Patents by Inventor Christophe Pfleger

Christophe Pfleger has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo [1,2-B]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives
    Patent number: 11390632
    Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
    Type: Grant
    Filed: March 19, 2020
    Date of Patent: July 19, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Serena Maria Fantasia, Daniel Vincent Fishlock, Fabienne Hoffmann-Emery, Gerard Moine, Christophe Pfleger, Christian Moessner
  • SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF
    Publication number: 20210284648
    Abstract: The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Application
    Filed: June 3, 2021
    Publication date: September 16, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[e]azulene and crytalline forms thereof
    Patent number: 11040977
    Abstract: The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: June 22, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • PROCESS FOR THE PREPARATION OF 7-(4,7-DIAZASPIRO[2.5]OCTAN-7-YL)-2-(2,8-DIMETHYLIMIDAZO[1,2-B]PYRIDAZIN-6-YL)PYRIDO[1,2-A]PYRIMIDIN-4-ONE DERIVATIVES
    Publication number: 20200216472
    Abstract: The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
    Type: Application
    Filed: March 19, 2020
    Publication date: July 9, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Serena Maria Fantasia, Daniel Vincent Fishlock, Fabienne Hoffmann-Emery, Gerard Moine, Christophe Pfleger, Christian Moessner
  • PROCESS FOR THE PREPARATION OF CHIRAL PYROLLIDINE-2-YL- METHANOL DERIVATIVES
    Publication number: 20190375707
    Abstract: The invention relates to a novel process for the preparation of a chiral pyrollidine-2-yl-methanol derivative or a salt thereof of the formula I wherein R1 is aryl or heteroaryl and both aryl or heteroaryl are optionally substituted by C1-4-alkyl, halo-C1-4-alkyl, C1-4-alkoxy or halogen. The chiral pyrollidine-2-yl-methanol derivatives of the formula I are versatile building blocks in the synthesis of pharmacologically active compounds, such as for the stereospecific synthesis of oligonucleotides carrying chiral phosphonate moieties (see e.g. Int. PCT Publication WO 2010/064146).
    Type: Application
    Filed: August 21, 2019
    Publication date: December 12, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Raffael Josef Koller, Christophe Pfleger
  • SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF
    Publication number: 20190194210
    Abstract: The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Application
    Filed: March 4, 2019
    Publication date: June 27, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[E]azulene and crytalline forms thereof
    Patent number: 10246460
    Abstract: The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: April 2, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • (3,4-dichloro-phenyl)-((S)-3-propyl-pyrrolidin-3-yl)-methanone hydrochloride and manufacturing processes
    Patent number: 9527810
    Abstract: The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: December 27, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean-Michel Adam, Charles Alois Dvorak, Daniel Fishlock, Eric R. Humphreys, Hans Iding, Christophe Pfleger, Pankaj D. Rege, Xianqing Shi, Justin Vitale, Shaoning Wang, Marian Zajac
  • SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF
    Publication number: 20160280712
    Abstract: The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Application
    Filed: June 3, 2016
    Publication date: September 29, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Benno Rothenhaeusler, Rene Trussardi, Fabienne Hoffmann-Emery, Urs Schwitter, Jean-Michel Adam, Olaf Grassmann, Thomas Hartung, Frederic Ran, Ralph Diodone, Christophe Pfleger, Bjorn Bartels
  • (3,4-DICHLORO-PHENYL)-((S)-3-PROPYL-PYRROLIDIN-3-YL)-METHANONE HYDROCHLORIDE AND MANUFACTURING PROCESSES
    Publication number: 20150045408
    Abstract: The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Jean-Michel Adam, Charles Alois Dvorak, Daniel Fishlock, Eric R. Humphreys, Hans Iding, Christophe Pfleger, Pankaj D. Rege, Xianqing Shi, Justin Vitale, Shaoning Wang, Marian Zajac
  • Process for the preparation of proline derivatives
    Patent number: 8796471
    Abstract: The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.
    Type: Grant
    Filed: November 8, 2012
    Date of Patent: August 5, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Fritz Bliss, Philipp Cueni, Christophe Pfleger, Ulrich Zutter
  • Process for the preparation of halogenated benzoic acid derivatives
    Patent number: 8642802
    Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: February 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Stefan Hildbrand, James Jappy, Dinesh Maganbhai Patel, Christophe Pfleger, Robert John Ernest Tidswell, Rene Trussardi
  • PROCESS FOR THE PREPARATION OF HALOGENATED BENZOIC ACID DERIVATIVES
    Publication number: 20120330055
    Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
    Type: Application
    Filed: September 7, 2012
    Publication date: December 27, 2012
    Inventors: Stephan Bachmann, Stefan Hildbrand, James Jappy, Dinesh Maganbhai Patel, Christophe Pfleger, Robert John Ernest Tidswell, Rene Trussardi
  • Process for the preparation of halogenated benzoic acid derivatives
    Patent number: 8329939
    Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: December 11, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Stefan Hildbrand, James Jappy, Dinesh Maganbhai Patel, Christophe Pfleger, Robert John Ernest Tidswell, Rene Trussardi
  • PROCESS FOR THE PREPARATION OF HALOGENATED BENZOIC ACID DERIVATIVES
    Publication number: 20120130121
    Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
    Type: Application
    Filed: February 3, 2012
    Publication date: May 24, 2012
    Inventors: Stephan Bachmann, Stefan Hildbrand, James Jappy, Dinesh Maganbhai Patel, Christophe Pfleger, Robert John Ernest Tidswell, Rene Trussardi
  • PREPARATION OF DIHYDROPYRROL DERIVATIVES AS INTERMEDIATES
    Publication number: 20120041205
    Abstract: The invention is concerned with a new scalable process for the preparation of compounds of formula I comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula II or a salt thereof.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Inventors: Christophe Pfleger, Paul Spurr, Rene Trussardi, Pius Waldmeier, Shaoning Wang
  • NOVEL PROCESS
    Publication number: 20110313196
    Abstract: The present invention relates to a process for the preparation of benzamide derivatives which are useful as intermediates in the preparation of pharmaceutically active compounds.
    Type: Application
    Filed: June 6, 2011
    Publication date: December 22, 2011
    Inventors: Stephan Bachmann, Fritz Bliss, Ralph Diodone, Stefan Hildbrand, Michael Kammerer, Christophe Pfleger, Reinhard Reents, Michelangelo Scalone
  • Synthesis of GlyT-1 inhibitors
    Patent number: 7812161
    Abstract: The present invention relates to a process for preparation of a compound of formula I wherein Het, R1, R2, R3, and n are as defined herein and pharmaceutically acceptable acid addition salts thereof, which comprises reacting a compound of formula 21 with a compound of formula 8 to obtain a compound of formula 11 and coupling the compound of formula 11 in the presence of a coupling reagent or the corresponding acid halogenide with a compound of formula 15 to obtain a compound of formula I.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: October 12, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Christophe Pfleger, Pius Waldmeier, Shaoning Wang
  • PROCESS FOR THE PREPARATION OF HALOGENATED BENZOIC ACID DERIVATIVES
    Publication number: 20090306423
    Abstract: The present invention comprises a process for the preparation of 3-chloro-2-fluoro-5-trifluoromethyl benzoic acid of the formula or of a salt thereof. 3-Chloro-2-fluoro-5-trifluoromethyl benzoic acid or salts thereof are versatile intermediates for the preparation of active pharmaceutical or agrochemical agents.
    Type: Application
    Filed: May 29, 2009
    Publication date: December 10, 2009
    Inventors: Stephan Bachmann, Stefan Hildbrand, James Jappy, Dinesh Maganbhai Patel, Christophe Pfleger, Robert John Ernest Tidswell, Rene Trussardi
  • Preparation of dihydropyrrol derivatives as intermediates
    Publication number: 20090143589
    Abstract: The invention is concerned with a new scalable process for the preparation of compounds of formula I comprising a new process for the preparation of the key intermediate, a dihydropyrrole derivative formula II or a salt thereof.
    Type: Application
    Filed: November 26, 2008
    Publication date: June 4, 2009
    Inventors: Christophe Pfleger, Paul Spurr, Rene Trussardi, Pius Waldmeier, Shaoning Wang