The Nitrogen Is Attached Indirectly To A Benzene Ring By Acyclic Nonionic Bonding Patents (Class 558/422)
  • Patent number: 10253002
    Abstract: The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.
    Type: Grant
    Filed: May 1, 2014
    Date of Patent: April 9, 2019
    Assignee: NEOCULI PTY LTD
    Inventors: Stephen Page, Sanjay Garg, Martine Keenan, Adam McCluskey, Andrew Stevens
  • Publication number: 20150065725
    Abstract: In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.
    Type: Application
    Filed: October 9, 2014
    Publication date: March 5, 2015
    Inventors: Poopathy KATHIRGAMANATHAN, Yun Fu CHAN
  • Patent number: 8815870
    Abstract: The present teachings provide a compound of Formula (I-B): wherein R1-R10 are as described herein; a pharmaceutically acceptable salt of the compound, a geometric isomer of the compound, or a pharmaceutically acceptable salt of the geometric isomer. Also described are methods of preparing the same, as well as methods for preparing vilazodone using the same.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: August 26, 2014
    Inventors: Henning Böttcher, Timo Heinrich
  • Publication number: 20140209872
    Abstract: A compound having an electron injection capability and/or electron transport capability represented by Formula 1, an organic light emitting device including the compound; and a flat display device including the organic light emitting device. The descriptions of substituents are referred to in the detailed description.
    Type: Application
    Filed: July 26, 2013
    Publication date: July 31, 2014
    Inventors: Jun-Ha Park, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
  • Publication number: 20140200239
    Abstract: The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.
    Type: Application
    Filed: August 3, 2012
    Publication date: July 17, 2014
    Applicant: National Taiwan University
    Inventors: Chung-Wai Shiau, Kuen-Feng Chen
  • Publication number: 20140142304
    Abstract: There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50° C. to 150° C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol.
    Type: Application
    Filed: July 6, 2012
    Publication date: May 22, 2014
    Applicant: Agency for Science, Technology and Research
    Inventors: Yugen Zhang, Dingyi Yu, Zhewang Lin
  • Publication number: 20140005395
    Abstract: The present teachings provide a compound of Formula (I-B): wherein R1-R10 are as described herein; a pharmaceutically acceptable salt of the compound, a geometric isomer of the compound, or a pharmaceutically acceptable salt of the geometric isomer. Also described are methods of preparing the same, as well as methods for preparing vilazodone using the same.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 2, 2014
    Inventor: Matthew Ronsheim
  • Patent number: 8431514
    Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.
    Type: Grant
    Filed: April 14, 2010
    Date of Patent: April 30, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Maienfisch
  • Patent number: 8314137
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: November 20, 2012
    Assignee: Trustess of Dartmouth College
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20120289595
    Abstract: The present invention relates to a novel biarylamide derivative and a pharmaceutical composition or a cosmetic composition comprising the same as an active ingredient. More particularly, the present invention relates to a novel biarylamide derivative, a pharmaceutical composition or a cosmetic composition for preventing or treating a pigmentation disorder caused by an abnormal excess of melanin or a disease caused by melanocyte hyperplasia comprising the same as an active ingredient. The biarylamide derivative of the present invention inhibits melanin production and thus inhibits melanocyte hyperplasia. Therefore, a cosmetic composition comprising the biarylamide is excellent in a whitening effect, and a pharmaceutical composition comprising the biarylamide is effective in the prevention or treatment of pigmentation disorders of skin such as lentigo, melasma, freckle, etc. and malignant melanoma.
    Type: Application
    Filed: July 25, 2012
    Publication date: November 15, 2012
    Applicant: Catholic University Industry Academy Cooperation Foundation
    Inventor: Dong Heon Shin
  • Publication number: 20120282629
    Abstract: The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.
    Type: Application
    Filed: August 19, 2010
    Publication date: November 8, 2012
    Applicant: MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN
    Inventors: Erich Wanker, Thomas Wiglenda, Julius Tachu Babila, Annett Boddrich, Michael Schmidt, Sandra Neuendorf, Franziska Schiele
  • Publication number: 20120205638
    Abstract: In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 16, 2012
    Applicant: Merck Patent GmbH
    Inventors: Poopathy Kathirgamanathan, Yun Fu Chan
  • Publication number: 20120004262
    Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.
