Vitamin receptor drug delivery conjugates for treating inflammation
AssigneeEndocyte, Inc.
InventorsChristopher Paul Leamon, Iontcho Radoslavov Vlahov, Yingjuan June Lu
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Abstract
Described herein are compositions, methods, compounds, conjugates, and kits for use in targeted drug delivery using drug delivery conjugates containing hydrophilic spacer linkers for use in treating disease states caused by pathogenic cell populations, such as inflammatory cells.
Claims24
-43. (canceled)
A method for treating a patient with an inflammatory disease, the method comprising the step of administering to the patient a composition comprising a drug delivery conjugate of the formula
- B-L-A3
- or a pharmaceutically acceptable salt, isomer, mixture of isomers, crystalline form, non crystalline form, hydrate, or solvate thereof;
- wherein
- B is a folate;
- L is a linker that comprises one or more hydrophilic spacer linkers;
- and
- A3 has the formula
- wherein
- YA is ORC or OCH2CH2ORC;
- one of RA, RB, or RC is a bond connected to L;
- and
- the other two of RA, RB, and RC are independently selected in each case from the group consisting of hydrogen, optionally substituted heteroalkyl, prodrug forming group, and C(O)RD, where RD is in each instance independently selected from the group consisting of hydrogen, and alkyl, alkenyl, heteroalkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl, each of which is optionally substituted.
(canceled)
A pharmaceutical composition comprising a drug delivery conjugate of the formula
- B-L-A
- or a pharmaceutically acceptable salt, isomer, mixture of isomers, crystalline form, non crystalline form, hydrate, or solvate thereof;
- wherein
- B is a folate;
- L is a linker that comprises one or more hydrophilic spacer linkers;
- and
- A has the formula
- wherein
- YA is ORC or OCH2CH2ORC;
- one of RA, RB, or RC is a bond connected to L;
- and
- the other two of RA, RB, and RC are independently selected in each case from the group consisting of hydrogen, optionally substituted heteroalkyl, prodrug forming group, and C(O)RD, where RD is in each instance independently selected from the group consisting of hydrogen, and alkyl, alkenyl, heteroalkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl, each of which is optionally substituted.
(canceled)
-81. (canceled)
Dependencies are inferred from the claim text.