Nitrogen Attached Directly Or Indirectly To The Hetero Ring By Acyclic Nonionic Bonding Patents (Class 549/467)
  • Benzofuran derivatives
    Publication number: 20040220415
    Abstract: The invention relates to novel benzofuran derivatives, to processes for preparing them and to their uses in medicaments.
    Type: Application
    Filed: April 12, 2004
    Publication date: November 4, 2004
    Inventors: Carsten Schmeck, Ulrich Muller, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Christiane Faeste, Helmut Haning, Markus Hauswald, Delf Schmidt, Martin Zoche, Heiner Apeler, Willi Jonghaus, Peter Reinemer
  • Process for the manufacture of citalopram hydrobromide from 5-bromophthalide
    Patent number: 6812355
    Abstract: A process for the preparation of 1-(4′-fluorophenyl)-1-(3-dimethylamino-propyl)-5-phthalanecarbonitrile of formula (I), or a pharmaceutically acceptable salt thereof, comprising performing two successive Grignard reactions on 5-bromophthalide, wherein the 5-bromophthalide is reacted with the first Grignard reagent in the presence of a Lewis acid, so reducing by-product formation and improving yields.
    Type: Grant
    Filed: October 22, 2002
    Date of Patent: November 2, 2004
    Assignee: Sekhsaria Chemicals Limited
    Inventors: Nandkumar Chodankar, Ajit Bhobhe, Ganesh Mukund Oak, Philip Eappen
  • Method for the preparation of citalopram
    Publication number: 20040215025
    Abstract: The present invention relates to a method for the preparation of citalopram by alkylation of a 1-(4-fluorophenyl)-1,3-dihydroisobenzofurane derivative.
    Type: Application
    Filed: May 21, 2004
    Publication date: October 28, 2004
    Applicant: H. Lundbeck A/S
    Inventor: Hans Petersen
  • Method for the preparation of citalopram
    Patent number: 6806376
    Abstract: The invention relates to a method for the preparation of citalopram comprising, in either order, subjecting a compound of formula wherein Y is a cyano group or a group which may be converted to a cyano group, R is hydrogen, —O—R1, NH2, NHCH3 or —N(CH3)2 wherein R1 is selected from hydrogen, alkyl, alkenyl, alkynyl and optionally alkyl substituted aryl or aralkyl; to i) reduction of the double bond in the side chain of formula —CH═CH—COR: ii) conversion of the group—COR or a reduced form thereof to a dimethylaminomethyl group; and iii) if Y is not cyano, conversion of the group Y to a cyano group; followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: October 19, 2004
    Assignee: H. Lundbeck A.S
    Inventor: Hans Petersen
  • Compounds that modulate the activity of PTP-1B and TC-PTP
    Patent number: 6784205
    Abstract: The present invention relates to a new and improved method for treating diabetes and or its associated complications by modulating the activity of protein tryosin phosphatase 1B (“PTP-1B”). The inventive compounds modulate the activity PTP-1B by binding to a novel binding site referred herein as the PTP-1B exosite that is distal to the active site of PTP-1B. The present invention also relates to a new and improved method of treating immune system disorders by modulating the activity of T-cell protein tyrosine phosphatase (“TC-PTP”). The inventive compound modulate the activity of TC-PTP by binding to a novel binding site referred herein as the TC-PTP exosite that is distal to the active site of PTP-1B.
    Type: Grant
    Filed: February 25, 2003
    Date of Patent: August 31, 2004
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Barr, Bruce Fahr, Stig Hansen, Christian Wiesmann
  • Crystalline base of citalopram
    Publication number: 20040167210
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug citalopram, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.
    Type: Application
    Filed: December 30, 2003
    Publication date: August 26, 2004
    Inventors: Hans Petersen, Klaus Peter Bogeso, Per Holm
  • Escitalopram hydrobromide and a method for the preparation thereof
    Publication number: 20040167209
    Abstract: Escitalopram (S-citalopram) in the form of its hydrobromide, methods for the preparation thereof and pharmaceutical compositions thereof.
