Benzene Ring Bonded Directly To The Hetero Ring Patents (Class 540/611)
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Patent number: 8686134
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: April 1, 2014
    Assignee: Invista North America S.A R.L.
    Inventors: Stewart Forsyth, Kenneth Richard Seddon, Keith Whiston
  • Patent number: 8653304
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Publication number: 20120270847
    Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid pro-drug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    Type: Application
    Filed: July 16, 2010
    Publication date: October 25, 2012
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20120184735
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Application
    Filed: September 30, 2010
    Publication date: July 19, 2012
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20120165315
    Abstract: The present invention relates to salts of meptazinol carbamate prodrugs, and to their synthesis and use.
    Type: Application
    Filed: December 22, 2011
    Publication date: June 28, 2012
    Inventors: Paul McGee, R. Melling, Jean-Luc Coudret, A. Manage, Jean-Francois Camiaux, Colin Lindley
  • Publication number: 20120165520
    Abstract: The present invention provides a process for the synthesis of opioid prodrugs. In particular, the present invention provides a process for the synthesis of opioid prodrugs comprising: treating an opioid, in the form of a salt or a freebase, with a carbonyl synthon to form an activated intermediate and subsequently reacting the activated intermediate with an amine, in the form of a salt or a freebase.
    Type: Application
    Filed: December 22, 2011
    Publication date: June 28, 2012
    Inventors: Paul McGee, Ian Garnett, E. Juan, A. Manage, Jean-Francois Carniaux
  • Publication number: 20120149900
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: June 14, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Patent number: 8088917
    Abstract: The invention relates to an ionic liquid composition and a method for preparing the ionic liquid. The ionic liquid comprises a cation containing the Formula I, as herein disclosed, and wherein: n is 2, R1 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R2 may form a heterocyclic ring, and R2 is selected from the group consisting of: H, C1-C12 alkyl, aryl or together with R1 may form a heterocyclic ring, and R3 is selected from the group consisting of hydrogen and C1-C12 alkyl, and wherein R1 and R2 are not simultaneously selected from hydrogen.
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: January 3, 2012
    Assignee: Invista North America S.A R.L.
    Inventors: Stewart Forsyth, Kenneth R. Seddon, Keith Whiston, Sudhir Aki
  • Publication number: 20110190267
    Abstract: The present invention concerns prodrugs of opioid analgesics and pharmaceutical compositions containing such prodrugs. Methods for providing more consistent pain relief by increasing the bioavailability of the opioid analgesic with the aforementioned prodrugs are provided. The invention also provides for decreasing the adverse GI side effects of opioid analgesics.
    Type: Application
    Filed: December 23, 2010
    Publication date: August 4, 2011
    Applicant: Shire Pharmaceuticals, Inc.
    Inventors: Richard Franklin, Karl Swift, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20110136787
    Abstract: Compounds of the formula I: wherein m, n, X1, X2, Y1, Y2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 9, 2011
    Inventor: Ryan Craig Schoenfeld
  • Publication number: 20110065915
    Abstract: The present invention provides compositions comprising metal complexes, and related methods. In some embodiments, metal complexes of the invention may be useful as catalysts for chemical reactions, including metathesis reactions, wherein the catalysts exhibit enhanced activity and stereoselectivity. In some embodiments, the invention may advantageously provide metal complexes comprising a stereogenic metal atom. Such metal complexes may be useful in enantioselective catalysis.
    Type: Application
    Filed: January 23, 2009
    Publication date: March 17, 2011
    Applicant: TRUSTEES OF BOSTON COILEGE
    Inventors: Steven J. Malcolmson, Amir H. Hoveyda, Simon J. Meek, Richard R. Schrock
  • Publication number: 20110014186
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.
    Type: Application
    Filed: March 23, 2009
    Publication date: January 20, 2011
    Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
  • Publication number: 20110015182
    Abstract: Carbamate linked prodrugs of meptazinol and other opioid analgesics are provided. The prodrug moiety may comprise a single amino acid or short peptide. Additionally, the present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a prodrug moiety, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    Type: Application
    Filed: July 16, 2010
    Publication date: January 20, 2011
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Patent number: 7858613
    Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.
    Type: Grant
    Filed: May 17, 2006
    Date of Patent: December 28, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Claudia Hinze, Robert Frank, Ruth Jostock, Klaus Schiene, Michael Haurand, Hagen-Heinrich Hennies
  • Patent number: 7700585
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: April 20, 2010
    Assignee: sanofi-aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Publication number: 20090192095
    Abstract: The present invention relates to methods for reducing gastrointestinal side effects in a subject, the gastrointestinal side effects being associated with the administration of an opioid analgesic. The methods comprise orally administering an opioid prodrug or pharmaceutically acceptable salt thereof to a subject, wherein the opioid prodrug is comprised of an opioid analgesic covalently bonded through a carbamate linkage to a peptide of 1-5 amino acids in length, and wherein upon oral administration, the prodrug or pharmaceutically acceptable salt minimizes at least one gastrointestinal side effect associated with oral administration of the opioid analgesic alone. Compositions for use with the method are also provided.
