Chemical conjugates of evans blue derivatives and their use in the production of long-acting therapeutics
AssigneeThe United States of America, as Represented by th e Secretary,Department of Health and Human Servic
InventorsXiaoyuan Chen, Lixin Lang, Gang Niu
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Abstract
The present invention is directed to a compound of Formula I or Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: Formula I Formula II The compounds of Formula I may be covalently bonded to a therapeutic compound or fragment thereof to provide a compound of Formula II and thereby extend the half-life of the therapeutic compound. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use in the diagnosis or treatment of diseases.
Claims35
A compound of Formula I or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester, amide, or salt,
- wherein:
- R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R11 are chosen independently from hydrogen, halogen, hydroxyl, cyano, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl, and C1-C6haloalkoxy;
- and
- L1 is —(CH2)m— wherein m is an integer from 0 to 12, wherein each CH2 can be individually replaced with —O—, —NH(CO)—, or —(CO)NH—, providing no two adjacent CH2 groups are replaced, and wherein L1 is optionally substituted with 1 substituent -A-B—X, wherein A is a bond, —NH—, —NH(CO)—, —(CO)NH—, B is C0-12alkyl, or phenylC0-12alkyl, and X is a hydrogen, halogen or an Sn derivative, and wherein when m is 0, the compound additionally comprises a radionuclide.
(canceled)
(canceled)
A compound of Formula II or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt,
- wherein:
- R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, and R1 are chosen independently from hydrogen, halogen, hydroxyl, cyano, C1-C6alkyl, C1-C6alkoxy, C1-C6haloalkyl, and C1-C6haloalkoxy;
- L1 is —(CH2)m— wherein m is an integer from 0 to 12, wherein each CH2 can be individually replaced with —O—, —NH(CO)—, or —(CO)NH—, providing no two adjacent CH2 groups are replaced, and wherein L1 is optionally substituted with 1 substituent which is -A-B—X, wherein A is a bond, —NH—, —NH(CO)—, —(CO)NH—, B is C0-12alkyl, or phenylC0-12alkyl, and X is a hydrogen, halogen or an Sn derivative;
- L2 is —(CH2)r— wherein r is an integer from 0 to 12, wherein each CH2 can be individually replaced with —O—, —NH(CO)—, or —(CO)NH—, providing no two adjacent CH2 groups are replaced;
- and
- R is a therapeutic compound.
A pharmaceutical composition comprising the compound of Formula II together with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.