    Type: Application
    Filed: December 23, 2003
    Publication date: August 26, 2004
    Applicant: H. Lundbeck A/S
    Inventors: Robert Dancer, Hans Petersen, Peter Ellegaard, Lawrence Martel
  • Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists
    Patent number: 6780859
    Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: August 24, 2004
    Assignee: Bayer Pharmaceuticals Corporation
    Inventors: Gaetan H. Ladouceur, William R. Schoen, Michael J. Burke
  • Preparation of pure citalopram
    Patent number: 6781003
    Abstract: The present invention relates to an industrially advantageous method for the purification of Citalopram (Formula I) wherein desmethyl citalopram (Formula II), present in crude Citalopram as an impurity, is methylated to produce pure Citalopram.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: August 24, 2004
    Assignee: Aurobindo Pharma Ltd.
    Inventors: Vipin Kumar Kaushik, Divvela Venkata Naga Srinivasa Rao, Vijay Kumar Handa, Meenakshisunderam Sivakumaran
  • Method for the preparation of citalopram
    Patent number: 6768011
    Abstract: The invention relates to a method for the preparation of citalopram comprising reaction of a compound of formula II with a compound having the formula wherein R is halogen or —O—SO2—X, wherein X is alkyl, alkenyl, alkynyl or optionally alkyl substituted aryl or aralkyl, and R1 is dimethylamino, halogen, —O—SO2—X wherein X is as defined above, provided that R is not halogen when R1 is dimethylamino; and if R1 is dimethylamino followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof, and if R1 is halogen or —O—SO2—X, wherein X is as defined above, followed by conversion of the resulting compound of formula wherein R2 is halogen or a group of formula —O—SO2—X wherein X is as defined above to citalopram, followed by isolation of citalopram base or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: August 29, 2002
    Date of Patent: July 27, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Michael Harold Rock, Haleh Ahmadian
  • Agents useful for reducing amyloid precursor protein and treating demantia and methods of use thereof
    Publication number: 20040138282
    Abstract: The present invention provides compounds and methods of administering compounds to a subject taht can reduce &bgr;APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce &bgr;APP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease &bgr;APP production.
    Type: Application
    Filed: February 6, 2004
    Publication date: July 15, 2004
    Inventors: Nigel H. Greig, Karen T. Y. Shaw, Qiang-Sheng Yu, Harold W. Holloway, Timothy T. Sencrant, Tada Utsuki, Donald K. Ingram, Arnold Brossi, Anthony Giordano, Gordon Powers, Diane Davidson, Michael Sturgess
  • Method for the preparation of citalopram
    Patent number: 6762308
    Abstract: The present invention relates to a method for the preparation of citalopram by alkylation of a 1-(4-fluorophenyl)-1,3-dihydroisobenzofurane derivative.
    Type: Grant
    Filed: September 5, 2002
    Date of Patent: July 13, 2004
    Assignee: H. Lundbeck A/S
    Inventor: Hans Petersen
  • Method for the preparation of citalopram
    Patent number: 6762307
    Abstract: The present invention relates to a method for the preparation of citalopram or any of its enantiomers and acid addition salts thereof comprising reaction of a compound of formula II with a diene having the formula wherein X is O, S, SO2, —N═N—, —CO—O—, —O—CO—, or or with a diene having the formula wherein R is alkyl or optionally substituted aryl or arylalkyl. The invention also relates to intermediates used in the new process for the preparation of citalopram, as well as citalopram prepared according to the new process.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: July 13, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Jakob Felding
  • Crystalline base of citalopram
    Publication number: 20040132808
    Abstract: The present invention relates to the crystalline base of the well known antidepressant drug citalopram, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of citalopram, such as the hydrobromide, using the base, the salts obtained by said process and formulations containing such salts.
