Benzene Ring Bonded Directly To The Hetero Ring Patents (Class 540/611)
-
Publication number: 20150051194Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.Type: ApplicationFiled: October 31, 2014Publication date: February 19, 2015Applicant: RENSSELAER POLYTECHNIC INSTITUTEInventor: Mark P. WENTLAND
-
Patent number: 8686134Abstract: 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: GrantFiled: July 20, 2011Date of Patent: April 1, 2014Assignee: Invista North America S.A R.L.Inventors: Stewart Forsyth, Kenneth Richard Seddon, Keith Whiston
-
Patent number: 8653304Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: GrantFiled: September 30, 2010Date of Patent: February 18, 2014Assignee: Toray Industries, Inc.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
-
Publication number: 20140039181Abstract: 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: ApplicationFiled: December 28, 2012Publication date: February 6, 2014Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of SciencesInventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
-
Publication number: 20120270847Abstract: 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: ApplicationFiled: July 16, 2010Publication date: October 25, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
-
Publication number: 20120184735Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:Type: ApplicationFiled: September 30, 2010Publication date: July 19, 2012Applicant: TORAY INDUSTRIES, INC.Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
-
Publication number: 20120165315Abstract: The present invention relates to salts of meptazinol carbamate prodrugs, and to their synthesis and use.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Inventors: Paul McGee, R. Melling, Jean-Luc Coudret, A. Manage, Jean-Francois Camiaux, Colin Lindley
-
Publication number: 20120165520Abstract: 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: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Inventors: Paul McGee, Ian Garnett, E. Juan, A. Manage, Jean-Francois Carniaux
-
Publication number: 20120149900Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.Type: ApplicationFiled: January 8, 2010Publication date: June 14, 2012Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
-
Patent number: 8088917Abstract: 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: GrantFiled: May 29, 2008Date of Patent: January 3, 2012Assignee: Invista North America S.A R.L.Inventors: Stewart Forsyth, Kenneth R. Seddon, Keith Whiston, Sudhir Aki
-
Publication number: 20110190267Abstract: 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: ApplicationFiled: December 23, 2010Publication date: August 4, 2011Applicant: Shire Pharmaceuticals, Inc.Inventors: Richard Franklin, Karl Swift, Bernard T. Golding, Robert G. Tyson
-
Publication number: 20110136787Abstract: 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: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Inventor: Ryan Craig Schoenfeld
-
CATALYSTS FOR METATHESIS REACTIONS INCLUDING ENANTIOSELECTIVE OLEFIN METATHESIS, AND RELATED METHODS
Publication number: 20110065915Abstract: 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: ApplicationFiled: January 23, 2009Publication date: March 17, 2011Applicant: TRUSTEES OF BOSTON COILEGEInventors: Steven J. Malcolmson, Amir H. Hoveyda, Simon J. Meek, Richard R. Schrock -
Publication number: 20110014186Abstract: 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: ApplicationFiled: March 23, 2009Publication date: January 20, 2011Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
-
Publication number: 20110015182Abstract: 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: ApplicationFiled: July 16, 2010Publication date: January 20, 2011Inventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
-
Patent number: 7858613Abstract: 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: GrantFiled: May 17, 2006Date of Patent: December 28, 2010Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Robert Frank, Ruth Jostock, Klaus Schiene, Michael Haurand, Hagen-Heinrich Hennies
-
Patent number: 7700585Abstract: 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: GrantFiled: April 30, 2007Date of Patent: April 20, 2010Assignee: sanofi-aventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
-
Publication number: 20090192095Abstract: 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: ApplicationFiled: January 19, 2009Publication date: July 30, 2009Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
-
Publication number: 20090186832Abstract: 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: ApplicationFiled: January 19, 2009Publication date: July 23, 2009Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
-
Publication number: 20090054401Abstract: [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: ApplicationFiled: March 30, 2007Publication date: February 26, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Akiko Matsumoto, Motoshi Shoda, Hiroshi Kuriyama
-
Patent number: 7473779Abstract: 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: GrantFiled: September 12, 2003Date of Patent: January 6, 2009Assignee: 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: 20080261952Abstract: 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: ApplicationFiled: August 16, 2005Publication date: October 23, 2008Inventors: 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: 7226917Abstract: 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: GrantFiled: April 17, 2006Date of Patent: June 5, 2007Assignee: Sanofi-AventisInventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Florence Medaisko, Nathalie Rakotoarisoa
-
Patent number: 7153958Abstract: 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: GrantFiled: November 15, 2001Date of Patent: December 26, 2006Assignee: Janssen Pharmaceutica N.V.Inventors: Patrick René Angibaud, Marc Gaston Venet, Virginie Sophie Poncelet
-
Patent number: 7148238Abstract: 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: GrantFiled: December 6, 2005Date of Patent: December 12, 2006Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Benny Bang-Andersen, Ask Puschl
-
