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US 2011/0257583 A2Published application
Thiadiazole Compounds and Uses Thereof
OwnerRaghavan RAJAGOPALAN, Frederick JACOBS +1inventors
InventorsRaghavan RAJAGOPALAN, Frederick JACOBS, Richard DORSHOW
Life of this patent
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Abstract
Thiadiazole compounds, compositions, bioconjugates, and methods for targeting and photoactivation at target sites.
Claims16
A compound of Formula I
- wherein:
- each of R1, R2, R3, and R4 is independently hydrogen, C1-C10 alkyl, C5-C10 aryl, C5-C10 heteroaryl, C1-C10 acyl, halogen, nitro, cyano, —(CH2)aOR5, —(CH2)aCO2R5, —(CH2)aNR5R6, —NR6COR5, —(CH2)aCONR5R6, —(CH2)aSR5, —(CH2)aSOR5, —(CH2)aSO2R5, —(CH2)aCON(R5)E, —(CH2)aN(R5)COE, —(CH2)aN(R5)CON(R6)E, or —(CH2)aN(R5)CSN(R6)E;
- or R1 and R2, R2 and R3, or R3 and R4, together with the carbon atoms to which they are attached, independently form alicyclic or heterocyclic structures wherein a combination of R1 and R2, or a combination of R2 and R3, or a combination of R3 and R4 is —(CH2)bX(CH2)c—, —C(R7)═C(R8)—C(R9)═C(R10)—, —N═C(R7)—C(R8)═C(R9)—, —C(R7)═N—C(R8)═C(R9)—, —C(R7)═C(R8)—N═C(R9)—, —C(R7)═C(R8)—C(R9)═N—, —C(R7)═C(R8)—N(R9)—, —C(R7)═C(R8)—O—, —C(R7)═C(R8)—S—, —N═C(R7)—N(R8)—, —N═C(R7)O—, —N═C(R7)—S—, —C(R7)═N—N(R8)—, —C(R7)═N—N(R8)—, —C(R7)═N—O—, —N═N—N(R8)—, —N═N—O—, or —N═N—S—;
- each of b and c independently varies from 0 to 3;
- X is from —O—, —NR11—, —S—, —SO—, or —SO2—;
- each of R5 to R11 is independently hydrogen, C1-C10 alkyl, C5-C10 aryl, C1-C10 hydroxyalkyl, C1-C10 alkoxyalkyl, C5-C10 heteroaryl, C1-C10 acyl, halogen, nitro, cyano, —(CH2)aOR12, —(CH2)aCO2R12, —(CH2)aNR12R13, —NR13COR12, —(CH2)aCONR12R13, —(CH2)aSR12, —(CH2)aSOR12, —(CH2)aSO2R12, —(CH2)aCON(R12)E, —(CH2)aN(R12)COE, —(CH2)aN(R12)CON(R13)E, or —(CH2)aN(R12)CSN(R13)E;
- wherein at least one of R1 to R4 is independently —(CH2)aCON(R5)E, —(CH2)aN(R5)COE, —(CH2)aN(R5)CON(R6)E, or —(CH2)aN(R5)CSN(R6)E;
- or wherein at least one of R5 to R11 is independently —(CH2)aCON(R12)E, —(CH2)aN(R12)COE, —(CH2)aN(R12)CON(R13)E, or —(CH2)aN(R12)CSN(R13)E;
- a varies from 0 to 10;
- each of R12 and R13 is independently hydrogen, C1-C10 alkyl, C5-C10 aryl, C1-C10 hydroxyalkyl, C1-C10 alkoxyalkyl, C5-C10 heteroaryl, and C1-C10 acyl;
- and
- each E is independently a whole or fragmented somatostatin receptor binding molecule, a whole or fragmented ST receptor binding molecule, a whole or fragmented neurotensin receptor binding molecule, a whole or fragmented bombesin receptor binding molecule, a whole or fragmented CCK receptor binding molecule, a whole or fragmented steroid receptor binding molecule, or a whole or fragmented carbohydrate receptor binding molecule.
9 more elements
10-19. (canceled)
Dependencies are inferred from the claim text.