Back to results
US 2022/0016269 A1Published application
Compositions and methods for assessing eye vasculature
AssigneeMediBeacon Inc.
InventorsRichard B. Dorshow, Thomas E. Rogers
Life of this patent
Estimating the term…
Abstract
Compositions and methods for assessing blood vessels and organs of the body are disclosed herein, specifically methods for assessing the vasculature of the eye.
Claims31
A method for assessing the eye vasculature in a subject in need thereof, comprising the steps of:
- a. administering an effective amount of a compound of structural Formula I
- or a salt thereof;
- wherein
- X1 and X2 are independently chosen from —CO(AA), —CN, —CO2R1, —CONR2R3, —COR4, —NO2, —SOR35, —SO2R6, —SO2OR7 and —PO3R8R9;
- wherein at least one of X1 and X2 is —CO(AA);
- Y1 and Y2 are independently chosen from —OR10, —SR11, NR12R13, —N(R14)COR15, —CONH(PS);
- —P(R16)2, —P(OR17)2 and
- each Z1 is independently chosen from a bond, —CR18R19—, —O—, —NR20—, —NCOR21—, —S—, —SO—, and —SO2—;
- each R1 to R21 are independently chosen from hydrogen, C1-C10 alkyl, C1-C10 alkyl substituted with hydroxyl and carboxylic acid, C3-C6 polyhydroxylated alkyl, C5-C10 aryl, C5-C10 heteroaryl, C3-C5 heterocycloalkyl, C3-C5 heterocycloalkyl substituted with C(O), —(CH2)aCO2H, —(CH2)aCO2H substituted with C5-10 heteroaryl, —(CH2)aCONR30R31, —(CH2)aNHSO3−, —(CH2)aNHSO3H, —(CH2)aOH, —(CH2)aOPO3═, —(CH2)aOPO3H2, —(CH2)aOPO3H−, (CH2)aOR22, —(CH2)aOSO3−, —(CH)aOSO3H, —(CH2)aPO3═, —(CH2)aPO3H2, —(CH2)aPO3H−, —(CH2)aSO3, —(CH2)aSO3H, —CH2)dCO(CH2CH2O)cR23, —(CH2)d(CH2CH2O)cR24, —(CHCO2H)aCO2H, —CH2(CHNH2)aCH2NR25R26, —CH2(CHOH)aCO2H, —(CH2(CHOH)aR27, —CH[(CH2)bNH2]aCH2OH, —CH[(CH2)bNH2]aCO2H, and —(CH2)aNR28R29;
- each R22 to R31 are independently chosen from hydrogen, C1-C10 alkyl, and C1-C5-dicarboxylic acid;
- R35 is chosen from C1-C10 alkyl, C1-C10 alkyl substituted with hydroxyl and carboxylic acid, C3-C6 polyhydroxylated alkyl, C5-C10 aryl, C5-C10 heteroaryl, C3-C5 heterocycloalkyl, C3-C5 heterocycloalkyl substituted with C(O), —(CH2)aCO2H, —(CH2)aCO2H substituted with C5-C10 heteroaryl, —(CH2)aCONR30R31, —(CH2)aNHSO3−, —(CH2)aNHSO3H, —(CH2)aOH, —(CH2)aOPO3−, —(CH2)aOPO3H2, —(CH2)aOPO3H−, —(CH2)aOR22, —(CH2)aOSO3−, —(CH2)aOSO3H, —(CH2)aPO3═, —(CH2)aPO3H2, —(CH2)aPO3H−, —(CH2)aSO3−, —(CH2)aSO3H, —(CH2)dCO(CH2CH2O)cR23, —(CH2)d(CH2CH2O)cR24, —(CHCO2H)aCO2H, —CH2(CHNH2)aCH2NR25R26, —CH2(CHOH)aCO2H, —CH2(CHOH)aR27, —CH[(CH2)bNH2]aCH2OH, —CH[(CH2)bNH2]aCO2H, and —(CH2)aNR25R29;
- (AA) is a polypeptide chain comprising one or more natural or unnatural amino acids linked together by peptide bonds;
- (PS) is a sulfated or non-sulfated polysaccharide chain comprising one or more monosaccharide units connected by glycosidic linkages;
- and
- each ‘a’, ‘b’, and ‘d’ are independently chosen from 0 to 10, ‘c’ is chosen from 1 to 100 and each of ‘m’ and ‘n’ independently is an integer from 1 to 3;
- and
- b. irradiating the subject's eye vasculature with non-ionizing radiation, wherein the radiation causes the compound to fluoresce;
- c. detecting the fluorescence of the compound in the subject's eye vasculature;
- and
- d. assessing the eye vasculature within the subject based on the detected fluorescence.
