Patents by Inventor Francis Gosselin

Francis Gosselin 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).

  • Publication number: 20220241279
    Abstract: The present invention relates to pharmaceutical compositions comprising Akt protein kinase inhibitors with therapeutic activity against diseases such as cancer as well as processes for their preparation and their use as medicament.
    Type: Application
    Filed: April 19, 2022
    Publication date: August 4, 2022
    Inventors: Reinhard Reents, Pirmin Hidber, Andre Hell, Peter Steidle, Martin Wunderlich, Marie Pepelnjak, Francis Gosselin, Edward Yost
  • Patent number: 11337977
    Abstract: The present invention relates to pharmaceutical compositions comprising Akt protein kinase inhibitors with therapeutic activity against diseases such as cancer as well as processes for their preparation and their use as medicament.
    Type: Grant
    Filed: August 9, 2017
    Date of Patent: May 24, 2022
    Assignee: Genentech, Inc.
    Inventors: Reinhard Reents, Pirmin Hidber, Andre Hell, Peter Steidle, Martin Wunderlich, Marie Pepelnjak, Francis Gosselin, Edward Yost
  • Patent number: 11325912
    Abstract: A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb) comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2 This annulation reaction between ?-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines.
    Type: Grant
    Filed: May 7, 2020
    Date of Patent: May 10, 2022
    Assignee: Genentech, Inc.
    Inventors: Kyle Bradley Pascual Clagg, Nicholas Andrew White, Haiming Zhang, Francis Gosselin, William Nack, Paul D. O'Shea
  • Publication number: 20220081413
    Abstract: Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.
    Type: Application
    Filed: August 10, 2021
    Publication date: March 17, 2022
    Applicants: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Ngiap-Kie Lim, Jeff Shen, Lauren E. Sirois, Jacob C. Timmerman, Etienne Trachsel, Nicholas A. White, Jie Xu, Haiming Zhang, Stephan Bachmann, Raphael Bigler, Kyle Bradley Pascual Clagg, Antonio Dipasquale, Francis Gosselin, Ugo Jonathan Orcel, Roland Christoph Meier
  • Publication number: 20220056078
    Abstract: Methods for making an arylomycin ring of formula t or salts or solvates thereof, wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R5, R10 and Pg1 are as defined herein.
    Type: Application
    Filed: November 2, 2021
    Publication date: February 24, 2022
    Applicant: Genentech, Inc.
    Inventors: Filip PETRONIJEVIC, Ngiap-Kie LIM, Nicholas WONG, Allen HONG, Haiyun HOU, Xin LINGHU, Francis GOSSELIN
  • Publication number: 20220041587
    Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
    Type: Application
    Filed: December 3, 2020
    Publication date: February 10, 2022
    Applicants: Hoffmann-La Roche Inc., GENENTECH, INC.
    Inventors: CHEOL KEUN CHUNG, JIE XU, HANS IDING, KYLE CLAGG, MICHAEL DALZIEL, ALEC FETTES, FRANCIS GOSSELIN, NGIAP-KIE LIM, ANDREW MCCLORY, HAIMING ZHANG, PAROMA CHAKRAVARTY, KARTHIK NAGAPUDI, SARAH ROBINSON
  • Patent number: 11192924
    Abstract: Methods for making an arylomycin ring of formula t or salts or solvates thereof, wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R5, R10 and Pg1 are as defined herein.
    Type: Grant
    Filed: September 24, 2019
    Date of Patent: December 7, 2021
    Assignee: Genentech, Inc.
    Inventors: Filip Petronijevic, Ngiap-Kie Lim, Nicholas Wong, Allen Hong, Haiyun Hou, Xin Linghu, Francis Gosselin
  • Patent number: 11136330
    Abstract: A method of synthesizing comprising a step of making an imidazo-pyrimidine compound by coupling a first compound of formula (II) with a second compound of formula (III) Followed by a deprotection and tosylation step. The methods are able to produce an isotopically substituted molecule having upwards of 95% purity relative to non-isotopically substituted molecules.
    Type: Grant
    Filed: May 7, 2020
    Date of Patent: October 5, 2021
    Assignee: Genentech, Inc.
    Inventors: Kyle Bradley Pascual Clagg, Nicholas Andrew White, Haiming Zhang, Francis Gosselin, William Nack, Paul D. O'Shea
  • Publication number: 20210244717
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: September 11, 2020
    Publication date: August 12, 2021
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Patent number: 10954234
    Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: March 23, 2021
    Assignees: Genentech, Inc., Hoffmann-La Roche, Inc.
