100875-69-2

Usage

Uses

Used in Pharmaceutical Industry:
4-[2-(4-METHYL-PIPERAZIN-1-YL)-ETHOXY]-BENZALDEHYDE serves as a crucial building block in the synthesis of an array of pharmaceuticals. Its unique structure allows it to be a key component in the development of new drugs, contributing to medicinal chemistry and drug discovery.
Used in Agrochemical Industry:
In the agrochemical sector, 4-[2-(4-METHYL-PIPERAZIN-1-YL)-ETHOXY]-BENZALDEHYDE is utilized in the creation of various agrochemicals. Its incorporation can lead to the development of innovative products designed to enhance crop protection and management.
Used in Organic Compounds Synthesis:
Beyond its applications in pharmaceuticals and agrochemicals, 4-[2-(4-METHYL-PIPERAZIN-1-YL)-ETHOXY]-BENZALDEHYDE is also used as a fundamental component in the synthesis of other organic compounds. Its versatility in chemical reactions makes it a valuable asset in organic chemistry.
Used in Medicinal Chemistry and Drug Discovery:
Due to its potential biological activities, 4-[2-(4-METHYL-PIPERAZIN-1-YL)-ETHOXY]-BENZALDEHYDE holds promise in the fields of medicinal chemistry and drug discovery. Researchers can leverage its properties to explore and develop new therapeutic agents and treatments.

Upstream product

• 39123-20-1 1-(2-chloroethyl)-4-methylpiperazine 
• 109-01-3 1-methyl-piperazine 
• 54373-15-8 4-(2-chloroethoxy)benzaldehyde 
• 123-08-0 4-hydroxy-benzaldehyde 
• 52191-15-8 4-(2-bromoethyloxy)benzaldehyde 

Downstream Products

• 103157-10-4 1-[2-(4-fluoren-9-ylidenemethyl-phenoxy)-ethyl]-4-methyl-piperazine 
• 1616111-02-4 (Z)-2-{4-[2-(4-methylpiperazin-1-yl)ethoxy]-benzylidene}-3-oxo-2,3-dihydrobenzofuran-7-carboxamide 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 4-anlinoquinazoline derivatives as EGFR inhibitors with the potential to inhibit the gefitinib-resistant nonsmall cell lung cancers

A series of quinazoline derivatives with benzylidene hydrazine carboxamide were designed and synthesised as EGFR inhibitors. Most compounds exhibited exceptional anti-proliferative activity against A549, HepG2, MCF-7 and H1975 cells. Furthermore, six compounds demonstrated excellent inhibition activity against EGFRWT with the IC50 value both less than 2 nM. Among the six compounds, 44 exhibited the strongest activity (0.4 nM) and potently inhibited EGFRL858R/T790M (0.1 μM). Excitingly, the most potent compound 14 showed excellent enzyme inhibitory activity with 6.3 nM and 8.4 nM for both EGFRWT and EGFRT790M/L858R. The result of AO single staining and Annexin V/PI staining showed that the compound 14 and 44 could induce remarkable apoptosis of A549 cells. The compound 14 arrested the cell cycle at the S phase and compound 44 arrested the cell cycle at the G0 phase in A549 cells. These preliminary results demonstrate that compound 14 and 44 may be promising lead compound-targeting EGFR.

Discovery and structure-activity relationship of novel 2,3- dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2 h)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 Inhibitors

Novel substituted 2,3-dihydrobenzofuran-7-carboxamide (DHBF-7-carboxamide) and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide (DHBF-3-one-7-carboxamide) derivatives were synthesized and evaluated as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1). A structure-based design strategy resulted in lead compound 3 (DHBF-7-carboxamide; IC50 = 9.45 μM). To facilitate synthetically feasible derivatives, an alternative core was designed, DHBF-3-one-7-carboxamide (36, IC50 = 16.2 μM). The electrophilic 2-position of this scaffold was accessible for extended modifications. Substituted benzylidene derivatives at the 2-position were found to be the most potent, with 3′,4′-dihydroxybenzylidene 58 (IC50 = 0.531 μM) showing a 30-fold improvement in potency. Various heterocycles attached at the 4′-hydroxyl/4′-amino of the benzylidene moiety resulted in significant improvement in inhibition of PARP-1 activity (e.g., compounds 66-68, 70, 72, and 73; IC50 values from 0.718 to 0.079 μM). Compound 66 showed selective cytotoxicity in BRCA2-deficient DT40 cells. Crystal structures of three inhibitors (compounds (-)-13c, 59, and 65) bound to a multidomain PARP-1 structure were obtained, providing insights into further development of these inhibitors.

IMIDAZO [4, 5 - B] PYRIDINE DERIVATIVES AS ALK AND JAK MODULATORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS

This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.

SELECTIVE ESTROGEN RECEPTOR MODULATORS

The invention provides compounds of Formula (I) : wherein R1 is hydrogen, OH, halo, -CN, -NO2, -N=0, -NHOQ2, -OQ2, -SOQ2, -SO2Q2, -SON(Q2)2, - SO2N(Q2)2, -N(Q2)2, -C(O)OQ2, -C(O)Q2, -C(O)N(Q2)2, -C(=NQ2)NQ2, -NQ2C(=NQ2)NQ2, - C(O)N(Q2)(OQ2), -N(Q2)C(O)-Q2, -N(Q2)C(O)N(Q2)2, -N(Q2)C(O)O-Q2, -N(Q2)SO2Q2, -N(Q2)SOQ2, aliphatic, alkoxy, cycloaliphatic, aryl, arylalkyl, heterocyclic, or heteroaryl ring, each aliphatic, alkoxy, cycloaliphatic, aryl, arylalkyl, heterocyclic, and heteroaryl ring optionally including 1-3 substituents independently selected Q3; R2 and R3 are each independently hydrogen, OH, oxo, aliphatic, cycloaliphatic, heterocycloaliphatic, aryl, or heteroaryl, optionally substituted with 1-3 of Q1 or Q2; X is a branched or straight C1-12 aliphatic chain wherein up to two carbon units are optionally and independently replaced by -C(Q1)2-, -C(Q2)2-, CHQ1, CHQ2-, -CO-, -CS-, -CONQ2, -CO2-, -OCO-, -NQ2-, -NQ2CO2-, - O-, -NQ2CONQ2-, -OCONQ2-, -NQ2CO-, -S-, -SO-, -SO2-, -SO2NQ2-, -NQ2SO2-, or -NQ2SO2NQ2-; G and G1 are each independently a branched or straight C1-2 aliphatic chain, or heterocycloalkyl, wherein up to two carbon units are optionally and independently replaced by -C(Q1)2-, -C(Q2)2-, CHQ1, CHQ2-, -CO-, - CS-, -CONQ2, -CO2-, -OCO-, -NQ2-, -NQ2CO2-, -O-, -NQ2CONQ2-, -OCONQ2-, -NQ2CO-, -S-, -SO-, - SO2-, -SO2NQ2-, -NQ2SO2-, or -NQ2SO2NQ2-, and pharmaceutically acceptable salts, solvates or prodaigs thereof, as well as methods of treating estrogen receptor mediated diseases and disorders using the compounds of Formula (I).

4,6-diarylpyrimidine derivatives and salts thereof

Described are a 4,6-diarylpyrimidine derivative represented by the following formula (1): STR1 wherein R represents a heterocyclic ring which may be substituted by one to four lower alkyl groups or an amino group and Ar represents a phenyl, naphthyl or ar