	US 12,030,888 B2
	Himastatin derivatives, and processes of preparation thereof, and uses thereof
Mohammad Movassaghi, Lincoln, MA (US); Bradley L. Pentelute, Cambridge, MA (US); Carly Schissel, Cambridge, MA (US); and Kyan Anthony D'Angelo, Cambridge, MA (US)
Assigned to Massachusetts Institute of Technology, Cambridge, MA (US)
Filed by Massachusetts Institute of Technology, Cambridge, MA (US)
Filed on Dec. 23, 2021, as Appl. No. 17/561,680.
Claims priority of provisional application 63/153,286, filed on Feb. 24, 2021.
Prior Publication US 2022/0289750 A1, Sep. 15, 2022
Int. Cl. C07D 519/00 (2006.01); C07D 209/86 (2006.01); C07D 487/04 (2006.01); C07D 487/14 (2006.01); C07D 487/22 (2006.01); C07D 498/22 (2006.01)

CPC C07D 487/04 (2013.01) [C07D 209/86 (2013.01); C07D 487/14 (2013.01); C07D 487/22 (2013.01); C07D 498/22 (2013.01); C07D 519/00 (2013.01); C07B 2200/05 (2013.01); C07B 2200/07 (2013.01)]

40 Claims

1. A compound of the Formula I:

or a tautomer or isotopically labeled compound thereof, or a salt thereof, wherein:

the bond a1 and the bond a2 are syn or anti to each other;

the bond b1 and the bond b2 are syn or anti to each other;

each of R^A1and R^B1is independently hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted phenyl;

each of R^A2and R^B2is independently hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted phenyl;

R^A3and R^A4aor R^A4bare joined with their intervening atoms to form substituted or unsubstituted heterocyclyl; and the remaining one of R^A4aand R^A4bis hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, —C(═O)OR^a, a peptide, or a depsipeptide, wherein each R^ais independently substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, or hydrogen;

R^B3and R^B4aor R^B4bare joined with their intervening atoms to form substituted or unsubstituted heterocyclyl; and the remaining one of R^B4aand R^B4bis hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, —C(═O)OR^a, a peptide, or a depsipeptide, wherein each R^ais independently substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, or hydrogen:

or each of R^A3and R^B3is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, —C(═O)R^a, —C(═O)OR^a, a nitrogen protecting group, a peptide, or a depsipeptide, wherein each R^ais independently substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, or hydrogen; and

each of R^A4a, R^A4b, R^B4a, and R^B4bis independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, a peptide, or a depsipeptide, wherein each R^ais independently substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, or hydrogen;

each of R^A5a, R^B5a, R^A5b, and R^B5bis independently hydrogen or substituted or unsubstituted alkyl;

each of R^A6and R^B6is independently substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, or —OR^a, wherein each R^ais independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted carbocyclyl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or an oxygen protecting group; and

each of R^A7, R^B7, R^A8, R^B8, R^A9, and R^B9is independently hydrogen, halogen, substituted or unsubstituted alkyl, or —OR^a, wherein each R^ais independently hydrogen or substituted or unsubstituted alkyl;

provided that the compound is not of the formula:

or a tautomer or isotopically labeled compound thereof, or a salt thereof.