861218-15-7

Upstream product

• 1765-93-1 4-fluoroboronic acid 
• 360575-29-7 methyl 4-bromobenzo[b]thiophene-2-carboxylate 
• 360575-28-6 2-bromo-6-fluorobenzaldehyde 
• 1073-06-9 3-fluorobromobenzene 

Relevant academic research and scientific papers

Benzothiophene derivatives and medical use thereof for treating or preventing retinal diseases

The present invention relates to a novel benzo[b]thiophene derivative having RIPK1 inhibitory activity, a method for preparing the same, and a pharmaceutical composition for preventing or treating a retinal disease containing the same as an active component. According to the present invention, the novel benzo[b]thiophene derivative, or a pharmaceutically acceptable salt thereof has an excellent effect of inhibiting receptor-interacting serine/threonine-protein kinase 1 (RIPK1), thereby being usefully used for treating or preventing various retinal diseases including macular degeneration.

Novel bezo[b]thiophene derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating blindness related diseases containing the same as an active ingredient

The present invention relates to a novel methanone derivative, a manufacturing method thereof, and a pharmaceutical composition for preventing and treating retinal diseases comprising the same as an active ingredient. The methanone derivative, an optical isomer thereof or salt pharmaceutically acceptable thereof has an excellent suppression effect on RIPK1 (Receptor-interacting serine/threonine-protein kinase 1). Therefore, the composition comprising the same as an active ingredient can be useful as a pharmaceutical composition for preventing or treating retinal diseases such as retinitis pigmentosa (RP), Leberandprime;s congenital amaurosis (LCA), Stargardts disease, Usher syndrome, choroideremia, Cone-Rod or Rod-Cone dystrophy, symptoms of ciliation disease, dysfunction of mitochondria, progressive retinal atrophy, degenerative retinal disease, age-related macular degeneration (AMD), wet AMD, dry AMD, atrophy figuratum, genetic or acquired maculopathy, retinal photoreceptor disease, retinis pigmentosa-system disease, diabetic retinopathy, cystic macular edema, uveitis, retinal detachment, traumatic retinal damage, iatrogenic retinal damage, macular hole, macular capillary telangiectasia, ganglion cell disease, optic nerve cell disease, glaucoma, symptoms of optic nerve cell disease, ischemic retinal disease, retinopathy of prematurity, retinal occlusion, genetic macroaneurysm, retinal vascular disease, ophthalmic vascular disease, degeneration of retinal nerve cell by glaucoma, or symptoms of ischemic optical nerve cell disease.COPYRIGHT KIPO 2015

4-Substituted (benzo[b]thiophene-2-carbonyl)guanidines as novel Na +/H+ exchanger isoform-1 (NHE-1) inhibitors

A series of 4-substituted (benzo[b]thiophene-2-carbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficacy. Especially the 4-nitro 20 and cyano 50 compounds excellently improved the cardiac function and reduced infarct size against ischemia/reperfusion injury.