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US 2019/0343958 A1Published application
Conjugates of kinase inhibitors and cyanine dyes
AssigneeSmall Molecule PPI Mimics LLC
InventorsKevin Burgess, Syed Muhammad Usama
Life of this patent
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Abstract
The present disclosure provides conjugates of kinase inhibitors and cyanine dyes, as well as related compositions, methods and uses.
Claims35
A conjugate of Formula (I):
- Cy-L-K (I)
- or a pharmaceutically acceptable salt thereof, wherein:
- Cy is a cyanine dye;
- L is a linker selected from optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, or a combination thereof;
- K is moiety comprising a kinase inhibitor;
- and
- each — is a covalent bond, or
- a conjugate of Formula (II):
- K-L-Cy-L-K (II)
- or a pharmaceutically acceptable salt thereof, wherein:
- Cy is a cyanine dye;
- each L independently is a linker;
- each K independently is moiety comprising a kinase inhibitor;
- and
- each — is a covalent bond.
12 more elements
(canceled)
4-5. (canceled)
(canceled)
9-11. (canceled)
(canceled)
(canceled)
20-24. (canceled)
26-28. (canceled)
31-35. (canceled)
37-39. (canceled)
(canceled)
43-44. (canceled)
46-47. (canceled)
A compound of Formula (III):
- or a pharmaceutically acceptable salt thereof, wherein:
- X is a leaving group;
- Z is one or more anions to achieve electrical neutrality;
- R13 and R14 independently are hydrogen or halogen;
- R17 and R18 independently are alkyl, heteroalkyl, aryl or heteroaryl;
- and
- R19 and R20 independently are hydrogen, optionally substituted aliphatic, optionally substituted heteroaliphatic, or a nitrogen protecting group.
4 more elements
49-55. (canceled)
A conjugate of Formula (IV):
- A-Cy-L-K (IV)
- or a pharmaceutically acceptable salt thereof, wherein:
- A is a biomolecule;
- Cy is a cyanine dye;
- L is a linker selected from optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, or a combination thereof;
- K is moiety comprising a kinase inhibitor;
- and
- each — is a covalent bond;
- or
- a conjugate of Formula (V):
- or a pharmaceutically acceptable salt thereof, wherein:
- A is a biomolecule:
- Cy is a cyanine dye;
- each L independently is a linker selected from optionally substituted aliphatic, optionally substituted heteroaliphatic, optionally substituted aryl, optionally substituted heteroaryl, or a combination thereof:
- each K independently is moiety comprising a kinase inhibitor;
- and
- each — is a covalent bond.
14 more elements
(canceled)
Dependencies are inferred from the claim text.