Water soluble anionic bacteriochlorophyll derivatives and their uses

Abstract

The invention provides anionic water-soluble tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one, preferably two or three, negatively charged groups and/or acidic groups that are converted to negatively charged groups at the physiological pH, preferably Bchls having a group COO<->, COS<->, SO3<->, PO3<2->, COOH, COSH, SO3H, and/or PO3H2 bound through an ester or amide bond to one or more of the positions 17<3>, 13<3>, and 3<2> of the tetracyclic or pentacyclic Bchl molecule, for photodynamic therapy and diagnosis.

1 - 50 . (canceled) 
     
     
         51 . A method of treating a tumor in a patient by vascular-targeted photodynamic therapy (VTP), the method comprising:
 (a) administering to a patient having a tumor an effective amount of a compound selected from the group consisting of:   Palladium 3 1 -(3-sulfopropylimino)-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 ,17 3 -di(3-sulfopropyl)amide tripotassium salt;   Palladium 3 1 -(3-sulfopropylamino)-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 ,17 3 -di(3-sulfopropyl)amide tripotassium salt;   Palladium 3 1 -oxo-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 -(3-phosphopropyl)amide tripotassium salt;   Palladium 3 1 -oxo-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 ,17 3 -di(3-sulfopropyl)amide dipotassium salt; and   Palladium 3 1 -oxo-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1  2-carboxyethyl)amide dipotassium salt; and   (b) irradiating local area of the tumor with an effective dose of light of appropriate wavelength,   wherein the tumor is selected from melanoma, brain tumor, esophageal tumor, and bladder tumor.   
     
     
         52 . The method of  claim 51 , wherein the tumor is melanoma. 
     
     
         53 . The method of  claim 51 , wherein the tumor is brain tumor. 
     
     
         54 . The method of  claim 51 , wherein the tumor is esophageal tumor. 
     
     
         55 . The method of  claim 51 , wherein the tumor is bladder tumor. 
     
     
         56 . The method of  claim 51 , wherein the compound is Palladium 3 1 -(3-sulfopropylimino)-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 ,17 3 -di(3-sulfopropyl)amide tripotassium salt. 
     
     
         57 . The method of  claim 51 , wherein the compound is Palladium 3 1 -(3-sulfopropylamino)-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 ,17 3 -di(3-sulfopropyl)amide tripotassium salt. 
     
     
         58 . The method of  claim 51 , wherein the compound is Palladium 3-oxo-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 -(3-phosphopropyl)amide tripotassium salt. 
     
     
         59 . The method of  claim 51 , wherein the compound is Palladium 3-oxo-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1 ,17 3 -di(3-sulfopropyl)amide dipotassium salt. 
     
     
         60 . The method of  claim 51 , wherein the compound is Palladium 3 1 -oxo-15-methoxycarbonylmethyl-rhodobacteriochlorin 13 1  2-carboxyethyl)amide dipotassium salt. 
     
     
         61 . The method of  claim 51 , wherein the light has a wavelength of about 670-780 nm.