1032903-66-4

Upstream product

• 1692-15-5 4-pyridylboronic acid 
• 452-73-3 2-chloro-4-fluorotoluene 
• 1032903-62-0 4-[2-methyl-4-nitro-5-(propan-2-yloxy)phenyl]pyridine 
• 1032903-50-6 1-chloro-2-methyl-4-nitro-5-(propan-2-yloxy)benzene 
• 112108-73-3 1-chloro-5-fluoro-2-methyl-4-nitrobenzene 
• 1032903-65-3 4-(5-isopropoxy-2-methyl-4-nitrophenyl)-1-methyl-pyridinium iodide 

Downstream Products

• 1445895-01-1 5-chloro-N₂-(2-isopropoxy-5-methyl-4-(1-methylpiperidin-4-yl)phenyl)-N₄-(2-(isopropylsulfonyl)phenyl)pyridine-2,4-diamine 
• 1445894-99-4 4-bromo-5-chloro-N-(2-isopropoxy-5-methyl-4-(1-methylpiperidin-4-yl)phenyl)pyridin-2-amine 
• 1032902-87-6 C₃₁H₃₈N₆O₃S 
• 1032902-58-1 C₃₄H₄₃N₅O₄S 
• 1032902-57-0 C₃₃H₄₁N₅O₃S 
• 1125592-33-7 C₃₂H₄₁N₅O₃S 
• 1190399-79-1 C₃₀H₄₀N₈O₃S 
• 1190115-51-5 N₂-(2-isopropoxy-5-methyl-4-(1-methylpiperidin-4-yl)phenyl)-N₄-(2-(isopropylsulfonyl)phenyl)pyrazolo[1,5-a][1,3,5]triazine-2,4-diamine 

Relevant academic research and scientific papers

Novel sulfinyl anilino pyrimidine derivative and application thereof in preparation of antitumor drugs

The invention relates to the field of medicines. A novel sulfinyl anilino pyrimidine derivative is disclosed, and the structural formula of the novel sulfinyl anilino pyrimidine derivative is as shown in the specification. Compared with an existing L858R/T790M inhibitor and EGFR / ALK double-target-target reference substance, the aniline-based pyrimidine derivative containing the sulfoxide group has better antitumor H 1975 activity compared with ALK the prior art BaF3 inhibitor and the EGFR/ALK double ALK-target reference substance. As proved by human liver microsomal experiments, the aniline-based pyrimidine derivatives containing the sulfoxide group in the invention are compared with the existing anisyl-containing anilino pyrimidine derivatives. There is a great increase in stability.

ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF

An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro- N 2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)- N 4-(2-(isopropylsulfonyl) phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials

The synthesis, preclinical profile, and in vivo efficacy in rat xenograft models of the novel and selective anaplastic lymphoma kinase inhibitor 15b (LDK378) are described. In this initial report, preliminary structure-activity relationships (SARs) are described as well as the rational design strategy employed to overcome the development deficiencies of the first generation ALK inhibitor 4 (TAE684). Compound 15b is currently in phase 1 and phase 2 clinical trials with substantial antitumor activity being observed in ALK-positive cancer patients.

COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS

The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.