    Type: Application
    Filed: December 19, 2003
    Publication date: July 8, 2004
    Inventors: Hans Petersen, Klaus Peter Bogeso, Per Holm
  • Process for the preparation of citalopram
    Publication number: 20040133017
    Abstract: This invention discloses an improved process for the preparation of citalopram of the formula III which comprises (i) preparing the compound of the formula VIII by reducing an unisolable magnesium salt of a benzophenone derivative of the formula V using sodium borohydride in the presence of a protic solvent, (ii) reacting the compound of the formula VIII obtained in step (i) with an acid catalyst in a non-polar solvent to obtain a compound of the formula I, (iii) reacting the compound of the formula I obtained in step (ii) with copper (I) cyanide in a polar solvent medium and isolating the resulting cyano compound, by recrystallization by using polar and/or alcoholic solvents to obtain the compound of the formula II and (III) reacting the resulting compound of the formula II by conventional methods to form citalopram of the formula III. Citalopram is widely used as an antidepressant.
    Type: Application
    Filed: March 3, 2004
    Publication date: July 8, 2004
    Inventors: Reddy Muddasani Pulla, Chowdary Venkaiah
  • Process for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile
    Patent number: 6753433
    Abstract: Method for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile (citalopram) comprising the reaction of a compound of formula wherein X is a halogen, with organometallic dimethylaminopropyl halide. Other aspects of the invention are new compounds of formula II and formula III and their preparation.
    Type: Grant
    Filed: February 24, 2003
    Date of Patent: June 22, 2004
    Assignee: Orion Corporation, FERMION
    Inventors: Leif Hilden, Tuomas Huuhtanen, Petteri Rummakko, Arne Grumann, Pekka Pietikaeinen
  • Method for the preparation of citalopram
    Patent number: 6750358
    Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is Cl or Br with a cyanide source in the presence of a nickel catalyst and isolation of the corresponding 5-cyano compound, i.e. citalopram.
    Type: Grant
    Filed: November 6, 2001
    Date of Patent: June 15, 2004
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
    Publication number: 20040106794
    Abstract: There are disclosed compounds of the formula 1
    Type: Application
    Filed: September 11, 2002
    Publication date: June 3, 2004
    Applicant: Schering Corporation
    Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, Laura L. Rokosz
  • 3,4-Di-substituted cyclobutene-1,2-diones as CXC-chemokine receptor ligands
    Publication number: 20040097547
    Abstract: There are disclosed compounds of the formula 1
    Type: Application
    Filed: July 30, 2002
    Publication date: May 20, 2004
    Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Kingsley H. Nelson, Laura L. Rokosz
  • Preparation of phthalanes
    Publication number: 20040092755
    Abstract: Citalopram and other phthalanes are made by reacting a salt of a compound of formula (II) where R1 is halogen and R2 is halogen, trifluoromethyl, cyano or R—CO— where R is a C1-4 alkyl group, with cuprous cyanide.
    Type: Application
    Filed: November 18, 2003
    Publication date: May 13, 2004
    Inventors: Yusuf Khwaja Hamied, Rajendra Narayaurao Kankan, Dhanmaraj Ramachandra Rao
  • Process for preparing 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines
    Patent number: 6730799
    Abstract: The present invention relates to a plurality of novel processes and novel intermediates for preparing 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines, which are known as intermediates for preparing compounds having fungicidal properties (WO 95-04728).
    Type: Grant
    Filed: June 5, 2002
    Date of Patent: May 4, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Bernd Gallenkamp, Peter Gerdes, Ulrich Heinemann, Bernd-Wieland Krüger, Reinhard Lantzsch, Thomas Seitz, Uwe Stelzer
  • Method for producing benzo annelated heterocycles
    Patent number: 6723848
    Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: in which X, R1, R2, R3, R4, R5 and n are as defined in claim 1, by reacting tetrahydrobenzo-fused heterocycles of formula II: in which X, R1, R2, R3, R4, R5, n and Ac are as defined in claim 1, with a catalytic amount of a noble metal catalyst in the presence of a hydrogen acceptor and then deacylating the acylated amino group by the addition of an amine.
    Type: Grant
    Filed: October 9, 2002
    Date of Patent: April 20, 2004
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
  • Foundation building system with antiseismic plates
    Publication number: 20040068125
    Abstract: The invention aims at isolating the foundations and the remaining part of the building from the earthquake. The antiseismic plates (2) are hermetic containers divided into two parts. Vacuum has been produced in part “B” so that most of the longitudinal or primary seismic waves propagating through the solids and fluids are cancelled. A pressurized liquid has been introduced into part “A” to cancel the transversal or secondary waves that propagate through the solids. “F1” is the lateral force of the surface seismic wave acting upon the plate and producing a pressure on the liquid pressing against the base (1) with nil results. “F4” is the decompensation of the faces pressing against the ground. The invention can be used in all types of foundations and large surfaces to preserve infrastructures, etc. It can alternatively be used for conical bases, buried walls, beam supports, etc.
