134697-63-5

Upstream product

• 100-52-7 benzaldehyde 
• 55-51-6 N,N-bis(2-chloro-ethyl)-benzenemethanamine 
• 530-93-8 1,2,3,4-tetrahydronaphthalen-2-one 

Downstream Products

• 134697-85-1 C₂₁H₂₄N₂O₂ 
• 134697-73-7 C₂₂H₂₇NO 
• 134697-87-3 C₂₁H₂₄ClN 
• 134697-75-9 C₂₂H₂₇N 
• 134697-81-7 C₂₂H₂₇N 
• 134697-83-9 1'-cyclohexylmethyl-3,4-dihydrospiro(naphthalene-1(2H),4'-piperidine) 
• 95417-67-7 L 687384 

Relevant academic research and scientific papers

Novel heterocyclic derivative capable of being used as SHP2 inhibitor

The invention relates to a novel heterocyclic derivative capable of being used as an SHP2 inhibitor, specifically relates to a compound shown by a formula I or pharmaceutically acceptable salts thereof, further relates to a use of the compound shown by the formula I or the pharmaceutically acceptable salts thereof and a pharmaceutical composition thereof in drug preparation, and particularly relates to a use in preparation of drugs for treatment, inhibition or prevention of diseases or discomforts mediated by SHP2 activity.

NOVEL HETEROCYCLIC DERIVATIVES USEFUL AS SHP2 INHIBITORS

This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.

Spiropiperidines as high-affinity, selective σ ligands

A variety of achiral conformationally restricted spirocyclic piperidines have been prepared in an attempt to investigate the functional role of the central σ recognition site. All the compounds possessed a lipophilic N- substituent incorporating either a tetralin, indan, or benzocycloheptane skeleton. Their in vitro affinity at the σ site was assessed in radioligand displacement experiments with guinea pig cerebellum homogenates using the σ- specific radioligand [3H]-N,N'-di-o-tolylguanidine ([3H]-DTG, [3H]-6). A study of the structure-activity relationships identified the N-butyl and N- dimethylallyl substituents as the optimum groups for high affinity and selectivity at the σ site (e.g., 3,4-dihydro-1'-(3-methylbut-2- enyl)spiro[1H-indene-1,4'-piperidine] (48), pIC50 = 8.9 vs [3H]-6 and greater than 10 000-fold selective over the dopamine D2 receptor). Such compounds are amongst the highest affinity σ ligands reported to date, with excellent selectivity over the dopamine D2 receptor, and may serve as a useful tool for exploring the physiological role of the σ site.