603281-60-3

Usage

Uses

Used in Pharmaceutical Industry:
3-IMidazo[1,2-a]pyridin-3-yl-4-[1,2,3,4-tetrahydro-2-(1-piperidinylcarbonyl)pyrrolo[3,2,1-jk][1,4]benzodiazepin-7-yl]-1H-pyrrole-2,5-dione is used as a therapeutic agent for the treatment of type 2 diabetes. 3-IMidazo[1,2-a]pyridin-3-yl-4-[1,2,3,4-tetrahydro-2-(1-piperidinylcarbonyl)pyrrolo[3,2,1-jk][1,4]benzodiazepin-7-yl]-1H-pyrrole-2,5-dione acts as a potent and selective biarylmaleimide GSK3 inhibitor, which may help in lowering plasma glucose levels, providing a potential treatment option for patients with type 2 diabetes.
Additionally, due to its inhibitory properties, 3-IMidazo[1,2-a]pyridin-3-yl-4-[1,2,3,4-tetrahydro-2-(1-piperidinylcarbonyl)pyrrolo[3,2,1-jk][1,4]benzodiazepin-7-yl]-1H-pyrrole-2,5-dione may also have potential applications in other areas of pharmaceutical research, such as the development of drugs targeting other kinases or signaling pathways involved in various diseases. However, further research and development would be required to explore these possibilities.

Upstream product

• 13939-69-0 piperidine carbamoyl chloride 
• 504-29-0 2-aminopyridine 
• 345264-15-5 S-6-(tert-butoxycarbonyl)-5,6-dihydro-6H-[1,4]diazepino[6,7,1-hi]indole 
• 748811-03-2 2-[(tert-butoxycarbonyl)(1H-indol-7-ylmethyl)amino]ethyl methanesulfonate 
• 748811-02-1 tert-butyl (2-hydroxyethyl)(1Hindol-7-ylmethyl)carbamate 
• 408356-56-9 2-[(1H-indol-7-ylmethyl)-amino]-ethanol 
• 1074-88-0 1H-indole-7-carbaldehyde 
• 848483-50-1 7-(4-imidazo[1,2-a]pyridin-3-yl-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)-3,4-dihydro-1H-[1,4]diazepino[6,7,1-hi]indole-2-carboxylic acid tert-butyl ester 
• 345264-16-6 (6-(tert-butoxycarbonyl)-5,6-dihydro-6H-[1,4]diazepino[6,7,1-hi]indol-1-yl)oxoacetic acid methyl ester 
• 101820-69-3 imidazo[1,2-α]pyridin-3-yl-acetic acid ethyl ester 
• 21801-86-5 2-(imidazo-[1,2-a]pyridin-3-yl)acetamide 
• 603310-08-3 3-imidazo[1,2-a]pyridin-3-yl-4-(1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-7-yl)-pyrrole-2,5-dione 

Relevant academic research and scientific papers

The development of potent and selective bisarylmaleimide GSK3 inhibitors

Many 3-aryl-4-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl) maleimides exhibit potent GSK3 inhibitory activity (50), although few show significant selectivity (>100 ×) versus CDK2, CDK4, or PKCβII. However, combining 3-(imidazo[1,2-a]pyridin-3-yl), 3-(pyrazolo[1,5-a]pyridin-3-yl) or aza-analogs with a 4-(2-acyl-(1,2,3,4- tetrahydro[1,4]diazepino[6,7,1-hi]indol -7-yl)) group on the maleimide resulted in very potent inhibitors of GSK3 (≤5 nM) with >160 to >10,000-fold selectivity versus CDK2/4 and PKCβII. These compounds also inhibited tau phosphorylation in cells and were effective in lowering plasma glucose in a rat model of type 2 diabetes (ZDF rat).

Substituted 3-imidazo[1,2-a]pyridin-3-yl-4-(1,2,3,4-tetrahydro-[1,4] diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3

Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose similar to insulin, making GSK3 an attractive target for the treatment of type 2 diabetes. Herein we report the discovery of a series of potent and selective GSK3 inhibitors. Compounds 7-12 show oral activity in an in vivo model of type II diabetes, and 9 and 12 have desirable PK properties.