160358-08-7

Upstream product

• 85118-01-0 alpha-bromo-3,4-difluorotoluene 
• 328083-90-5 carbamic acid, [1-[(3,4-difluorophenyl)methyl]-4-piperidinyl]-, 1,1-dimethylethyl ester 
• 73874-95-0 (piperidin-4-yl)carbamic acid tert-butyl ester 
• 698-80-6 4-(chloromethyl)-1,2-difluorobenzene 
• 380424-03-3 1-(3,4-difluoro-benzyl)-piperidine-4-carboxylic acid amide 

Downstream Products

• 1073635-52-5 5-[1-(3,4-difluoro-benzyl)-piperidin-4-ylamino]-[1,3,4]thiadiazole-2-carbonitrile 
• 380425-95-6 2-chloro-6-[4-[1-(3,4-difluorobenzyl)]piperidinylamino]-9-cyclopentylpurine 

Relevant academic research and scientific papers

Rational Design and Multibiological Profiling of Novel Donepezil-Trolox Hybrids against Alzheimer's Disease, with Cholinergic, Antioxidant, Neuroprotective, and Cognition Enhancing Properties

A novel series of donepezil-trolox hybrids were designed, synthesized, and evaluated as multifunctional ligands against Alzheimer's disease (AD). Biological assays showed that these derivatives possessed moderate to good inhibitory activities against acetylcholinesterase (AChE) and monoamine oxidase B (MAO-B) as well as remarkable antioxidant effects. The optimal compound 6d exhibited balanced functions with good inhibition against hAChE (IC50 = 0.54 μM) and hMAO-B (IC50 = 4.3 μM), significant antioxidant activity (41.33 μM IC50 by DPPH method, 1.72 and 1.79 trolox equivalent by ABTS and ORAC methods), excellent copper chelation, and Aβ1-42 aggregation inhibition effect. Furthermore, cellular tests indicated that 6d has very low toxicity and is capable of combating oxidative toxin (H2O2, rotenone, and oligomycin-A) induced neurotoxicity. Most importantly, oral administration of 6d demonstrated notable improvements on cognition and spatial memory against scopolamine-induced acute memory deficit as well as d-galactose (d-gal) and AlCl3 induced chronic oxidative stress in a mouse model without acute toxicity and hepatotoxicity. In summary, both in vitro and in vivo results suggested that 6d is a valuable candidate for the development of a safe and effective anti-Alzheimer's drug.

2-PHENYL-3H-IMIDAZO[4,5-B]PYRIDINE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN TYROSINE KINASE ROR1 ACTIVITY

A compound of formula (I′) or (I′′) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of mammalian kinase enzyme activity, including ROR1 tyrosine kinase activity and may be used in the treatment of disorders associated with such activity.

THIA(DIA)ZOLES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS

The present invention relates to [1- (benzyl) -piperidin-4-yl] -( [1, 3,4] thiadiazol-2-yl) - amine and [1- (benzyl) -piperidin-4-yl] - (thiazol-2-yl) -amine derivatives of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.

NOVEL 1 -BENZYL-4-PIPERIDINAMINES THAT ARE USEFUL IN THE TREATMENT OF COPD AND ASTHMA

The invention provides 1 -benzyl- 4 -piperidinamines of the general formula (I), processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are useful in the treatment of respiratory diseses such a

The design and synthesis of purine inhibitors of CDK2. III

Cyclin-dependent kinases (CDKs) belong to a class of enzymes that control the ability of a cell to enter into and proceed through the cell division cycle. Using purine as a scaffold, we have synthesized a number of nanomolar inhibitors of CDK-2/cyclin E. In this report, the synthesis of a series of piperidine-substituted purine analogs will be presented, as well as some of their in vitro and in vivo biological effects.