Use of fullerenes in diagnostic and/or therapeutic agents

Claim 2

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent.

Claim 3

A compound as claimed in claim 1 of formula I R.sub.2.sbsb.n @R.sub.3.sbsb.m R.sub.4.sbsb.n' (I) where n and n' are zero or positive integers; m is an integer having a value of at least 20; @R 3m is a closed curved met-car, fullerene, faux fullerene or fulleroid formed from m mesh aperture ring atoms R 3 which may be the same or different; each R 2 which may be the same or different is a mono or polyatomic species entrapped within the @R 3 .sbsb.m cage; and each R 4 which may be the same or different is a mono or polyatomic species covalently bound to the @R 3 .sbsb.m cage) or a salt thereof.

Claim 4

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, said compound being of formula I R.sub.2.sbsb.n @R.sub.3.sbsb.m R.sub.4.sbsb.n' (I) (where n and n' are zero or positive integers; m is an integer having a value of at least 20; @R 3m is a closed curbed met-car, fullerene, faux fullerene or fulleroid formed from m mesh aperture ring atoms R 3 which may be the same or different; each R 2 which may be the same or different is a mono or polyatomic species entrapped within the @R 3m cage; and each R 4 which may be the same or different is a mono or polyatomic species covalently bound to the @R 3 m cage) or a salt thereof, wherein at least one R 2 is present which is a transition or lanthanide metal and at least one R 4 is present which is a halogen atom.

Claim 5

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, said compound being of formula I R.sub.2.sbsb.n @R.sub.3.sbsb.m R.sub.4.sbsb.n' (I) (where n and n' are zero or positive integers; m is an integer having a value of at least 20; @R 3m is a closed curbed met-car, fullerene, faux fullerene or fulleroid formed from m mesh aperture ring atoms R 3 which may be the same or different; each R 2 which may be the same or different is a mono or polyatomic species entrapped within the @R 3m cage; and each R 4 which may be the same or different is a mono or polyatomic species covalently bound to the @R 3 m cage) or a salt thereof, wherein at least one R 2 is present which is a transition or lanthanide metal and at least one R 4 is present which is a halogen atom.

Claim 6

A compound as claimed in claim 1 comprising a fullerene or fullerene derivative.

Claim 7

A compound as claimed in claim 4 comprising a M n @ C m fullerene derivative (wherein n and m are positive integers and M is a metal) or a conjugate or salt thereof.

Claim 8

A compound as claimed in claim 5 wherein m is an even number 44 to 112, and n is 1, 2, 3 or 4.

Claim 9

A compounds as claimed in claim 6 wherein m is 60, 70, 80 or 82 and n is 1 or 2.

Claim 10

A compound as claimed in claim 5 wherein at least one M in M n @ C m is paramagnetic.

Claim 11

A compound as claimed in claim 2 comprising a @ C m Hal n' fullerene halide (wherein m and n' are positive integers and Hal is F, Cl, Br or I) or a conjugate, inclusion compound or salt thereof.

Claim 12

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, comprising a metallo-carbohedrane or a derivative thereof.

Claim 13

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, comprising a metallo-carbohedrane or a derivative thereof.

Claim 14

A compound as claimed in claim 10 comprising a @M' m .sbsb.1 C m .sbsb.2 metallo-carbohedrane (wherein M' is a transition metal and m 1 and m 2 are positive integers) or a derivative thereof.

Claim 15

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, comprising a Gd encapsulating molecular mesh structure.

Claim 16

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, comprising a Gd encapsulating molecular mesh structure.

Claim 17

A compound as claimed in claim 1 being a dendrimeric compound of formula II (Fu).sub.x (L).sub.y (II) where each Fu is a moiety of formula Ia R.sub.2.sbsb.n @R.sub.3.sbsb.m R'.sub.4.sbsb.n' (Ia) where each R 2 which may be the same or different is a mono or polyatomic species entrapped within the @R 3 .sbsb.m cage; @R 3 .sbsb.m is a closed curved met-car, fullerene, faux fullerene or fulleroid formed from m mesh aperture ring atoms R 3 which may be the same or different, n and n' are zero or positive integers, m is an integer having a value or at least 20, and each R' 4 which may be the same or different is a mono or polyatomic species covalently bound to the @R 3 .sbsb.m cage or is a bond to an L moiety linked to at least one linker moiety L; and x and y are integers each having a value of 1 to 100.

Claim 18

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, comprising at least one curved molecular mesh structure linked to a metal or metal complex coordinating chelant group.

