69383-72-8

Upstream product

• 50-00-0 formaldehyd 
• 34231-22-6 [3-(aminomethyl)phenyl]methanol 
• 1129-28-8 3-methoxycarbonylbenzyl bromide 
• 124-40-3 dimethyl amine 
• 82072-22-8 3-hydroxymethylbenzyl bromide 
• 99-36-5 1-methoxycarbonyl-3-methylbenzene 
• 31719-77-4 3-chloromethylbenzoic acid 
• 155412-73-0 3-((dimethylamino)methyl)benzoic acid 
• 626-18-6 1,3-dimethanol benzene 
• 175464-51-4 3-(chloromethyl)-phenyl methanol 
• 4885-18-1 3-bromo-N,N-dimethylbenzylamine 
• 1877-71-0 benzene 1,3-dicarboxylic acid monomethyl ester 
• 89999-70-2 3-Dimethylaminomethyl-benzoic acid methyl ester 
• 69383-71-7 N,N-dimethylisophthalamic acid methyl ester 

Downstream Products

• 1400941-90-3 6-((3-((dimethylamino)methyl)benzyl)oxy)-9H-purin-2-amine 
• 80708-77-6 3-[(dimethylamino)methyl]-benzaldehyde 
• 69384-56-1 C₁₅H₂₄N₄O₂S 
• 69384-52-7 C₁₅H₂₃N₅S 
• 145832-35-5 3-acetoxymethyl-N,N,N-trimethylbenzenemethanaminium iodide 
• 78441-87-9 3-amino-4-{2-[(3-{dimethylaminomethyl}phenyl)methylthio]ethylamino}-1,2,5-thiadiazole 1-oxide 
• 69384-24-3 2-[[3-(N,N-Dimethylaminomethyl)phenyl]methylthio]ethanamine 

Relevant academic research and scientific papers

BIS-BENZIMIDAZOLE COMPOUNDS AND METHODS OF USING SAME

Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1 ), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.

OXABOROLE ESTERS AND USES THEREOF

The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.

TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE

The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.

Aromatic PCN palladium pincer complexes. Probing the hemilability through reactions with nucleophiles

A series of unsymmetrical PCN pincer ligands (1-(3-((di-tert-butylphosphino)methyl)phenyl)-N,N-dialkylmethanamine) were cyclometalated with palladium to generate a series of new PCN supported Pd(II) chloro complexes, (PCN)PdCl (4-6), where alkyl = methyl, ethyl, and n-propyl, which were fully characterized by NMR spectroscopy and X-ray crystallography. The N,N-dimethyl complex 4 reacts with methyl lithium to give the corresponding methyl and dimethyl complexes (PCN)PdMe (12) and Li[(PCN)PdMe2] (13), which could not be isolated but were characterized in solution. The substitution reactions of (PCN)PdCl (4-6) with iodide to form the corresponding iodo complexes (PCN)PdI (7-9) were investigated by use of UV-vis stopped-flow spectrophotometry. The experiments were performed in methanol over a temperature range from 293 to 325 K. The reactions are reversible and were shown to proceed exclusively via the solvento complex in two reversible consecutive steps. Activation parameters for both the forward and reverse reactions were determined, and they, together with reactivity trends, support an associative pathway. No displacement of the nitrogen donor was detected, and overall this points to a limited hemilability of the ligands on palladium.

Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents

Phenyl imidazolidin-2-one was introduced as the linker for novel HDAC inhibitors. A focused library of 20 compounds was designed and synthesized, among which eight compounds showed equivalent or higher potencies against HDAC1 as compared to vorinostat. In vitro antitumor activity assays in HCT-116, PC-3 and HL-60 cancer cells revealed six compounds with potent antitumor activities, and compound 1o showed 6- to 9-fold higher potencies compared to vorinostat. In an HCT-116 nude mice xenograft model, compound 1o displayed significant antitumor activity in both continuous and intermittent dosing schedules.

