1229457-91-3

Upstream product

• 756520-66-8 1-(2,6-dichloro-3-fluorophenyl)ethanol 
• 124-63-0 methanesulfonyl chloride 
• 290835-85-7 2',6'-dichloro-3'-fluoroacetophenone 

Downstream Products

• 1229457-92-4 6-bromo-1-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-1H-pyrrolo[3,2-b]pyridine 
• 877397-71-2 (R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethyoxyl)-2-aminopyridine 
• 756520-67-9 (±)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine 
• 756521-08-1 (±)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-2-nitropyridine 

Relevant academic research and scientific papers

Discovery of 2-aminopyridines bearing a pyridone moiety as potent ALK inhibitors to overcome the crizotinib-resistant mutants

Despite the initial benefit demonstrated in clinical setting with ALK inhibitors, the challenging resistant mutants (F1174L, L1196M and G1202R) invariably developed. In this work, a series of 2-aminopyridine derivatives were designed and synthesized by C-5 position incorporation of a 2-pyridone moiety and bioisosteric replacement of the C-3 position linkers. Optimization of the 2-aminopyridine derivatives led to the identification of hit 18d displaying a significant growth inhibition against a variety of ALK-addicted cancer cells. Especially in the case of ALK-positive Karpas-299 cell, 18d exhibited excellent anti-proliferative potency with an IC50 value of about 40 nM. Moreover, 18d demonstrated encouraging activities against wild-type ALK (19 nM), ROS1 (2.3 nM) as well as challenging crizotinib-resistant ALKL1196M and ALKG1202R mutants with IC50 values of 45 nM and 22 nM, respectively. Additionally flow cytometric analysis indicates that 18d inhibited Karpas-299 cell viability via G1 phase arrest. Taken together, this work provided a promising ALK inhibitor to circumvent the clinical crizotinib-resistant mutants.

As c - Met inhibitors of amino aromatic heterocyclic compound and its preparation method

The invention relates to an amino heterocyclic aromatic compound serving as a c-Met inhibitor, and a preparation method thereof, and in particular relates to a compound in the formula (I) in the specification and a pharmaceutically acceptable salt, prodru

Pyrazolopyridine derivative anti-tumor compound and preparation method and application thereof

The invention provides a pyrazolopyridine derivative anti-tumor compound with the excellent anti-tumor activity. The anti-tumor compound is shown by the formula I, wherein Y represents halogen, X represents -NHX2 or amino acid residues or the formula shown in the specification, and the definitions of R1, R2 and X2 are the same as those in the specification. The invention further provides a preparation method of the anti-tumor agent shown in the formula I and application of the pyrazolopyridine derivative anti-tumor compound in anti-tumor drugs of the lung cancer, the colon cancer and the ovarian cancer.

Method for preparing Crizotinib chiral intermediate

The invention relates to a method for preparing a Crizotinib chiral intermediate, which belongs to the field of medicine synthesis. The preparation method of the intermediate (1) is characterized in that chiral organic acidity is taken as a resolving agen

Synthesis and biological evaluation of 2-amino-5-aryl-3-benzylthiopyridine scaffold based potent c-Met inhibitors

A series of 2-amino-N-benzylpyridine-3-carboxnamides, 2-amino-N- benzylpyridine-3-sulfonamides and 2-amino-3-benzylthiopyridines against c-Met were designed by means of bioisosteric replacement and docking analysis. Optimization of the 2-amino-3-benzylthiopyridine scaffold led to the identification of compound (R)-10b displaying c-Met inhibition with an IC 50 up to 7.7 nM. In the cytotoxic evaluation, compound (R)-10b effectively inhibited the proliferation of c-Met addictive human cancer cell lines (IC50 from 0.19 to 0.71 μM) and c-Met activation-mediated cell metastasis. At a dose of 100 mg/Kg, (R)-10b evidently inhibited tumor growth (45%) in NIH-3T3/TPR-Met xenograft model. Of note, (R)-10b could overcome c-Met-activation mediated gefitinib-resistance, which indicated its potential use for drug combination. Taken together, 2-amino-3-benzylthiopyridine scaffold was first disclosed and exhibited promising pharmacological profiles against c-Met, which left room for further exploration.

Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors

A series of 2-aminopyridine-3-carboxamide derivatives against c-Met were designed and synthesized by employing bioisosteric replacement of heterocyclic moieties with the amide bond. The structure-activity relationship (SAR) at various positions of the sca

AZAINDOLE DERIVATIVES AS KINASE INHIBITORS

This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.