791577-47-4

Usage

Chemical structure

A piperidine ring with a methyl group at the 1 position and a 4-(4-nitrophenoxy) substitution at the 4 position.

Common uses

Development of pharmaceutical drugs in medicinal chemistry.

Potential biological activity

Dopamine receptor antagonist, antipsychotic and antihistaminic properties.

Organic synthesis

Used as a starting material for the preparation of various chemical compounds with diverse pharmacological properties.

Upstream product

• 106-52-5 N-methyl-4-hydroxypiperidine 
• 100-02-7 4-nitro-phenol 
• 1972-28-7 diethylazodicarboxylate 
• 350-46-9 4-Fluoronitrobenzene 

Downstream Products

• 358789-72-7 4-(1-methylpiperidin-4-yloxy)benzenamine 
• 857953-11-8 acetic acid-[4-(1-methyl-[4]piperidyloxy)-anilide] 

Relevant academic research and scientific papers

Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors

In present study, we described the synthesis and biological evaluation of a new class of EGFR inhibitors containing 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine scaffold. Thirty-one compounds were synthesized. Among them, compound C9 displayed the IC50 of 29.4 nM against HCC827 cell line and 1.9 nM against EGFRL858R. Compound C12 showed moderate inhibitory activity against EGFRL858R/T790M/C797S (IC50 = 114 nM). Western bolt assay suggested that compound C9 significantly inhibited EGFR phosphorylation. In vivo test, compound C9 remarkably exhibited inhibitory effect on tumor growth at 5.0 mg/kg by oral administration in established nude mouse HCC827 xenograft model. These results indicate that the 2,9-disubstituted 8-phenylsulfinyl/phenylsulfinyl-9H-purine derivatives can act as potent EGFR(L858R) inhibitors and effective anticancer agents. Additionally, optimization of compound C12 may result in discovering the fourth-generation EGFR-TKIs.

INHIBITORS OF BRUTON'S TYROSINE KINASE

Disclosed herein are reversible and irreversible inhibitors of Bruton's tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

INDOLINONE DERIVATIVES AND THEIR USE IN TREATING DISEASE-STATES SUCH AS CANCER

The present invention encompasses compounds of general formula (1) wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.

2,4-Di(hetero-)arylamino(-oxy)-5-substituted pyrimidines as antineoplastic agents

Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.