Clofutriben
Cas 1204178-50-6
HCL 1203941-88-1
- ASP 3662
- 4-(5-(2-(4-Chloro-2,6-difluorophenoxy)propan-2-yl)-4-methyl-4H-1,2,4-triazol-3-yl)-3-fluorobenzamide
- 4-{5-[2-(4-Chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-4H-1,2,4-triazol-3-yl}-3-fluorobenzamide
- 4-[5-[2-(4-chloro-2,6-difluorophenoxy)propan-2-yl]-4-methyl-1,2,4-triazol-3-yl]-3-fluorobenzamide
- 4L1TY1U5VC
| Molecular Weight | 424.80 |
|---|---|
| Formula | C19H16ClF3N4O2 |
Clofutriben (ASP3662) is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor.
Clofutriben is an orally bioavailable selective inhibitor of the enzyme 11beta-hydroxysteroid dehydrogenase type 1 (11b-HSD1; 11bHSD1; HSD11B1; HSD1; HSD-1), with potential protective activity for disorders of corticosteroid excess. Upon oral administration, clofutriben selectively binds to and inhibits the activity of HSD-1. This prevents the conversion of cortisone to the active hormone cortisol and thereby preventing the activation of the glucocorticoid receptors (GRs). By blocking cortisol production in metabolic tissues, clofutriben may inhibit the adverse metabolic effects that are caused by exogenous administration of glucocorticoids or in disorders in which cortisol is secreted in excess. HSD-1 is highly expressed in metabolic tissues, such as liver, skeletal muscle, and adipose tissue. It plays a crucial role in regulating the production of cortisol to activate the GRs.
SCHEME
PATENTS
Clinical and Translational Science (2019), 12(3), 291-301
British Journal of Pharmacology (2018), 175(19), 3784-3796
Sparrow Pharmaceuticals, Inc. WO2020106337
WO2019075394
WO2018117063
WO2010001946
PATENT
PDT PAT FOR HCL SALT, WO2012033070
https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2012033070
PATENT
PDT PAT FOR BASE, WO2018117063
PATENT
WO2010001946
[1]. Kiso T, et al. Analgesic effects of ASP3662, a novel 11尾-hydroxysteroid dehydrogenase 1 inhibitor, in rat models of neuropathic and dysfunctional pain. Br J Pharmacol. 2018 Oct;175(19):3784-3796. [Content Brief]
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