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)
  • Publication number: 20110124859
    Abstract: The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R3 denotes hydrogen, C1-4-alkyl, OH, halogen, O—C1-4-alkyl, O—C1-4-alkylene-COOH, O—C1-4-alkylene-COO—C1-4-alkyl.
    Type: Application
    Filed: February 7, 2011
    Publication date: May 26, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thomas KRUEGER, Uwe RIES, Juergen SCHNAUBELT, Werner RALL, Zeno A. LEUTER, Adil DURAN, Rainer SOYKA
  • Patent number: 7947852
    Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, X represents a group N—OR2 wherein R2 represents a hydrogen atom or an alkyl group. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: May 24, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Said Yous, Mohamed Ettaoussi, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Patent number: 7939566
    Abstract: Crystalline form III of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: May 10, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Gerard Coquerel, Julie Linol, Jean-Claude Souvie
  • Publication number: 20110097269
    Abstract: The present invention relates to phenyloxyaniline derivatives, to methods of their production and to uses thereof.
    Type: Application
    Filed: November 12, 2010
    Publication date: April 28, 2011
    Inventors: Lutz LEHMANN, Axel Rother
  • Patent number: 7910625
    Abstract: Crystalline form IV of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: March 22, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Gerard Coquerel, Julie Linol, Jean-Claude Souvie
  • Publication number: 20110064662
    Abstract: Disclosed is a kit for use in the production of a molecular probe for PET drug screening for the purpose of producing a compound containing a short-lived radionuclide for PET applications. Specifically disclosed is a kit comprising a compound represented by the formula (I), (II) or (III) or a salt thereof. In the formulae, X1, X2, X3, X4, X5 and X6 are as defined in the description.
    Type: Application
    Filed: October 24, 2008
    Publication date: March 17, 2011
    Applicants: RIKEN, HAMAMATSU PHOTONICS K.K.
    Inventors: Hisashi Doi, Masaaki Suzuki, Hideo Tsukada
  • Publication number: 20100305352
    Abstract: A method for the production of optically active ?-alkylcarbonyl compounds with retention of the stereo information of the starting compound. The starting compound used here is a carbonyl compound which has, in the ?-position, a leaving group which is substituted by an alkyl group with inversion of the configuration. The substitution of the leaving group is effected with the use of an alkylmagnesium Grignard and a zinc (II) salt or a zinc organyl. The method permits the production of optically active ?-alkylcarbonyl compounds at very mild temperatures (for example 0° C.) with the use of starting compounds which are easy to prepare and economical and nontoxic catalysts, it also being possible to achieve a very high yield.
    Type: Application
    Filed: September 18, 2008
    Publication date: December 2, 2010
    Inventors: Bernhard Breit, Christopher Studte
  • Publication number: 20100256358
    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: Application
    Filed: May 22, 2008
    Publication date: October 7, 2010
    Applicants: TOPHARMAN SHANGHAI CO., LTD., WEIFANG TEHUA CHEMICAL CO., LTD.
    Inventors: Fuqiang Zhu, Haihong Li, Wenzhong Wang, Hui Zhang, Jingshan Shen
  • Patent number: 7754920
    Abstract: This invention relates to an improved method for crystallizing 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, the present invention provides an industrial process for crystallization of Compound A by evaporating methanol and water from the mother liquor after an initial crystallization of Compound A following the acetylation reaction. Specifically, the mother liquor is maintained at more than about 75% (v/v) of water and less than about 25% (v/v) of alcoholic solvent.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: July 13, 2010
    Assignee: GE HealthCare AS
    Inventors: Lars Terje Holmaas, Kristin Rypestol
  • Publication number: 20100137446
    Abstract: Compounds of formula (I): wherein: R1 represents alkyl, alkenyl, haloalkyl, polyhaloalkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, heteroaryl or heteroarylalkyl, R2 represents a fluorine atom or an alkyl group substituted by one or more fluorine atoms. Medicinal products containing the same which are useful in treating disorders of the melatoninergic system.
    Type: Application
    Filed: July 1, 2008
    Publication date: June 3, 2010
    Inventors: Said Yous, Mohamed Ettaoussi, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Publication number: 20100137628
    Abstract: Process for the industrial synthesis of the compound of formula (I) Application of such process in the synthesis of agomelatine.
    Type: Application
    Filed: August 1, 2008
    Publication date: June 3, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Thierry Dubuffet, Jean-Pierre Lecouve, Jean-Paul Hermet
  • Publication number: 20100036165
    Abstract: Process for obtaining the crystalline form V of the compound of formula (I):
    Type: Application
    Filed: August 4, 2009
    Publication date: February 11, 2010
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Damien Martins, Gérard Coquerel, Julie Linol, Pascal Langlois
  • Patent number: 7645905
    Abstract: Crystalline form IV of the compound of formula (I): characterised by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: January 12, 2010
    Assignee: Les Laboratoires Servier
    Inventors: Gerard Coquerel, Julie Linol, Jean-Claude Souvie
  • Publication number: 20100004340
    Abstract: This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist.
    Type: Application
    Filed: September 21, 2009
    Publication date: January 7, 2010
    Applicant: CONCERT PHARMACEUTICALS, INC.
    Inventors: Julie F. Liu, Roger Tung
  • Patent number: 7635721
    Abstract: Crystalline form III of the compound of formula (I): characterized by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful in the treatment of melatoninergic disorders.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: December 22, 2009
    Assignee: Les Laboratoires Servier
    Inventors: Gerard Coquerel, Julie Linol, Jean-Claude Souvie
  • Publication number: 20090299098
    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: Application
    Filed: December 1, 2008
    Publication date: December 3, 2009
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Christen Bell Smith, Denis A. Kissounko, Samuel H. Gellman, Shannon S. Stahl
  • Patent number: 7608737
    Abstract: This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: October 27, 2009
    Assignee: Concert Pharmaceuticasl Inc.
    Inventors: Julie F. Liu, Roger Tung
  • Patent number: 7601870
    Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: October 13, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornøe, Mario Rottländer, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
  • Patent number: 7589237
    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 15, 2008
    Date of Patent: September 15, 2009
    Assignee: Sepracor Inc.
    Inventors: Thomas Jerussi, Qun Kevin Fang, Mark G. Currie
  • Publication number: 20090069434
    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: Application
    Filed: November 6, 2008
    Publication date: March 12, 2009
    Applicant: LES LABORATOIRES SEVIER
    Inventors: Gerard Coquerel, Julie Linol, Lionel Le Pape, Jean-Pierre Lecouve
  • Patent number: 7470814
    Abstract: The present invention relates to a novel process for the industrial manufacture of substituted 7-allyl-6-hydroxy-indanes of formula (I) wherein R is a straight or branched (C1-C6)alkyl group and X is a halogen and enantiomers thereof.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: December 30, 2008
    Assignee: Ferrer Internacional, S.A.
    Inventors: Josep Lluis Falco, Albert Palomer, Antonio Guglietta
  • Patent number: 7462741
    Abstract: A compound selected from those of formula (I): Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.
    Type: Grant
    Filed: June 28, 2007
    Date of Patent: December 9, 2008
    Assignee: Les Laboratoires Servier
    Inventors: Said Yous, Basile Peres, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Publication number: 20080280908
    Abstract: This disclosure relates to novel melatonin analogues or naphthyl(ethyl)acetamides, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a dual melatoninergic agonist and serotoninergic antagonist.
    Type: Application
    Filed: April 30, 2008
    Publication date: November 13, 2008
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventors: Julie F. Liu, Roger Tung
  • Publication number: 20080280991
    Abstract: Disclosed herein are substituted naphthalene-based melatonin (MT) receptor modulators and/or 5-HT receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: May 7, 2008
    Publication date: November 13, 2008
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Sepehr Sarshar
  • Patent number: 7423179
    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: May 3, 2006
    Date of Patent: September 9, 2008
    Assignee: Sepracor Inc.
    Inventors: Thomas Jerussi, Qun Kevin Fang, Mark G. Currie
  • Publication number: 20080207950
    Abstract: Compounds of the formula (I) wherein R is phenyl, or phenyl substituted by Cl, Br, C1-C4alkyl or CF3; R1 is H or methyl or ethyl; R2 is H or methyl or acyl; R3 is H or methyl; R?4 is —CH3 or ?CH2; may be obtained in high enantiopurity by hydrogenation of a compound of the formula (II) wherein R and R3 are as in formula (I); A is acyl; and R4 is —CH3 or ?CH2; in the presence of a chiral Rhodium or Ruthenium catalyst. Residues R1 as methyl or ethyl and/or R2 as H or methyl may subsequently be introduced without racemization by deacylation and optional alkylation.
    Type: Application
    Filed: December 12, 2005
    Publication date: August 28, 2008
    Applicant: CIBA SPECIALTY CHEMICALS CORP.
    Inventors: Ulrich Berens, Christophe Malan, Hans Jurg Kirner
  • Publication number: 20080004350
    Abstract: A compound selected from those of formula (I): Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.
