130307-08-3

Usage

Uses

1-(4-Bromophenyl)-4-methylpiperazine is a useful research chemical.

InChI:InChI=1/C11H15BrN2/c1-13-6-8-14(9-7-13)11-4-2-10(12)3-5-11/h2-5H,6-9H2,1H3

Upstream product

• 66698-28-0 1-(4-bromophenyl)piperazine 
• 74-88-4 methyl iodide 
• 109-01-3 1-methyl-piperazine 
• 106-37-6 1.4-dibromobenzene 
• 50-00-0 formaldehyd 
• 51-75-2 nitrogen mustard 
• 106-40-1 4-bromo-aniline 
• 3074-43-9 1-methyl-4-phenylpiperazine 

Downstream Products

• 770706-25-7 4-(4-methyl-piperazin-1-yl)-benzenesulfinate 
• 1401625-26-0 (1R,2R)-methyl 1-((S)-2-(tert-butoxycarbonylamino)butanamido)-2-(4'-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropanecarboxylate 
• 1401625-27-1 (1S,2S)-methyl 1-((S)-2-(tert-butoxycarbonylamino)butanamido)-2-(4'-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropanecarboxylate 
• 1401625-28-2 tert-butyl (S)-1-((1R,2R)-1-carbamoyl-2-(4'(4-methylpiperazine-1-yl)biphenyl-4-yl)cyclopropylamino)-1-oxobutan-2-ylcarbamate 
• 1401625-29-3 tert-butyl (S)-1-((1S,2S)-1-carbamoyl-2-(4'(4-methylpiperazine-1-yl)biphenyl-4-yl)cyclopropylamino)-1-oxobutan-2-ylcarbamate 
• 1401625-30-6 tert-butyl (S)-1-((1R,2R)-1-cyano-2-(4'(4-methylpiperazine-1-yl)biphenyl-4-yl)cyclopropylamino)-1-oxobutan-2-ylcarbamate 
• 1401625-31-7 tert-butyl (S)-1-((1S,2S)-1-cyano-2-(4'(4-methylpiperazine-1-yl)biphenyl-4-yl)cyclopropylamino)-1-oxobutan-2-ylcarbamate 
• 1401624-42-7 (S)-2-amino-N-((1R,2R)-1-cyano-2-(4'-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropyl)butanamide 
• 1401624-43-8 (S)-2-amino-N-((1S,2S)-1-cyano-2-(4'-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropyl)butanamide 
• 1401625-55-5 (1R,2R)-methyl 1-((S)-2-(tert-butoxycarbonylamino)-3-(furan-2-yl)propanamido)-2-(4'-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropanecarboxylate 
• 1401625-56-6 (1S,2S)-methyl 1-((S)-2-(tert-butoxycarbonylamino)-3-(furan-2-yl)propanamido)-2-(4'-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropanecarboxylate 
• 1401625-57-7 tert-butyl (S)-1-((1R,2R)-1-carbamoyl-2(4-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropylamino)-3-(furan-2-yl)-1-oxopropan-2-ylcarbamate 
• 1401625-58-8 tert-butyl (S)-1-((1S,2S)-1-carbamoyl-2(4-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropylamino)-3-(furan-2-yl)-1-oxopropan-2-ylcarbamate 
• 1401625-59-9 tert-butyl (S)-1-((1R,2R)-1-cyano-2(4-(4-methylpiperazin-1-yl)biphenyl-4-yl)cyclopropylamino)-3-(furan-2-yl)-1-oxopropan-2-ylcarbamate 

Relevant academic research and scientific papers

COMPOUND SIMULTANEOUSLY INHIBITING LSD1 AND HDAC TARGETS AND APPLICATION THEREOF

A compound having a general structural formula as shown in Formula I: X-AB-Y (Formula I); in the above Formula I, X is selected from any one of -CO2H, -CONHZ, -CH=CH-CO2H, -CH=CH-CONHZ, wherein Z is selected from any one of substituted or unsubstituted C1-C12 alkyl, substituted or unsubstituted aryl, and hydroxyl; Y = -NR1R2, wherein NR1R2 is a substituted or unsubstituted 3- to 9-membered nitrogen-containing heterocycloalkyl; A and B are each independently selected from substituted or unsubstituted phenylene, substituted or unsubstituted azaphenylene. The compound or corresponding pharmaceutical salt thereof can inhibit LSD1 and HDAC target proteins at the same time, thus inhibit the proliferation of many kinds of tumor cells and have good antitumor effect.

Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs

Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).

Novel inhibitors of bacterial biofilms and related methods

Multi-cyclic compounds of chemical structure represented by formula given below and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.

PEPTIDASE INHIBITORS

Novel compounds of the formula (I) wherein R1, R2, D, A, B and X have the meanings defined herein, pharmaceutical compositions comprising them as active ingredient, as well as their use in medicine, in particular as peptidase inhibitors, more specifically

Inhibitors of bacterial biofilms and related methods

Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms.

PREPARATION AND USES OF 1,2,4-TRIAZOLO [1,5a] PYRIDINE DERIVATIVES

This application relates to compounds of the general Formula I and salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of treatment of hyperproliferative diseases or disorders.

KINASE INHIBITOR COMPOUNDS

Pyridine and pyridazine derivatives have unexpected drug properties as inhibitors of protein kinases and are useful in treating disorders related to abnormal protein kinase activities such as cancer.

Benzofurans as suppressors of neurodegeneration

A compound of the formula: wherein R1 and R2 each is H or a hydrocarbon group which may be substituted, or R1 and R2 form a 3- to 8-membered carbo or heterocyclic ring which may be substituted; R3 is H, a lower alkyl which may be substituted or an aromatic group which may be substituted; R4 is (1) an aromatic group which may be substituted, (2) an aliphatic hydrocarbon group substituted by an aromatic group which may be substituted, which hydrocarbon group may be further substituted or (3) an acyl; X and Y each is oxygen or sulfur which may be oxidized; and ring A is a benzene ring which may be further substituted, or a salt thereof, is useful for an agent for suppressing neurodegeneration.

Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERα-selective tetrahydroisoquinoline ligands

We disclose herein the discovery of estrogen receptor α (ERα) selective estrogen receptor modulators (SERMs) of the tetrahydroisoquinoline series that incorporate novel conformationally restricted side chains as replacement of the aminoethoxy residue typical of SERMs. Molecular modeling studies used in conjunction with the X-ray crystal structure of the ERα ligand binding domain (LBD) with raloxifene (7) suggested a diazadecaline moiety as a viable mimic of the SERM side chain. On the basis of this knowledge, the piperidinylethoxy moiety of our lead compound 60 was replaced by a diazadecaline subunit, providing the novel tetrahydroisoquinoline 29. In addition to exhibiting a binding affinity to ERα and antagonistic properties in the estrogen response element and MCF-7 assays similar to those of the parent compound 60, ligand 29 showed a reduced agonist behavior in the MCF-7 assay in the absence of 17β-estradiol. These data point toward the fact that 29 may have a potential for breast cancer prevention/treatment in vivo, a feature which is particularly attractive in the quest for safe alternatives to hormone replacement therapy. In a pharmacokinetic experiment carried out in rats, 29 displayed an interesting profile, with a bioavailability of 49%. We also disclose the X-ray crystal structure of 29 in complex with ERα-LBD, which reveals the preferred configurations of 29 at the two chiral centers and the details of its interactions with the receptor. Finally, our structure-activity relationship studies show that other analogues bearing constrained side chains retain potency and antagonist activity and that a 3-OH substituted phenyl D-ring increases the selectivity of a set of piperazinyl-containing ligands in favor of ERα over ERβ.

PROMOTERS FOR THE PROLIFERATION AND DIFFERENTIATION OF STEM CELLS AND/OR NEURON PRECURSOR CELLS

An agent for promoting the proliferation or differentiation of a stem cell and/or neural progenitor cell, comprising a compound represented by Formula: wherein each of R1 and R2 is H, a hydrocarbon group or a heterocyclic group, or taken together with the adjacent carbon atom to form a ring, R3 is H, a hydrocarbon group or a heterocyclic group, W is a group represented by Formula: wherein Ring A is an optionally substituted benzene ring, Ring B is an optionally substituted 5- to 7-membered nitrogen-containing heterocyclic ring, R4 is an acyl group having an aliphatic hydrocarbon group, which is substituted by an aromatic group and may have a further substitutent, or aromatic group, R5 is H, C1-6 alkyl or acyl, R4c is an aromatic group, an aliphatic hydrocarbon group or acyl, and X is O or S; Y is O, S or NH, Ring C is an optionally substituted benzene ring, or a salt or prodrug thereof is provided.