Halogen Attached Directly Or Indirectly To The Acyclic Carbon Or Chain By Acyclic Nonionic Bonding With No Amino Nitrogen Between The Halogen And The Aryl Ring Or Ring System Patents (Class 564/366)
  • Patent number: 8822727
    Abstract: The present invention provides processes and intermediates useful in the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, a serotonin (5-HT) receptor agonist that is useful in the treatment or prophylaxis of, for example, central nervous system disorders, such as obesity.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: September 2, 2014
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Marlon V. Carlos, Ryan O. Castro, Tawfik Gharbaoui, Xiao-Xiong Lu, You-An Ma, Nicholas D. San Martin
  • Patent number: 8637708
    Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula hydrochloride salt of formula (I) i.e. Cinacalcet.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: January 28, 2014
    Assignee: Zach System S.p.A.
    Inventors: Nicola Catozzi, Livius Cotarca, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
  • Publication number: 20130195883
    Abstract: The present invention relates to inhibitors of VAP-1 and their use as medicaments in treating fibrotic conditions. Furthermore, the present invention relates to a method of diagnosing a fibrotic condition on the basis of elevated level of soluble VAP-1 or SSAO activity in a bodily fluid, and to a kit for use in said diagnostic method.
    Type: Application
    Filed: September 7, 2010
    Publication date: August 1, 2013
    Applicants: THE UNIVERSITY OF BIRMINGHAM, BIOTIE THERAPIES CORP.
    Inventors: Christopher Weston, Lee Charles Claridge, David Adam, David Smith, Nina Westerlund, Marjo Pihlavisto, Thua Österman
  • Publication number: 20120238778
    Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula hydrochloride salt of formula (I) i.e. Cinacalcet.
    Type: Application
    Filed: September 8, 2010
    Publication date: September 20, 2012
    Applicant: ZACH SYSTEM S.P.A.
    Inventors: Nicola Catozzi, Livius Cotarca, Johnny Foletto, Massimiliano Forcato, Roberto Giovanetti, Giorgio Soriato, Massimo Verzini
  • Patent number: 8268894
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: September 18, 2012
    Assignees: The United States of America as Represented by the Secretary, Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva, Leo Einck, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III
  • Publication number: 20120172392
    Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.
    Type: Application
    Filed: March 7, 2012
    Publication date: July 5, 2012
    Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
  • Patent number: 8202910
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: June 19, 2012
    Assignee: Sequella, Inc.
    Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
  • Publication number: 20120101302
    Abstract: This invention relates to novel compounds suitable as precursors for the preparation of certain F-18 labeled positron emission tomography (PET) tracers. Furthermore, the invention relates to the preparation of such precursor molecules and to the preparation of PET tracers by F-18 labeling of such precursors.
    Type: Application
    Filed: April 10, 2010
    Publication date: April 26, 2012
    Applicant: Bayer Pharma Aktiengesellschaft
    Inventors: Georg Kettschau, Tobias Heinrich, Lutz Lehmann, Stephan Siegel, Sangram Nag
  • Patent number: 8163951
    Abstract: The present invention relates to a process for preparing quaternary ammonium compounds, which comprises reacting compounds comprising an sp3-hybridized nitrogen atom with a dialkyl sulfate or trialkyl phosphate and subjecting the resulting ammonium compound to an anion exchange.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: April 24, 2012
    Assignee: BASF Aktiengesellschaft
    Inventors: Laszlo Szarvas, Klemens Massonne, Matthias Maase, Alfred Oftring
  • Patent number: 8093429
    Abstract: Provided are a fluorous-tag-introduced fluoroamine of a general formula (I), its production method, a method of fluorination of a substrate having functional group containing oxygen with the fluoroamine serving as a fluorinating agent, and a method of recovering a fluorous-tag-introduced amide after the fluorination. The fluoroamine and its production method, as well as the fluorination method with the fluoroamine and the method of recovery of a fluorous-tag-introduced amide are ecological and advantageous in industrial use, as the load for separating and collecting the product after the fluorination with the fluoroamine serving as a fluorinating agent is small. (In the formula, R0 is an alkyl group or an aryl group having substituent(s) of Rf—(CH2)m—; Rf is a perfluoroalkyl group; m is from 0 to 2; R1 and R2 each are an alkyl group or an aryl group.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: January 10, 2012
    Assignees: National University Corporation Hokkaido University, Mitsubishi Gas Chemical Company, Inc.