    Type: Application
    Filed: June 29, 2007
    Publication date: January 3, 2008
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Said Yous, Basile Peres, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Publication number: 20080004349
    Abstract: A compound selected from those of formula (I): Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.
    Type: Application
    Filed: June 28, 2007
    Publication date: January 3, 2008
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Said Yous, Basile Peres, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Mark Millan
  • Publication number: 20080004348
    Abstract: A compound selected from those of formula (I): wherein: R1 represents a group R4 or NHR4, wherein R4 is as defined in the description; R2 represents a substituted linear or branched (C1-C6)alkyl group; R3 represents a hydrogen or halogen atom or a linear or branched (C1-C6)alkyl or linear or branched (C2-C6)alkenyl group. Medicinal products containing the same which are useful in the treatment of disorders of the melatoninergic system.
    Type: Application
    Filed: June 27, 2007
    Publication date: January 3, 2008
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Said Yous, Basile Peres, Ahmed Sabaouni, Pascal Berthelot, Michael Spedding, Philippe Delagrange, Daniel-Henri Caignard, Matthieu Desroses, Jean-Albert Boutin, Valerie Audinot
  • Patent number: 7312345
    Abstract: The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: December 25, 2007
    Assignee: ISP Investments Inc.
    Inventors: Arie Gutman, Gennadi Nisnevich, Lev Yudovitch
  • Patent number: 7262326
    Abstract: A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: August 28, 2007
    Assignee: Teva Pharmaceuticals Industries Ltd.
    Inventors: Sylvie Blanchet, Bertrand Blandine, Alain Burgos, Yvon Derrien, Marie-Laure Moreau
  • Patent number: 7154004
    Abstract: Disclosed is a method of manipulating the carboxamide functionality in a catalytic manner. The method includes the steps of reacting amides with or without amines in the presence of various types of metal catalysts, at a temperature of about 250° C. or less.
    Type: Grant
    Filed: February 24, 2004
    Date of Patent: December 26, 2006
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Shannon S. Stahl, Samuel H. Gellman, Sarah E. Eldred
  • Patent number: 7141674
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: October 21, 2003
    Date of Patent: November 28, 2006
    Assignee: Johnson & Johnson Consumer Companies, Inc.
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 7138547
    Abstract: New spisulosine derivatives of use in treating tumors are of the formula (I) wherein: each X is the same or different, and represents H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, CN, halogen, C(?O)H, C(?O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaromatic, or two groups X may together form ?O; Y is NR1, OR1, PR1, SR1, or halogen, wherein the number of substituents R1 is selected to suit the valency and each R1 is independently selected of H, OH, C(?O)R?, P(?O)R?R?, substituted or unsubstituted C1–C18 alkyl, substituted or unsubstituted C2–C18 alkenyl, substituted or unsubstituted C2–C18 alkynyl, substituted or unsubstituted aryl, and wherein the dotted line indicates an optional double bond; each Z is the same different, and represents H, OH, OR?, SH, SR?, SOR?, SO2R?, NO2, NH2, NHR?, N(R?)2, NHC(O)R?, CN, halogen, C(?O
    Type: Grant
    Filed: June 6, 2001
    Date of Patent: November 21, 2006
    Assignee: Pharma Mar, S.A.
    Inventors: Jose Luis Aceña, Javier Adrio, Carmen Cuevas, Pilar Gallego, Ignacio Manzanares, Simon Munt, Ignacio Rodriguez
  • Patent number: 7105699
    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: September 7, 2005
    Date of Patent: September 12, 2006
    Assignee: Sepracor Inc.
    Inventors: Thomas P. Jerussi, Qun Kevin Fang, Mark G. Currie
  • Patent number: 7087785
    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: September 16, 2003
    Date of Patent: August 8, 2006
    Assignee: Sepracor Inc.
    Inventors: Thomas P. Jerussi, Qun Kevin Fang, Mark G. Currie
  • Patent number: 6888015
    Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16. (in the formula, X is an aliphatic alkyl group, desirably is an aliphatic alkyl group having 7 to 15 carbon atoms).
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: May 3, 2005
    Assignee: Japan Science and Technology Agency
    Inventors: Shu Kobayashi, Kentaro Hanada
  • Patent number: 6870069
    Abstract: A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: March 22, 2005
    Assignees: National Institute of Radiological Sciences, Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.
    Inventors: Kazutoshi Suzuki, Ming-Rong Zhang, Tetsuya Suhara, Atsuro Nakazato, Makoto Goto
  • Patent number: 6855847
    Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an ?,?-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an ?,?-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.
