SOVESUDIL
PHP-201; AMA 0076, C23O3R93BM
CAS 1333400-14-8
| Molecular Weight | 407.44 |
|---|---|
| Formula | C23H22FN3O3 |
Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia.
SCHEME
PATENTS
Bioorganic & Medicinal Chemistry Letters (2013), 23(23), 6442-6446
https://www.sciencedirect.com/science/article/abs/pii/S0960894X13011141
Figure 2. Synthetic scheme for synthesis of compounds 10–35. (a) H2SO4, MeOH, 60 C, 16 h; (b) NBS, AIBN, CCl4, reflux, 16 h; (c) Boc2NH, t-BuOK, DMF, rt, 16 h; (d) DCM/TFA
(50:1), 0 C ? rt, 4 h; (e) NaOH, MeOH, 50 C, 2 h; (f) HATU, DMAP, NEt3, DMA, 30 C, 16 h; (g) Pd(dppf)Cl2, Na2CO3, H2O, DMF, 100 C; 16 h; (h) ROH, TBTU, HOBT, DIEA, DMF,
rt, 16 h or ROH, DCC, DMAP, DCM, rt, 16 h or Me2C@C(Cl)NMe2, THF or DCM, rt, followed by ROH, 16 h; (i) DCM/TFA (7:1), 30 C, 16 h or HCl(g) in DCM, 30 C, 16 h.
PATENT
WO2011107608
- [1]. Van de Velde S, et al. AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014;55(2):1006-1016. Published 2014 Feb 18. [Content Brief][2]. Ha A, et al. Sovesudil (locally acting rho kinase inhibitor) for the treatment of normal-tension glaucoma: the randomized phase II study [published online ahead of print, 2021 Jul 28]. Acta Ophthalmol. 2021;10.1111/aos.14949. [Content Brief]
////////SOVESUDIL, 1333400-14-8, PHP 201, AMA 0076, C23O3R93BM
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