    Inventors: Toshio Hidaka, Takafumi Yoshimura, Shoji Hara, Tsuyoshi Fukuhara
  • Publication number: 20110015438
    Abstract: The present invention provides processes and intermediates useful in the preparation of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, a serotonin (5-HT) receptor agonist that is useful in the treatment or prophylaxis of, for example, central nervous system disorders, such as obesity.
    Type: Application
    Filed: March 3, 2009
    Publication date: January 20, 2011
    Inventors: Marlon V. Carlos, Ryan O. Castro, Tawfik Gharbaoui, Xiao-Xiong Lu, You-An Ma, Nicholas D. San Martin
  • Patent number: 7842729
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: November 30, 2010
    Assignees: The United States of America as represented by the Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Patent number: 7834062
    Abstract: The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Conrad P. Dorn, Mary Ann Powles, Thomas F. Walsh, Matthew J. Wyvratt
  • Patent number: 7829741
    Abstract: A process for producing an ?,?-difluoroamine which comprises using hydrogen fluoride and a Lewis base in specific amounts in the halogen-fluorine exchange reaction using an ?,?-dihaloamine as the substrate. The process can be industrially applied, enables to obtain the object compound in a short time at a great yield and can be conducted easily with excellent productivity.
    Type: Grant
    Filed: October 20, 2005
    Date of Patent: November 9, 2010
    Assignees: National University Corporation, Mitsubishi Gas Chemical Company, Inc.
    Inventors: Tsuyoshi Fukuhara, Shoji Hara, Toshio Hidaka
  • Publication number: 20100280127
    Abstract: This document relates to compounds as well as methods and materials involved in modulating neurotransmitter reuptake. For example, compounds, methods for synthesizing compounds, and methods for inhibiting neurotransmitter reuptake are provided.
    Type: Application
    Filed: January 9, 2009
    Publication date: November 4, 2010
    Inventors: Elliott Richelson, Abdul H. Fauq
  • Publication number: 20100233086
    Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).
    Type: Application
    Filed: October 14, 2008
    Publication date: September 16, 2010
    Inventors: Lutz Lehmann, Andrea Thiele, Tobias Heinrich, Thomas Brumby, Christer Halldin, Balazs Gulyas, Sangram Nag
  • Patent number: 7763752
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects: .
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: July 27, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Publication number: 20100105942
    Abstract: The present invention relates to a process for the synthesis of aryloxypropylamine and heteroaryloxypropylamine of formula I: where: A is aryl or heteroaryl, where the aryl is preferably a phenyl, optionally substituted, selected from benzyl and tolyl and the heteroaryl is preferably thiophenyl; Y is an aryl, preferably phenyl, a substituted phenyl or a naphthyl, where the substituted phenyl is preferably selected from tolyl, trihalomethyltolyl and alkoxytolyl, starting from a suitable amino alcohol of formula II:
    Type: Application
    Filed: October 4, 2007
    Publication date: April 29, 2010
    Inventors: Giorgio Bertolini, Barbara Verzola, Domenico Vergani
  • Publication number: 20100016638
    Abstract: This invention relates to methods of making O-desmethylvenlafaxine from venlafaxine. In the methods venlafaxine is contacted with a polythiolate. The polythiolate may be prepared from the corresponding polythiol in the presence of base. The present methods provide the O-desmethylvenlafaxine in good yields and high purity and are suitable for use on an industrial scale.