    Type: Application
    Filed: January 21, 2010
    Publication date: January 5, 2012
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
  • Patent number: 8067640
    Abstract: The present invention relates to a novel method for the preparation of diol intermediates having the formula (II) and/or the opposite enantiomer of an acylated diol having the formula (IV) useful for the preparation of escitalopram involving selective enzymatic acylation or deacylation.
    Type: Grant
    Filed: May 17, 2010
    Date of Patent: November 29, 2011
    Assignee: H. Lundbeck A/S
    Inventors: Naoki Taoka, Takahisa Kato, Shogo Yamamoto, Takashi Yoshida, Toshihiro Takeda, Yasuyoshi Ueda, Hans Petersen, Robert Dancer, Haleh Ahmadian, Lars O. Lyngso
  • Publication number: 20110269834
    Abstract: Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).
    Type: Application
    Filed: August 21, 2009
    Publication date: November 3, 2011
    Applicants: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, PURDUE RESEARCH FOUNDATION
    Inventors: Arun K. Ghosh, Jun Takayama, Andrew David Mesecar, Michael E. Johnson, Kiira M. Ratia, Rima Chaudhuri, Debbie C. Mulhearn
  • Publication number: 20110230465
    Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.
    Type: Application
    Filed: September 16, 2010
    Publication date: September 22, 2011
    Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBH
    Inventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
  • Patent number: 8022232
    Abstract: This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallizing 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)-(S,S)- or (?)-(R,R)-enantiomer of O,O?-di-p-toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: September 20, 2011
    Assignee: H. Lundbeck A/S
    Inventors: Carla De Faveri, Florian Anton Martin Huber, Robert Dancer
  • Publication number: 20110196007
    Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.
    Type: Application
    Filed: July 22, 2009
    Publication date: August 11, 2011
    Inventors: Tadashi Honda, Emilie David, Dale Mierke
  • Publication number: 20110118325
    Abstract: This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described.
    Type: Application
    Filed: January 7, 2009
    Publication date: May 19, 2011
    Inventors: Youhai H. Chen, Ramachandran Murali, Jing Sun
  • Publication number: 20110092719
    Abstract: The present patent application relates to an improved process for the preparation of escitalopram, its salts and intermediates. It also relates to a novel crystalline form S of citalopram diol intermediate, process for preparation and its use in the preparation of citalopram, escitalopram and their salts.
    Type: Application
    Filed: May 28, 2009
    Publication date: April 21, 2011
    Applicant: SHODHANA LABORATORIES LIMITED
    Inventors: Thota Giridhar, Gudipati Srinivasulu, Kotaru Srinivasa Rao
  • Publication number: 20110009648
    Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.
    Type: Application
    Filed: January 22, 2007
    Publication date: January 13, 2011
    Applicant: Sandoz AG
    Inventors: Martin Albert, Hubert Sturm, Andreas Berger, Peter Kremminger
  • Publication number: 20100298330
    Abstract: The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
    Type: Application
    Filed: November 19, 2008
    Publication date: November 25, 2010
    Applicant: PHARMAXIS LTD.
    Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
  • Publication number: 20100179216
    Abstract: Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.
    Type: Application
    Filed: June 13, 2008
    Publication date: July 15, 2010
    Inventors: Masatoshi Kiuchi, Kaoru Tashiro, Maiko Hamada, Kunio Sugahara
  • Publication number: 20100174090
    Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.
    Type: Application
    Filed: March 28, 2008
    Publication date: July 8, 2010
    Inventors: Avinash N. Thadani, Bhartesh Dhudshia
  • Patent number: 7585982
    Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: September 8, 2009
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Kazuhiro Yoshizawa, Taiju Nakamura, Shigeto Negi
  • Patent number: 7582780
    Abstract: The invention relates to a method of separating and isolating an acylated derivative of 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile by reaction of a mixture of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile and an acylated derivative thereof with a compound which form a derivative of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile containing a carboxylic acid group. The acylated derivative containing a carboxylic acid group precipitates once it is formed and may easily be separated from the reaction mixture.
