Patent ID: 11931414
Assignee: SEAGEN INC.
Field: Pharmaceuticals (Chemistry)
Classification: CPC A  C | IPC A  C

Claim 11:
12. The Ligand-Drug Conjugate compound of claim 11, wherein the Formula 1a′ or Formula 1b′ structure is represented by the structure of:, respectively, or a salt thereof, wherein
R45 is —CH2OH or —CO2H;
Ra3 is —H, optionally substituted C1-C6 alkyl, optionally substituted —C1-C4 alkylene-(C6-C10 aryl), or —RPEG1—O—(CH2CH2O)1-36—RPEG2, wherein RPEG1 is C1-C4 alkylene and RPEG2 is —H or C1-C4 alkyl; and
wherein the basic nitrogen atom bonded to Ra3 is optionally protonated;
—O′— represents the oxygen atom of the 0-glycosidic bond cleavable by the glycosidase,
or wherein the Formula 1a′ or Formula 1b′ structure is represented by the structure of:, respectively, or a salt thereof, wherein
R45 is —CH2OH or —CO2H;
BU is —CH2—NH2, optionally protonated;
Ra2 is hydrogen; and
—O′— represents the oxygen atom of the 0-glycosidic bond cleavable by the glycosidase,
or wherein the Formula 1c′ or Formula 1d′ structure is represented by the structure of:, respectively, or a salt thereof, wherein
R45 is —CH2OH or —CO2H; and
—O′— represents the oxygen atom of the 0-glycosidic bond cleavable by the glycosidase,
or wherein the Formula 1a′ or Formula 1b′ structure is represented by the structure of:, respectively, or a salt thereof, wherein
W is the Peptide Cleavable Unit;
Ra3 is —H, optionally substituted C1-C6 alkyl, optionally substituted —C1-C4 alkylene-(C6-C10 aryl), or —RPEG1—O—(CH2CH2O)1-36—RPEG2, wherein RPEG1 is C1-C4 alkylene and RPEG2 is —H or C1-C4 alkyl; and
wherein the basic nitrogen atom bonded to Ra3 is optionally protonated; and
wherein protease action on the Peptide Cleavable Unit is capable of cleaving the W—NH bond, wherein said cleavage within a drug linker moiety of a Ligand Drug Conjugate compound initiates release of the quaternized NAMPT Drug (D+) Unit as a NAMPTi compound from that Ligand Drug Conjugate compound,
or wherein the Formula 1a′ or Formula 1b′ structure is represented by the structure of:, respectively, or a salt thereof, wherein
W is the Peptide Cleavable Unit;
BU is —CH2—NH2, optionally protonated;
Ra2 is hydrogen; and
wherein protease action on the Peptide Cleavable Unit is capable of cleaving the W—NH bond, wherein said cleavage within a drug linker moiety of a Ligand Drug Conjugate compound initiates release of the quaternized NAMPT Drug (D+) Unit as a NAMPTi compound from that Ligand Drug Conjugate compound,
or wherein the Formula 1c′ or Formula 1d′ structure is represented by the structure of:, respectively, or a salt thereof, wherein
W is the Peptide Cleavable Unit,
wherein protease action on the Peptide Cleavable Unit is capable of cleaving the W—NH bond, wherein said cleavage within a drug linker moiety of a Ligand Drug Conjugate compound initiates release of the quaternized NAMPT Drug Unit (D+) as a NAMPTi compound from that Ligand Drug Conjugate compound.