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US 10,500,204 B2Granted
Vitamin receptor drug delivery conjugates for treating inflammation
AssigneeEndocyte, Inc.
InventorsChristopher Paul Leamon, Iontcho Radoslavov Vlahov, Yingjuan June Lu, Kevin Yu Wang, Fei You, Paul Joseph Kleindl, Hari Krishna R. Santhapuram
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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.
Claims20
A compound of the formula
- BLA
- or a pharmaceutically acceptable salt thereof;
- wherein
- B is a vitamin receptor binding ligand;
- L is a linker that comprises one or more hydrophilic spacer linkers selected from the group consisting of
- wherein
- R is selected from the group consisting of H, alkyl, cycloalkyl, and arylalkyl;
- m is an integer from 1 to about 3;
- n is an integer from 1 to about 6;
- p is an integer from 1 to about 5;
- and (*) indicates the point of attachment to the rest of the compound and
- a fragment of the formula
- wherein
- each Ra and Rb is independently hydrogen or alkyl;
- or Ra and Rb are taken together with the attached carbon atom to form a carbocyclic ring;
- n1 is an integer selected from 1 to 4;
- and
- (**) indicates points of attachment for other parts of the conjugate;
- and
- A is an adrenocorticoid or a corticosteroid.
17 more elements
A pharmaceutical composition comprising a compound of the formula
- BLA
- or a pharmaceutically acceptable salt thereof;
- wherein
- B is a vitamin receptor binding ligand;
- L is a linker that comprises one or more hydrophilic spacer linkers selected from the group consisting of
- wherein
- R is selected from the group consisting of H, alkyl, cycloalkyl, and arylalkyl;
- m is an integer from 1 to about 3;
- n is an integer from 1 to about 6;
- p is an integer from 1 to about 5;
- and (*) indicates the point of attachment to the rest of the compound and
- a fragment of the formula
- wherein
- each Ra and Rb is independently hydrogen or alkyl;
- or Ra and Rb are taken together with the attached carbon atom to form a carbocyclic ring;
- n1 is an integer selected from 1 to 4;
- and
- (**) indicates points of attachment for other parts of the conjugate;
- and
- A is an adrenocorticoid or a corticosteroid.
17 more elements
Dependencies are inferred from the claim text.