Patent ID: 8372380
Filing Date: 2013-02-12
Classification: A61B,A61K,G01N

Abstract:
1. A method of assessing sulfotransferase (SULT) distribution or activity in a mammal, in vivo, comprising: administering to the mammal a bolus of a radiolabeled tracer; generating radiographic data indicative of tracer uptake in the mammal by scanning the mammal using a radiographic technique; and using the radiographic data to assess SULT distribution or activity in the mammal; wherein the radiolabeled tracer comprises at least one compound selected from the group consisting of (a) phenols having the formula (1) where A 1 is OH and each of A 2 -A 6 is independently selected from the group of moieties denoted by “K” (defined below), provided that at least one of A 2 -A 6 is or contains a radioisotope; or A 1 and A 3 are both OH and each of A 2 , A 4 -A 6 is independently selected from the group of moieties denoted by K, provided that at least one of A 2 , A 4 -A 6 is or contains a radioisotope; (b) naphthols having the formula (2) where B 1 is OH and each of B 2 -B 8 is independently selected from the group of moieties denoted by K, provided that at least one of B 2 -B 8 is or contains a radioisotope; or B 2 is OH and each of B 1 , B 3 -B 8 is independently selected from the group of moieties denoted by K, provided that at least one of B 1 , B 3 -B 8 is or contains a radioisotope; or B 1 and B 3 are each OH and each of B 2 , B 4 -B 8 is independently selected from the group of moieties denoted by K, provided that at least one of B 4 -B 8 is or contains a radioisotope; (c) coumarins having the formula (3) where X and Y are, independently, O, S, or N—R 1 (wherein R 1 is H, alkyl, aryl, [ 11 C]methyl, [ 18 F]fluoroalkyl, [ 18 F]fluoroaryl, [ 123 I]iodoalkyl, [ 123 I]iodoaryl, [ 124 I]iodoalkyl, [ 124 I]iodoaryl,] [ 125 I]iodoalkyl, or [ 125 I]iodoaryl); and wherein C 3 is OH and each of C 1 -C 2 , C 4 -C 6 is independently selected from the group of moieties denoted by K; or C 4 is OH and each of C 1 -C 3 , C 5 -C 6 is independently selected from the group of moieties denoted by K; or C 5 is OH and each of C 1 -C 4 , C 6 is independently selected from the group of moieties denoted by K; or C 6 is OH and each of C 1 -C 5 is independently selected from the group of moieties denoted by K; or C 2 and C 3 ═OH and each of C 1 , C 4 -C 6 is independently selected from the group of moieties denoted by K; or C 2 and C 4 ═OH and each of C 1 , C 3 , C 5 -C 6 is independently selected from the group of moieties denoted by K; or C 2 and C 5 ═OH and each of C 1 , C 3 -C 4 , C 6 is independently selected from the group of moieties denoted by K; or C 2 and C 6 ═OH and each of C 1 , C 3 -C 5 is independently selected from the group of moieties denoted by K; or C 3 and C 5 ═OH and each of C 1 -C 2 , C 4 , C 6 is independently selected from the group of moieties denoted by K; or C 4 and C 6 ═OH and each of C 1 -C 3 , C 5 is independently selected from the group of moieties denoted by K; or C 2 ═C 3 ═C 5 ═OH and each of C 1 , C 4 , C 6 is independently selected from the group of moieties denoted by K; or C 2 , C 4 and C 6 ═OH and each of C 1 , C 3 , C 5 is independently selected from the group of moieties denoted by K; wherein in each case at least one of C 1 -C 6 , X, or Y is or contains a radioisotope; (d) flavones having the formula (4) where X and Y are, independently, O, S, or N—R 1 (wherein R 1 is H, alkyl, aryl, [ 11 C]methyl, [ 18 F]fluoroalkyl, [ 18 F]fluoroaryl, [ 123 I]iodoalkyl, [ 123 I]iodoaryl, [ 124 ]iodoalkyl, [ 124 I]iodoaryl,] [ 125 I]iodoalkyl, or [ 125 I]iodoaryl); and wherein D 3 is OH and each of D 1 -D 2 , D 4 -D 6 is independently selected from the group of moieties denoted by K; or D 4 is OH and each of D 1 -D 3 , D 5 -D 6 is independently selected from the group of moieties denoted by K; or D 5 is OH and each of D 1 -D 4 , D 6 is independently selected from the group of moieties denoted by K; or D 6 is OH and each of D 1 -D 5 is independently selected from the group of moieties denoted by K; or D 2 and D 3 are OH and each of D 1 , D 4 -D 6 is independently selected from the group of moieties denoted by K; or D 2 and D 4 are OH and each of D 1 , D 3 , D 5 -D 6 is independently selected from the group of moieties denoted