Patents Assigned to Araxes Pharma LLC
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Patent number: 10723738Abstract: 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 B, W, X, Y, R1, R2a, R2b, R3a, R3b, R4a, R4b, G1, G2, m1, m2, L1, L2 and E are 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: GrantFiled: April 3, 2019Date of Patent: July 28, 2020Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Pingda Ren, Yi Liu
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Patent number: 10689356Abstract: 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, R1, R3a, R3b, R4a, R4b, 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: GrantFiled: September 28, 2016Date of Patent: June 23, 2020Assignee: ARAXES PHARMA LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Pingda Ren, Yi Liu
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Patent number: 10647703Abstract: 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, X, R3a, R3b, R4a, R4b, G1, G2, G3, G4, L1, L2, m1, m2, m3, m4, 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: GrantFiled: September 27, 2016Date of Patent: May 12, 2020Assignee: ARAXES PHARMA LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
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Patent number: 10646488Abstract: Conjugates of a cereblon-binding compound and compounds having modulatory activity against G12C mutant KRAS, HRAS or NRAS G12C proteins are provided. Methods associated with preparation and use of such conjugates, pharmaceutical compositions comprising such conjugates and methods to modulate the activity of G12C mutant KRAS, HRAS or NRAS G12C proteins for treatment of disorders, such as cancer, are also provided.Type: GrantFiled: July 13, 2017Date of Patent: May 12, 2020Assignee: ARAXES PHARMA LLCInventors: Yi Liu, Liansheng Li, Pingda Ren
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Patent number: 10428064Abstract: 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, stereoisomer or prodrug thereof, wherein A is a heterocyclic or heteroaryl ring, and R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, A, G1, G2, L1, L2, m1, m2, 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: GrantFiled: April 15, 2016Date of Patent: October 1, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
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Patent number: 10414757Abstract: 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: GrantFiled: November 16, 2016Date of Patent: September 17, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
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Patent number: 10377743Abstract: 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, R?, Q, W, X, Y, Z, n1, n2 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: GrantFiled: October 6, 2017Date of Patent: August 13, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yuan Liu, Pingda Ren, Yi Liu, Tao Wu, Yi Wang
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Patent number: 10370386Abstract: 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: GrantFiled: November 7, 2017Date of Patent: August 6, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Tao Wu, Pingda Ren, Yi Liu, Yuan Liu, Yun Oliver Long
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Patent number: 10351550Abstract: 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 R, R1, R2a, R2b, R2c, A, B, 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.Type: GrantFiled: March 8, 2018Date of Patent: July 16, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
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Patent number: 10280172Abstract: 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 B, W, X, Y, 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: GrantFiled: September 29, 2017Date of Patent: May 7, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Pingda Ren, Yi Liu
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Patent number: 10273207Abstract: 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: GrantFiled: February 7, 2018Date of Patent: April 30, 2019Assignee: Araxes Pharma LLCInventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
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Patent number: 10246424Abstract: 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: GrantFiled: April 8, 2016Date of Patent: April 2, 2019Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
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Patent number: 10144724Abstract: 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 R, R1, R2a, R2b, R2c, A, B, 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.Type: GrantFiled: July 22, 2016Date of Patent: December 4, 2018Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Tao Wu, Pingda Ren, Yi Liu
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Patent number: 10111874Abstract: Combination therapies for treatment of cancers associated with mutations in the KRAS gene are provided. Compositions comprising therapeutic agents for treatment of cancers associated with mutations in the KRAS gene are also provided.Type: GrantFiled: September 18, 2015Date of Patent: October 30, 2018Assignee: Araxes Pharma LLCInventors: Matthew Robert Janes, Matthew Peter Patricelli, Liansheng Li, Pingda Ren, Yi Liu
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Patent number: 10011600Abstract: Inhibitors of Ras protein, methods to modulate the activity of Ras protein, and methods of treatment of disorders mediated by Ras protein are provided. A method for regulating activity of a K-Ras, H-Ras or N-Ras mutant protein with a compound is described. Disorders that can be treated include cancer, such as hematological cancer, pancreatic cancer, MYH associated polyposis, colorectal cancer, or lung cancer.Type: GrantFiled: September 25, 2015Date of Patent: July 3, 2018Assignee: ARAXES PHARMA LLCInventors: Liansheng Li, Jun Feng, Yun Oliver Long, Pingda Ren, Yi Liu
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Patent number: 9988357Abstract: Methods for preparing compounds having the following structure (I): or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b and R4c, are as defined herein are provided. Related compounds and methods for making the same are also provided.Type: GrantFiled: December 9, 2016Date of Patent: June 5, 2018Assignee: Araxes Pharma LLCInventors: Neelakandha S. Mani, Brett D. Allison, Zachary S. Sales, Jimmy T. Liang, Xiaohu Deng, Liansheng Li, Yun Oliver Long, Yuan Liu, Pingda Ren
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Patent number: 9926267Abstract: 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: GrantFiled: November 5, 2015Date of Patent: March 27, 2018Assignee: Araxes Pharma LLCInventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
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Patent number: 9862701Abstract: 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, R2, R3a, R3b, R4a, R4b, G1, G2, L, m1, m2 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: GrantFiled: September 25, 2015Date of Patent: January 9, 2018Assignee: Araxes Pharma LLCInventors: Liansheng Li, Jun Feng, Pingda Ren, Yi Liu
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Patent number: 9840516Abstract: 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: GrantFiled: October 10, 2014Date of Patent: December 12, 2017Assignee: ARAXES PHARMA LLCInventors: Liansheng Li, Jun Feng, Tao Wu, Pingda Ren, Yi Liu, Yuan Liu, Yun Oliver Long
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Patent number: 9810690Abstract: Provided herein are compositions, reactions mixtures, mutant Ras proteins, kits, substrates, and systems for selecting a Ras antagonist, as well as methods of using the same.Type: GrantFiled: November 2, 2016Date of Patent: November 7, 2017Assignee: ARAXES PHARMA LLCInventors: Matthew P. Patricelli, Ulf Peters, Liansheng Li, Pingda Ren, Yi Liu