    Type: Application
    Filed: November 12, 2003
    Publication date: April 8, 2004
    Inventor: Angel Castillo Senal
  • Method for the preparation of citalopram
    Patent number: 6717000
    Abstract: The present invention relates to a method for the preparation of citalopram comprising reduction of a compound of formula wherein X is a cyano group or a group which can be converted to a cyano group, and if X is not a cyano group followed by conversion of X to a cyano group.
    Type: Grant
    Filed: September 9, 2002
    Date of Patent: April 6, 2004
    Assignee: H. Lundbeck A/S
    Inventor: Hans Petersen
  • Derivatives of benzofuran or benzodioxazole compounds
    Patent number: 6716987
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)— C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: April 6, 2004
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
  • Methanesulphonamido-benzofuran, preparation method and use thereof as synthesis intermediate
    Publication number: 20040048921
    Abstract: The invention relates to 2-butyl-5-(methanesulfonamido)benzofuran, its preparation and its use.
    Type: Application
    Filed: June 10, 2003
    Publication date: March 11, 2004
    Inventors: Noel Fino, Corinne Leroy
  • Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6683210
    Abstract: Selected bis-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: March 15, 2002
    Date of Patent: January 27, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P Getman, Gary A DeCrescenzo, John N Freskos, Michael L Vazquez, James A Sikorski, Balekudru Devadas, Srinivasan Raj Nagarajan, David L Brown, Joseph J McDonald
  • Enantiomeric compounds for treatment of cardiac arrhythmias and methods of use
    Patent number: 6683195
    Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: January 27, 2004
    Assignee: ARYx Therapeutics
    Inventors: Pascal Druzgala, Peter G. Milner
  • Process for the preparation of citalopram
    Publication number: 20040014997
    Abstract: Preparation of citalopram comprises the steps of: (a) converting the compound of Formula (I) to a compound of Formula (II), wherein R in Formula (I) represents a C2 to C5 alkylene group which may be substituted or unsubstituted, and R1 in the compounds of Formula (II) represents a carboxylic acid group or a salt or an ester thereof; and (b) converting the compound of Formula (II) to form citalopram or a pharmaceutically acceptable salt thereof, or a direct conversion of the compound of Formula (I) to citalopram 1
    Type: Application
    Filed: December 16, 2002
    Publication date: January 22, 2004
    Inventors: Alan Kenneth Greenwood, Derek McHattie, Josef A. Rechka, Paul C.M. Hedger, Mark P. Gamble
  • 2-butyl-3-(4-[3(dibutylamino)propoxy]benzoyl)-5-nitro-benzofuran hydrochloride and preparation thereof
    Publication number: 20040010032
    Abstract: The invention relates to 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl-5-nitrobenzofuran hydrochloride, to its preparation and to its use as synthetic intermediate, in particular in preparing 2-butyl-3-(4-[3-(dibutylamino)propoxy]benzoyl)-5-nitrobenzofuran, itself an intermediate for dronedarone.
    Type: Application
    Filed: June 4, 2003
    Publication date: January 15, 2004
    Inventor: Michel Biard
  • N-(3-benzofuranyl)urea-derivatives
    Patent number: 6677372
    Abstract: N-(3-benzofuranyl)urea-derivatives are prepared by reacting of 3-amino-substituted benzofuranes with appropriate substituted isocyanates or isothiocyanates. The N(3-benzofuranyl)urea-derivatives can be used as active ingredients in medicaments particularly for the treatment of acute and chronic inflammatory processes.
    Type: Grant
    Filed: May 24, 2002
    Date of Patent: January 13, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gabriele Bräunlich, Rüdiger Fischer, Mazen Es-Sayed, Rolf Henning, Michael Sperzel, Karl-Heinz Schlemmer, Ulrich Nielsch, Stephen Tudhope, Graham Sturton, Trevor S. Abram, Mary F. Fitzgerald
  • Electrophilic ketones for the treatment of herpesvirus infections
    Patent number: 6673784
    Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.
