The Spiro Includes The Five-membered Hetero Ring Patents (Class 548/408)
  • Patent number: 9000026
    Abstract: The invention relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumor disorders. The invention also relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selectively herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: April 7, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Ningshu Liu, Kai Thede, Ursula Mönning, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Reiner Fischer
  • Patent number: 8993782
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising, firstly, the cis-alkoxyspirocyclic biphenyl-substituted tetramic acid derivatives of the formula (I) and, secondly, at least one crop plant compatibility-improving compound. The invention relates furthermore to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.
    Type: Grant
    Filed: November 22, 2007
    Date of Patent: March 31, 2015
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Christian Arnold, Olga Malsam, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Martin Jeffrey Hills, Christopher Hugh Rosinger
  • Publication number: 20150051407
    Abstract: The present invention relates to a novel process for preparing cis-alkoxy-substituted spirocyclic phenylacetylamino acid esters and cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives, and also to novel intermediates and starting materials which are produced and/or used in the process according to the invention.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 19, 2015
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Taraneh Farida, Berndt Maiwald, Martin Littmann, Winfried Etzel
  • Patent number: 8946124
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selective herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth. The invention also relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Thomas Bretschneider, Reiner Fischer, Stefan Lehr, Elmar Gatzweiler, Ulrich Görgens, Isolde Häuser-Hahn, Ines Heinemann, Arnd Voerste
  • Patent number: 8927739
    Abstract: The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors.
    Type: Grant
    Filed: November 18, 2013
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Xiaowen Peng, In Jong Kim, Hui Cao, Datong Tang, Yat Sun Or, Guoqiang Wang, Guoyou Xu
  • Publication number: 20140371468
    Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Inventors: Reiner FISCHER, Thomas HIMMLER
  • Patent number: 8901038
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or fungicides. Moreover, the invention relates to selectively herbicidal compositions comprising, firstly, the biphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising in particular biphenyl-substituted cyclic ketoenols through the addition of ammonium or phosphium salts and optionally penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as insecticides and/or nematicides and/or acaricides and/or fungicides and/or for preventing unwanted plant growth.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: December 2, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Chieko Ueno, Arnd Voerste, Elmar Gatzweiler, Ines Heinemann, Ulrich Görgens
  • Patent number: 8859782
    Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: October 14, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Himmler
  • Patent number: 8859608
    Abstract: A spiro-amino compound of Formula (VI) wherein m is 1 or 2 or 3, n is 1 or 2, R is selected from a 5- or 6-membered aromatic ring and a 5- or 6-membered heteroaromatic ring comprising 1 to 3 heteroatoms selected from S, O and N, such ring being substituted with one or two substituents selected from the group consisting of (C1-C3)alkyl, halogen, (C3-C5)cycloalkyloxy, (C1-C3)alkylcarbonyl, phenyl optionally substituted with one or more halogen atoms, a 5- or 6-membered heterocycle comprising at least one nitrogen atom; P is a substituent Q or COQ, wherein Q is selected from the group consisting of phenyl, pyridyl, pyrimidyl, quinolyl, isoquinolyl, quinoxalyl, benzofuranyl, imidazotriazolyl, being such Q optionally substituted with one or more substituents selected from the group consisting of (C1-C3)alkyl, halogen, trifluoromethyl, carbammido, methylcarbammido, carboxy, methylcarboxy or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 15, 2010
    Date of Patent: October 14, 2014
    Assignee: Rottapharm Biotech S.R.L.
    Inventors: Luigi Piero Stasi, Lucio Rovati
  • Patent number: 8859466
    Abstract: The present invention relates to novel oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, B, D, Q1, Q2, and G have the meanings given above, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, oxaspirocyclic spirophenyl-substituted tetramic acid and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by addition of ammonium salts or phosphonium salts and, if appropriate, penetrants.
    Type: Grant
    Filed: July 22, 2008
    Date of Patent: October 14, 2014
    Assignee: Bayer CropScience AG
    Inventors: Thomas Bretschneider, Reiner Fischer, Gudrun Lange, Stefan Lehr, Christian Arnold, Dieter Feucht, Eva-Maria Franken, Martin Jeffrey Hills, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Jan Dittgen, Ulrich Görgens, Isolde Häuser-Hahn
  • Publication number: 20140275199
    Abstract: The invention relates to substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-ones, in particular for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of neoplastic disorders.
