1421373-32-1

Basic information

• Product Name: N₁-(4-(1H-indol-3-yl)pyrimidin-2-yl)-N₄-(2-(dimethylamino)ethyl)-2-methoxy-N₄-methyl-5-nitrobenzene-1,4-diamine
• Synonyms: N₁-(4-(1H-indol-3-yl)pyrimidin-2-yl)-N₄-(2-(dimethylamino)ethyl)-2-methoxy-N₄-methyl-5-nitrobenzene-1,4-diamine
• CAS NO: 1421373-32-1
• Molecular Weight: 461.523
• Mol File: 1421373-32-1.mol

Chemical Properties

• CAS DataBase Reference: N₁-(4-(1H-indol-3-yl)pyrimidin-2-yl)-N₄-(2-(dimethylamino)ethyl)-2-methoxy-N₄-methyl-5-nitrobenzene-1,4-diamine(CAS DataBase Reference)
• NIST Chemistry Reference: N₁-(4-(1H-indol-3-yl)pyrimidin-2-yl)-N₄-(2-(dimethylamino)ethyl)-2-methoxy-N₄-methyl-5-nitrobenzene-1,4-diamine(1421373-32-1)
• EPA Substance Registry System: N₁-(4-(1H-indol-3-yl)pyrimidin-2-yl)-N₄-(2-(dimethylamino)ethyl)-2-methoxy-N₄-methyl-5-nitrobenzene-1,4-diamine(1421373-32-1)

Safety Data

• Hazardous Substances Data: 1421373-32-1(Hazardous Substances Data)

Upstream product

• 450-91-9 4-fluoro-2-methoxyaniline 
• 120-72-9 indole 
• 945016-63-7 3-(2-chloro-pyrimidin-4-yl)-1H-indole 
• 1421372-34-0 N- (4-fluoro-2-methoxy-5-nitrophenyl)-4-(1H-indol-3-yl)pyrimidin-2-amine 
• 142-25-6 N,N',N'-trimethylenediamine 
• 1075705-01-9 4-fluoro-2-methoxy-5-nitro-phenylamine 

Downstream Products

• 1421373-31-0 N⁴-(4-(1H-indol-3-yl)pyrimidin-2-yl)-N¹-(2-(dimethylamino)ethyl)-5-methoxy-N¹-methylbenzene-1,2,4-triamine 
• 1421373-98-9 N-[2-[2-(dimethylamino)ethyl-methylamino]-5-[[4-(1H-indol-3-yl)pyrimidin-2-yl]amino]-4-methoxyphenyl]prop-2-enamide 

Relevant articles and documents

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,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)

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.

2 - (2, 4, 5 - SUBSTITUTED -ANILINO) PYRIMIDINE DERIVATIVES AS EGFR MODULATORS USEFUL FOR TREATING CANCER

The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.