    Type: Grant
    Filed: February 2, 2005
    Date of Patent: September 1, 2009
    Assignee: H. Lundbeck A/S
    Inventor: Lars Ole Lyngso
  • Publication number: 20090137800
    Abstract: A compound represented by the following general formula (I), wherein ring A and ring B each independently represent a benzene, naphthalene, or heterocyclic ring which may be substituted; R1 and R2 each independently represent an alkyl group having 1 to 8 carbon atoms which may be substituted; R1 and R2 may be linked together to form a ring; a methylene group of the alkyl group having 1 to 8 carbon atoms may be replaced by —O— or —CH?CH—; Anq- represents a q-valent anion, where q is 1 or 2; p represents a coefficient to keep the charge neutral.
    Type: Application
    Filed: March 5, 2007
    Publication date: May 28, 2009
    Inventor: Satoshi Yanagisawa
  • Publication number: 20080214834
    Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).
    Type: Application
    Filed: July 27, 2005
    Publication date: September 4, 2008
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Kazuhiro Yoshizawa, Taiju Nakamura, Shigeto Negi
  • Patent number: 7256312
    Abstract: The invention relates to a process for preparing 4-[aminoalkoxy]benzylamines of the general formula (I) by catalytically hydrogenating 4-[aminoalkoxy]benzonitriles of the general formula (II) where, in the compounds of the general formulae I and II, R1 is C1-C8-alkylene, R2 and R3 are each independently C1-C8-alkyl or are joined to give a ring which may additionally contain a heteroatom, which comprises carrying out the hydrogenation at elevated pressure and elevated temperatures. The invention further relates to a process for preparing the intermediate (II).
    Type: Grant
    Filed: July 18, 2003
    Date of Patent: August 14, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Oliver Löber, Christoph Benisch, Klaus Ebel, Johann-Peter Melder
  • Patent number: 7241625
    Abstract: A carbonyl compound scavenger comprising a mineral acid salt of a benzylhydroxyamine-based compound of the formula (1) and at least one adsorbent selected from the group consisting of silica gel, alumina, cellulose and activated carbon: [wherein, R represents an alkyl group having 1 to 8 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, nitro group or cyano group, and R1 and R2 represent each independently a hydrogen atom or alkyl group having 1 to 8 carbon atoms, and a hydrogen atom on a benzene ring to which a cyano group and R are connected may be substituted with an alkyl group having 1 to 8 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, aryl group having 6 to 10 carbon atoms, nitro group or cyano group.].
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: July 10, 2007
    Assignee: Sumika Chemical Analysis Service, Limited
    Inventors: Kazuya Kitasaka, Hatsumi Shimajiri, Koichi Sugihara
  • Patent number: 7223794
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy.
    Type: Grant
    Filed: July 26, 2002
    Date of Patent: May 29, 2007
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, Antonio Mete
  • Patent number: 6953797
    Abstract: There is disclosed the use of a compound of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: October 11, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Ian Millichip
  • Patent number: 6914074
    Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 11, 2002
    Date of Patent: July 5, 2005
    Assignee: Wyeth
    Inventors: Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Eric S. Manas
  • Patent number: 6900243
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: May 31, 2005
    Assignee: AstraZeneca AB
    Inventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
  • Patent number: 6890955
    Abstract: The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive.
    Type: Grant
    Filed: January 3, 2003
    Date of Patent: May 10, 2005
    Assignee: Virbac SA
    Inventors: Ahmed El Hadri, Philippe Archimbault, Gérard Leclerc, Arthur Donny Strosberg, France Pietri-Rouxel
  • Patent number: 6861561
    Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Grant
    Filed: September 26, 2002
    Date of Patent: March 1, 2005
    Assignee: G. D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6743939
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.