    Type: Application
    Filed: July 31, 2012
    Publication date: September 18, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Ursula Mönning, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Reiner Fischer
  • Publication number: 20140275005
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: May 5, 2014
    Publication date: September 18, 2014
    Applicant: Sanofi
    Inventor: Zhongli GAO
  • Patent number: 8816097
    Abstract: The new active compound combinations comprising compounds of the formula (I) and the active compounds (1) to (3) recited in the description possess very good insecticidal and/or acaricidal properties.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: August 26, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Wolfram Andersch, Thomas Bretschneider, Anton Kraus, Heike Hungenberg, Olga Malsam
  • Patent number: 8809384
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 19, 2012
    Date of Patent: August 19, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Werner Neidhart
  • Publication number: 20140187793
    Abstract: The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors.
    Type: Application
    Filed: November 18, 2013
    Publication date: July 3, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yao-Ling Qiu, Xiaowen Peng, In Jong Kim, Hui Cao, Datong Tang, Yat Sun Or, Guoqiang Wang, Guoyou Xu
  • Publication number: 20140179638
    Abstract: The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
    Type: Application
    Filed: July 26, 2012
    Publication date: June 26, 2014
    Applicant: KBP BIOSCIENCES CO., LTD.
    Inventors: Hui Zhang, Yanyan Dong
  • Patent number: 8735385
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Grant
    Filed: November 6, 2012
    Date of Patent: May 27, 2014
    Assignee: Sanofi
    Inventor: Zhongli Gao
  • Patent number: 8722721
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: May 13, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Werner Neidhart
  • Patent number: 8703807
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: April 22, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Werner Neidhart
  • Patent number: 8697739
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: April 15, 2014
    Assignee: Novartis AG
    Inventors: David Weninger Barnes, Gregory Raymond Bebernitz, Kevin Clairmont, Scott Louis Cohen, Robert Edson Damon, Robert Francis Day, Stephanie Kay Dodd, Christoph Gaul, Hatice Belgin Gulgeze Efthymiou, Monish Jain, Rajeshri Ganesh Karki, Louise Clare Kirman, Kai Lin, Justin Yik Ching Mao, Tajesh Jayprakash Patel, Brian Kenneth Raymer, Liansheng Su
  • Publication number: 20140057790
    Abstract: The invention relates to novel 2-acyloxypyrrolin-4-ones of the formula (I) in which A, B, G, W, X, Y and Z have the meaning given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 2-acyloxypyrrolin-4-ones and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 2-acyloxypyrrolin-4-ones, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or nematicides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: February 27, 2012
    Publication date: February 27, 2014
    Inventors: Guido Bojack, Taraneh Farida, Reiner Fscher, Stefan Lehr, Albert Schnatterer, Thomas Auler, Ulrich Görgens, Heinz Kehne, Olga Maslam
  • Publication number: 20140045696
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selective herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, halogen-substituted spirocyclic ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as pesticides and/or fungicides and/or for preventing unwanted plant growth. The invention also relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.
    Type: Application
    Filed: February 14, 2012
    Publication date: February 13, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Thomas Bretschneider, Reiner Fischer, Stefan Lehr, Elmar Gatzweiler, Ulrich Gõrgens, Isolde Häuser-Hahn, Ines Heinemann, Arnd Voerste
  • Patent number: 8633190
    Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
    Type: Grant
    Filed: October 26, 2010
    Date of Patent: January 21, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
  • Publication number: 20140011853
    Abstract: The invention relates to substituted 3-(biphenyl-3-yl)-8,8-difluoro-4-hydroxy-1-azaspiro[4.5]dec-3-en-2-ones of the formula (Ia) for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders. The invention also relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B, D and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides and/or fungicides. The invention also relates to selectively herbicidal compositions comprising, firstly, the halogen-substituted spirocyclic ketoenols and, secondly, a crop plant compatibility-improving compound.
    Type: Application
    Filed: February 14, 2012
    Publication date: January 9, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Ursula Mönning, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Reiner Fischer
  • Patent number: 8518985
    Abstract: The invention relates to novel compounds of the formula (I), in which W, X, Y, Z and CKE are each as defined above, to several methods and intermediates for preparation thereof and to the use thereof as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions which comprise firstly haloalkylmethyleneoxyphenyl-substituted ketoenols and secondly a compound which improves crop plant compatibility. The present invention further relates to the enhancement of the action of crop protection compositions comprising especially haloalkylmethyleneoxyphenyl-substituted ketoenols, by the addition of ammonium or phosphonium salts and optionally penetration enhancers, to the corresponding compositions, to methods for production thereof and to the use thereof in crop protection as insecticides and/or acaricides and/or for preventing undesired plant growth.
    Type: Grant
    Filed: March 11, 2010
    Date of Patent: August 27, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Gorgens, Jan Dittgen, Dieter Feucht, Isolde Hauser-Hahn, Christopher Hugh Rosinger, Alfred Angermann
  • Patent number: 8507537
    Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: October 13, 2007
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
  • Publication number: 20130136719
    Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, and R3 are as defined herein, are useful for treating flaviviridae viral infections.