    Type: Grant
    Filed: November 14, 2000
    Date of Patent: January 6, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
  • Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
    Patent number: 6667307
    Abstract: Selected sulfonylalkanoylamino hydroxyethylamine sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.
    Type: Grant
    Filed: February 26, 2002
    Date of Patent: December 23, 2003
    Assignee: G.D. Searle & Co.
    Inventors: Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Michael L. Vazquez, James A. Sikorski, Balekudru Devadas, Srinivasan Nagarajan, Joseph J. McDonald
  • Crystals of pharmaceutically acceptable salts of citalopram, methods of crystallization, and pharmaceutical compositions comprising them
    Publication number: 20030232881
    Abstract: The invention is directed to methods of crystallizing pharmaceutically acceptable salts of citalopram, the resulting crystals, and pharmaceutical compositions comprising the crystals.
    Type: Application
    Filed: December 5, 2002
    Publication date: December 18, 2003
    Applicant: H. LUNDBECK A/S
    Inventors: Ken Liljegren, Per Holm, Ole Nielsen, Sven Wagner
  • Compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them
    Publication number: 20030229083
    Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1
    Type: Application
    Filed: November 27, 2002
    Publication date: December 11, 2003
    Applicant: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Bhuniya Debnath, Saibal Kumar Das, Gurram Ranga Madhavan, Javed Iqbal, Ranjan Chakrabarti, Reeba Kannimel Vikramadithyan
  • Sulfonamide derivatives
    Publication number: 20030229102
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders 1
    Type: Application
    Filed: November 15, 2002
    Publication date: December 11, 2003
    Inventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Method for the preparation of citalopram
    Patent number: 6660873
    Abstract: A method for the preparation of citalopram comprising reaction of a compound of formula 5-aminomethyl-1-(3-dimethylamino-propyl)-1-(4-fluoro-phenyl)-1,3-dihydro-isobenzofuran with an oxidising agent to prepare citalopram.
    Type: Grant
    Filed: November 8, 2002
    Date of Patent: December 9, 2003
    Assignee: H. Lundbeck A/S
    Inventors: Hans Petersen, Robert Dancer
  • Method of producing methoxyimino acetic amide
    Patent number: 6660872
    Abstract: The present invention relates to novel processes for preparing methoxyimino-acetamides.
    Type: Grant
    Filed: November 21, 2001
    Date of Patent: December 9, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Bernd Gallenkamp, Peter Gerdes, Ulrich Heinemann, Walter Hübsch, Bernd-Wieland Krüger, Fritz Maurer, Holger Weintritt
  • N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
    Patent number: 6660756
    Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2 R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.
    Type: Grant
    Filed: March 12, 2002
    Date of Patent: December 9, 2003
    Assignee: Pfizer Inc.
    Inventors: Stephen Challenger, Andrew Simon Cook, Adam Thomas Gillmore, Donald Stuart Middleton, David Cameron Pryde, Alan Stobie
  • Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method of preparing same and compositions containing same
    Publication number: 20030225100
    Abstract: Benzothiophenes and related compounds of formula (1), wherein A, B, Z are independently —CH═, —CR4═ or ═N—; X is —S—, —O—, —NH—, —NR2, —CH2—CH2—, CH2—CH2—CH2—, —CH2—O—; —OCH2—, —CH2—S—, —CO—, —SCH2—.
    Type: Application
    Filed: February 20, 2003
    Publication date: December 4, 2003
    Inventors: Jean-Louis Assens, Claude Bernhart, Frederique Cabanel-Haudricourt, Patrick Gautier, Dino Nisato
  • Carboxylic acid derivatives as IP antagonists
    Publication number: 20030220367
    Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented.
