Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement
摘要:
A series of 1-phenyl-3-(1-phenylethyl)urea derivatives were identified as novel and potent complement inhibitors through structural modification of the original compound from high-throughput screening. Various analogues (7 and 13-15) were synthesized and identified as complement inhibitors, with the introduction of a five- or six-carbon chain (7c, 7d, 7k, 7I, and 7o) greatly improving their activity. Optimized compound 7I has an excellent inhibition activity with IC50 values as low as 13 nM. We demonstrated that the compound 7I inhibited C9 deposition through the classical, the lectin, and the alternative pathways but had no influence on C3 and C4 depositions.
[EN] COMPLEMENT MODULATORS AND RELATED METHODS<br/>[FR] MODULATEURS DU COMPLÉMENT ET PROCÉDÉS ASSOCIÉS
申请人:RA PHARMACEUTICALS INC
公开号:WO2020205501A1
公开(公告)日:2020-10-08
The present disclosure presents compounds and compositions that interact with complement components. Some compounds inhibit complement activity. Included are small molecule compounds and compositions that function as C5 inhibitor compounds. Methods for inhibiting complement activity and methods of treating complement-related indications with the C5 inhibitor compounds and compositions are provided.
An inkjet ink including: a stilbene-based compound represented by General Formula (1) below;
where in the General Formula (1), R1 and R3 each independently represent, for example, an alkyl group including 1 to 20 carbon atoms, an alkenyl group including 1 to 20 carbon atoms, a phenyl group, or a naphthyl group.
An inkjet ink including: a stilbene-based compound represented by General Formula (1) below;
where in the General Formula (1), R
1
and R
3
each independently represent, for example, an alkyl group including
1
to
20
carbon atoms, an alkenyl group including
1
to
20
carbon atoms, a phenyl group, or a naphthyl group.