1338320-20-9

Upstream product

• 771-99-3 4-phenylpiperidine 
• 15037-34-0 1-(3-Chloropropyl)-4-phenyl-1,2,4,6-tetrahydropyridine 
• 1133065-98-1 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-b]indazol-1-one 
• 4498-67-3 1H-Indazole-3-carboxylic acid 
• 43120-28-1 methyl 1H-indazole-3-carboxylate 
• 1338227-14-7 methyl 2-[3-(tert-butoxycarbonylamino)propyl]-2H-indazol-3-carboxylate 

Relevant academic research and scientific papers

Targeting Serotonin 2A and Adrenergic α1 Receptors for Ocular Antihypertensive Agents: Discovery of 3,4-Dihydropyrazino[1,2-b]indazol-1(2H)-one Derivatives

Glaucoma affects millions of people worldwide and causes optic nerve damage and blindness. The elevation of the intraocular pressure (IOP) is the main risk factor associated with this pathology, and decreasing IOP is the key therapeutic target of current pharmacological treatments. As potential ocular hypotensive agents, we studied compounds that act on two receptors (serotonin 2A and adrenergic α1) linked to the regulation of aqueous humour dynamics. Herein we describe the design, synthesis, and pharmacological profiling of a series of novel bicyclic and tricyclic N2-alkyl-indazole-amide derivatives. This study identified a 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivative with potent serotonin 2A receptor antagonism, >100-fold selectivity over other serotonin subtype receptors, and high affinity for the α1 receptor. Moreover, upon local administration, this compound showed superior ocular hypotensive action in vivo relative to the clinically used reference compound timolol.

TRICYCLIC INDAZOLE COMPOUND, METHOD OF PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING IT

Tricyclic indazole compound and its pharmaceutically acceptable salts of acid addition, use thereof, method and intermediates for preparing them, and a pharmaceutical composition containing them. The tricyclic indazole compound has the following general F