    Type: Application
    Filed: January 19, 2009
    Publication date: July 30, 2009
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20090186832
    Abstract: Prodrugs of meptazinol and other phenolic analgesics exhibiting low oral bioavailability with amino acids or lower peptides, pharmaceutical compositions containing such prodrugs and a method for providing pain relief with such prodrugs are provided. In addition, the present invention relates to methods for increasing the oral bioavailability of a phenolic analgesic. The method comprises orally administering a phenolic analgesic prodrug, wherein the phenolic analgesic is bound to an amino acid or peptide via a carbamate linkage, to a subject in need thereof. Prodrugs having side chains of valine, leucine, isoleucine and glycine amino acids and mono-, di- and tripeptides thereof are preferred.
    Type: Application
    Filed: January 19, 2009
    Publication date: July 23, 2009
    Applicant: SHIRE LLC
    Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
  • Publication number: 20090054401
    Abstract: [Object] To provide a compound having prostaglandin production-suppressing action and leukotriene production-suppressing action. [Means for Solution] A compound represented by the formula (I): [In the formula, represents a single bond, or a double bond, Link represents a single bond, or a saturated or unsaturated straight hydrocarbon having 1 or 2 carbon atoms, W represents a single bond, oxygen atom, sulfur atom, N(Rw) etc., Rw represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms etc, Rs represents -D-Rx etc., D represents a single bond, oxygen atom, sulfur atom etc., Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms etc., one of V1 and V2 represents Zx, and the other represents AR, Zx represents hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms etc.
    Type: Application
    Filed: March 30, 2007
    Publication date: February 26, 2009
    Applicant: Asahi Kasei Pharma Corporation
    Inventors: Akiko Matsumoto, Motoshi Shoda, Hiroshi Kuriyama
  • Patent number: 7473779
    Abstract: Novel derivatives of amidines of formula wherein the substituents are defined as in the specification which are useful for inhibiting activity on NO-synthase enzymes producing nitrogen mono oxide and/or trapping the reactive oxygen species (ROS) making them useful for treating various diseases.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: January 6, 2009
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
  • Publication number: 20080261952
    Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2005
    Publication date: October 23, 2008
    Inventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Andrew Simon Swain, Phillppe Wong-Kai-In
  • Patent number: 7226917
    Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.
    Type: Grant
    Filed: April 17, 2006
    Date of Patent: June 5, 2007
    Assignee: Sanofi-Aventis
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
  • Patent number: 7153958
    Abstract: This invention comprises the novel compounds of formula (I) wherein r, s, t, X, Z, R1, R2, R3, R4, R5, R6 and R7 have defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: December 26, 2006
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Patrick René Angibaud, Marc Gaston Venet, Virginie Sophie Poncelet
  • Patent number: 7148238
    Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: December 12, 2006
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Benny Bang-Andersen, Ask Puschl
  • Patent number: 7138407
    Abstract: The invention provides compounds represented by the general formula I wherein the substituents are defined in the application. The compounds are useful in the treatment of an affective disorder, including depression, anxiety disorders including general anxiety disorder and panic disorder and obsessive compulsive disorder.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: November 21, 2006
    Assignee: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
  • Patent number: 6849203
    Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: February 1, 2005
    Assignee: Merck Patent Gesellschaft Mit Beschraenkter Haftung
    Inventors: Louise Diane Farrand, Christopher Worrall, Owain Llyr Parri
  • Publication number: 20040186287
    Abstract: The invention relates to novel cyclic imines of the formula (I) 1
    Type: Application
    Filed: January 30, 2004
    Publication date: September 23, 2004
    Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Potter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Publication number: 20040063933
    Abstract: This invention discloses a rubbery polymer which is comprised of repeat units that are derived from (1) at least one conjugated diolefin monomer, and (2) at least one functionalized monomer having of the structural formula: 1
    Type: Application
    Filed: June 30, 2003
    Publication date: April 1, 2004
    Inventors: Stephan Rodewald, Steven Kristofer Henning, Brian Earl Burkhart
  • Publication number: 20040024205
    Abstract: A process for the monomethylation of nitrogenous heterocycles having at least one nitrogen atom bonded to a hydrogen atom by reacting the nitrogenous heterocycle with dimethyl carbonate at a temperature of between 100° and 200° C. and a pressure of between 0.93×105 Pa and 1.07×105 Pa while methanol produced during the reaction is distilled off as it is formed.
