Patents by Inventor Liansheng Li

Liansheng Li 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: 20210380595
    Abstract: The present invention provides e.g. 2-(2-acryloyl-2, 6-diazaspiro[3.4]octan-6-yl)-6-(1H-indazol-4-yl)-benzonitrile and e.g. 2-(2-acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-6-(1H-indazol-4-yl)-benzonitrile derivatives and related compounds of formula (I) as inhibitors of G12C mutant KRAS protein for treating tumor metastasis. The present description discloses exemplary compounds (e.g. pages 53 to 90; table 1; compounds I-1 to I-141), pharmacological data (e.g. page 125 to 128; table 2; example 1) and synthesis thereof (e.g. pages 129 to 143; examples 2 to 7). Exemplary compounds are e.g. 2-(2-acryloyl-2,6-diazaspiro[3.4]octan-6-yl)-6-(5-methyl-1H-indazol-4-yl)-4-morpholinobenzonitrile (example 2; compound I-1) and 6-(2-acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-3-methoxy-2-(5-methyl-1H-indazol-4-yl)-4-morpholinobenzonitrile (example 7; compound I-84).
    Type: Application
    Filed: October 23, 2019
    Publication date: December 9, 2021
    Inventors: Liansheng LI, Yuan LIU, Tao WU, Jun FENG, Pingda REN, Yi LIU
  • Publication number: 20210317127
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1, L1, L2, L3, A1, A2, A3, A4, G1, G2, E, W, X, Y, Z, m, and n are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Application
    Filed: August 1, 2019
    Publication date: October 14, 2021
    Inventors: Liansheng LI, Jun FENG, Tao WU, Yuan LIU, Yi WANG, Alana K. BORUM, Pingda REN, Yi LIU
  • Patent number: 11136308
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (Formula (I)) or a pharmaceutically acceptable salt, stereoisomer thereof, wherein G, Y, R, R1, R2a, R2b, R2c, L, L1 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. Preferred compounds are quinazoline and quinazolinone derivatives and in particular 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds.
    Type: Grant
    Filed: January 24, 2018
    Date of Patent: October 5, 2021
    Assignees: ARAXES PHARMA LLC, JANSSEN BIOTECH, INC.
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu
  • Patent number: 11059819
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I), or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, W, X, Y, Z, and are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: July 13, 2021
    Assignees: Janssen Biotech, Inc., Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu
  • Publication number: 20210188869
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Application
    Filed: December 17, 2020
    Publication date: June 24, 2021
    Inventors: Liansheng LI, Jun FENG, Tao WU, Pingda REN, Yi LIU, Yuan Liu, Yun Oliver Long
  • Patent number: 11021470
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, G1, G2, L1, L2, m1, m2, n, X and E are as defined herein, and wherein at least one of R3a, R3b, R4a or R4b is not H. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: July 17, 2019
    Date of Patent: June 1, 2021
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Publication number: 20210107917
    Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.
    Type: Application
    Filed: July 13, 2020
    Publication date: April 15, 2021
    Inventors: Tao WU, Liansheng LI, Yi WANG, Pingda REN, Jolanta GREMBECKA, Tomasz CIERPICKI, Szymon KLOSSOWSKI, Jonathan POLLOCK, Dmitry BORKIN
  • Patent number: 10975071
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, B R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: April 13, 2021
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Pingda Ren, Yi Liu
  • Publication number: 20210101908
    Abstract: The present disclosure provides methods of inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The methods are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin. Compositions for use in these methods are also provided.
    Type: Application
    Filed: July 30, 2020
    Publication date: April 8, 2021
    Inventors: Tao WU, Liansheng LI, Yi WANG, Pingda REN, Jolanta GREMBECKA, Tomasz CIERPICKI, Szymon KLOSSOWSKI, Jonathan POLLOCK, Dmitry BORKIN
  • Patent number: 10927125
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: February 23, 2021
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Tao Wu, Pingda Ren, Yi Liu, Yuan Liu, Yun Oliver Long
  • Patent number: 10919850
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: February 16, 2021
    Assignee: ARAXES PHARMA LLC
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20210024501
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, isotopic form or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5, L1, L2, L3, E, m1, m2 and * are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Application
    Filed: June 29, 2020
    Publication date: January 28, 2021
    Inventors: Liansheng Li, Jun Feng, Tao Wu, Yuan Liu, Yi Wang, Pingda Ren, Yi Liu
  • Patent number: 10882847
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R1, R3a, R3b, R4a, R4b, G1, G2, G2, G3, G4, m1, m2, m3, m4, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: January 5, 2021
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
  • Patent number: 10875842
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein R1, R3a, R3b, R4a, R4b, G1, G2, G3, G4, m1, m2, m3, m4, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: December 29, 2020
    Assignee: Araxes Pharma LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
  • Publication number: 20200385364
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I) or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, E, L1, Ra. Rb, Rc and ? are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Application
    Filed: January 25, 2018
    Publication date: December 10, 2020
    Inventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu
  • Patent number: 10858343
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (I) or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof wherein Z, Y R3a, R3b, R4a, R4b, G1, G2, G3, G4, L1, m1, m2, m3, m4, n and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: December 8, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
  • Patent number: 10829458
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have one of the following structures (I), (II) or (III): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5a, R5b, R6, A, B, G1, G2, L1, L2, m1, m2, n, x, y, X and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: February 21, 2019
    Date of Patent: November 10, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
  • Patent number: 10822312
    Abstract: The present disclosure provides inhibitors of Ras protein of Formula (I-A): Also disclosed are methods to modulate the activity of Ras protein and methods of treatment of disorders mediated by Ras protein with compounds of Formula (I-A).
    Type: Grant
    Filed: March 29, 2017
    Date of Patent: November 3, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Pingda Ren, Yi Liu
  • Patent number: 10781218
    Abstract: The present disclosure provides compounds of Formula (II-A), which inhibit the interaction of menin with one or more of MLL1, MLL2 and MLL-fusion oncoproteins. Also disclosed are methods for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: September 22, 2020
    Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin
  • Patent number: 10752639
    Abstract: The present disclosure provides compounds of Formula (I-E) for inhibiting the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compounds are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.
    Type: Grant
    Filed: March 15, 2017
    Date of Patent: August 25, 2020
    Assignees: KURA ONCOLOGY, INC., THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Tao Wu, Liansheng Li, Yi Wang, Pingda Ren, Jolanta Grembecka, Tomasz Cierpicki, Szymon Klossowski, Jonathan Pollock, Dmitry Borkin