by K; or D 2 and D 5 are OH and each of D 1 , D 3 -D 4 , D 6 is independently selected from the group of moieties denoted by K; or D 2 and D 6 are OH and each of D 1 , D 3 -D 5 is independently selected from the group of moieties denoted by K; or D 3 and D 5 are OH and each of D 1 -D 2 , D 4 , D 6 is independently selected from the group of moieties denoted by K; or D 4 and D 6 are OH and each of D 1 -D 3 , D 5 is independently selected from the group of moieties denoted by K; or D 2 , D 3 and D 5 are OH, and D 1 , D 4 , D 6 is independently selected from the group of moieties denoted by K; or D 2 , D 4 and D 6 are OH, and D 1 , D 3 , D 5 is independently selected from the group of moieties denoted by K; wherein in each case at least one of D 1 -D 6 , X, or Y is or contains a radioisotope; (e) fused ring compounds having the formula (5) where Z is O, S, N—R 1 (wherein R 1 is H, alkyl, aryl, [ 11 C]methyl, [ 18 F]fluoroalkyl, [ 18 F]fluoroaryl, [ 123 I]iodoalkyl, [ 123 I]iodoaryl, [ 124 1]iodoalkyl, [ 124 1]iodoaryl,] [ 125 I]iodoalkyl, or [ 125 I]iodoaryl), CH 2 , or CH═CH; and W is N or CH; and wherein E2 is OH and each of E1, E 3 -E 5 is independently selected from the group of moieties denoted by K; or E 3 is OH and each of E1-E2, E 4 -E 5 is independently selected from the group of moieties denoted by K; or E 4 is OH and each of E1-E 3 , E 5 is independently selected from the group of moieties denoted by K; or E 5 is OH and each of E1-E 4 is independently selected from the group of moieties denoted by K; or E2 and E 4 are OH and each of E1-E 4 is independently selected from the group of moieties denoted by K; or E 3 and E 5 are OH and each of E1, E2, E 4 , is independently selected from the group of moieties denoted by K; and wherein in each case at least one of E1-E 5 or Z is or contains a radioisotope; (e′) structurally related fused ring compounds in which E1 is a substituted aryl group, said compounds having the formula 5a: where Z is O, S, N—R 1 (wherein R 1 is H, alkyl, aryl, [ 11 C]methyl, [ 18 F]fluoroalkyl, [ 18 F]fluoroaryl, [ 123 I]iodoalkyl, [ 123 I]iodoaryl, [ 124 I]iodoalkyl, [ 124 I]iodoaryl,] [ 125 I]iodoalkyl, or [ 125 I]iodoaryl), CH 2 , or CH═CH; W is N or CH; and P is H, alkyl, aryl, [ 11 C]methyl, 18 F, [ 18 F]fluoroalkyl, [ 18 F]fluoroaryl, 123 I, [ 123 I]iodoalkyl, [ 123 I]iodoaryl, 124 I, [ 124 I]iodoalkyl, [ 124 I]iodoaryl,] 125 I, [ 125 I]iodoalkyl, or [ 125 I]iodoaryl); and wherein E2 is OH and each of E 3 -E 5 is independently selected from the group of moieties denoted by K; or E 3 is OH and each of E2, E 4 -E 5 is independently selected from the group of moieties denoted by K; or E 4 is OH and each of E2-E 3 , E 5 is independently selected from the group of moieties denoted by K; or E 5 is OH and each of E2-E 4 is independently selected from the group of moieties denoted by K; or E2 and E 4 are OH and each of E 3 , E 5 is independently selected from the group of moieties denoted by K; or E 3 and E 5 are OH and each of E2, E 4 is independently selected from the group of moieties denoted by K; wherein in each case at least one of E1-E 5 , I′, or Z is or contains a radioisotope; and wherein R′ is selected from the group consisting of H, NH—CH 3 , N(CH 3 ) 2 NH 2 , OCH 3 , NH—CO—CH 3 , F, I, CN, NO 2 , SO 2 —CH 3 , and radiolabeled isotopes thereof; (f) imidazopyridines having the formula (6): where F 1 -F 5 are the same as E1-E 5 , and wherein at least one of F 1 -F 5 is or contains a radioisotope; or (g) stilbenes having the formula (7): where W 1 and W 2 are, independently, alkyl, aryl, or OH; and wherein G 3 is OH and each of G 1 -G 2 , G 4 -G 10 is independently selected from the group of moieties denoted by K; or G 2 and G 4 are OH and each of G 1 , G 3 , G 5 -G 10 is independently selected from the group of moieties denoted by K; or G 3 and G 8 are OH and each of G 1 -G 3 , G 4 -G 7 , G 9 -G 10 is independently selected from the group of moieties denoted by K; or G 2 =G 4 =G 8 ═OH and each of G 1 , G 3 , G 5 -G 7 , G 9 -G 10 is independently selected from the group of moieties denoted by K; and wherein in each case at least one of G 1 -G 10 is or contains a radioisotope; and wherein, in each of compounds (a)-(g), K is selected from the group consisting of H; alkyl; aryl;