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: 20240034739
    Abstract: Processes are provided herein for the preparation of a bicyclic ketone compound of formula (I), or a stereoisomer thereof: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and n are as defined herein; and compounds prepared by these processes.
    Type: Application
    Filed: October 2, 2023
    Publication date: February 1, 2024
    Applicants: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Allen Yu HONG, Nicholas WONG, Sean M. KELLY, Lauren Elizabeth SIROIS, Sara SCHWEGLER, Xin LINGHU, Francis GOSSELIN, Katarzyna Aleksandra PIECHOWICZ, Carmela MOLINARO, Dennis WETZL
  • Publication number: 20230346753
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Application
    Filed: December 2, 2022
    Publication date: November 2, 2023
    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: 11780834
    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: December 3, 2020
    Date of Patent: October 10, 2023
    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: 20230250103
    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: April 12, 2023
    Publication date: August 10, 2023
    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: 20230250074
    Abstract: Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.
    Type: Application
    Filed: February 3, 2023
    Publication date: August 10, 2023
    Applicants: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Rene LEBL, Ngiap Kie LIM, Roland Christoph MEIER, Ugo Jonathan ORCEL, Joerg SEDELMEIER, Jeff SHEN, Lauren Elizabeth SIROIS, Jacob C. TIMMERMAN, Etienne TRACHSEL, Nicholas Andrew WHITE, Jie XU, Haiming ZHANG, Stephan BACHMANN, Thomas Michael BASS, Raphael BIGLER, Johannes Adrian BURKHARD, Kyle Bradley Pascual CLAGG, Francis GOSSELIN, Chong HAN, Dainis KALDRE, Sean M. KELLY, Sebastian HEROLD, Christian LEITNER
  • Patent number: 11702452
    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: November 2, 2021
    Date of Patent: July 18, 2023
    Assignee: Genentech, Inc.
    Inventors: Filip Petronijevic, Ngiap-Kie Lim, Nicholas Wong, Allen Hong, Haiyun Hou, Xin Linghu, Francis Gosselin
  • Patent number: 11661424
    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: November 23, 2020
    Date of Patent: May 30, 2023
    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
  • Publication number: 20230028651
    Abstract: A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective PtN/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N?,N?-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.
    Type: Application
    Filed: June 28, 2022
    Publication date: January 26, 2023
    Applicants: Genentech, Inc., Hoffmann-La Roche Inc.
    Inventors: Francis GOSSELIN, Stefan G. KOENIG, Eduardo V. MERCADO-MARIN, Andreas STUMPF, Daniel ZELL, Haiming ZHANG, Stephan BACHMANN, Diane E. CARRERA, Michael E. DALZIEL, Yonghui GE, Jie ZHANG, Raphael BIGLER, Laure Elizabeth Simone FINET, Regis Jean Georges MONDIERE, Yuki NAKAGAWA
  • Patent number: 11547701
    Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.
    Type: Grant
    Filed: September 11, 2020
    Date of Patent: January 10, 2023
    Assignees: Valo Health, Inc., Genentech, Inc.
    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: 11414412
    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) wherein the vicinal amino fluoro substituents are introduced by treating 5 with sodium chloro((4-nitrophenyl)sulfonyl)amide and N-bromosucinimide and unraveling the resulting substituted aziridine (6) with trimethylamine trihydrofluoride to afford 7 which is further processed to afford 1.
    Type: Grant
    Filed: September 10, 2020
    Date of Patent: August 16, 2022
    Inventors: Francis Gosselin, Andrew McClory, Zhigang Cheng
  • 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