    Type: Application
    Filed: July 21, 2009
    Publication date: January 21, 2010
    Inventors: Zdenko Hamersak, Amir Avdagic
  • Patent number: 7638652
    Abstract: Provided is a one-step efficient production method for an ?,?-difluoroamine of a general formula (1) below from an amide compound. The method is an economical method capable of producing the intended ?,?-difluoroamine at high yield by reacting a starting amide compound with carbonyl fluoride and/or oxalyl fluoride under a specific condition.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: December 29, 2009
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Takafumi Yoshimura, Toshio Hidaka, Norio Fushimi
  • Patent number: 7589127
    Abstract: The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.
    Type: Grant
    Filed: June 20, 2003
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Mary Ann Powles, Thomas F. Walsh, Matthew J. Wyvratt
  • Publication number: 20090163588
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: February 25, 2009
    Publication date: June 25, 2009
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
  • Publication number: 20090124833
    Abstract: The present invention relates to the economical and separation of benzphetamine hydrochloride and methamphetamine by liquid extraction. An extraction process employing a suitable organic solvent and water at a pH in the range of from about 6 to about 8 provides excellent removal of the methamphetamine by dissolution in the water phase while the benzphetamine dissolves in the organic phase. Simple separation of the two phases results in separation of the two amines.
    Type: Application
    Filed: November 2, 2005
    Publication date: May 14, 2009
    Applicant: MALLINCKRODT INC.
    Inventor: Keith G. Tomazi
  • Patent number: 7482491
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: January 27, 2009
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Publication number: 20080319228
    Abstract: A method of fluorination comprising reacting monosaccharides, oligosaccharides, polysaccharides, composite saccharides formed by bonding of these saccharides with proteins and lipids and saccharides having polyalcohols, aldehydes, ketones and acids of the polyalcohols, and derivatives and condensates of these compounds with a fluorinating agent represented by general formula (I) thermally or under irradiation with microwave or an electromagnetic wave having a wavelength around the microwave region. In accordance with the method, the fluorination at a selected position can be conducted safely at a temperature in the range of 150 to 200° C. where the reaction is difficult in accordance with conventional methods. The above method comprising the irradiation with microwave or an electromagnetic wave having a wavelength around the microwave region can be applied to substrates other than saccharides.
    Type: Application
    Filed: February 7, 2008
    Publication date: December 25, 2008
    Inventors: Shoji Hara, Tsuyoshi Fukuhara
  • Patent number: 7459586
    Abstract: The present invention relates to a method of producing an optically active 1-aryl-2-fluoro-substituted ethylamine compound of the formula [2] or a salt thereof by hydrogenolysis of an optically active secondary amine compound of the formula [1] or a salt thereof in the presence of a transition metal catalyst of Group VIII [Chem. 59] [where Ar represents an aryl group; n represents an integer of 1 or 2; and * represents an asymmetric carbon] [Chem. 60] [where Ar represents an aryl group; n represents an integer of 1 or 2; and * represents an asymmetric carbon].
    Type: Grant
    Filed: February 21, 2005
    Date of Patent: December 2, 2008
    Assignee: Central Glass Company Limited
    Inventors: Akihiro Ishii, Masatomi Kanai, Yokusu Kuriyama, Manabu Yasumoto, Kenjin Inomiya, Takashi Ootsuka, Katsuhide Suto, Koji Ueda
  • Patent number: 7456222
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: November 25, 2008
    Assignees: Sequella, Inc., The United States of America as represented by the Secretary, Department of Health and Human Services
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Patent number: 7351863
    Abstract: A method of fluorination comprising reacting monosaccharides, oligosaccharides, polysaccharides, composite saccharides formed by bonding of these saccharides with proteins and lipids and saccharides having polyalcohols, aldehydes, ketones and acids of the polyalcohols, and derivatives and condensates of these compounds with a fluorinating agent represented by general formula (I) thermally or under irradiation with microwave or an electromagnetic wave having a wavelength around the microwave region. In accordance with the method, the fluorination at a selected position can be conducted safely at a temperature in the range of 150 to 200° C. where the reaction is difficult in accordance with conventional methods.