    Type: Application
    Filed: May 25, 2012
    Publication date: May 30, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Laval Chan Chun Kong, Sanjoy Kumar Das, Carl Poisson
  • Patent number: 8440710
    Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts thereof. The are useful as HSL inhibitors and may, for example, be used in treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, and obesity.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: May 14, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Stephan Brugger, Aurelia Conte, Daniel Hunziker, Werner Neidhart, Matthias Nettekoven, Tanja Schulz-Gasch, Stanley Wertheimer
  • Patent number: 8435549
    Abstract: The invention relates to novel haloalkoxyspirocyclic tetramic and tetronic acid derivatives of the formula (I) in which W, X, Y, Z, A, D, Q1, Q2, m and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. Moreover, the invention provides selective herbicidal compositions comprising, firstly, haloalkoxyspirocyclic tetramic and tetronic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: September 12, 2008
    Date of Patent: May 7, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Stefan Lehr, Christian Arnold, Jan Dittgen, Dieter Feucht, Heinz Kehne, Olga Malsam, Christopher Hugh Rosinger, Eva-Maria Franken, Ulrich Görgens
  • Patent number: 8404740
    Abstract: Spirocyclic cyclohexane compounds corresponding to formula I In which R1, R2, R3 and R5 through R10 and X have defined meanings, a process for their preparation, pharmaceutical compositions containing such compounds, and the use of such spirocyclic cyclohexane compounds in the treatment and/or inhibition of pain and other conditions mediated by the ORL-1 or the ?-opioid receptor.
    Type: Grant
    Filed: August 21, 2009
    Date of Patent: March 26, 2013
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Schunk, Saskia Zemolka, Derek Saunders, Michael Gruss, Heinz Graubaum
  • Publication number: 20130065877
    Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 14, 2013
    Applicant: SANOFI
    Inventor: SANOFI
  • Publication number: 20130065882
    Abstract: This invention relates to a VLA-4 inhibitory drug, having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally, wherein an active ingredient is represented by formula (I), or a salt thereof: Q represents an optionally-substituted monocyclic or bicyclic nitrogen-containing heterocyclic group having a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents an optionally-substituted bicyclic aromatic hydrocarbon ring group or an optionally-substituted bicyclic aromatic heterocyclic group; A1 represents a nitrogen atom or C—R3d wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; R1 represents H or a C1-8 alkyl group; R2 represents H, a halogen, a C1-8 alkoxy
    Type: Application
    Filed: October 3, 2012
    Publication date: March 14, 2013
    Inventors: Nobuo Machinaga, Shin Iimura, Yoshiyuki Yoneda, Jun Chiba, Fumihito Muro, Hideko Hoh, Atsushi Nakayama
  • Publication number: 20130059874
    Abstract: The present disclosure relates to a series of substituted N-phenyl spirolactam bipyrrolidines of formula (I). wherein R1, R2, R3, R4, m, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-phenyl spirolactam bipyrrolidines of formula (I) and intermediates therefor.
    Type: Application
    Filed: November 6, 2012
    Publication date: March 7, 2013
    Applicant: SANOFI
    Inventor: Sanofi
  • Patent number: 8389443
    Abstract: The invention relates to novel compounds of the formula (I): in which W, X, Y, Z, A, B and G have the meanings given herein, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides; relates to selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound; and relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: March 5, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
  • Patent number: 8378119
    Abstract: The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent.
    Type: Grant
    Filed: February 28, 2012
    Date of Patent: February 19, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Yuichiro Tani, Yutaka Kitagawa, Makoto Muto, Toshiaki Jyono
  • Publication number: 20130040935
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of tumour disorders.
    Type: Application
    Filed: February 8, 2011
    Publication date: February 14, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Ningshu Liu, Kai Thede, Philip Lienau, Arne Scholz, Christoph-Stephan Hilger, Ulf Bömer, Maher Najjar, Knut Eis, Reiner Fischer, Wahed Ahmed Moradi
  • Patent number: 8334300
    Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.
    Type: Grant
    Filed: March 24, 2011
    Date of Patent: December 18, 2012
    Assignee: Bayer Aktiengesellshaft
    Inventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christophe Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
  • Patent number: 8329718
    Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: December 11, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
  • Patent number: 8314254
    Abstract: The present invention relates to novel intermediates used in the preparation of substituted spirocyclic ketoenols of the formula (I) in which W, X, Y, Z, A, B, D and G are as defined in the disclosure.
