podlogar, Roger Frechette
  • Patent number: 8242264
    Abstract: The present invention relates to a process for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine and the intermediates thereof. The present invention provides a compound represented by formula I and a compound represented by formula II, and processes for preparing 4-acetyl-2,3,4,5-tetrahydro-benzo[1,4]diazepine by using the compound represented by formula I, the compound represented by formula II and o-nitrobenzaldehyde. The invention has the advantages of the shorter synthesis steps, easily available raw materials and simple operation. Moreover, the process is economic and safe by avoiding the use of expensive and dangerous lithium aluminum hydride.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: August 14, 2012
    Assignees: Topharman Shanghai Co., Ltd., Weifang Tehua Chemical Co., Ltd.
    Inventors: Fuqiang Zhu, Haihong Li, Wenzhong Wang, Hui Zhang, Jingshan Shen
  • Patent number: 8212077
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Grant
    Filed: August 4, 2009
    Date of Patent: July 3, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Christophe Hardouin, Jean-Pierre Lecouve, Nicolas Baragnier
  • Publication number: 20120129894
    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.
    Type: Application
    Filed: May 19, 2011
    Publication date: May 24, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Patent number: 8183415
    Abstract: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: May 22, 2012
    Assignee: Amgen, Inc.
    Inventors: Oliver Thiel, Charles Bernard, Robert Larsen, Michael John Martinelli, Masooma Tamim Raza
  • Publication number: 20120088837
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R1 and R2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.
    Type: Application
    Filed: December 8, 2011
    Publication date: April 12, 2012
    Inventors: Robert Greenhouse, Ralph New Harris, III, Saul Jaime-Figueroa, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Patent number: 8143449
    Abstract: Process for the industrial synthesis of the compound of formula (I)
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: March 27, 2012
    Assignee: Les Laboratoires Servier
    Inventors: Christophe Hardouin, Jean-Pierre Lecouve
  • Patent number: 8134029
    Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: March 13, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Thomas Jerussi, Qun Kevin Fang, Mark G. Currie
  • Publication number: 20120046479
    Abstract: The present disclosure relates to a method for preparing a metal catalyst comprising at least one ligand that is coordinated to the metal through at least one phosphorous (P) atom and at least one nitrogen (N) atom, the method comprising reacting a metal pre-cursor complex with an acid ad salt of an aminophosphine, diaminophosphine, aminodiphosphine or diaminodiphosphine, in the presence of a base.
    Type: Application
    Filed: October 8, 2009
    Publication date: February 23, 2012
    Inventors: Kamaluddin Abdur-Rashid, Dino Amoroso, Xuanhua Chen, Rongwei Guo, Shuiming Lu, Chi-Wing Tsang
  • Patent number: 8110706
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: February 7, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20120010403
    Abstract: A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I): Ra(Rb)N—CH2—BF3M??(I) as an aminomethylating agent for an aromatic ring; and reacting the aminomethylating agent with an aromatic ring-containing compound, which can react with the aminomethylating agent, under the presence of a metal catalyst such as a palladium compound so as to perform the direct aminomethylation of the aromatic ring.
    Type: Application
    Filed: September 21, 2011
    Publication date: January 12, 2012
    Inventor: Keigo TANAKA
  • Publication number: 20120004313
    Abstract: The invention provides a new crystalline form of agomelatine, preparation and use thereof. The X-ray powder diffraction diagram of the agomelatine crystalline form shows main peaks at the diffraction angles 2? 11.13°, 11.82°, 17.49°, 18.29°, 19.48°, 19.72°, 20.50°, 21.76°, 22.54°, 22.97°, 24.56°, 25.36°, 27.16° and 31.93°. Said new crystalline form is characterized by high purity, stability and good reproducibility, and thus is advantageous for the pharmaceutical formulation. In addition, the stability and solubility of said crystalline form are also superior over the several existing crystalline forms.