    Type: Grant
    Filed: July 22, 2002
    Date of Patent: February 15, 2005
    Assignee: Takasago International Corporation
    Inventors: Kazuhiko Matsumura, Takao Saito
  • Publication number: 20040248985
    Abstract: The invention provides a novel &bgr;2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel &bgr;2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
    Type: Application
    Filed: May 26, 2004
    Publication date: December 9, 2004
    Inventors: Ioanna Stergiades, Edward Yost, Cristin Hubbard, Weijiang Zhang
  • Publication number: 20040152703
    Abstract: The invention relates to bisaryl derivatives of the formula I, 1
    Type: Application
    Filed: July 21, 2003
    Publication date: August 5, 2004
    Inventors: Tao Guo, Koc-Kan Ho, Edward McDonald, Roland Ellwood Dolle, Kurt W. Saionz, Steven G. Kultgen, Ruiyan Liu, Guizhen Dong, Peng Geng, Anton Egbert Peter Adang, Nicole Corine Renee Van Straten
  • Publication number: 20040092600
    Abstract: A inhibitor of sphingolipids synthesis comprising a compound represented by general formula A. Desirably, a novel inhibitor of sphingolipids synthesis comprising (1R, 3R) N-(3-hydroxy-1-hydroxymethyl-3-phenylpropyl) alkaneamide, wherein carbon number of alkanoyl group is 8-16.
    Type: Application
    Filed: September 23, 2003
    Publication date: May 13, 2004
    Inventors: Shu Kobayashi, Kentaro Hanada
  • Patent number: 6720453
    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: September 10, 2002
    Date of Patent: April 13, 2004
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W Kessler
  • Patent number: 6635650
    Abstract: The invention relates to compounds of formula (I): A-G1-Cy-G2-Cy-G3-B  (I) wherein: A represents NR1C(Q)R2, C(Q)NR2R3 or NR1C(Q)NR2R3, B represents NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 or NR2R3, G1 and G3 represent an optionally substituted alkylene chain, Cy represents a ring structure G2 represents a chain and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: August 8, 2001
    Date of Patent: October 21, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Daniel Lesieur, Said Yous, Carole Descamps-Francois, François Lefoulon, Gérald Guillaumet, Marie-Claude Viaud, Caroline Bennejean, Philippe Delagrange, Pierre Renard
  • Patent number: 6617351
    Abstract: The present invention provides certain amide, carbamate and urea derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: September 9, 2003
    Assignee: Eli Lilly and Company
    Inventors: Macklin Brian Arnold, David Michael Bender, Thomas John Bleisch, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Patent number: 6602903
    Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: August 28, 2001
    Date of Patent: August 5, 2003
    Assignee: Les Laboratories Servier
    Inventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
  • Patent number: 6583319
    Abstract: The invention relates to compounds of for a (I): wherein: R represents ORa, SRa or Ra or a cyclic group A is a cyclic structure G1 and G2 represent an alkylene chain or a single bond B represents —NR1aC(Q)R2a, —NR1aC(Q)NR2aR3a or C(Q)NR1aR2a p and q are such that 1≦p+q≦4, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
    Type: Grant
    Filed: October 12, 1999
    Date of Patent: June 24, 2003
    Assignee: Les Laboratoires Servier
    Inventors: Michel Langlois, Monique Mathe-Allainmat, Marie Lefas-Le Gall, Caroline Bennejean, Pierre Renard, Philippe Delagrange
  • Patent number: 6509369
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: January 21, 2003
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
  • Patent number: 6498276
    Abstract: The present invention relates to a method for producing a compound of the formula [71] wherein R1 is an optionally substituted cycloalkyl group, an optionally substituted aryl group or an optionally substituted heterocyclic group, R2 is a lower alkyl or a halogenated lower alkyl and R3 is a halogen atom or a hydrogen atom. The method of the present invention includes reacting compound [1] with thionyl chloride to give compound [2] and obtaining the objective compound [7] at a high yield via intermediate [5], and is utilizable for industrial production.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: December 24, 2002
    Assignee: Japan Tobacco Inc.
    Inventors: Koji Matsuda, Katsuyoshi Hara, Minoru Akamatsu
  • Patent number: 6482985
    Abstract: Disclosed is a compound comprising a 2-benzyloxy-5-haloacylanilide having the structural formula I: wherein R is hydrogen or an alkyl group, RA is a substituent and n is 0-5; and X is a halogen. Also disclosed is a method for preparing a coupler using the compound. The compound and method simplify the preparation of photographic couplers.
    Type: Grant
    Filed: December 3, 2001
    Date of Patent: November 19, 2002
    Assignee: Eastman Kodak Company
    Inventor: Chang-Kyu Kim