US 12,391,733 B2
Stapled intracellular-targeting antimicrobial peptides to treat infection
Loren D. Walensky, Newton, MA (US); and Rida Mourtada, Brookline, MA (US)
Assigned to Dana-Farber Cancer Institute, Inc., Boston, MA (US)
Filed by Dana-Farber Cancer Institute, Inc., Boston, MA (US)
Filed on Feb. 28, 2024, as Appl. No. 18/590,636.
Application 18/590,636 is a continuation of application No. 16/813,528, filed on Mar. 9, 2020, granted, now 11,945,846, issued on Apr. 2, 2024.
Application 16/813,528 is a continuation of application No. 15/445,502, filed on Feb. 28, 2017, abandoned.
Claims priority of provisional application 62/301,426, filed on Feb. 29, 2016.
Prior Publication US 2024/0343765 A1, Oct. 17, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 38/08 (2019.01); A61K 38/10 (2006.01); A61K 38/17 (2006.01); A61K 45/06 (2006.01); C07K 7/06 (2006.01); C07K 7/08 (2006.01); C07K 14/435 (2006.01); C07K 14/46 (2006.01); C07K 14/47 (2006.01)
CPC C07K 14/461 (2013.01) [A61K 38/08 (2013.01); A61K 38/10 (2013.01); A61K 38/1703 (2013.01); A61K 38/1706 (2013.01); A61K 38/1709 (2013.01); A61K 38/1767 (2013.01); A61K 45/06 (2013.01); C07K 7/06 (2013.01); C07K 7/08 (2013.01); C07K 14/43504 (2013.01); C07K 14/463 (2013.01); C07K 14/47 (2013.01)] 28 Claims
 
1. A stapled peptide or a pharmaceutically acceptable salt thereof comprising the amino acid sequence:
 
 (SEQ ID NO: 41)
 
 TRSSRAGLQWPVX1RVHX2LLRK,
 
 
 
 (SEQ ID NO: 37)
 
 TRSSRAGLQWPVGRVHX1LLRX2,
 
 
 
 (SEQ ID NO: 39)
 
 TRSSRAGLQWPVGRX1HRLX2RK,
 
 
 
 (SEQ ID NO: 40)
 
 TRSSRAGLQWPVGX1VHRX2LRK,
 
 
 
 (SEQ ID NO: 44)
 
 TRSSRAGX1QWPX2GRVHRLLRK,
 
 
 
 (SEQ ID NO: 45)
 
 TRSSX1AGLX2WPVGRVHRLLRK,
 
 
 
 (SEQ ID NO: 46)
 
 TRSX1RAGX2QWPVGRVHRLLRK,
 
 
 
 (SEQ ID NO: 48)
 
 TX1SSRX2GLQWPVGRVHRLLRK,
 
 
 
 (SEQ ID NO: 49)
 
 X1RSSX2AGLQWPVGRVHRLLRK,
 
 
 
 (SEQ ID NO: 50)
 
 TRSSRAGLQWPVGX3VHRLLRX4,
 
 
 
 (SEQ ID NO: 51)
 
 TRSSRAGLQWPVX3RVHRLLX4K,
 
 
 
 (SEQ ID NO: 52)
 
 TRSSRAGLQWPX3GRVHRLX4RK,
 
 
 
 (SEQ ID NO: 53)
 
 TRSSRAGLX3WPVGRVX4RLLRK,
 
 
 
 (SEQ ID NO: 54)
 
 TRSSRAGX3QWPVGRX4HRLLRK,
 
 
 
 (SEQ ID NO: 56)
 
 TRSSRX3GLQWPVX4RVHRLLRK,
 
 
 
 (SEQ ID NO: 58)
 
 TX3SSRAGLX4WPVGRVHRLLRK,
 
 or
 
 
 
 (SEQ ID NO: 59)
 
 X3RSSRAGX4QWPVGRVHRLLRK,
wherein each of X1, X2, X3, and X4 is a non-natural amino acid,
wherein X1 and X2 are cross-linked to each other where present, and
wherein X3 and X4 are cross-linked to each other where present.