    Type: Application
    Filed: May 9, 2003
    Publication date: November 27, 2003
    Inventors: Richard Leo Cournoyer, Paul Francis Keitz, Lee Edwin Lowrie, Alexander Victor Muehldorf, Counde O'Yang, Dennis Mitsugu Yasuda
  • Compounds useful in the complement, coagulat and kallikrein pathways and method for their preparation
    Patent number: 6653340
    Abstract: The present invention is concerned with new compounds, and particularly those having a fused bicyclic ring substituted with an amidine moiety. These compounds are each potent inhibitors of Factor D of the alternate pathway of complement, C1s of the classical pathway of complement, Factors Xa, XIIa, VIIa and thrombin of the coagulation pathway, plasmin in the fibrinolytic pathway, and kallikrein and high molecular weight kininogen in the inflammatory pathways. These proteases, which have serine in their active site, are called serine proteases and they are pivotal to most of the processes of inflammation and coagulation. In fact, these various systems are interactive with one another and it is difficult to activate one pathway without it influencing the others.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: November 25, 2003
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, J. Claude Bennett, Shri Niwas, R. Scott Rowland
  • Dihydrobenzofuran and dihydrobenzothiophene 2,4-pentadienoic acid derivatives having selective activity for retinoid X (RXR) receptors
    Publication number: 20030216570
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: April 30, 2002
    Publication date: November 20, 2003
    Inventors: Jayasree Vasudevan, Dehua Huang, Vidyasagar Vuligonda, Roshantha S. Chandraratna
  • Chroman and benzofuran derivatives as 5-hydroxytryptamine-6 ligands
    Patent number: 6638972
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: October 3, 2002
    Date of Patent: October 28, 2003
    Assignee: Wyeth
    Inventors: Michael Gerard Kelly, Lynne Padilla Greenblatt, Gan Zhang, Yvette L. Palmer, Steven Edward Lenicek
  • Process for preparing citalopram
    Patent number: 6635773
    Abstract: Process for preparing purified citalopram or one of its salts that comprises the purification of citalopram by selective extractions of citalopram or of its impurities with organic solvents and water under specific conditions of pH and temperature. The crude citalopram can be prepared by a process that comprises reacting 1-[3-(dimethylamine)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-bromoisobenzofuran with copper cyanide.
    Type: Grant
    Filed: January 24, 2003
    Date of Patent: October 21, 2003
    Assignee: Esteve Quimica, S.A.
    Inventors: Laura Coppi, Yolanda Gasanz Guillen, Julio Campon Pardo
  • (Oxime)carbamoyl fatty acid amide hydrolase inhibitors
    Publication number: 20030195226
    Abstract: The present invention relates to novel oxime carbamyl derivatives and pharmaceutical compositions comprising said derivatives which inhibit fatty acid amide hydrolase. These pharmaceutical compositions are useful for the treatment of conditions which can be effected by inhibiting fatty acid amide hydrolase including, but not limited to, neuropathic pain, emesis, anxiety, altering feeding behaviors, movement disorders, glaucoma, brain injury, and cardiovascular disease.
    Type: Application
    Filed: February 4, 2003
    Publication date: October 16, 2003
    Inventors: Sing-Yuen Sit, Kai Xie, Hongfeng Deng
  • Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists
    Publication number: 20030195352
    Abstract: This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.
    Type: Application
    Filed: September 10, 2002
    Publication date: October 16, 2003
    Inventors: Gaetan H. Ladouceur, William R. Schoen, Michael J. Burke
  • Novel bicyclic compounds
    Publication number: 20030191174
    Abstract: Compounds of the general formula (I): 1
    Type: Application
    Filed: October 28, 2002
    Publication date: October 9, 2003
    Inventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
  • Triamide-substituted heterobicyclic compounds
    Publication number: 20030187053
    Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1
    Type: Application
    Filed: June 20, 2002
    Publication date: October 2, 2003
    Applicant: Pfizer Inc.
    Inventors: Peter Bertinato, Alan E. Blize, Brian S. Bronk, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
  • Novel compounds and their use as glycine transport inhibitors
    Publication number: 20030181445
    Abstract: The invention provides novel compounds of the formula I below: 1
    Type: Application
    Filed: January 17, 2003
    Publication date: September 25, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Ejner Knud Moltzen, Garrick Paul Smith, Christian Krog-Jensen, Klaus Peter Bogeso