US 11,655,269 B2
Prodrug-type anticancer agent using cancer-specific enzymatic activity
Yasuteru Urano, Tokyo (JP); Mako Kamiya, Tokyo (JP); and Kento Hayashi, Tokyo (JP)
Appl. No. 16/977,607
Filed by The University of Tokyo, Tokyo (JP)
PCT Filed Mar. 4, 2019, PCT No. PCT/JP2019/008483
§ 371(c)(1), (2) Date Sep. 2, 2020,
PCT Pub. No. WO2019/172210, PCT Pub. Date Sep. 12, 2019.
Claims priority of provisional application 62/638,075, filed on Mar. 3, 2018.
Prior Publication US 2020/0399305 A1, Dec. 24, 2020
Int. Cl. C07H 23/00 (2006.01); A61P 35/00 (2006.01); C07C 237/04 (2006.01); C07D 207/16 (2006.01); C07F 7/08 (2006.01); C07H 15/203 (2006.01)
CPC C07H 23/00 (2013.01) [A61P 35/00 (2018.01); C07C 237/04 (2013.01); C07D 207/16 (2013.01); C07F 7/081 (2013.01); C07F 7/0812 (2013.01); C07H 15/203 (2013.01)] 4 Claims
1. A compound represented by general formula (I) or a salt thereof,

OG Complex Work Unit Chemistry
X is selected from the group consisting of a fluorine atom, ester group (—OC(═O)—R′), and carbamate group (—OCONH—R′),
where R′ is selected from unsubstituted alkyl groups or substituted or unsubstituted aryl groups;
Y is —NH—CO-L, —NH-L′, or —OL′,
where L, together with the C═O to which L bonds, constitutes an amino acid residue or a peptide,
L′ is a saccharide or a partial structure of a saccharide, or a saccharide or partial structure of a saccharide having a self-cleaving linker, an amino acid or a peptide having a self-cleaving linker, wherein the partial structure of the saccharide is a saccharide in which a hydroxyl group is lacking, and wherein —Y bonds to —C(R1)(R2)X on the ortho position or para position of the benzene ring;
R1 and R2 are each a hydrogen atom;
R3 represents a hydrogen atom or one to four monovalent substituents present on a benzene ring, which are the same or different,
wherein the monovalent substituent of R3 is an alkyl group, OR″, OCOR″, or a halogen atom, wherein R″ is a substituted or unsubstituted alkyl group or a substituted or unsubstituted aryl group.