1926172-50-0Relevant articles and documents
INHIBITORS OF KRAS G12C PROTEIN AND USES THEREOF
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Paragraph 00378; 00379, (2021/12/28)
Provided are novel compounds useful as inhibitors of the KRAS protein, as well as pharmaceutical compositions comprising these compounds and methods of treatment by administration of these compounds or the pharmaceutical compositions.
Pyrimidine derivative and application thereof in medicines
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Paragraph 0651-0656, (2021/07/21)
The invention discloses a pyrimidine derivative and application thereof in medicines, and particularly relates to a novel pyrimidine derivative and a pharmaceutical composition containing the compound. The invention also relates to a method for preparing the compound and the pharmaceutical composition, and application of the compound and the pharmaceutical composition in preparation of drugs for treating KRAS G12C-mediated diseases and/or symptoms, especially in preparation of drugs for treating cancers.
Kras-G12C inhibitor heterocyclic compounds
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Paragraph 0513-0519, (2021/06/23)
The invention relates to Kras-G12C inhibitor heterocyclic compounds represented by formula I, a preparation method thereof, and application of the Kras-G12C inhibitor heterocyclic compounds in prevention and treatment of tumor diseases such as lung cancer, colorectal cancer and pancreatic cancer. In the preparation process, the compounds of the general formula I are obtained through a series of reactions such as SN2 reaction, protection, coupling reaction, deprotection, condensation reaction and the like.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0214, (2021/12/28)
The present disclosure relates to inhibitors of one or more isoforms of RAS, such as inhibitors of one or more of KRAS, HRAS and NRAS, or mutants thereof, such as G12D, G12V, G13D or G12C mutants thereof. Therapeutic methods of treating conditions and diseases using these inhibitors are also provided.
HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 0267, (2021/12/28)
The present disclosure relates to inhibitors of one or more isoforms of RAS, such as inhibitors of one or more of KRAS, HRAS and NRAS, or mutants thereof, such as G12D, G12V, G13D or G12C mutants thereof. Therapeutic methods of treating conditions and dis
KRAS G12C INHIBITORS
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Paragraph 0282, (2020/03/23)
The present invention relates to compounds that, inhibit KRas G12C, In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Benzopyridone heterocyclic compound and application thereof
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Paragraph 0096; 0099; 0107-0109, (2020/08/18)
The invention relates to a benzopyridone heterocyclic compound and an application thereof. The compound is a compound represented by a formula I, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, or a tautomer thereof, or a hydrate thereof, or a solvate thereof, or a metabolite thereof, or a prodrug thereof, and R1, R2, R3, R4 and R5 and an A group are as defined in the specification. The compound disclosed by the invention can be used for preparing a medicine for treating and/or preventing cancers.
KRAS G12C INHIBITORS
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Paragraph 0278, (2020/07/25)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12CInhibitor for the Treatment of Cancer
Fell, Jay B.,Fischer, John P.,Baer, Brian R.,Blake, James F.,Bouhana, Karyn,Briere, David M.,Brown, Karin D.,Burgess, Laurence E.,Burns, Aaron C.,Burkard, Michael R.,Chiang, Harrah,Chicarelli, Mark J.,Cook, Adam W.,Gaudino, John J.,Hallin, Jill,Hanson, Lauren,Hartley, Dylan P.,Hicken, Erik J.,Hingorani, Gary P.,Hinklin, Ronald J.,Mejia, Macedonio J.,Olson, Peter,Otten, Jennifer N.,Rhodes, Susan P.,Rodriguez, Martha E.,Savechenkov, Pavel,Smith, Darin J.,Sudhakar, Niranjan,Sullivan, Francis X.,Tang, Tony P.,Vigers, Guy P.,Wollenberg, Lance,Christensen, James G.,Marx, Matthew A.
supporting information, p. 6679 - 6693 (2020/04/20)
Capping off an era marred by drug development failures and punctuated by waning interest and presumed intractability toward direct targeting of KRAS, new technologies and strategies are aiding in the target's resurgence. As previously reported, the tetrahydropyridopyrimidines were identified as irreversible covalent inhibitors of KRASG12C that bind in the switch-II pocket of KRAS and make a covalent bond to cysteine 12. Using structure-based drug design in conjunction with a focused in vitro absorption, distribution, metabolism and excretion screening approach, analogues were synthesized to increase the potency and reduce metabolic liabilities of this series. The discovery of the clinical development candidate MRTX849 as a potent, selective covalent inhibitor of KRASG12C is described.
KRAS G12C INHIBITORS
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Paragraph 0410-0411, (2019/05/24)
The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
