US 12,453,779 B2
Chemoselective thiol-conjugation with alkene or alkyne-phosphonothiolates and -phosphonates
Christian Hackenberger, Berlin (DE); Alice Leonie Baumann, Berlin (DE); Marc-André Kasper, Munich (DE); Stephen Byrne, Sydney (AU); Jonas Helma-Smets, Munich (DE); Heinrich Leonhardt, Munich (DE); Tina Stoscheck, Munich (DE); Marcus Gerlach, Munich (DE); and Dominik Schumacher, Munich (DE)
Assigned to FORSCHUNGSVERBUND BERLIN E.V., Berlin (DE); and LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, Munich (DE)
Appl. No. 16/977,680
Filed by FORSCHUNGSVERBUND BERLIN E.V., Berlin (DE); and LUDWIG-MAXIMILIANS-UNIVERSITÄT MÜNCHEN, Munich (DE)
PCT Filed Mar. 6, 2019, PCT No. PCT/EP2019/055509
§ 371(c)(1), (2) Date Sep. 2, 2020,
PCT Pub. No. WO2019/170710, PCT Pub. Date Sep. 12, 2019.
Claims priority of application No. 18160384 (EP), filed on Mar. 7, 2018.
Prior Publication US 2020/0390901 A1, Dec. 17, 2020
Int. Cl. A61K 9/00 (2006.01); A61K 47/68 (2017.01); C07F 9/40 (2006.01)
CPC A61K 47/6849 (2017.08) [A61K 47/68031 (2023.08); A61K 47/6889 (2017.08); C07F 9/4015 (2013.01); C07F 9/4071 (2013.01)] 11 Claims
OG exemplary drawing
 
1. A compound of formula (III)

OG Complex Work Unit Chemistry
wherein
custom character represents a bond and X represents (R3 R4)C, wherein R3 and R4 independently represent H or C1-C8-alkyl; or
custom character represents a double bond and X represents R3C, wherein R3 represents H or C1-C8-alkyl; and
Y represents S;
R1 represents an optionally substituted aliphatic or aromatic residue;
custom character represents an aliphatic or aromatic residue; and
custom character represents an amino acid, a peptide, a protein, an antibody, or a nucleotide.