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US 9,539,342 B2Granted
Auristatin tyramine phosphate salts and auristatin aminoquinoline derivatives and prodrugs thereof
AssigneeArizona Board of Regents, a body corporate of the State of Arizona, acting for and on behlaf of Arizona State University
InventorsGeorge R. Pettit, Fiona Hogan, Steven Toms
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Abstract
The present invention relates to new auristatin compounds and prodrugs thereof, compositions comprising them and uses thereof.
Claims19
A compound of formula (I):
- wherein R is selected from the group consisting of:
- R1 and R2 are independently selected from the group consisting of H, methyl and a Linker Unit;
- R3 and R4 are independently selected from the group consisting of lithium (Li+), sodium (Na+), potassium (K+), hydrogen (H), morpholine, quinine, tris(hydroxymethyl)aminomethane (TRIS), serine, nitroarginine and a Linker Unit;
- and
- each R5 is selected from H or a Linker Unit.
2 more elements
A compound having the formula:
- wherein the compound is selected from:
- Compd.
- No.
- R
- R1
- R2
- R3
- R4
- R5
- 3a
- CH3
- CH3
- Li+
- Li+
- H
- 3b
- CH3
- CH3
- Na+
- Na+
- H
- 3c
- CH3
- CH3
- K+
- K+
- H
- 3d
- CH3
- CH3
- H
- morpholine
- H
- 3e
- CH3
- CH3
- H
- quinine
- H
- 3f
- CH3
- CH3
- H
- TRIS
- H
- 3g
- CH3
- CH3
- H
- serine
- H
- 3h
- CH3
- CH3
- H
- nitro- arginine
- H
- 4
- CH3
- CH3
- —
- —
- —
- 5
- CH3
- CH3
- —
- —
- —.
66 more elements
Dependencies are inferred from the claim text.