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: April 1, 2008
    Assignee: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Shoji Hara, Tsuyoshi Fukuhara
  • Patent number: 7288678
    Abstract: A process for the preparation of terbinafine, comprising the reaction of a compound of formula (II), or a salt thereof, wherein X is a leaving group, with tert-butylacetylene, in the presence of a platinum catalyst
    Type: Grant
    Filed: November 21, 2003
    Date of Patent: October 30, 2007
    Assignee: Dipharma S.p.A.
    Inventors: Antonio Tarquini, Graziano Castaldi, Gianluca Galdi, Pietro Allegrini
  • Patent number: 7196226
    Abstract: The present invention relates to fluorination reagents comprising 1-fluoro-1-aminoolefins and also processes for preparing fluorination reagents comprising 1-fluoro-1-aminoolefins.
    Type: Grant
    Filed: December 16, 2004
    Date of Patent: March 27, 2007
    Assignee: Lanxess Deutschland GmbH
    Inventors: Wolfgang Ebenbeck, Albrecht Marhold
  • Patent number: 7186864
    Abstract: A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: May 28, 2003
    Date of Patent: March 6, 2007
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Thomas Martin Kirrane, Jr., Daniel Kuzmich, John Robert Proudfoot, David Thomson
  • Patent number: 7064236
    Abstract: The invention relates to substituted 1-aryl-but-3-enylamine and 1-aryl-but-2-enylamine compounds, to a method for the production thereof, to medicaments containing said compounds and to their use in the production of medicaments.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: June 20, 2006
    Assignee: Grunenthal GmbH
    Inventors: Bernd Sundermann, Corinna Sundermann, Helmut Buschmann, Babette-Yvonne Koegel
  • Patent number: 6784175
    Abstract: The use of at least one substituted 1-amino-5-phenylpentane-3-ol and/or 1-amino-6-phenylhexane-3-ol compound and/or one of the enantiomers thereof and/or one of the diastereomers thereof and/or one of the physiologically acceptable salts thereof for producing a medicament that has an N-methyl-D-aspartate-(NMDA)-antagonistic effect.
    Type: Grant
    Filed: November 18, 2002
    Date of Patent: August 31, 2004
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Werner Englberger, Boris Chizh
  • Patent number: 6765022
    Abstract: Described are cyclobexylamine derivatives of Formula I, Formula II, or Formula III and their pharmaceutically acceptable salts thereof: The compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are described in the specification.
    Type: Grant
    Filed: December 2, 2002
    Date of Patent: July 20, 2004
    Assignee: Warner-Lambert Company
    Inventors: Russell Joseph Deorazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer, Lawrence David Wise
  • Publication number: 20040015015
    Abstract: Disclosed herein are trifluoromethylepinephrine compounds having the following structural formula (I) 1
    Type: Application
    Filed: March 3, 2003
    Publication date: January 22, 2004
    Inventor: Jeffrey R. Ammann
  • Publication number: 20040010020
    Abstract: A compound of Formula (IA) or Formula (IB) 1
    Type: Application
    Filed: May 28, 2003
    Publication date: January 15, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Thomas Martin Kirrane, Daniel Kuzmich, John Robert Proudfoot, David Thomson
  • Publication number: 20040010148
    Abstract: A compound of Formula (IA) or Formula (IB) 1
    Type: Application
    Filed: May 28, 2003
    Publication date: January 15, 2004
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Thomas Martin Kirrane, Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, David Thomson
  • Patent number: 6596863
    Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: July 22, 2003
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Patent number: 6586633
    Abstract: The present invention relates to amine derivatives represented by formula (1) or salts thereof. R3 represents C1-C3 alkyl, hydroxylated C1-C5 alkyl, C1-C5 acyl; C2-C5 alkenyl, or a halogen atom; and k, l, and m are each an integer of 1 to 4.) Exhibiting excellent antifungal effect, these compounds are highly useful as antifungal agents, antifungal compositions, drugs, etc.
