Patents by Inventor Rene Trussardi

Rene Trussardi 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).

  • SALTS AND CRYSTALLINE FORMS OF A TAAR1 AGONIST
    Publication number: 20230120311
    Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the TAAR1 agonist 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the TAAR1 agonist, and methods of using the TAAR1 agonist, alone and in combination with other compounds, for treating diseases or conditions that are associated with TAAR1 activity.
    Type: Application
    Filed: September 16, 2022
    Publication date: April 20, 2023
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Kirsten Andrea Graeser, Urs Schwitter, Frank Stowasser, Florence Nicole Antoinette Tixeront, Rene Trussardi
  • PROCESS FOR THE PREPARATION OF SUBSTITUTED PYRAZOLE DERIVATIVES
    Publication number: 20220127236
    Abstract: The invention provides a process for manufacturing 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide (Formula I), or a pharmaceutically acceptable salt thereof, on an industrial scale, comprising a one-pot process for manufacturing 5-ethyl-4-methyl-1H-pyrazole-3-carboxylic acid (1).
    Type: Application
    Filed: January 7, 2022
    Publication date: April 28, 2022
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Paul Spurr, Rene Trussardi
  • 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 GalNAc oligonucleotide conjugates
    Patent number: 11021503
    Abstract: The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.
    Type: Grant
    Filed: November 21, 2019
    Date of Patent: June 1, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Simon Breitler, Joerg Lill, Kurt Puentener, René Trussardi
  • Processes for the preparation of GalNAc acid derivatives
    Patent number: 10597417
    Abstract: The invention comprises a new process for the preparation of GalNAc derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: March 24, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joerg Lill, Rene Trussardi
  • Galnac cluster phosphoramidite
    Patent number: 10590156
    Abstract: The invention comprises GalNAc phosphoramidite derivatives of the formula I wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.
    Type: Grant
    Filed: May 14, 2018
    Date of Patent: March 17, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Rene Trussardi
  • PROCESS FOR GALNAC OLIGONUCLEOTIDE CONJUGATES
    Publication number: 20200079807
    Abstract: The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.
    Type: Application
    Filed: November 21, 2019
    Publication date: March 12, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Simon BREITLER, Joerg LILL, Kurt PUENTENER, René TRUSSARDI
  • Process for the preparation of chiral 2-aryl morpholines
    Patent number: 10337039
    Abstract: The invention relates to a novel process for the preparation of chiral 2-(4-aminophenyl) morpholines of the formula wherein R1 is hydrogen an amino protecting group. The chiral 2-(4-aminophenyl) morpholines of the formula I are key intermediates for the preparation of compounds that have a good affinity to the trace amine associated receptors (TAARs).
    Type: Grant
    Filed: June 7, 2016
    Date of Patent: July 2, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rene Trussardi, Hans Iding
  • 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
  • Solid forms
    Patent number: 10221125
    Abstract: The instant invention relates to novel solid forms of the compound of formula (I) or salts thereof as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
    Type: Grant
    Filed: May 2, 2016
    Date of Patent: March 5, 2019
    Assignee: Oryzon Genomics, S.A.
    Inventors: Ralph Diodone, Urs Schwitter, René Trussardi
  • GALNAC CLUSTER PHOSPHORAMIDITE
    Publication number: 20180258122
    Abstract: The invention comprises GalNAc phosphoramidite derivatives of the formula I wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/or optical isomers thereof. The invention further comprises a process for the preparation of the GalNAc phosphoramidite derivatives of the formula I and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.
    Type: Application
    Filed: May 14, 2018
    Publication date: September 13, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventor: RENE TRUSSARDI
  • PROCESSES FOR THE PREPARATION OF GALNAC ACID DERIVATIVES
    Publication number: 20180162894
    Abstract: The invention comprises a new process for the preparation of GalNAc derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.
    Type: Application
    Filed: February 6, 2018
    Publication date: June 14, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Joerg Lill, Rene Trussardi
  • SOLID FORMS
    Publication number: 20180086692
    Abstract: The instant invention relates to novel solid forms of the compound of formula (I) or salts thereof as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
    Type: Application
    Filed: May 2, 2016
    Publication date: March 29, 2018
    Inventors: Ralph DIODONE, Urs SCHWITTER, René TRUSSARDI
  • Process for the preparation of 2-trifluoromethyl isonicotinic acid and esters
    Patent number: 9481650
    Abstract: The invention relates to a novel process for the preparation of 2-trifluoromethyl isonicotinic acid and esters of the formula I which involves a palladium catalyzed carbonylation or cyanation step wherein R1 is hydrogen or Q1-6-alkyl. The 2-trifluoromethyl isonicotinic acid and esters of the formula I are versatile intermediates for the preparation of active pharmaceutical and agrochemical agents such as for instance TAAR 1 agonists of the formula III.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: November 1, 2016
    Assignee: Hoffmann La Roche Inc.
    Inventor: René Trussardi
  • PROCESS FOR THE PREPARATION OF CHIRAL 2-ARYL MORPHOLINES
    Publication number: 20160289718
    Abstract: The invention relates to a novel process for the preparation of chiral 2-(4-aminophenyl) morpholines of the formula wherein R1 is hydrogen an amino protecting group. The chiral 2-(4-aminophenyl) morpholines of the formula I are key intermediates for the preparation of compounds that have a good affinity to the trace amine associated receptors (TAARs).
    Type: Application
    Filed: June 7, 2016
    Publication date: October 6, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Rene Trussardi, Hans Iding
  • 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
  • PROCESS FOR THE PREPARATION OF 2-TRIFLUOROMETHYL ISONICOTINIC ACID AND ESTERS
    Publication number: 20150291530
    Abstract: The invention relates to a novel process for the preparation of 2-trifluoromethyl isonicotinic acid and esters of the formula I which involves a palladium catalysed carbonylation or cyanation step wherein R1 is hydrogen or Q1-6-alkyl. The 2-trifluoromethyl isonicotinic acid and esters of the formula I are versatile intermediates for the preparation of active pharmaceutical and agrochemical agents such as for instance TAAR 1 agonists of the formula III.
    Type: Application
    Filed: November 13, 2013
    Publication date: October 15, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventor: René TRUSSARDI
  • 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