Patents by Inventor Pius Waldmeier

Pius Waldmeier 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).

  • Processes for the manufacture of propane-1-sulfonic acid (3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl)-amide
    Patent number: 9556172
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: August 27, 2015
    Date of Patent: January 31, 2017
    Assignee: Hoffman La-Roche Inc.
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • NOVEL PROCESSES FOR THE MANUFACTURE OF PROPANE-1-SULFONIC ACID (3-[5-(4-CHLORO-PHENYL)-1H-PYRROLO[2,3-b]PYRIDINE-3-CARBONYL]-2,4-DIFLUORO-PHENYL)-AMIDE
    Publication number: 20160083378
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: August 27, 2015
    Publication date: March 24, 2016
    Inventors: Corey James BRUMSTED, Hendrik MOORLAG, Roumen Nikolaev RADINOV, Yi REN, Pius WALDMEIER
  • Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
    Patent number: 9150594
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: June 4, 2014
    Date of Patent: October 6, 2015
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • NOVEL PROCESSES FOR THE MANUFACTURE OF PROPANE-1-SULFONIC ACID -AMIDE
    Publication number: 20140288308
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Inventors: Corey James BRUMSTED, Hendrik MOORLAG, Roumen Nikolaev RADINOV, Yi REN, Pius WALDMEIER
  • Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
    Patent number: 8779150
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: July 15, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • 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
  • 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds
    Patent number: 8450313
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: May 22, 2012
    Date of Patent: May 28, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 2,3-diaryl- or heteroaryl-substituted 1,1,1-trifluoro-2-hydroxypropyl compounds
    Patent number: 8268820
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: September 18, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Daniel Hunziker, Chrisitan Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20120232071
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • Substituted isoxazoles
    Patent number: 8222246
    Abstract: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: July 17, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Stephen Deems Gabriel, Steven Paul Hanlon, Roland Jakob-Roetne, Matthew C. Lucas, Paul Spurr, Andrew Thomas, Pius Waldmeier
  • PROCESS FOR THE PREPARATION OF NICOTINAMIDE DERIVATIVES
    Publication number: 20120101282
    Abstract: The present invention relates to a process for the preparation of nicotinamide derivatives of formula I, wherein R1 to R7 are as defined above and to pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of cannabinoid 1 receptors (CB1 receptors) as described in the PCT Publ. WO 2006/106054.
    Type: Application
    Filed: October 12, 2011
    Publication date: April 26, 2012
    Inventors: Pascal Dott, Pius Waldmeier
  • Substituted benzene compounds as modulators of the glucocorticoid receptor
    Patent number: 8138189
    Abstract: The present invention relates to compounds of formula I wherein R.sup.1a to R.sup.1e and R.sup.2 to R.sup.5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: March 20, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Daniel Hunziker, Chrisitan Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 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 Processes for the manufacture of Propane-1-sulfonic acid -amide
    Publication number: 20120022258
    Abstract: According to the present invention there are provided novel processes for the manufacture of the compound of formula 1 as well as intermediates and novel synthesis routes for key intermediates used in those processes.
    Type: Application
    Filed: July 15, 2011
    Publication date: January 26, 2012
    Inventors: Corey James Brumsted, Hendrik Moorlag, Roumen Nikolaev Radinov, Yi Ren, Pius Waldmeier
  • 2-trifluoromethylnicotinamide derivatives as HDL-cholesterol raising agents
    Patent number: 7897621
    Abstract: The present invention relates to compounds formula I: and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.
    Type: Grant
    Filed: March 16, 2009
    Date of Patent: March 1, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Pius Waldmeier, Matthew Wright
  • 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
  • SUBSTITUTED ISOXAZOLES
    Publication number: 20100256127
    Abstract: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: March 29, 2010
    Publication date: October 7, 2010
    Inventors: Bernd Buettelmann, Stephen Deems Gabriel, Steven Paul Hanlon, Roland Jakob-Roetne, Matthew C. Lucas, Paul Spurr, Andrew Thomas, Pius Waldmeier
  • 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20100249139
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 2,3-DIARYL- OR HETEROARYL-SUBSTITUTED 1,1,1-TRIFLUORO-2-HYDROXYPROPYL COMPOUNDS
    Publication number: 20100249124
    Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.
    Type: Application
    Filed: March 19, 2010
    Publication date: September 30, 2010
    Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
  • 2-TRIFLUOROMETHYLNICOTINAMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS
    Publication number: 20090247588
    Abstract: The present invention relates to compounds formula I: and pharmaceutically acceptable salts thereof, wherein R1 to R8 are as defined in the description and claims for use as HDL-cholesterol raising agents in the treatment and/or prophylaxis of diseases or disorders that can be treated with such agents such as dyslipidemia.
    Type: Application
    Filed: March 16, 2009
    Publication date: October 1, 2009
    Inventors: Paul Hebeisen, Constantinos G. Panousis, Stephan Roever, Pius Waldmeier, Matthew Wright