17 more elements
A method of assessing the location of a disease or an injury in a subject's eye vasculature, comprising the steps of:
- a. administering an effective amount of a compound of structural Formula I
- or a salt thereof;
- wherein
- X1 and X2 are independently chosen from —CO(AA), —CN, —CO2R1, —CONR2R3, —COR4, —NO2, —SOR35, —SO2R6, —SO2OR7 and —PO3R8R9;
- wherein at least one of X1 and X2 is —CO(AA);
- Y1 and Y2 are independently chosen from —OR10, —SR11, —NR12R13, —N(R14)COR15, —CONH(PS);
- —P(R16)2, —P(OR17)2 and
- each Z1 is independently chosen from a bond, —CR18R19—, —O—, —NR20—, —NCOR21—, —S—, —SO—, and —SO2—;
- each R1 to R21 are independently chosen from hydrogen, C1-C10 alkyl, C1-C10 alkyl substituted with hydroxyl and carboxylic acid, C3-C6 polyhydroxylated alkyl, C5-C10 aryl, C5-C10 heteroaryl, C3-C5 heterocycloalkyl, C3-C5 heterocycloalkyl substituted with C(O), —(CH2)aCO2H, —(CH2)aCO2H substituted with C5-10 heteroaryl, —(CH2)aCONR30R31, —(CH2)aNHSO3−, —(CH2)aNHSO3H, —(CH2)aOH, —(CH2)aOPO3═, —(CH2)aOPO3H2, —(CH2)aOPO3H−, (CH2)aOR22, —(CH2)aOSO3−, —(CH)aOSO3H, —(CH2)aPO3═, —(CH2)aPO3H2, —(CH2)aPO3H−, —(CH2)aSO3, —(CH2)aSO3H, —(CH2)dCO(CH2CH2O)cR23, —(CH2)d(CH2CH2O)cR24, —(CHCO2H)aCO2H, —CH2(CHNH2)aCH2NR25R26, —CH2(CHOH)aCO2H, —(CH2(CHOH)aR27, —CH[(CH2)bNH2]aCH2OH, —CH[(CH2)bNH2]aCO2H, and —(CH2)aNR28R29;
- each R22 to R31 are independently chosen from hydrogen, C1-C10 alkyl, and C1-C5-dicarboxylic acid;
- R35 is chosen from C1-C10 alkyl, C1-C10 alkyl substituted with hydroxyl and carboxylic acid, C3-C6 polyhydroxylated alkyl, C5-C10 aryl, C5-C10 heteroaryl, C3-C5 heterocycloalkyl, C3-C5 heterocycloalkyl substituted with C(O), —(CH2)aCO2H, —(CH2)aCO2H substituted with C5-C10 heteroaryl, —(CH2)aCONR30R31, —(CH2)aNHSO3−, —(CH2)aNHSO3H, —(CH2)aOH, —(CH2)aOPO3−, —(CH2)aOPO3H2, —(CH2)aOPO3H−, —(CH2)aOR22, —(CH2)aOSO3−, —(CH2)aOSO3H, —(CH2)aPO3═, —(CH2)aPO3H2, —(CH2)aPO3H−, —(CH2)aSO3−, —(CH2)aSO3H, —(CH2)dCO(CH2CH2O)cR23, —(CH2)d(CH2CH2O)cR24, —(CHCO2H)aCO2H, —CH2(CHNH2)aCH2NR25R26, —CH2(CHOH)aCO2H, —CH2(CHOH)aR27, —CH[(CH2)bNH2]aCH2OH, —CH[(CH2)bNH2]aCO2H, and —(CH2)aNR25R29;
- (AA) is a polypeptide chain comprising one or more natural or unnatural amino acids linked together by peptide bonds;
- (PS) is a sulfated or non-sulfated polysaccharide chain comprising one or more monosaccharide units connected by glycosidic linkages;
- and
- each ‘a’, ‘b’, and ‘d’ are independently chosen from 0 to 10, ‘c’ is chosen from 1 to 100 and each of ‘m’ and ‘n’ independently is an integer from 1 to 3;
- and;
- b. irradiating the subject's eye vasculature with non-ionizing radiation, wherein the radiation causes the compound to fluoresce;
- c. detecting the fluorescence of the compound in the subject's eye vasculature;
- and
- d. assessing the location of disease or injury in the subject's eye vasculature, based on the detected fluorescence.
17 more elements
Dependencies are inferred from the claim text.