    Type: Grant
    Filed: April 5, 2001
    Date of Patent: July 1, 2003
    Assignee: Pola Chemical Industries, Inc.
    Inventors: Masayuki Yuasa, Yukio Kawazu, Toshimitsu Suzuki, Toshiro Majima, Takao Itoh, Takuji Nakashima, Akira Nozawa, Hiroyuki Takimoto, Kouji Yokoyama
  • Patent number: 6495685
    Abstract: A process for preparing a piperazine derivative represented by the formula (V): comprising reacting 1-methyl-3-phenylpiperazine with 2-chloro-3-cyanopyridine in an aprotic polar organic solvent in the presence of a base and an alkali metal halide. The piperazine derivative and its oxalate are compounds useful as preparation intermediates of mirtazapine.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: December 17, 2002
    Assignee: Sumika Fine Chemicals Co., Ltd.
    Inventors: Chiharu Maeda, Eiichi Iishi, Weiqi Wang, Yoshiyuki Imamiya
  • Patent number: 6485799
    Abstract: A aniline derivative represented by general formula (1) wherein R and R′ represent independently each other alkyl with 1 to 10 carbon, alkoxyalkyl with 1 to 10 carbon, or hydrogen; x represents cyano, halogen, haloalkyl, haloalkyloxy, or 2-cyanoethynyl; Y represents fluorine or hydrogen; na and nc represent independently each other 0 or 1; Za, Zb, and Zc represent independently each other a single bond, 1,2-ethylene, carbonyloxy, or oxymethylene; ring A1 represents 1,4-phenylene in which hydrogen may be substituted by fluorine; ring A2 and ring A3 represent independently each other 1,4-cyclohexylene, 1,4-phenylene in which hydrogen may be substituted by fluorine, or 1,3-pyrimidine-2,5-diyl.
    Type: Grant
    Filed: July 24, 2000
    Date of Patent: November 26, 2002
    Assignee: Chisso Corporation
    Inventors: Atsuko Fujita, Norio Tamura, Hiroyuki Tekeuchi, Fusayuki Takeshita, Nobumasa Nakamura, Etsuo Nakagawa
  • Patent number: 6451792
    Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: September 17, 2002
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Patent number: 6441237
    Abstract: The present patent application relates to new substituted 3-phenoxy- or 3-phenylalkyloxy-2-phenyl-propylamines of general formula 1, processes for preparing them and their use as pharmaceutical compositions.
    Type: Grant
    Filed: February 18, 2000
    Date of Patent: August 27, 2002
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Werner Stransky, Matthias Grauert, Adrian Carter, Thomas Weiser, Wolf-Dietrich Bechtel, Helmut Ensinger, Ralf Richard H. Lotz, Rainer Palluk, Uwe Pschorn
  • Patent number: 6057371
    Abstract: The invention relates to methods for the treatment of central nervous system disorders, gastrointestinal disorders, drug abuse, angina, migraine, hypertension and depression by administering a pharmaceutical composition comprising an effective amount of certain sigma receptor ligands to a patient in need of such treatment. The invention further relates to novel sigma receptor ligands having high binding to the sigma receptor and pharmaceutical compositions thereof. Unexpectedly, certain of the sigma receptor ligands of the present invention have selectivity for the sigma receptor over the DA, PCP and 5-HT.sub.1A receptors.
    Type: Grant
    Filed: June 10, 1992
    Date of Patent: May 2, 2000
    Assignee: Virginia Commonwealth University
    Inventor: Richard A. Glennon
  • Patent number: 6011068
    Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca.sup.2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.
