Cationic technetium complexes useful as radiodiagnostic agents

Claim 1

A cationic lipophilic complex of technetium wherein all of the coordination positions of the technetium atom are filled with a donor atom having a pair of electrons available for forming a coordinate bond with technetium to form said cationic complex, said donor atoms being provided by ligands or salts thereof, said ligands having the following structure: ##STR9## wherein: i is an integer from 1 to 6; R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups, and R plus R i may be taken together to form a cyclic compound or separately to form a linear compound; Y 1 , Y 2 , Y 3 , Y 4 , Y 5 and Y 6 are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; A 1 , A 2 , A 3 , A 4 , A 5 and A 6 are each, independently, a donor atom having a free electron pair available for complexing with Tc-99m or Tc-99 to form a cationic complex; and k 1 , k 2 , k 3 , k 4 , k 5 and k 6 are each independently zero or one; ##STR10## wherein: R, R' and R" are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocylcloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; X and X' are saturated or unsaturated alkyl groups; A, A' and A" are independently selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99 to form a cationic complex; t and t' are independently 0 or 1; n is 0, 1 or 2; and n' and n" are independently the integer 1 or 2; or ##STR11## wherein R, R', R" and R'" are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocylcloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; A', A" and A'" are independently selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99 to form a cationic complex; B is an atom selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99, boron, or from the elements of Group IV A of the periodic table; m is 0 or 1; and n', n" and n'" are independently the integer 1 or 2.

Claim 10

A method for making a cationic complex comprising Tc-99m for radioscintigraphic imaging, said method comprising admixing, in a suitable solvent at a basic pH, 99m Tc pertechnetate and a ligand or a salt thereof, said ligand having the formula: ##STR17## wherein: i is an integer from 1 to 6; R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups, and R plus R i may be taken together to form a cyclic compound or separately to form a linear compound; Y 1 , Y 2 , Y 3 , Y 4 , Y 5 and Y 6 are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; A 1 , A 2 , A 3 , A 4 , A 5 and A 6 are each, independently a donor atoms having a free-electron pair available for complexing with Tc-99m or Tc-99 to form a cationic complex; and k 1 , k 2 , k 3 , k 4 , k 5 and k 6 are each independently zero or one; ##STR18## wherein: R, R' and R" are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocylcloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; X and X' are saturated or unsaturated alkyl groups; A, A' and A" are independently selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99 to form a cationic complex; t and t' are independently 0 or 1; n is 0, 1 or 2; and n' and n" are independently the integer 1 or 2; or ##STR19## wherein R, R', R" and R'" are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; A', A" and A'" are independently selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99 to form a cationic complex; B is an atom selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99, boron, or from the elements of Group IV A of the periodic table; m is 0 or 1; and n', n" and n'" are independently the integer 1 or 1; thus forming the cationic complex.

Claim 11

A method for making a cationic complex comprising Tc-99m for radioscintigraphic imaging, said method comprising admixing, in a suitable solvent at a basic pH, 99m Tc pertechnetate and a ligand or a salt thereof, said ligand having the formula: ##STR17## wherein: i is an integer from 1 to 6; R, R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are each independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups, and R plus R i may be taken together to form a cyclic compound or separately to form a linear compound; Y 1 , Y 2 , Y 3 , Y 4 , Y 5 and Y 6 are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; A 1 , A 2 , A 3 , A 4 , A 5 and A 6 are each, independently a donor atoms having a free-electron pair available for complexing with Tc-99m or Tc-99 to form a cationic complex; and k 1 , k 2 , k 3 , k 4 , k 5 and k 6 are each independently zero or one; ##STR18## wherein: R, R' and R" are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocylcloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; X and X' are saturated or unsaturated alkyl groups; A, A' and A" are independently selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99 to form a cationic complex; t and t' are independently 0 or 1; n is 0, 1 or 2; and n' and n" are independently the integer 1 or 2; or ##STR19## wherein R, R', R" and R'" are independently selected from hydrogen or substituted or unsubstituted alkyl, aryl, alkylaryl, arylalkyl, monocycloalkyl, polycycloalkyl, heterocyclic and carbocyclic groups; A', A" and A'" are independently selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99 to form a cationic complex; B is an atom selected from the group of donor atoms having a pair of electrons available for complexing with Tc-99m or Tc-99, boron, or from the elements of Group IV A of the periodic table; m is 0 or 1; and n', n" and n'" are independently the integer 1 or 1; thus forming the cationic complex.

Claim 22

A method for visualizing the heart or the hepatobiliary system of a mammal by radioscintigraphy, said method comprising injecting into the mammal the cationic complex of any of claims 1 through 8, and scanning the mammal using radioscintigraphic imaging apparatus.