111627-46-4

Upstream product

• 767-00-0 4-cyanophenol 
• 109-70-6 1.3-chlorobromopropane 
• 147749-97-1 4-(3-hydroxypropoxy)benzonitrile 
• 107167-08-8 1-bromo-1-chloropropane 

Downstream Products

• 111626-37-0 4-[3-[4-[bis(4-fluorophenyl)methyl]-1-piperidinyl]propoxy]benzonitrile 
• 111626-36-9 4-[3-[4-[bis(4-fluorophenyl)hydroxymethyl]-1-piperidinyl]propoxy]benzonitrile 
• 596810-17-2 4-(3-(4-[3-(4-cyanophenoxy)propyl]-1-piperazinyl}propoxy)benzonitrile 
• 1158961-23-9 C₁₅H₁₈F₂N₂O 
• 596809-75-5 benzyl 4-[3-(4-cyanophenoxy)propyl]-5-oxo-1,4-diazepane-1-carboxylate 
• 82625-25-0 4-(3-chloropropoxy)benzaldehyde 

Relevant academic research and scientific papers

Design of the First-in-Class, Highly Potent Irreversible Inhibitor Targeting the Menin-MLL Protein–Protein Interaction

The structure-based design of M-525 as the first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction is presented. M-525 targets cellular menin protein at sub-nanomolar concentrations and achieves low nanomolar potencies in cell growth inhibition and in the suppression of MLL-regulated gene expression in MLL leukemia cells. M-525 demonstrates high cellular specificity over non-MLL leukemia cells and is more than 30 times more potent than its corresponding reversible inhibitors. Mass spectrometric analysis and co-crystal structure of M-525 in complex with menin firmly establish its mode of action. A single administration of M-525 effectively suppresses MLL-regulated gene expression in tumor tissue. An efficient procedure was developed to synthesize M-525. This study demonstrates that irreversible inhibition of menin may be a promising therapeutic strategy for MLL leukemia.

Fluorinated non-imidazole histamine H3 receptor antagonists

Fluorine substituents have become a widespread and important component in drug design and development. Here, the synthesis of fluorine containing compounds and some corresponding precursor molecules are presented for potential isotope labelling as well as their data obtained with in vitro and in vivo screenings. The compounds vary in the basic centres (piperidine or pyrrolidine) and are fluoro substituted in different positions of the basic alicyclic moiety. Pharmacological evaluation resulted in ligands with high affinities at hH3 receptor in the nanomolar and subnanomolar concentration range and some with high antagonist in vivo potencies.

Azabicyclic compounds, a process for their preparation and pharmaceutical compositions containing them.

A compound selected from those of formula (I): wherein m and n, which may be identical or different, each represent an integer from 0 to 2 inclusive, with the sum of the two integers being from 2 to 3 inclusive, p and q, which may be identical or differen

Design and synthesis of amidino-tyrosine derivatives as non-peptide fibrinogen receptor antagonists

The design, synthesis and antiaggregation activity of amidino-tyrosine derivatives based on Arg-Gly-Asp (RGD) tripepride sequence as non-peptide fibrinogen receptor antagonists is described. Optimization of the spacer and the substituent at the C-terminal is reported.

Arylalkylheterocyclic amines,N-substituted by aryloxyalkyl group in a method for allergy treatment

A method of inhibiting Type 1 allergic responses in a living animal body with substituted heterocyclic amines is disclosed wherein the active agents are expressed generally by the formula which includes certain known and certain known compounds: STR1 wherein P is zero, one or two; m is one to six inclusive; A is selected from hydrogen, hydroxy or cyano; d is zero or one; Q is --CH--, CH2 -- or STR2 n is zero or one and when Q is --CH-- and n is one, a double bond is formed with one of the adjacent carbons but not both at the same time, and when n and d are zero at the same time, a double bond is formed between the α carbon and a carbon of the central heterocyclic amine ring; Ar, D and R are selected from phenyl, substituted phenyl, pyridinyl, thienyl, furanyl or naphthyl and in addition, R may have the values benzyl, substituted benzyl, cycloalkyl or loweralkyl and D may additionally have the values: 2H-1-benzopyran-2-one,4-oxo-4H-1-benzopyran-2-carboxylic acid loweralkyl ester, 2,3-dihydro-4H-1-benzopyran-4-one, 1,4-benzodioxanloweralkyl-2-yl or 1,1'-biphenyl-4-yl and the pharmaceutically acceptable salts thereof.

Synthesis and Antiallergy Activity of 4-(Diarylhydroxymethyl)-1-piperidines and Structurally Related Compounds

A series of 4-(diarylhydroxymethyl)-1-piperidines was synthesized and evaluated for antiallergy activity.Several analogues had potent activity in the passive foot anaphylaxis (PFA) assay, an IgE-mediated model useful in the detection of compounds possessing antiallergic activity.In particular 1--1-piperidinyl>propoxy>-3-methoxyphenyl>ethanone (1, AHR-5333) was more potent than oxatomide and terfenadine in this assay.