    Type: Grant
    Filed: December 8, 1994
    Date of Patent: January 4, 2000
    Assignees: NPS Pharmaceuticals, Inc., The Brigham and Women's Hospital
    Inventors: Edward F. Nemeth, Bradford C. Van Wagenen, Manuel F. Balandrin, Eric G. DelMar, Scott T. Moe
  • Patent number: 5977413
    Abstract: Disclosed is a method for producing bis(3-amino-4-hydroxyphenyl) compounds, which comprises reducing bis(3-nitro-4-hydroxyphenyl) compounds with hydrazines in the presence of a catalyst. The method produces bis(3-amino-4-hydroxyphenyl) compounds of high quality under mild conditions at high yields. The products can be isolated and purified in a simple manner to have a higher purity. The method is suitable to industrial-scale production of the products.
    Type: Grant
    Filed: July 28, 1998
    Date of Patent: November 2, 1999
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Jun-ichiro Tomaru, Kenji Kunikata, Masaki Fujimoto
  • Patent number: 5939588
    Abstract: The present invention, which is aimed at providing a novel reaction for converting a fluorine-containing carbonyl compound to an asymmetric fluorine-containing primary amine, relates to a method in which a Schiff base obtained by the condensation of a fluorine-containing carbonyl compound and an asymmetric amine ((S)- or (R)-1-phenylethylamine) is treated in the presence of an appropriate organic base to hydrolyze a tautomeric imine obtained by asymmetrically performing an enzyme-like transamination reaction, yielding an asymmetric fluorine-containing amine.
    Type: Grant
    Filed: December 17, 1997
    Date of Patent: August 17, 1999
    Assignee: Agency of Industrial Science and Technology
    Inventors: Vadim A. Soloshonok, Taizo Ono, Takashi Abe
  • Patent number: 5679854
    Abstract: The present invention relates to a novel process for preparing (E)-1-amino-2-(fluoromethylene)-4-(p-fluorophenyl)butane, also known in the art as (E)-(p-fluorophenethyl)-3-fluoroallylamine, novel intermediates thereof, a novel process for the preparing (E)-2-(fluoromethylene)-4-(p-fluorophenyl)butan-1-ol, and a novel process for preparing alkali metal salts of diformylamide.
    Type: Grant
    Filed: August 25, 1995
    Date of Patent: October 21, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Jonathan C. Evans, Christian T. Goralski, Daniel R. Henton, Cynthia L. Rand, Paul C. Vosejpka
  • Patent number: 5639895
    Abstract: Disclosed is a process for producing .beta.-nitroenamine represented by the formula I: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and independently indicate a hydrogen atom or a C.sub.1 -C.sub.10 alkyl group which may be optionally substituted with at least one group selected from the group consisting of a halogen atom, a lower alkoxy group, an aryloxy group, a hydroxyl group or an aryl group, or an aryl group which may be optionally substituted with a halogen atom, a lower alkyl group, a lower alkoxy group, an aryl group, an aryloxy group, a nitro group, a cyano group, an acylamino group, a di-lower alkylamino group, an arylamino group, a hydroxyl group, an arylsulfonyl group, a mercapto group, a lower alkylthio group or an arylthio group, R.sub.1 and R.sub.2 may bond together to form a cycloalkyl or bicycloalkyl and R.sub.3 is a hydrogen atom, a lower alkyl group, a cycloalkyl group or an aralkyl group; and an intermediate for producing the .beta.-nitroenamine.
    Type: Grant
    Filed: September 13, 1996
    Date of Patent: June 17, 1997
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Shinzo Seko
  • Patent number: 5639906
    Abstract: This invention relates to compositions and methods useful for measuring pH generally, and intracellular pH specifically, and, more particularly, to a new class of fluorescent and fluorinated (NMR sensitive) aromatic compounds having excitation emission wavelengths in the ultraviolet or or visible portions of the electromagnetic spectrum, useful as pH indicators, as well as fluorine containing analogs useful in NMR spectroscopic determinations.
    Type: Grant
    Filed: October 11, 1994
    Date of Patent: June 17, 1997
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Robert E. London, Louis A. Levy, Chung K. Rhee