    Type: Application
    Filed: March 9, 2010
    Publication date: January 5, 2012
    Inventors: Hanbin Shan, Peng Zhang, Zhedong Yuan, Xudong Jiang, Yu Huang, Hubo Wang, Xufeng Cao, Xingdong Cheng, Xiong Yu
  • Publication number: 20120003330
    Abstract: The present invention relates to new benzoquinolone inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: May 31, 2011
    Publication date: January 5, 2012
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Chengzhi Zhang, Manoucherhr Shahbaz
  • Publication number: 20110313198
    Abstract: The present invention relates to a complex of agomelatine and to preparation thereof. The hydrogen halide complex of agomelatine obtained through the present method is more soluble, more stable, and of higher purity than agomelatine itself, making it more suitable to be used in pharmaceutical preparation. Using this method, product of high purity can be obtained through a simple process, without having to incur further complicated steps.
    Type: Application
    Filed: February 26, 2010
    Publication date: December 22, 2011
    Inventors: Peng Zhang, Hanbin Shan, Zhedong Yuan, Xudong Jiang, Yu Huang, Hubo Wang, Xufeng Cao, Xingdong Cheng, Hongjuan Pan, Xiong Yu
  • Publication number: 20110305618
    Abstract: The invention pertains to a method for eluting a radionuclide-label or a radionuclide-labeled compound using a solid phase extraction resin, to a device for performing such a method, and to a computer program for controlling such a device.
    Type: Application
    Filed: December 12, 2009
    Publication date: December 15, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Axel Rother, Dominic Franck
  • Patent number: 8067639
    Abstract: Crystalline form VI of the compound of formula (I): characterised by its X-ray powder diffraction diagram. Medicinal products containing the same which are useful in treating melatoninergic disorders.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: November 29, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Gerard Coquerel, Julie Linol, Lionel Le Pape, Jean-Pierre Lecouve
  • Patent number: 8039669
    Abstract: The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demonstrated for substrates bearing a variety of N-alkyl and N-aryl substituents.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: October 18, 2011
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Christen Bell Smith, Denis A. Kissounko, Samuel H. Gellman, Shannon S. Stahl
  • Publication number: 20110230465
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
  • Publication number: 20110213146
    Abstract: One aspect of the invention relates to a method of animation or amidation, comprising the step of combining a substrate, comprising a reactive C—H bond, and an amine or amide, comprising a reactive N—H bond, in the presence of an oxidizing agent and a metal-containing catalyst, thereby forming a product with a covalent bond between the carbon of the reactive C—H bond and the nitrogen of the reactive N—H bond.
    Type: Application
    Filed: September 3, 2009
    Publication date: September 1, 2011
    Applicant: Georgetown University
    Inventor: Timothy H. Warren
  • Patent number: 7981923
    Abstract: Compounds of the formula I, II or III: or pharmaceutically acceptable salts thereof, wherein m, n, q, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formulas I-III.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: July 19, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Ralph New Harris, III, James M. Kress, David Bruce Repke, Russell Stephen Stabler
  • Publication number: 20110130571
    Abstract: A process for the manufacture of agomelatine and its intermediate N-[2-(7-methoxy-1-naphthyl)ethyl]phthalimide is provided and includes reacting 7-methoxy-1-naphthyl ethanol (III) with benzenesulfonyl chloride to obtain 7-methoxy-1-naphthylethyl benzene sulfonate (IV), which is reacted with potassium phthalimide to produce N-[2-(7-methoxy-1-naphthyl)ethyl]phthalimide (II); and subjecting N-[2-(7-methoxy-1-naphthyl)ethyl]phthalimide (II) to alkaline hydrolysis and acetylation, to obtain agomelatine.
    Type: Application
    Filed: July 23, 2009
    Publication date: June 2, 2011
    Inventors: Guisen Zhang, Daopeng Chen, Yanqin Ma, Xiangping Yang, Shixia Zhou, Liang Chen