    Type: Application
    Filed: July 31, 2003
    Publication date: February 5, 2004
    Inventors: Elisabeth Borredon, Berhard Chabaud, Antoine Gaset, Sophie Thiebaud-Roux, Samedy Ouk
  • Patent number: 6680314
    Abstract: Compounds of formula (1) or (2), enantiomers thereof, mixtures thereof, and pharmaceutically acceptable salts thereof: wherein: n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteroaryl group, or R is a monocyclic 5 to 6-membered heteroaryl group optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl, or a monocyclic 5 to 6-membered heteraryl group, or R is a bicyclic heteroaryl group composed of a monocyclic 5 to 6-membered heteroaryl group fused to a benzene ring, optionally substituted with alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cy
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: January 20, 2004
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
  • Publication number: 20030121110
    Abstract: 1,4-Diamino-2-alkenylbenzene derivatives of general formula (I) or physiologically tolerated water-soluble salts thereof 1
    Type: Application
    Filed: July 10, 2002
    Publication date: July 3, 2003
    Inventors: Laurent Chassot, Hans-Juergen Braun
  • Publication number: 20030109700
    Abstract: 1 Compounds of formula (1) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re, are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmac
    Type: Application
    Filed: July 11, 2002
    Publication date: June 12, 2003
    Inventor: Gary Michael Ksander
  • Publication number: 20030055260
    Abstract: This invention relates to the novel use of diphenyl sulfamido in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: August 30, 2002
    Publication date: March 20, 2003
    Inventors: Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
  • Publication number: 20020169156
    Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteraryl group, or a bicyclic heteroaryl group composed of a monocyclic
    Type: Application
    Filed: April 30, 2002
    Publication date: November 14, 2002
    Applicant: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
  • Patent number: 6451789
    Abstract: Compound of formula (I): wherein: n represents 0 or 1, R1 represents hydrogen, arylalkyl, alkyl, acyl, alkoxycarbonyl, arylalkoxycarbonyl or trifluoroacetyl, R2 represents alkyl, X represents oxygen, chlorine, OR3, SR4 or NOR5, R3 represents hydrogen , alkyl, acyl, alkoxycarbonyl or arylalkoxycarbonyl, R4 represents hydrogen, alkyl or aryl, R5 represents hydrogen or optionally substituted alkyl, represents a single or double bond, Ar represents aryl or heteroaryl, its isomers and addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful as facilitators of memory and cognition and antalgic agents.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: September 17, 2002
    Assignee: Les Labortoires Servier
    Inventors: Sylvain Rault, Olivier Renault, Jean Guillon, Patrick Dallemagne, Pierre Renard, Bruno Pfeiffer, Pierre Lestage, Marie-Cécile Lebrun
  • Patent number: 6436925
    Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be arom
    Type: Grant
    Filed: October 3, 2000
    Date of Patent: August 20, 2002
    Assignee: Abbott Laboratories
    Inventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
  • Patent number: 6420395
    Abstract: The present invention discloses compounds of formula (1) or (2), any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein n is 0, or 1; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalky-alkyl, aryl or aralkyl; and R1 is aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cyloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3.
    Type: Grant
    Filed: November 29, 1999
    Date of Patent: July 16, 2002
    Assignee: Neurosearch A/S
    Inventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
  • Patent number: 6399771
    Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, 2 and 3, to a plurality of processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: September 9, 2000
    Date of Patent: June 4, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
  • Patent number: 6352981
    Abstract: Aza- and diazacyclohexane and -cyclooctane compounds of the following formula: Ar1—A—B—Ar2  (I) where Ar1, A, B and Ar2 have the meanings stated in the description have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: March 5, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Jörg Treiber, Stefan Blank, Dorothea Starck, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke
  • Patent number: 6191182
    Abstract: A novel process for the preparation of compounds of formula I by aminolysis of a p-halophenyl alkyl ketone of formula II with a cyclic amine of formula III in water at a temperature of at least 130° C., in which formulae X is a halogen atom and R1, R2 and R3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.
