	US 12,479,927 B2
	Compounds comprising cleavable linker and uses thereof
Taekyo Park, Daejeon (KR); Sung Ho Woo, Sejong-Si (KR); Sunyoung Kim, Daejeon (KR); Suho Park, Daejeon (KR); Jongun Cho, Daejeon (KR); Doohwan Jung, Daejeon (KR); Donghoon Seo, Daejeon (KR); Jaeho Lee, Daejeon (KR); Sangkwang Lee, Daejeon (KR); Sanghyeon Yun, Daejeon (KR); Hyang Sook Lee, Daejeon (KR); Okku Park, Daejeon (KR); and Beomseok Seo, Daejeon (KR)
Assigned to IntoCell, Inc., Daejeon (KR)
Filed by IntoCell, Inc., Daejeon (KR)
Filed on May 30, 2023, as Appl. No. 18/203,326.
Application 18/203,326 is a division of application No. 16/628,482, granted, now 11,753,431, previously published as PCT/IB2018/000847, filed on Jul. 3, 2018.
Claims priority of provisional application 62/597,226, filed on Dec. 11, 2017.
Claims priority of application No. 10-2017-0084805 (KR), filed on Jul. 4, 2017.
Prior Publication US 2023/0406877 A1, Dec. 21, 2023
Int. Cl. C07H 15/207 (2006.01); A61K 47/54 (2017.01); A61K 47/68 (2017.01); A61K 51/04 (2006.01); A61P 35/00 (2006.01); C07K 16/32 (2006.01)

CPC C07K 16/32 (2013.01) [A61K 47/549 (2017.08); A61K 47/6803 (2017.08); A61K 47/68031 (2023.08); A61K 47/68037 (2023.08); A61K 47/6835 (2017.08); A61K 51/04 (2013.01); A61P 35/00 (2018.01); C07H 15/207 (2013.01)]

15 Claims

1. A compound of Formula (Ia):

or a pharmaceutically acceptable salt thereof, wherein:

each Q is independently an active agent linked to L′ by a heteroatom;

Z′ is absent or a linking group;

L′ is a linking group attached to the SO₂via a heteroatom selected from O, S, and N, and is selected such that cleavage of the bond between L′ and SO₂promotes cleavage of the bond between L′ and Q to release the active agent;

X is —O—, —CR^a₂—, or —NR′—;

Ar represents aryl, heteroaryl, cycloalkyl, or heterocycloalkyl;

Y′ is —(CR^b₂)_yN(R^a)—, —(CR^b₂)_yO—, or —(CR^b₂)_yS—, positioned such that the N, O, or S atom is attached to TG if y is 1;

X and Y′ are positioned on adjacent atoms of Ar;

TG is a triggering group that, when activated, generates an N, O, or S atom capable of reacting with the SO₂to displace (Q)_q-(L′)_wand form a 5-6-membered ring including X—SO₂and the intervening atoms of Ar;

q is an integer having a value from 1 to about 20;

w, x, and y are each independently an integer having a value of 0 or 1;

each R^aand R' is independently hydrogen or lower alkyl; and

each R^bis independently hydrogen or lower alkyl; or

two R^b, together with the carbon atom to which they are attached, form a 3-5-membered ring;

provided that when w is 0, q is 1.