	US 11,883,501 B2
	Selective CXCR4 binding peptide conjugate and methods for making and using the same
Junge Zhang, Malvern, PA (US); and Liang Zeng Yan, Camel, IN (US)
Assigned to Mainline Biosciences (Shanghai) Co., Ltd., Shanghai (CN)
Filed by Mainline Biosciences (Shanghai) Co., Ltd., Shanghai (CN)
Filed on Sep. 20, 2021, as Appl. No. 17/479,920.
Application 17/479,920 is a continuation of application No. 16/752,690, filed on Jan. 26, 2020, granted, now 11,123,437.
Application 16/752,690 is a continuation in part of application No. 15/898,434, filed on Feb. 17, 2018, granted, now 10,639,379, issued on May 5, 2020.
Claims priority of provisional application 62/554,354, filed on Sep. 5, 2017.
Prior Publication US 2022/0062433 A1, Mar. 3, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 47/64 (2017.01); C07K 7/06 (2006.01)

CPC A61K 47/64 (2017.08) [C07K 7/06 (2013.01)]

11 Claims

1. A selective CXCR4 binding peptide conjugate (“PC”) of the formula:

or a pharmaceutically acceptable salt thereof,

wherein:

a is 0 or 1;

b is 1;

AA¹along with the sulfur atom that is attached thereto is 3-mercaptopropionic acid, optionally substituted cysteine, optionally substituted homocysteine, or optionally substituted penicillamine;

AA²along with the sulfur atom that is attached thereto is cysteine or homocysteine;

Ar¹is phenylene;

X¹is Arg, Dap, Dab, Orn, Lys, Dap(iPr), Dab(iPr), Orn(iPr), or Lys(iPr);

AA³is Lys(iPr);

AA⁴is an amino acid or a derivative thereof;

Y¹is a side-chain function group of amino acid AA⁴;

L^1ais a polyethylene glycol of about 2 to about 20 monomers;

L²is a non-polymeric linker;

Z a medically useful compound; and

Y²is a functional group of said medically useful compound or a functional group of L²;

and wherein one or more of AA¹, AA², X¹, AA³, and AA⁴are optionally isotopically labelled.