    Inventors: Cheol Keun Chung, Jie Xu, Hans Iding, Kyle Clagg, Michael Dalziel, Alec Fettes, Francis Gosselin, Ngiap-Kie Lim, Andrew McClory, Haiming Zhang, Paroma Chakravarty, Karthik Nagapudi, Sarah Robinson
  • Publication number: 20210079004
    Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.
    Type: Application
    Filed: November 23, 2020
    Publication date: March 18, 2021
    Applicant: Genentech, Inc.
    Inventors: Danial BEAUDRY, Theresa CRAVILLION, Francis GOSSELIN, Ngiap-Kie LIM, Sushant MALHOTRA, Qingping TIAN, Haiming ZHANG, Alexander GMEHLING, Alec FETTES, Stephan BACHMANN
  • Publication number: 20210070749
    Abstract: A process for the manufacture N-(5-((5R,6S)-5-amino-6-fluorooxepan-2-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2,6-difluorophenyl)thiazole-4-carboxamide (I) is claimed
    Type: Application
    Filed: September 10, 2020
    Publication date: March 11, 2021
    Applicant: Genentech, Inc.
    Inventors: FRANCIS GOSSELIN, ANDREW MCCLORY, ZHIGANG CHENG
  • Patent number: 10882864
    Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3?-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4?]bipyridinyl-2?-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.
    Type: Grant
    Filed: July 2, 2019
    Date of Patent: January 5, 2021
    Assignee: Genentech, Inc.
    Inventors: Danial Beaudry, Theresa Cravillion, Francis Gosselin, Ngiap-Kie Lim, Sushant Malhotra, Qingping Tian, Haiming Zhang, Alexander Gmehling, Alec Fettes, Stephan Bachmann
  • Patent number: 10870626
    Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.
    Type: Grant
    Filed: September 18, 2019
    Date of Patent: December 22, 2020
    Assignees: F. Hoffman-La Roche AG, Genentech, Inc.
    Inventors: Francis Gosselin, Chong Han, Hans Iding, Reinhard Reents, Scott Savage, Beat Wirz
  • Patent number: 10858324
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.
    Type: Grant
    Filed: August 29, 2019
    Date of Patent: December 8, 2020
    Assignee: GENENTECH, INC.
    Inventors: Hans Iding, Reinhard Reents, Michelangelo Scalone, Francis Gosselin
  • Publication number: 20200369670
    Abstract: A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb) comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2 This annulation reaction between ?-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines.
    Type: Application
    Filed: May 7, 2020
    Publication date: November 26, 2020
    Applicant: Genentech, Inc.
    Inventors: Kyle Bradley Pascual Clagg, Nicholas Andrew White, Haiming Zhang, Francis Gosselin, William Nack, Paul D. O'Shea
  • Publication number: 20200354369
    Abstract: A method of synthesizing comprising a step of making an imidazo-pyrimidine compound by coupling a first compound of formula (II) with a second compound of formula (III) Followed by a deprotection and tosylation step. The methods are able to produce an isotopically substituted molecule having upwards of 95% purity relative to non-isotopically substituted molecules.
    Type: Application
    Filed: May 7, 2020
    Publication date: November 12, 2020
    Applicant: Genentech, Inc.
    Inventors: Kyle Bradley Pascual Clagg, Nicholas Andrew White, Haiming Zhang, Francis Gosselin, William Nack, Paul D. O'Shea
  • Patent number: 10781219
    Abstract: Methods of making benzoxazepin oxazolidinone compounds as well as synthetic intermediates are described, including compound 18, having the structure:
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: September 22, 2020
    Assignee: Genentech, Inc.
    Inventors: Francis Gosselin, Chong Han, Theresa Cravillion, Sean M. Kelly, Scott Savage
  • Patent number: 10772874
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Grant
    Filed: August 12, 2019
    Date of Patent: September 15, 2020
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
  • Publication number: 20200255476
    Abstract: Methods for making an arylomycin ring of formula t or salts or solvates thereof, wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R5, R10 and Pg1 are as defined herein.
    Type: Application
    Filed: September 24, 2019
    Publication date: August 13, 2020
    Applicant: Genentech, Inc.
    Inventors: Filip PETRONIJEVIC, Ngiap-Kie LIM, Nicholas WONG, Allen HONG, Haiyun HOU, Xin LINGHU, Francis GOSSELIN