US 12,258,423 B2
Stapled and stitched polypeptides and uses thereof
Gregory L. Verdine, Boston, MA (US); and Gerard Hilinski, Somerville, MA (US)
Assigned to PRESIDENT AND FELLOWS OF HARVARD COLLEGE, Cambridge, MA (US)
Filed by President and Fellows of Harvard College, Cambridge, MA (US)
Filed on Nov. 17, 2020, as Appl. No. 16/950,540.
Application 16/140,113 is a division of application No. 14/775,315, granted, now 10,081,654, issued on Sep. 25, 2018, previously published as PCT/US2014/025544, filed on Mar. 13, 2014.
Application 16/950,540 is a continuation of application No. 16/140,113, filed on Sep. 24, 2018, granted, now 11,332,496.
Claims priority of provisional application 61/779,917, filed on Mar. 13, 2013.
Prior Publication US 2022/0372075 A1, Nov. 24, 2022
Int. Cl. C07K 7/08 (2006.01); A61P 1/00 (2006.01); C07D 205/04 (2006.01); C07D 207/16 (2006.01); C07K 1/04 (2006.01); C07K 1/113 (2006.01); C07K 7/06 (2006.01); A61K 38/00 (2006.01)
CPC C07K 7/08 (2013.01) [A61P 1/00 (2018.01); C07D 205/04 (2013.01); C07D 207/16 (2013.01); C07K 1/04 (2013.01); C07K 1/113 (2013.01); C07K 7/06 (2013.01); A61K 38/00 (2013.01)] 14 Claims
 
1. An amino acid of Formula (D):

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt thereof,
wherein:
R1 is hydrogen; substituted or unsubstituted C1-6 alkyl; or an amino protecting group;
L1 is substituted or unsubstituted C1-10 alkylene, or —C(═O)OR6—;
RA is hydrogen or an amino protecting group;
RB is hydrogen;
X1 is N;
R6 is C1-6 alkylene; and
each of j and j1 is independently an integer between 1 and 10, inclusive, wherein when one of j and j1 is 2, the other is 1, or an integer between 3 and 10, inclusive.