Patents by Inventor Pingda Ren

Pingda Ren 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).

  • HETEROCYCLIC SPIRO COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF CANCER
    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
  • Substituted quinazoline and quinazolinone compounds and methods of use thereof
    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
  • SYNTHESIS OF TIPIFARNIB
    Publication number: 20210246114
    Abstract: Provided herein are methods of preparing a desired enantiomer 6-[amino(4-chlorophenyl) (1-methyl-1H-imidazol-5-yl) methyl]-4-(3-chlorophenyl)-1-methyl-2(1H)-quinolinone, otherwise known as tipifarnib.
    Type: Application
    Filed: May 17, 2019
    Publication date: August 12, 2021
    Applicant: KURA ONCOLOGY, INC.
    Inventors: Pingda REN, Xiaohu DENG, Wanping MAI
  • Fused hetero-hetero bicyclic compounds and methods of use thereof
    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
  • INHIBITORS OF KRAS G12C
    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
  • 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof
    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
  • BRIDGED BICYCLIC INHIBITORS OF MENIN-MLL AND METHODS OF USE
    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
  • Inhibitors of KRAS G12C mutant proteins
    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
  • SUBSTITUTED INHIBITORS OF MENIN-MLL AND METHODS OF USE
    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
  • Substituted cinnolines as inhibitors of KRAS G12C
    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
  • Covalent inhibitors of KRas G12C
    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
  • COVALENT INHIBITORS OF KRAS
    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
  • Inhibitors of KRAS G12C mutant proteins
    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
  • Inhibitors of KRAS G12C mutant proteins
    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
  • PROCESSES FOR PREPARING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES
    Publication number: 20200385388
    Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: January 3, 2020
    Publication date: December 10, 2020
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • FUSED N-HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
    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
  • Inhibitors of KRAS G12C mutant proteins
    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
  • Substituted quinazoline compounds and methods of use thereof
    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
  • Substituted quinazoline compounds and methods of use
    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
  • Substituted inhibitors of menin-MLL and methods of use
    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