1825352-65-5

Basic information

• Product Name: 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)-4H-pyrido[l,2-a]pyrimidin-4-one
• CAS NO: 1825352-65-5
• Molecular Weight: 401.471
• Mol File: 1825352-65-5.mol
• Article Data: 6

Chemical Properties

• Density: 1.50±0.1 g/cm3(Predicted)
• CAS DataBase Reference: 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)-4H-pyrido[l,2-a]pyrimidin-4-one(CAS DataBase Reference)
• NIST Chemistry Reference: 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)-4H-pyrido[l,2-a]pyrimidin-4-one(1825352-65-5)
• EPA Substance Registry System: 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)-4H-pyrido[l,2-a]pyrimidin-4-one(1825352-65-5)

Safety Data

• Hazardous Substances Data: 1825352-65-5(Hazardous Substances Data)

Usage

Description

7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2b]pyridazin-6-yl)-4H-pyrido[l,2-a]pyrimidin-4-one, also known as Risdiplam, is a survival of motor neuron 2 (SMN2) splicing modifier. It is a light yellow to yellow powder with unique chemical properties that make it a promising candidate for the treatment of spinal muscular atrophy.

Uses

Used in Pharmaceutical Industry:
7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2b]pyridazin-6-yl)-4H-pyrido[l,2-a]pyrimidin-4-one is used as a gene splicing modulator for the preparation of Imidazopyridazinyl Pyridopyrimidinones. It is specifically designed to treat spinal muscular atrophy by modifying the splicing of the SMN2 gene, which plays a crucial role in the disease's progression.

Side effects

Body aches or pain, chest pain or tightness, chills, cough, ear congestion, fever, headache, loss of voice, runny or stuffy nose, sneezing, sore throat, trouble breathing, unusual tiredness or weakness and so on.

storage

0-4℃ for short term (days to weeks) or -20℃ for long term (months)

Upstream product

• 53939-30-3 5-bromo-2-chloropyridine 
• 2173992-48-6 tert-butyl 4,7-diazaspiro[2.5]octane-4-carboxylate oxalate 
• 1449598-85-9 7-fluoro-2-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one 
• 21717-96-4 2-amino-5-fluoropyridine 
• 145122-56-1 4,7-diazaspiro<2,5>octane dihydrochloride 
• 1825352-86-0 2,8-dimethyl-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)imidazo[1,2-b]pyridazine 
• 17412-23-6 6-chloro-2,8-dimethyl-imidazo[1,2-b]pyridazine 
• 19064-64-3 3,6-dichloro-4-methylpyridazine 

Relevant articles and documents

PROCESS FOR THE PREPRATION OF 7-(4,7-DIAZASPIRO[2.5]OCTAN-7-YL)-2-(2,8-DIMETHYLIMIDAZO[1,2-B]PYRIDAZIN-6-YL)PYRIDO[1,2-A]PYRIMIDIN-4-ONE DERIVATIVES

The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[l,2- b]pyridazin-6-yl)pyrido[l,2-a]pyrimidin-4-one derivatives useful pharmaceutically active compounds.

Discovery of Risdiplam, a Selective Survival of Motor Neuron-2 (SMN2) Gene Splicing Modifier for the Treatment of Spinal Muscular Atrophy (SMA)

SMA is an inherited disease that leads to loss of motor function and ambulation and a reduced life expectancy. We have been working to develop orally administrated, systemically distributed small molecules to increase levels of functional SMN protein. Compound 2 was the first SMN2 splicing modifier tested in clinical trials in healthy volunteers and SMA patients. It was safe and well tolerated and increased SMN protein levels up to 2-fold in patients. Nevertheless, its development was stopped as a precautionary measure because retinal toxicity was observed in cynomolgus monkeys after chronic daily oral dosing (39 weeks) at exposures in excess of those investigated in patients. Herein, we describe the discovery of 1 (risdiplam, RG7916, RO7034067) that focused on thorough pharmacology, DMPK and safety characterization and optimization. This compound is undergoing pivotal clinical trials and is a promising medicine for the treatment of patients in all ages and stages with SMA.

COMPOSITIONS FOR TREATING SPINAL MUSCULAR ATROPHY

The present invention provides pharmaceutical compositions comprising a compound of formula (I) wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the pharmaceutical compositions comprising a compound of formula (I) and their use as medicaments.