1421372-34-0

Upstream product

• 945016-63-7 3-(2-chloro-pyrimidin-4-yl)-1H-indole 
• 1075705-01-9 4-fluoro-2-methoxy-5-nitro-phenylamine 
• 450-91-9 4-fluoro-2-methoxyaniline 
• 120-72-9 indole 

Downstream Products

• 2129998-32-7 C₂₇H₂₅⁽²⁾H₆N₇O₂*CH₄O₃S 

Relevant academic research and scientific papers

Deuterated pyrimidine derivative and application thereof

The invention discloses a deuterated pyrimidine derivative and application thereof, and belongs to the field of medicines. The deuterated pyrimidine derivative and a pharmaceutically acceptable salt thereof have good activity of selectively inhibiting an

2 - (2,Anilino) pyrimidine compound and application thereof (by machine translation)

The invention relates to certain 2 - (2,anilino) pyrimidine compounds represented by the following formula I and application thereof. These compounds or salts thereof show a higher inhibition of EGFR than wild-type EGFR in the form of an activated or drug resistant mutant. Since the toxicity associated with the wild-type EGFR inhibition is reduced, it is expected that such a compound or salt thereof has excellent pharmacodynamic properties, higher metabolic stability, better blood-brain barrier permeability, and more suitable for use as a therapeutic agent, particularly for the treatment of cancer. , These compounds or salts thereof can be used to prepare EGFR-mediated diseases, in particular non-small cell lung cancer, for the treatment of certain mutated forms. (by machine translation)

Compound, containing conjugated dienamide structure, preparation method, pharmaceutical composition and application thereof

The invention relates to a compound containing a conjugated allene amide structure and a preparation method, a medicine composition and application thereof, in particular to a compound containing a conjugated allene amide structure shown in a formula (I), and a preparation method, a medicine composition and application thereof in preparation of an EGFR (epidermal growth factor receptor) inhibitoror a medicine for preventing and/or treating EGFR-related diseases, especially cancers. (The formula (I) is shown in the description.).

2-(2, 4, 5-substituted aniline) pyrimidine derivative

The invention relates to a 2-(2, 4, 5-substituted aniline) pyrimidine derivative, and more specifically discloses a compound represented by formula I or a pharmaceutically acceptable salt thereof, anda preparation method and applications of the compound represented by formula I and the pharmaceutically acceptable salt of the compound, wherein R1 to R9 are used for representing groups defined in the invention.

Indole-1-carbonate compound and preparation method and application thereof

The invention belongs to the field of medicine synthesis and specifically relates to indole-1-carbonate compound shown in a general formula (I), a pharmaceutically acceptable salt, a deuterium compound or a solvate of the indole-1-carbonate compound, a preparation method thereof and application thereof in preparing medicine for selectively inhibiting active EGFR resistance mutation T790M and activated mutation. The formula (I) is shown in the specification.

Phenylaminopyrimidine derivative used as ERK inhibitor

The invention specifically relates to a novel phenylaminopyrimidine derivative used as an ERK inhibitor and a pharmaceutically acceptable salt thereof, belonging to the field of medical chemistry. Theinvention specifically discloses a compound as shown in a formula I which is described in the specification and a pharmaceutically acceptable salt and a pharmaceutical composition thereof, and a method for applying the compound to treatment of diseases resulting from ERK inhibition.

2-(2,4,5-substituted aniline) pyrimidine derivative

Disclosed is a 2-(2,4,5-substituted aniline) pyrimidine derivative. Disclosed are a compound shown in the formula (I) or pharmaceutically-acceptable salt thereof, a preparation method of the compound shown in the formula (I) or the pharmaceutically-acceptable salt thereof, a pharmaceutical composition containing the compound shown in the formula (I) or the pharmaceutically-acceptable salt thereof, and an application of the compound shown in the formula (I) or the pharmaceutically-acceptable salt thereof. In the formula (I), R1 to R6 are defined as shown in the application.

EGFR INHIBITOR, AND PREPARATION AND APPLICATION THEREOF

A 4-substituted-2-(N-(5-substituted allyl amide)phenyl)amino)pyrimidine derivative as represented by formula (I), and a preparation and application thereof as an EGFR inhibitor. The compound has activity of inhibiting the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, may be used to treat diseases mediated alone or in part by EGFR mutant activity, and has a wide application in drugs preventing and treating cancers, particularly non-small cell lung cancer.

Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor

Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring sensitizing (or activating) mutations for a number of years. Despite encouraging clinical efficacy with these agents, in many patients resistance develops leading to disease progression. In most cases, this resistance is in the form of the T790M mutation. In addition, EGFR wild type receptor inhibition inherent with these agents can lead to dose limiting toxicities of rash and diarrhea. We describe herein the evolution of an early, mutant selective lead to the clinical candidate AZD9291, an irreversible inhibitor of both EGFR sensitizing (EGFRm+) and T790M resistance mutations with selectivity over the wild type form of the receptor. Following observations of significant tumor inhibition in preclinical models, the clinical candidate was administered clinically to patients with T790M positive EGFR-TKI resistant NSCLC and early efficacy has been observed, accompanied by an encouraging safety profile.

Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)

A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib. Our reported compounds also show selectivity over wild-type EGFR. Guided by molecular modeling, this series was evolved to target a cysteine residue in the ATP binding site via covalent bond formation and demonstrates high levels of activity in cellular models of the double mutant form of EGFR. In addition, these compounds show significant activity against the activating mutations, which gefitinib and erlotinib target and inhibition of which gives rise to their observed clinical efficacy. A glutathione (GSH)-based assay was used to measure thiol reactivity toward the electrophilic functionality of the inhibitor series, enabling both the identification of a suitable reactivity window for their potency and the development of a reactivity quantitative structure-property relationship (QSPR) to support design.