239073-94-0

Usage

Chemical class

Piperidine derivative

Structure

Contains a BOC (tert-butoxycarbonyl) protecting group

Functional groups

Hydroxymethyl and methoxy groups attached to the piperidine ring

Application

Potential intermediate in the synthesis of other organic compounds

Usage

Commonly used in pharmaceutical research and development

Purpose

Synthesis of drugs and bioactive molecules

Significance

Important for producing new pharmaceuticals with specific biological activities and properties

Upstream product

• 67-56-1 methanol 
• 147804-30-6 1-oxa-6-aza-spiro-[2.5]octane-6-caboxylic acid tert-butyl ester 
• 1345728-55-3 tert-butyl 4-[(benzyloxy)methyl]-4-methoxypiperidine-1-carboxylate 
• 1345728-48-4 tert-butyl 4-[(benzyloxy)methyl]-4-hydroxypiperidine-1-carboxylate 
• 1345728-54-2 tert-butyl 6-[(benzyloxy)methyl]-7-oxa-3-azabicyclo[4.1.0]heptane-3-carboxylate 
• 1345728-47-3 tert-butyl 4-[(benzyloxy)methyl]-3,6-dihydropyridine-1(2H)-carboxylate 
• 203663-26-7 t-butyl 4-(hydroxymethyl)-3,6-dihydropyridine-1(2H)-carboxylate 
• 6192-52-5 p-toluenesulfonic acid monohydrate 

Relevant academic research and scientific papers

Novel indirect AMP-activated protein kinase activators: Identification of a second-generation clinical candidate with improved physicochemical properties and reduced hERG inhibitory activity

This study reports the synthesis and evaluation of novel indirect AMP-activated protein kinase (AMPK) activators. The series of compounds selectively inhibited cell growth in several human breast cancer cell lines by activating AMPK. We performed back-up medicinal chemistry synthetic research on ASP4132, a previously reported as a compound for clinical development that acts as an indirect AMPK activator. This led to the successful identification of 4-({4-[5-({1-[(5-ethoxypyrazin-2-yl)methyl]-4-fluoropiperidin-4-yl}methoxy)-3-methylpyridine-2-carbonyl]piperazin-1-yl}methyl)benzonitrile succinate (27b), a potent, highly aqueous soluble and metabolically stable compound in human hepatocytes. Compound 27b also showed weaker human Ether-a-go-go Related Gene (hERG) inhibitory activity than that of compound 13 and ASP4132. Therefore, 27b was a promising AMPK activator and a second-generation clinical candidate for treatment for human cancer.

IMIDAZO[1,2-a]PYRIDINE DERIVATIVE

[Problem] To provide a compound useful as medicine having PDE4B inhibitory activity, in particular, as an active ingredient of a composition for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like. [Measures for Solution] The present inventors examined compounds having PDE4B inhibitory activity and found that a tricyclic or tetracyclic imidazo[1,2-a]pyridine derivative or salts thereof had a superior PDE4B inhibitory activity, thereby completing the present invention. The imidazo[1,2-a]pyridine derivative can be used as an agent for treating or preventing schizophrenia, Alzheimer's disease, dementia, depression and the like.

Sulfonamide derivatives, processes for producing the same and utilization thereof

The present invention is to provide a compound or a salt thereof represented by the formula: wherein R1is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, the ring A is an optionally substituted divalent nitrogen-containing heterocyclic group, X′ is an optionally substituted alkylene chain, Y is an optionally substituted divalent cyclic group, X is a chemical bond or an optionally substituted alkylene chain, and Z is (1) an optionally substituted amino group, (2) an optionally substituted imidoyl group or (3) an optionally substituted nitrogen-containing heterocyclic group, or a pro-drug thereof, which have activated coagulation factor X inhibitory activity and which are useful as anti-coagulants.