Patent number: 7138407Abstract: 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: GrantFiled: December 6, 2005Date of Patent: November 21, 2006Assignee: H. Lundbeck A/SInventors: Thomas Ruhland, Garrick Paul Smith, Benny Bang-Andersen, Ask Puschl, Ejner Knud Moltzen, Kim Andersen
-
Patent number: 6849203Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.Type: GrantFiled: April 5, 2002Date of Patent: February 1, 2005Assignee: Merck Patent Gesellschaft Mit Beschraenkter HaftungInventors: Louise Diane Farrand, Christopher Worrall, Owain Llyr Parri
-
Publication number: 20040186287Abstract: The invention relates to novel cyclic imines of the formula (I) 1Type: ApplicationFiled: January 30, 2004Publication date: September 23, 2004Inventors: Andrew Plant, Gerd Kleefeld, Thorsten Potter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
-
Publication number: 20040063933Abstract: 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: 1Type: ApplicationFiled: June 30, 2003Publication date: April 1, 2004Inventors: Stephan Rodewald, Steven Kristofer Henning, Brian Earl Burkhart
-
Publication number: 20040024205Abstract: 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: ApplicationFiled: July 31, 2003Publication date: February 5, 2004Inventors: Elisabeth Borredon, Berhard Chabaud, Antoine Gaset, Sophie Thiebaud-Roux, Samedy Ouk
-
Patent number: 6680314Abstract: 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, cyType: GrantFiled: April 30, 2002Date of Patent: January 20, 2004Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
-
Publication number: 20030121110Abstract: 1,4-Diamino-2-alkenylbenzene derivatives of general formula (I) or physiologically tolerated water-soluble salts thereof 1Type: ApplicationFiled: July 10, 2002Publication date: July 3, 2003Inventors: Laurent Chassot, Hans-Juergen Braun
-
Publication number: 20030109700Abstract: 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 pharmacType: ApplicationFiled: July 11, 2002Publication date: June 12, 2003Inventor: Gary Michael Ksander
-
Publication number: 20030055260Abstract: 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: ApplicationFiled: August 30, 2002Publication date: March 20, 2003Inventors: Michael R. Palovich, Joseph Weinstock, Katherine L. Widdowson
-
Publication number: 20020169156Abstract: 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 monocyclicType: ApplicationFiled: April 30, 2002Publication date: November 14, 2002Applicant: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
-
Patent number: 6451789Abstract: 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: GrantFiled: September 26, 2001Date of Patent: September 17, 2002Assignee: Les Labortoires ServierInventors: Sylvain Rault, Olivier Renault, Jean Guillon, Patrick Dallemagne, Pierre Renard, Bruno Pfeiffer, Pierre Lestage, Marie-Cécile Lebrun
-
Patent number: 6436925Abstract: 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 aromType: GrantFiled: October 3, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
-
Patent number: 6420395Abstract: 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: GrantFiled: November 29, 1999Date of Patent: July 16, 2002Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon F. Nielsen, Elsebet O. Nielsen
-
Patent number: 6399771Abstract: 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: GrantFiled: September 9, 2000Date of Patent: June 4, 2002Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
-
Patent number: 6352981Abstract: 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: GrantFiled: October 27, 2000Date of Patent: March 5, 2002Assignee: BASF AktiengesellschaftInventors: Hans-Jörg Treiber, Stefan Blank, Dorothea Starck, Liliane Unger, Hans-Jürgen Teschendorf, Karsten Wicke
-
Patent number: 6191182Abstract: 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: GrantFiled: June 10, 1999Date of Patent: February 20, 2001Assignee: Ciba Specialty Chemcials CorporationInventors: Rinaldo Hüsler, Rudolf Schwabe, Reto Luisoli
-
Patent number: 6165230Abstract: 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: GrantFiled: August 25, 1999Date of Patent: December 26, 2000Assignee: Henkel Kommanditgesellschaft auf AktienInventors: David Rose, Horst Hoeffkes, Bernd Meinigke
-
Patent number: 6140321Abstract: 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: GrantFiled: December 30, 1996Date of Patent: October 31, 2000Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka
-
Patent number: 5985864Abstract: 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: GrantFiled: June 6, 1997Date of Patent: November 16, 1999Assignee: Eisai Co., Ltd.Inventors: Akio Imai, Hideaki Watanabe, Takashi Kajima, Yasushi Ishihama, Akiyo Ohtsuka, Tomohide Tanaka, Yukio Narabu
-
Patent number: 5977357Abstract: 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: GrantFiled: June 1, 1998Date of Patent: November 2, 1999Assignee: Ciba Specialty Chemical CorporationInventors: Rinaldo Husler, Rudolf Schwabe, Reto Luisoli
-
Patent number: 5912343Abstract: 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: GrantFiled: December 31, 1996Date of Patent: June 15, 1999Assignee: Bridgestone CorporationInventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
-
Patent number: 5795890Abstract: 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: GrantFiled: September 24, 1996Date of Patent: August 18, 1998Assignee: ONO Pharmaceutical Co., Ltd.Inventors: Takahiko Nakae, Masashi Kato, Takehito Fujita, Kazuhito Kawabata, Hiroyuki Ohno
-
Patent number: 5276053Abstract: 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: GrantFiled: October 6, 1992Date of Patent: January 4, 1994Assignee: Warner-Lambert CompanyInventor: Graham Johnson
-
Patent number: 5223498Abstract: 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: GrantFiled: December 28, 1989Date of Patent: June 29, 1993Assignee: The Boots Company plcInventor: Balasubramanian Gopalan
-
Patent number: RE37035Abstract: Phenylacetic acid benzylamides having the following general structure wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: October 7, 1997Date of Patent: January 30, 2001Assignee: Boehringer Ingelheim KGInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht