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US 2009/0263327 A1Published application
Minimally invasive physiological function monitoring agents
AssigneeMallinckrodt Inc.
InventorsSamuel Achilefu, Raghavan Rajagopalan, Richard B. Dorshow, Joseph E. Bugaj, Muthunadar P. Periasamy
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Abstract
Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.
Claims38
A compound having the formula
- wherein R37, R38, R39, R40, R41, R42, R43, R44 and R45, Y5, and Z5 are independently selected from the group consisting of —H, C1-C10 alkoxyl, C1-C10 polyalkoxyalkyl, C1-C20 polyhydroxyalkyl, C5-C20 polyhydroxyaryl, saccharides, amino, C1-C10 aminoalkyl, cyano, nitro, halogen, hydrophilic peptides, arylpolysulfonates, C1-C10 alkyl, C5-C20 aryl, —SO3T, —CO2T, —OH, —(CH2)aSO3T, —(CH2)aOSO3T, —(CH2)aNHSO3T, —(CH2)aCO2(CH2)bSO3T, —(CH2)aOCO(CH2)bSO3T, —(CH2)aCONH(CH2)bSO3T, —(CH2)aNHCO(CH2)bSO3T, —(CH2)aNHCONH(CH2)bSO3T, —(CH2)aNHCSNH(CH2)bSO3T, —(CH2)aOCONH(CH2)bSO3T, —(CH2)aPO3HT, —(CH2)aPO3T2, —(CH2)aOPO3HT, —(CH2)aOPO3T2, —(CH2)aNHPO3HT, —(CH2)aNHPO3T2, —(CH2)aCO2(CH2)bPO3HT, —(CH2)aCO2(CH2)bPO3T2, —(CH2)aOCO(CH2)bPO3HT, —(CH2)aOCO(CH2)bPO3T2, —(CH2)aCONH(CH2)bPO3HT, —(CH2)aCONH(CH2)bPO3T2, —(CH2)aNHCO(CH2)bPO3HT, —(CH2)aNHCO(CH2)bPO3T2, —(CH2)aNHCONH(CH2)bPO3HT, —(CH2)aNHCON H(CH2)bPO3T2, —(CH2)aNHCSNH(CH2)bPO3HT, —(CH2)aNHCSNH(CH2)bPO3T2, —(CH2)aOCONH(CH2)bPO3HT, —(CH2)aOCONH(CH2)bPO3T2, —CH2(CH2—O—CH2)c-CH2—OH, —(CH2)d-CO2T, —CH2-(CH2—O—CH2)e-CH2-CO2T, —(CH2)f-NH2, —CH2-(CH2—O—CH2)g-CH2-NH2, —(CH2)h-N(Ra)-(CH2)i-CO2T, and —(CH2)j-N(Rb)-CH2 -(CH2—O—CH2)k-CH2-CO2T;
- each of W5 and X5 is independently selected from the group consisting of —NRc, —Se, and —S—;
- V5 is a single bond or is selected from —O—, —S—, —Se—, and —NRa;
- D5 is a single or a double bond;
- each of A5 and B5 is independently —O—, —S—, —Se—, —P—, —NRa, —CRcRd, alkyl, and —C=O;
- E5 is selected from the group consisting of —S—, —Se—, —P—, —NRa, CRcRd, —CRc, alkyl, and —C=O;
- A5, B5, D5, and E5 may together form a 6 or 7 membered carbocyclic ring or a 6 or 7 membered heterocyclic ring optionally containing one or more oxygen, nitrogen, or sulfur atom;
- each of a, b, d, f, h, i, and j independently vary from 1-10;
- each of c, e, g, and k independently vary from 1-100;
- each of a5 and b5 vary from 0 to 5;
- each of Ra, Rb, Rc, and Rd is defined in the same manner as Y5;
- and
- T is either H or a negative charge.
10 more elements
The compound of claim I wherein each of W5 and X5 is —S—.
Dependencies are inferred from the claim text.