Claim 19

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic or therapeutic agent, comprising at least one curved molecular mesh structure linked to a metal or metal complex coordinating chelant group.

Claim 20

A compound as claimed in claim 14 comprising at least one metal complex coordinating chelant group wherein the chelated complex comprises at least two metal atoms.

Claim 21

A compound as claimed in claim 12 being Gd n @C m (where n and m are positive integers) optionally water-solubilized by derivatisation or carrier enclosure.

Claim 22

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic imaging contrast agent.

Claim 23

A compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof, for use as a diagnostic imaging contrast agent.

Claim 24

A diagnostic composition comprising a sterile pharmaceutically acceptable carrier or excipient together with an image contrast enhancing physiologically tolerable compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof.

Claim 25

A diagnostic composition comprising a sterile pharmaceutically acceptable carrier or excipient together with an image contrast enhancing physiologically tolerable compound comprising a curved or planar molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof.

Claim 26

A composition as claimed in claim 18 wherein said compound contains a diagnostically effective moiety.

Claim 27

A composition as claimed in claim 19 wherein said moiety is enclosed by said molecular mesh structure.

Claim 28

A composition as claimed in claim 19 wherein said moiety is attached to said molecular mesh structure.

Claim 29

A composition as claimed in claim 19 wherein said moiety forms part of the skeleton of said molecular mesh structure.

Claim 30

A composition as claimed in claim 19 wherein said moiety is selected from radiolabels, magnetic labels, elements of atomic number greater than 50, chromophores and fluorophores.

Claim 31

A composition as claims in claim 18 wherein said compound is R.sub.2.sbsb.n @R.sub.3.sbsb.m R.sub.4.sbsb.n (I) where n and n' are zero or positive integers; m is an integer having a value of at least 20: @R 3 .sbsb.m is a closed curved met-car, fullerene, faux fullerene or fulleroid formed from m mesh aperture ring atoms R 3 which may be the same or different; each R 2 which may be the same or different is a mono or polyatomic species entrapped within the @R 3 .sbsb.m cage; and each R 4 which may be the same or different is a mono or polyatomic species covalently bound to the @R 3 .sbsb.m cage) or a salt thereof.

Claim 32

A pharmaceutical composition comprising a sterile pharmaceutically acceptable carrier or excipient together with a therapeutically effective compound comprising a curved molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof.

Claim 33

A pharmaceutical composition comprising a sterile pharmaceutically acceptable carrier or excipient together with a therapeutically effective compound comprising a curved molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof.

Claim 34

A composition comprising a sterile pharmaceutically acceptable carrier or excipient together with a therapeutically effective compound comprising a curved molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof wherein said compound contains a therapeutically effective metal.

Claim 35

A composition comprising a sterile pharmaceutically acceptable carrier or excipient together with a therapeutically effective compound comprising a curved molecular mesh structure in the skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof wherein said compound contains a therapeutically effective metal.

Claim 36

A composition as claimed in claim 25 wherein said compound contains a therapeutically active entity releasably conjugated to said molecular mesh structure.

Claim 37

A composition as claimed in claim 25 wherein said compound comprises a photo-activatable therapeutic entity.

Claim 40

A method as claimed in claim 29 wherein said moiety is a metal having a non-zero magnetic moment and said modality is magnetic resonance imaging or magnetometric imaging.

Claim 41

A method as claimed in claim 29 wherein said moiety is an element having an atomic number greater than 50 and said modality is X-ray CT.

Claim 42

A method as claimed in claim 29 wherein said modality is EIT, infra-red imaging, ultrasound, PET, or SPECT.

Claim 45

A medical apparatus characterized in that at least a portion of the apparatus incorporates or is coated with a curved molecular mesh structure compound comprising a diagnostically or therapeutically effective entity and in the mesh skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof.

Claim 46

A medical apparatus characterized in that at least a portion of the apparatus incorporates or is coated with a curved molecular mesh structure compound comprising a diagnostically or therapeutically effective entity and in the mesh skeleton of which essentially all mesh aperture ring atoms are branching sites, said compound being externally linked to a metal or metal complex coordinating chelant group, or a conjugate, intercalate, inclusion compound or salt thereof.

Claim 47

Apparatus as claimed in claim 34 wherein said diagnostically or therapeutically effective entity is selected from radiolabels, magnetic labels, elements of atomic number greater than 50, chromophores, fluorophores and singlet oxygen generators.