    Type: Grant
    Filed: May 25, 2010
    Date of Patent: November 20, 2012
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Thomas Bretschneider, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Jorg Konze, Peter Losel, Mark Wilhelm Drewes, Dieter Feucht, Karl-Heinz Kuck, Ulrike Wachendorff-Neumann
  • Publication number: 20120245191
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: March 19, 2012
    Publication date: September 27, 2012
    Inventors: Daniel Hunziker, Werner Neidhart
  • Publication number: 20120238613
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2 and R3 are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 20, 2012
    Inventors: Daniel Hunziker, Werner Neidhart
  • Publication number: 20120238594
    Abstract: The invention provides novel compounds having the general formula (I) wherein R1 and R2 are as described herein, compositions including the compounds, their pharmaceutically acceptable salts and esters and methods of using the compounds.
    Type: Application
    Filed: March 8, 2012
    Publication date: September 20, 2012
    Inventors: Daniel Hunziker, Werner Neidhart
  • Publication number: 20120232288
    Abstract: An intermediate for production of a quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria.
    Type: Application
    Filed: April 25, 2012
    Publication date: September 13, 2012
    Applicant: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Hisashi TAKAHASHI, Hiroaki INAGAKI, Satoshi KOMORIYA, Makoto TAKEMURA, Rie MIYAUCHI
  • Publication number: 20120190865
    Abstract: The present invention relates to a novel process for the preparation of 1-H-pyrrolidine-2,4-dione derivatives and to novel intermediates and to a process for their preparation.
    Type: Application
    Filed: January 25, 2012
    Publication date: July 26, 2012
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Thomas HIMMLER
  • Publication number: 20120190854
    Abstract: A method includes reacting an amino group, a composition including rhodium and an organic ligand, and a substrate having structural formula (I) in a reaction mixture. R1 is an organic group including a sp3 carbon atom bonded to CA. R2 is selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CA. R3 and R4 independently are selected from the group consisting of hydrogen, methyl, and an organic group including a sp3 carbon atom bonded to CB. The method further includes forming a hydroaminated product in the reaction mixture.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Akihiro Takemiya, Zhijian Liu, John F. Hartwig
  • Publication number: 20120178927
    Abstract: The invention relates to novel cycloalkylphenyl-substituted cyclic ketoenols of the formula (I) in which J, X, Y, m and CKE are as defined above, to processes and intermediates for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the cycloalkylphenyl-substituted cyclic ketoenols and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to increasing the activity of crop protection compositions comprising compounds of the formula (I) by adding ammonium or phosphonium salts and, if appropriate, penetrants.
    Type: Application
    Filed: July 12, 2011
    Publication date: July 12, 2012
    Applicant: Bayer CropScience AG
    Inventors: Reiner FISCHER, Thomas BRETSCHNEIDER, Stefan LEHR, Dieter FEUCHT, Eva-Maria FRANKEN, Olga MALSAM, Alfred ANGERMANN, Guido BOJACK, Christian ARNOLD, Martin Jeffery HILLS, Heinz KEHNE, Christopher Hugh ROSINGER
  • Publication number: 20120178786
    Abstract: Compounds of the formula (I) in which A, B, G, W, X, Y and Z can have the meanings given in the description are highly suitable for controlling animal pests such as insects and/or spider mites and/or nematodes by treating the soil/growth substrate by drenching or drip application or dipping or soil injection.
    Type: Application
    Filed: September 23, 2008
    Publication date: July 12, 2012
    Inventors: Thomas E. Macom, Reiner Fischer, Gerhard Baron, Erich Sanwald, Reed Nathan Royalty, Xavier Alain Marie Van Waetermeulen, Udo Reckmann, Alexandra Gladbach, Stephen Krueger, Peter Marczok
  • Publication number: 20120172605
    Abstract: The invention provides an industrial method for producing a spiroaminopyrrolidone derivative, which is an intermediate for producing a quinolone antibacterial agent.
    Type: Application
    Filed: February 28, 2012
    Publication date: July 5, 2012
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Yuichiro Tani, Yutaka Kitagawa, Makoto Muto, Toshiaki Jyono
  • Patent number: 8211932
    Abstract: The present application describes organic compounds of the Formula I that are useful for the treatment, prevention and/or amelioration of human diseases.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: July 3, 2012
    Assignee: Novartis AG
    Inventors: Michael Patane, Prakash Raman, David Thomas Parker, Jiping Fu, Branko Radetich, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng, Trixi Brandl, Francois Lenoir, Pascal Rigollier, Oliver Simic
  • Publication number: 20120129833
    Abstract: The invention relates to 5?-biphenyl-substituted cyclic ketoenols for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of diabetes, obesity, hyperlipidaemia, fatty livers and of disorders of the cardiovascular system.
    Type: Application
    Filed: August 19, 2011
    Publication date: May 24, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ningshu LIU, Kai Thede, Philip Lienau, Arne Scholz, Maher Najjar, Ulf Bomer, Knut Eis, Reiner Fischer