    Type: Grant
    Filed: August 22, 2002
    Date of Patent: June 1, 2004
    Assignee: AstraZeneca AB
    Inventors: Tim Birkinshaw, David Cheshire, Antonio Mete
  • Patent number: 6710080
    Abstract: Substituted 2-dialkylaminoalkylbiphenyl derivatives, processes for their preparation, pharmaceutical compositions comprising these compounds and methods using these compounds for the preparation of medicaments and for the treatment of diseases.
    Type: Grant
    Filed: February 11, 2002
    Date of Patent: March 23, 2004
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Babette-Yvonne Koegel, Helmut Buschmann
  • Publication number: 20040039033
    Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1
    Type: Application
    Filed: December 10, 2002
    Publication date: February 26, 2004
    Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
  • Patent number: 6576596
    Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, cyano, alkyl, haloalkyl, —OR7, —SR7 or —NR7R10; R4 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or NR8; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is a cyclohexane-1,3-dione ring with or without substitution attached in position 2; and agriculturally useful salts thereo
    Type: Grant
    Filed: June 23, 1999
    Date of Patent: June 10, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Regina Luise Hill, Uwe Kardorff, Michael Rack, Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Guido Mayer, Martina Otten, Joachim Rheinheimer, Matthias Witschel, Ulf Misslitz, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 6541670
    Abstract: A compound of the general formula I wherein R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C8)monocyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10)alkylthio, (C1-C10)alkoxycarbonyl, and phenyl; R4 represents hydrogen, (C1-C6)alkyl, (C2-C6)olefinic
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: April 1, 2003
    Assignee: Leo Pharmaceutical Products Ltd. A/S
    Inventor: Erik Rytter Ottosen
  • Patent number: 6521667
    Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: February 18, 2003
    Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, PLC, SmithKline Beecham, Corp.
    Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
  • Patent number: 6479550
    Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 12, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: André Jeanguenat, Martin Zeller, Hugo Ziegler
  • Patent number: 6448293
    Abstract: A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(O
    Type: Grant
    Filed: March 16, 2001
    Date of Patent: September 10, 2002
    Assignee: Pfizer Inc.
    Inventors: Mark David Andrews, David Hepworth, Donald Stuart Middleton, Alan Stobie
  • Patent number: 6437153
    Abstract: The present invention relates to a novel process for preparing 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines which are known as intermediates for preparing compounds having fungicidal properties (WO 95-04728). Furthermore, the invention relates to novel 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines, to novel intermediates for their preparation and to a plurality of processes for preparing the novel intermediates.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: August 20, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Gallenkamp, Lothar Rohe, Herbert Gayer, Peter Gerdes
  • Patent number: 6417215
    Abstract: Novel calcilytic compounds are provided.
    Type: Grant
    Filed: July 26, 2001
    Date of Patent: July 9, 2002
    Assignee: SmithKline Beecham Corporation
    Inventor: Amparo Maria Lago
  • Patent number: 6392083
    Abstract: A process for producing a salt of a cyanobenzylamine comprising reacting a cyanobenzylamine with an acid. A salt of a cyanobenzylamine can industrially easily be produced and the resulting salt of a cyanobenzylamine has a high bulk density.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: May 21, 2002
    Assignee: Showa Denko K.K.
    Inventors: Isao Yamagami, Hiroshi Yasuda, Masatoshi Murakami, Toru Yoshida
  • Publication number: 20020040003
    Abstract: Disclosed are compounds of the Formula I 1
    Type: Application
    Filed: July 5, 2001
    Publication date: April 4, 2002
    Inventors: Laurence E. Burgess, John J. Gaudino, Robert D. Groneberg, Mark H. Norman, Martha E. Rodriguez, Xicheng Sun, Eli M. Wallace
  • Publication number: 20020038045
    Abstract: Novel hydroxamic acid compounds, e.g.
    Type: Application
    Filed: October 9, 2001
    Publication date: March 28, 2002
    Inventors: Georg Kottirsch, Ulf Neumann
  • Publication number: 20020019374
    Abstract: Salicylohydrazide derivatives of the formula I 1
    Type: Application
    Filed: June 14, 2001
    Publication date: February 14, 2002
    Inventors: Andreas Gypser, Thomas Grote, Joachim Rheinheimer, Ingo Rose, Peter Schafer, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl