Patents by Inventor Stefan Hildbrand

Stefan Hildbrand 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 a Chiral Piperazine-2-carboxylic Acid
    Publication number: 20230175026
    Abstract: The invention relates to a novel process for the preparation of a chiral piperazine-2- carboxylic acid or of a salt thereof of the formula (I). The chiral piperazine-2-carboxylic acid derivatives of the formula (I) are key intermediates for the preparation of fused heteroaryl dihydro pyrimidines which are useful for the treatment and prophylaxis of hepatitis B virus infections.
    Type: Application
    Filed: April 26, 2021
    Publication date: June 8, 2023
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Joséphine Eliette Françoise CINQUALBRE, Stefan HILDBRAND, Paolo TOSATTI, Kurt PUENTENER, Dennis WETZL, Hans IDING, Patrick STOCKER, Nicolas Mickael FÉDOU, Paul SPURR
  • Process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one compounds
    Patent number: 10538536
    Abstract: The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
    Type: Grant
    Filed: October 26, 2018
    Date of Patent: January 21, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Pascal Dott, Fabian Feyen, Stefan Hildbrand, Ursula Hoffmann, Fabienne Hoffmann-Emery, Roland Meier, Gerard Moine, Pankaj Rege, Georg Wuitschik
  • PROCESS FOR THE MANUFACTURE OF DIAZEPINE DERIVATIVES
    Publication number: 20190284202
    Abstract: The invention relates to a process for the manufacture of diazepine derivatives as defined in the description and in the claims.
    Type: Application
    Filed: June 7, 2019
    Publication date: September 19, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Fritz Bliss, Xiaohua Du, Dawei He, Stefan Hildbrand, Paul Spurr, Wenfa Ye, Jianbing Zheng
  • NOVEL PROCESS
    Publication number: 20190144468
    Abstract: The present invention relates to a process for the preparation of 2-pyrazolo[1,5-a]pyrazin-2-ylpyrido[1,2-a]pyrimidin-4-one derivatives useful as pharmaceutically active compounds.
    Type: Application
    Filed: October 26, 2018
    Publication date: May 16, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Pascal DOTT, Fabian FEYEN, Stefan HILDBRAND, Ursula HOFFMANN, Fabienne HOFFMANN-EMERY, Roland MEIER, Gerard MOINE, Pankaj REGE, Georg WUITSCHIK
  • Process for the manufacture of 3-piperazin-1-yl-propylamine derivatives
    Publication number: 20190092739
    Abstract: The invention relates to the manufacture of a compound of formula (I) wherein R1 is defined as in the description and in the claims.
    Type: Application
    Filed: August 22, 2018
    Publication date: March 28, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Shaoning WANG, Stefan HILDBRAND
  • Process for the preparation of (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid
    Patent number: 9975856
    Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: May 22, 2018
    Assignee: Genentech, inc.
    Inventors: Stephan Bachmann, Serena Maria Fantasia, Francis Gosselin, Chong Han, Stefan Hildbrand, Theresa Humphries, Christian Jenny, Ngiap-Kie Lim, Andrew McClory, Christian Moessner, Pankaj Rege, Scott Savage, Haiming Zhang
  • PROCESS FOR THE PREPARATION OF (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID
    Publication number: 20170101380
    Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.
    Type: Application
    Filed: October 6, 2016
    Publication date: April 13, 2017
    Applicant: Genentech, Inc.
    Inventors: Stephan Bachmann, Serena Maria Fantasia, Francis Gosselin, Chong Han, Stefan Hildbrand, Theresa Humphries, Christian Jenny, Ngiap-Kie Lim, Andrew McClory, Christian Moessner, Pankaj Rege, Scott Savage, Haiming Zhang
  • Process to manufacture N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide
    Patent number: 9562009
    Abstract: The present invention provides processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: February 7, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Olaf Grassmann, Stefan Hildbrand, Roland Meier, Michelangelo Scalone, Urs Schwitter, Beat Wirz, Ulrich Zutter
  • Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine
    Patent number: 9447099
    Abstract: The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.
    Type: Grant
    Filed: September 27, 2012
    Date of Patent: September 20, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stephan Bachmann, Daniel Bailey, Jodie Brice, Miall Cedilote, Zhiming Dong, Stefan Hildbrand, Doreen Miller, Paul Spurr, Amit Srivastava, Juergen Wichmann, Thomas Woltering, Jason Yang, Pingsheng Zhang
  • PROCESS TO MANUFACTURE N-[(3S)-1-[4-[(3-FLUOROPHENYL)METHOXY]PHENYL]-5-OXO-PYRROLIDIN-3-YL]ACETAMIDE
    Publication number: 20160237032
    Abstract: The present invention provides processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are compounds useful as intermediates in the methods of the invention.
    Type: Application
    Filed: April 27, 2016
    Publication date: August 18, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Olaf Grassmann, Stefan Hildbrand, Roland Meier, Michelangelo Scalone, Urs Schwitter, Beat Wirz, Ulrich Zutter
  • Process For The Preparation Of A DPP-IV Inhibitor
    Publication number: 20150336951
    Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
    Type: Application
    Filed: May 1, 2015
    Publication date: November 26, 2015
    Inventors: Ulrike Bromberger, Ralph Diodone, Stefan Hildbrand, Roland Meier
  • Process For The Preparation Of Pyrido [2,1-A] Isoquinoline Derivatives Comprising Optical Resolution Of An Enamine
    Publication number: 20150126743
    Abstract: This invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the formula wherein R1 is lower alkyl, in the presence of an optical active resolving agent to form an (S)-enamine salt of the formula wherein RCO2? is the conjugate base of the resolving agent.
    Type: Application
    Filed: January 9, 2015
    Publication date: May 7, 2015
    Inventors: Stefan Abrecht, Jean-Michel Adam, Alec Fettes, Stefan Hildbrand
  • Process for the Preparation of a DPP-IV Inhibitor
    Publication number: 20140350257
    Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
    Type: Application
    Filed: July 3, 2014
    Publication date: November 27, 2014
    Inventors: Ulrike Bromberger, Ralph Diodone, Stefan Hildbrand, Roland Meier
  • Process for the manufacture of pharmaceutically active compounds
    Patent number: 8741920
    Abstract: The present invention relates to a composition comprising the compound of formula (1), and the compound of formula (B),
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright
  • PROCESS FOR THE PREPARATION OF DPP-IV INHIBITOR
    Publication number: 20140046066
    Abstract: The present invention is concerned with an improved process for the preparation of pyrido[2,1-a]isoquinoline derivatives of formula I wherein R1, R2 and R3 are each independently hydrogen, halogen, hydroxy, lower alkyl, lower alkoxy or lower alkenyl, wherein lower alkyl, lower alkoxy and lower alkenyl may optionally be substituted by lower alkoxycarbonyl, aryl or heterocyclyl, and the pharmaceutically acceptable salts thereof. The invention also relates to two crystalline forms of (2S,3S,11bS)-1-(2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl)-4(S)-fluoromethyl-pyrrolidin-2-one dihydrochloride, which are form A and form B and to an amorphous form of said compound.
    Type: Application
    Filed: September 13, 2013
    Publication date: February 13, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Ulrike Bromberger, Ralph Diodone, Stefan Hildbrand, Roland Meier
  • 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 PYRIDO [2,1-A] ISOQUINOLINE DERIVATIVES COMPRISING OPTICAL RESOLUTION OF AN ENAMINE
    Publication number: 20130338366
    Abstract: This invention relates to a process for the preparation of pyrido[2,1-a]isoquinoline derivatives of the formula wherein R1, R2, R3 and R4 are defined in the specification, comprising the optical resolution of an enamine of the formula wherein R1 is lower alkyl, in the presence of an optical active resolving agent to form an (S)-enamine salt of the formula wherein RCO2? is the conjugate base of the resolving agent.
    Type: Application
    Filed: July 29, 2013
    Publication date: December 19, 2013
    Inventors: Stefan Abrecht, Jean-Michel Adam, Alec Fettes, Stefan Hildbrand
  • Process for the preparation of isoxazolyl-methoxy nicotinic acids
    Patent number: 8604062
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: December 10, 2013
    Assignee: Hoffman-La Roche Inc.
    Inventors: Pascal Dott, Steven Paul Hanlon, Stefan Hildbrand, Hans Iding, Andrew Thomas, Pius Waldmeier
  • PROCESS FOR THE PREPARATION OF 2-DEOXY-2-FLUORO-2-METHYL-D-RIBOFURANOSYL NUCLEOSIDE COMPOUNDS
    Publication number: 20130324709
    Abstract: An improved process for the preparation of (2?R)-2?-deoxy-2?-fluoro-2?-methylcytidine derivatives of formula I wherein R1 is selected from C1-4-alkyl is described. The (2?R)-2?-deoxy-2?-fluoro-2?-methylcytidine derivatives of formula I have the potential to be useful as prodrugs for potent inhibitors of the Hepatitis C Virus (HCV) NS5B polymerase.
    Type: Application
    Filed: May 28, 2013
    Publication date: December 5, 2013
    Inventors: Robert Carr, Stefan Hildbrand, Mark L. Hodges, Michael Kammerer, John F. Lang, William J. Lawrimore, III, Dieu Nguyen
  • Process for the manufacture of pharmaceutically active compounds
    Patent number: 8530661
    Abstract: The present invention further relates to a process for the manufacture of compound (I), wherein X is —Br or —Cl.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: September 10, 2013
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Stefan Hildbrand, Hans-Juergen Mair, Roumen Nikolaev Radinov, Yi Ren, James Anderson Wright