92040-00-1

Upstream product

• 20691-92-3 1-methylpiperidine-4-carbonitrile 
• 107-06-2 1,2-dichloro-ethane 
• 1623-99-0 phenyl sodium 
• 71-43-2 benzene 
• 1557-31-9 N-methyl-4-benzylpiperidine 
• 64-17-5 ethanol 
• 60-29-7 diethyl ether 
• 107054-93-3 (4-chloro-1-methyl-[4]piperidyl)-phenyl ketone 
• 50-00-0 formaldehyd 
• 37586-22-4 4-benzoylpiperidine 
• 59084-16-1 1-acetylpiperidine-4-carbonyl chloride 
• 25503-90-6 1-acetyl-piperidine-4-carboxylic acid 
• 39546-32-2 4-carboxamidopiperidine 
• 38081-60-6 phenyl-piperidin-4-yl-methanol 

Downstream Products

• 875229-63-3 1-(1-methyl-[4]piperidyl)-1-phenyl-propan-1-ol 
• 6071-92-7 VUF 4589 
• 872816-82-5 (3-chloro-phenyl)-(1-methyl-[4]piperidyl)-phenyl-methanol 
• 92196-29-7 (1-methylpiperidin-4-yl)(phenyl)methanol 
• 872830-04-1 4-(3-chloro-benzhydrylidene)-1-methyl-piperidine 
• 878162-23-3 tert-butyl 4-[cyano(1-methylpiperidin-4-yl)phenylmethyl]piperazine-1-carboxylate 

Relevant academic research and scientific papers

Harnessing the Role of HDAC6 in Idiopathic Pulmonary Fibrosis: Design, Synthesis, Structural Analysis, and Biological Evaluation of Potent Inhibitors

Idiopathic pulmonary fibrosis (IPF) is an interstitial lung disease characterized by a progressive-fibrosing phenotype. IPF has been associated with aberrant HDAC activities confirmed by our immunohistochemistry studies on HDAC6 overexpression in IPF lung tissues. We herein developed a series of novelhHDAC6 inhibitors, having low inhibitory potency overhHDAC1 andhHDAC8, as potential pharmacological tools for IPF treatment. Their inhibitory potency was combined with lowin vitroandin vivotoxicity. Structural analysis of 6h and structure-activity relationship studies contributed to the optimization of the binding mode of the new molecules. The best-performing analogues were tested for their efficacy in inhibiting fibrotic sphere formation and cell viability, proving their capability in reverting the IPF phenotype. The efficacy of analogue 6h was also determined in a validated human lung model of TGF-β1-dependent fibrogenesis. The results highlighted in this manuscript may pave the way for the identification of first-in-class molecules for the treatment of IPF.

Iron-catalyzed oxyfunctionalization of aliphatic amines at remote benzylic C-H sites

We report the development of an iron-catalyzed method for the selective oxyfunctionalization of benzylic C(sp3)-H bonds in aliphatic amine substrates. This transformation is selective for benzylic C-H bonds that are remote (i.e., at least three carbons) from the amine functional group. High site selectivity is achieved by in situ protonation of the amine with trifluoroacetic acid, which deactivates more traditionally reactive C-H sites that are α to nitrogen. The scope and synthetic utility of this method are demonstrated via the synthesis and derivatization of a variety of amine-containing, biologically active molecules.

INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME

The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as T

KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME

The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.

Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors

A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC50 values in the range of 10-150 nM and selectivity over the L-type channels up to nearly 1200-fold. Orally administered compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain.

HETEROCYCLIC AMIDE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS

Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type or T-type calcium channel activity are disclosed. Specifically, a series of heterocyclic amides are disclosed of the general formula (I) where Z is N or CHNR2 and X is NR2, O, S, S=O or SO2. Among other definitions for R, R1, W and Y, the compounds of formula (1) are further characterized by at least one of W or Y being CR3Ar2 where Ar is an aromatic or heteroaromatic ring (for example, where W or Y is a benzhydryl moiety).

Urea derivatives as calcium channel blockers

Urea derivatives which comprise piperidine or piperazine rings and further substitution are effective in ameliorating conditions characterized by unwanted calcium ion channel activity.

Syntheses and Binding Studies of New [(Aryl)(aryloxy)methyl]piperidine Derivatives and Related Compounds as Potential Antidepressant Drugs with High Affinity for Serotonin (5-HT) and Norepinephrine (NE) Transporters

In a wide search program toward new, efficient, and fast-acting antidepressant drugs, we have prepared series of new compounds having an (aryl)(aryloxy)methyl moiety linked directly or through a methylene chain to different substituted and unsubstituted cycles (isoquinoline, piperazine, piperidine, tetrahydropyran, or cyclopentane). These compounds have been evaluated for their affinities for serotonin (5-HT) transporter (SERT) and 5-HT1A and 5-HT2A receptors. Racemic mixtures of 4-[(aryl)(aryloxy)methyl]piperidine derivatives showed much higher affinity values for SERT than fluoxetine and resulted in lack of affinity for 5-HT 1A and 5-HT2A receptors. Some of these racemic mixtures were resolved to their enantiomers and tested for binding to norepinephrine (NE) transporter (NET), dopamine (DA) transporter (DAT), and α2 receptor. Several of these enantiomers [(-)-15b, (-)-15j, (-)-15t, (+)-15u] displayed a dual binding profile with affinities for SERT and NET with K i i = 1.9 and 13.5 nM, respectively), and further pharmacological characterization is in progress for its evaluation as a antidepressant.