1638281-44-3

Upstream product

• 814-68-6 acryloyl chloride 
• 603-76-9 1-methylindole 
• 1032452-86-0 2-chloro-4-(1'-methyl-1H-indol-3-yl)pyrimidine 
• 450-91-9 4-fluoro-2-methoxyaniline 
• 1075705-01-9 4-fluoro-2-methoxy-5-nitro-phenylamine 
• 1421372-94-2 N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indole-3-yl)-pyrimidine-2-amine 
• 625-36-5 2-chloropropionyl chloride 
• 945016-63-7 3-(2-chloro-pyrimidin-4-yl)-1H-indole 

Relevant academic research and scientific papers

Deuterated pyrimidine compound, preparation method, pharmaceutical composition, preparation and application

The invention provides a deuterated pyrazolopyrimidine compound, pharmaceutically acceptable salt, stereoisomer, a prodrug molecule or a solvate thereof, a preparation method of the deuterated pyrazolopyrimidine compound, a pharmaceutical composition, a preparation and application. The compound or salt or a pharmaceutical composition and a pharmaceutical preparation thereof have an inhibitory effect on variation forms of EGFR (Epidermal Growth Factor Receptor) protease; production of multiple tumor cells can be effectively inhibited, and the deuterated pyrazolopyrimidine compound can be used for preparing anti-tumor medicines and the like; compared with AZD9291, the compound has the advantages that concentration and stability of the medicine in blood can be improved, so that the use dosageof the medicine can be reduced, and the toxic and side effects of the medicine are reduced.

[(Indole -3 - yl) pyrimidine -2 - yl] amino haloalkylpropanamide -2 - enamide derivatives and salts, preparation method, application

The invention provides a [(indole-3-yl)pyrimidine-2-yl]aminophenylpropyl-2-eneamide derivative and its salt, a preparation method of the derivative, and application of the derivative and the salt. The [(indole-3-yl)pyrimidine-2-yl]aminophenylpropyl-2-eneamide derivative has a structure shown in the formula I below. Deuterium-carbon bonds in the derivative enable the derivative to decompose slowly in a human body, a medicament of the derivative has a longer half-life period and a higher concentration in blood, the dosage of the medicament is finally reduced, and toxic and side effects of the medicament are decreased. Experiments show that compared with AZD 9291 mesylates, AZD 929-D9 mesylate of the deuterium-substituted derivative has Cmax which is 1.32 times as high as that of AZD 9291, exposed dose 1.41 times as high as that of AZD 9291, and elimination half-life 1.31 times as long as that of AZD 9291.

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

The invention discloses a compound as shown in a formula (I) or pharmaceutically acceptable salt thereof, a method for preparing the compound as shown in the formula (I) or pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the compound as shown in the formula (I) or pharmaceutically acceptable salt thereof, and an application of the compound as shown in the formula (I) or pharmaceutically acceptable salt thereof (as shown in the specification), wherein R1 to R7 are as defined in the invention.

DEUTERATED COMPOUNDS FOR TREATING CANCER AND RELATED DISEASES AND CONDITIONS, AND COMPOSITIONS AND METHODS THEREOF

The invention provides novel chemical compounds useful for treating cancer or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.

2-(2,4,5-SUBSTITUTED ANILINE) PYRIMIDINE DERIVATIVE, PHARMACEUTICAL COMPOSITION AND USE THEREOF

Disclosed are a 2-(2,4,5-substituted aniline) pyrimidine derivative, a pharmaceutical composition and a use thereof. The pharmaceutical composition comprises a therapeutically effective amount of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. Also disclosed is a use of the 2-(2,4,5-substituted aniline) pyrimidine derivative, a solvate, or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating cancers. The compounds of the present invention have a relatively high solubility in water and a relatively high permeability, and/or a relatively low binding ability to plasma proteins, and at the same time have a relatively low toxicity characteristic and a relatively high anti-tumor activity.

Pentadeuteropyridine compounds, and preparation method, pharmaceutical compositions and uses thereof

The invention relates to pentadeuteropyridine compounds represented by the following formula (I) and pharmaceutically acceptable salts, stereoisomers, prodrugs and solvates thereof, and a preparation method, pharmaceutical compositions and uses thereof. The compounds can generate an inhibitory effect on variation forms of epidermal growth factor receptor (EGFR) protein kinase, thereby effectively inhibiting the growth of a variety of tumor cells; the compounds can be used for preparation of antitumor drugs, are used for treatment or prevention of a plenty of different cancers, and moreover, can overcome the drug resistance induced by conventional drugs gefitinib, erlotinib and other first-generation EGFR inhibitors. More specifically, the compounds can be used for preparation of drugs for treatment or prevention of diseases, obstacles, disorders or illness conditions mediated by certain variation-form epidermal growth factor receptors (such as L858R activated mutants, Exon19 deletion activated mutants, and T790M resistance mutants).