Integrated photoactive agents and uses thereof
View Patent ↗The present invention discloses a number of photoactive compounds designed to bind and inhibit serine proteases. Compounds disclosed herein may be utilized in a number of appropriate medical diagnostic and/or therapeutic procedures such as the monitoring of hemostasis, imaging and/or treatment of vulnerable plaques, and/or tumor imaging and/or treatment.
1. A method of performing a diagnostic, imaging, or visualization procedure on a patient, comprising:
administering to a patient a diagnostically effective amount of a compound of Formula 1,
wherein:
each of R 1 , R 2 , R 3 , R 4 , X 1 , and X 2 is independently hydrogen, —OH, C1-C6 alkyl, C1-C6 acyl, C1-C6 alkoxycarbonyl, C1-C6 hydroxyalkyl, C1-C6 polyhydroxyalkyl, C1-C6 carboxyalkyl, C1-C6 aminoalkyl, C5-C10 aryl, —(CH 2 ) m —Y—C(═NH)NH 2 , —(CH 2 ) m (CHR 5 ) n —Y—C(═NH)NH 2 , —(CH 2 ) m (CHR 5 ) n —Y—NHC(═NH)NH 2 , —(CH 2 ) m —Y—NHC(═NH)NH 2 , —O—(CHR 5 ) n —Y—C(═NH)NH 2 , —O—(CHR 5 ) n —Y—NHC(═NH)NH 2 , —N(R 6 )—(CH 2 ) m (CHR 5 ) n —Y—C(═NH)NH 2 , or —N(R 7 )—(CH 2 ) m (CHR 5 ) n —Y—NHC(═NH)NH 2 ;
Y is
with the proviso that at least one of R 1 , R 2 , R 3 , R 4 , X 1 , or X 2 is —(CH 2 ) m —Y—C(═NH)NH 2 , —(CH 2 ) m (CHR 5 ) n —Y—C(═NH)NH 2 , —(CH 2 ) m (CHR 5 ) n —Y—NHC(═NH)NH 2 , —(CH 2 ) m —Y—NHC(═NH)NH 2 , —O—(CHR 5 )n—Y—C(═NH)NH 2 , —O—(CHR 5 ) n —Y—NHC(═NH)NH 2 , —N(R 6 )—(CH 2 ) m (CHR 5 ) n —Y—C(═NH)NH 2 , or —N(R 7 )—(CH 2 ) m (CHR 5 ) n —Y—NHC(═NH)NH 2 ;
each of ‘m,’ ‘n,’ and ‘p’ is independently 0, 1, 2, 3, 4, 5, or 6;
R 5 is hydroxyl, C1-C6 hydroxyalkyl, carboxyl, C1-C6 carboxyalkyl, amino, or C1-C6 aminoalkyl; and
each of R 6 and R 7 is independently hydrogen, C1-C6 alkyl, C1-C6 acyl, C1-C6 alkoxycarbonyl, C1-C6 hydroxyalkyl, C1-C6 polyhydroxyalkyl, C1-C6 carboxyalkyl, C1-C6 aminoalkyl, or C5-C10 aryl;
allowing the compound to become localized in or around a tissue or organ; and
performing a diagnostic, imaging, or visualization procedure on the patient.
2. The method of claim 1 , wherein the diagnostic procedure is monitoring hemostasis.
3. The method of claim 1 , wherein the diagnostic procedure is imaging vulnerable plaques.
4. The method of claim 1 , wherein the diagnostic procedure is tumor imaging.