Design of a hypoxia-activated prodrug inhibitor of O6- alkylguanine-DNA alkyltransferase

The efficacy of agents that alkylate the O-6 position of guanine is inhibited by O6-alkylguanine-DNA alkyltransferase (AGT) which removes these lesions from the tumor DNA. To increase differential toxicity, inhibitors must selectively deplete AGT in tumors, while sparing normal tissues where this protein serves a protective function. A newly synthesized prodrug of the AGT inhibitor O6-benzylguanine (O6-BG) with an α,α-dimethyl-4-nitrobenzyloxycarbonyl moiety masking the essential 2-amino group has demonstrated the feasibility of targeting hypoxic regions that are unique to solid tumors, for drug delivery. However, these modifications resulted in greatly decreased solubility. Recently, new potent global AGT inhibitors with improved formulatability such as O6-[(3-aminomethyl) benzylguanine (1) have been developed. However, acetylamino (N-(3-(((2-amino-9H- purin-6-yl)oxy)methyl)benzyl)acetamide) (2) exhibits a pronounced decrease in activity. Thus, 1 would be inactivated by N-acetylation and probably N-glucuronidation. To combat potential conjugational inactivation while retaining favorable solubility, we synthesized 6-((3-((dimethylamino)methyl) benzyl)oxy)-9H-purin-2-amine (3) in which the 3-aminomethyl moiety is protected by methylation; and to impart tumor selectivity we synthesized 2-(4-nitrophenyl)propan-2-yl(6-((3-((dimethylamino)methyl)benzyl)oxy) -9H-purin-2-yl)carbamate (7), a hypoxia targeted prodrug of 3 utilizing an α,α-dimethyl-4-nitrobenzyloxycarbonyl moiety. Consistent with this design, 7 demonstrates both hypoxia selective conversion by EMT6 cells of 7 to 3 and hypoxic sensitization of AGT containing DU145 cells to the cytotoxic actions of laromustine, while exhibiting improved solubility.

Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation and structure-activity relationships. Part 2

The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl group

Protonation Susceptibility and Fragmentation Capability of Functional Groups in Chemical Ionization Mass Spectrometry of Simple Bifunctional Compounds. Semi-quantitative Interpretation of Spectra.

Positive-ion, methane-mediated chemical ionization mass spectra were measured for simple bifunctional aromatic compounds of the type m-XCH2C6H4CH2Y, where X = NH2 and N(CH3)2, and Y = OH and OCH3.Essentially only three peaks of ions, +, + and +, have appeared for each compound.Since the two functional groups XCH2- and YCH2- do not interact with each other after protonation or after fragmentation, they are assumed to be protonated and to undergo fragmentation independently.The relative protonation susceptibility and fraction of fragmentating + can be estimated for each functional group in these compounds.A semi-quantitative interpretation of the observed spectra is presented.

Modulation of cholinergic profile of acetylcholine through its cyclovinylogues

The o-. m- and p-acetoxymethyl-N,N,N-trimethylbenzenemethanaminium iodide (2a-c) as cyclovinilogues of acetylcholine are described. This structural modification allows to modulate the cholinergic activity of the natural neurotransmitter along the sequence

PHARMACOLOGICALLY ACTIVE AMINOALKYLPHENYL COMPOUNDS AND THEIR USE

Compounds of the general formula: STR1 and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in whichR 1 and R 2, which may be the same or different, represent hydrogen or lower alkyl, cycloalkyl, aralkyl or lower alkenyl groups, or lower alkyl groups interrupted by an oxygen atom or a group STR2 in which R 4 represents hydrogen or lower alkyl; or R 1 and R 2 may, together with the nitrogen atom to which they are attached form a heterocyclic ring which may contain the hetero functions--O--and STR3 R 3 represents hydrogen, lower alkyl, alkenyl or alkoxyalkyl; X represents--O--,--S--or--CH 2--or STR4 where R 5 is hydrogen or lower alkyl; Y represents =S, =O, =NR 6 or =CHR. sub.7 ;in which R 6 represents hydrogen, nitro, cyano, lower alkyl, aryl, arylsulphonyl or lower alkylsulphonyl; R 7 represents nitro, lower alkylsulphonyl or arylsulphonyl; m is an integer from 2 to 4 inclusive; n is zero, 1 or 2; and Alk denotes a straight or branched alkylene chain of 1 to 6 carbon atoms. The compounds have therapeutic activity.