    Type: Grant
    Filed: June 10, 1999
    Date of Patent: February 20, 2001
    Assignee: Ciba Specialty Chemcials Corporation
    Inventors: Rinaldo Hüsler, Rudolf Schwabe, Reto Luisoli
  • Patent number: 6165230
    Abstract: A 1,4-diazacycloheptane derivative and an oxidative hair colorant containing the derivative as a primary intermediate is presented. The 1,4-diazacycloheptane derivative is of the formula: ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently of one another represent hydrogen, a C.sub.1-4 alkyl or hydroxyalkyl group or a C.sub.2-4, dihydroxyalkyl group, X and Y independently of one another represent hydrogen, chlorine, fluorine, a C.sub.1-4 alkyl, hydroxyalkyl, aminoakyl or alkoxy group, a C.sub.2-4 dihydroxyalkyl group or an allyl group and R.sup.5 and R.sup.6 independently of one another represent hydrogen or a C.sub.1-4 alkyl group. Natural color tones can be obtained in keratin fibers with oxidative hair colorants containing the 1,4-diazacycloheptane derivative, without the use of additional primary intermediates.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: December 26, 2000
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: David Rose, Horst Hoeffkes, Bernd Meinigke
  • Patent number: 6140321
    Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.
    Type: Grant
    Filed: December 30, 1996
    Date of Patent: October 31, 2000
    Assignee: Eisai Co., Ltd.
    Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
  • Patent number: 5985864
    Abstract: Donepezil hydrochloride, 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, is provided here in the form of four polymorphs which are stable against heat and humidity in the pharmaceutical use. They can be industrially produced. They are specified by peaks in X-ray powder diffraction pattern and absorption peaks in infrared absorption spectra in potassium bromide.
    Type: Grant
    Filed: June 6, 1997
    Date of Patent: November 16, 1999
    Assignee: Eisai Co., Ltd.
    Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka, Yukio Narabu
  • Patent number: 5977357
    Abstract: A novel process for the preparation of compounds of formula I ##STR1## by aminolysis of a p-halophenyl alkyl ketone of formula II ##STR2## with a cyclic amine of formula III ##STR3## in water at a temperature of at least 130.degree. C., in which formulae X is a halogen atom and R.sub.1, R.sub.2 and R.sub.3 are as claimed in claim 1, as well as the novel compounds of formula I and their use for the preparation of photoinitiators for the photopolymerisation of ethylenically unsaturated compounds.
    Type: Grant
    Filed: June 1, 1998
    Date of Patent: November 2, 1999
    Assignee: Ciba Specialty Chemical Corporation
    Inventors: Rinaldo Husler, Rudolf Schwabe, Reto Luisoli
  • Patent number: 5912343
    Abstract: A compound comprising at least one cyclic amine, having an organolithium side-chain, defined according to formula (I) ##STR1## wherein Z is a lithium atom (Li); R.sub.1 is selected from the group consisting of organic groups containing from 1 to about 12 carbon atoms and a bridging bond; each R.sub.2 is independently selected from the group consisting of hydrogen, organic groups containing from 1 to about 12 carbon atoms, and a bridging bond; each R.sub.3 is independently selected from the group consisting of hydrogen and organic groups containing from 1 to about 12 carbon atoms; a is an integer from 4 to about 16; and b is an integer from 0 to about 12; and optionally including a bridge, formed by the selection of two of said bridging bonds, the bridge having 0 to about 6 carbon atoms between the bridging ring members.
    Type: Grant
    Filed: December 31, 1996
    Date of Patent: June 15, 1999
    Assignee: Bridgestone Corporation
    Inventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
  • Patent number: 5795890
    Abstract: A sulfonamide derivatives of formula (I) ##STR1## a non-toxic salts, an acid addition salts or a solvates thereof which has an inhibitory effect on elastase.
    Type: Grant
    Filed: September 24, 1996
    Date of Patent: August 18, 1998
    Assignee: ONO Pharmaceutical Co., Ltd.
    Inventors: Takahiko Nakae, Masashi Kato, Takehito Fujita, Kazuhito Kawabata, Hiroyuki Ohno
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5223498
    Abstract: Compounds of formula I ##STR1## and their salts in which n=0 or 1, R.sub.1 and R.sub.2 are each aliphatic or cycloalkyl or NR.sub.1 R.sub.2 is an optionally substituted heterocyclic ring, R.sub.3 is alkyl, cycloalkyl or optionally substituted amino, R.sub.5 is an aliphatic group, R.sub.6 is H, an optionally substituted aliphatic group or a cycloalkyl group, or R.sub.3 and R.sub.5 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R.sub.5 and R.sub.6 together with the nitrogen to which they are attached form a heterocyclic ring optionally substituted by alkyl and R.sub.7 is optionally substituted alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, trifluoromethyl or cyano have utility as hypoglycemic agents.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: June 29, 1993
    Assignee: The Boots Company plc
    Inventor: Balasubramanian Gopalan
  • Patent number: RE37035
    Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.
    Type: Grant
    Filed: October 7, 1997
    Date of Patent: January 30, 2001
    Assignee: Boehringer Ingelheim KG
    Inventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht