Fibroblast activation protein ligand-containing compounds and their uses

Claims

1. A compound selected from the group consisting of compounds Hex-[Cys(tMeBn(DOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-3554) of the following formula And compounds Hex-[Cys(tMeBn(DOTA-PP))-Pro-Pro-Thr-Gln-Phe-Cys]-Asp-NH2 (3BP-3407) of the following formula .

2. The compound of claim 1, wherein the compound is a compound Hex-[Cys(tMeBn(DOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-3554) of the following formula .

3. The compound of claim 1, wherein the compound is a compound Hex-[Cys(tMeBn(DOTA-PP))-Pro-Pro-Thr-Gln-Phe-Cys]-Asp-NH2 (3BP-3407) of the following formula .

4. The compound according to any one of claims 1 to 3, wherein the compound comprises a diagnostically active nuclide or a therapeutically active nuclide, wherein preferably the diagnostically active nuclide is a diagnostically active radionuclide, more preferably selected from the group consisting of 43 Sc, 44 Sc, 51 Mn, 52 Mn, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 94m Tc, 99m Tc, 111 In, 152 Tb, 155 Tb, 201 Tl, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I, 125 I, preferably 43 Sc, 44 Sc, 64 Cu, 67 Ga, 68 Ga, 86 Y, 89 Zr, 99m Tc, 111 In, 152 Tb, 155 Tb, 203 Pb, 18 F, 76 Br, 77 Br, 123 I, 124 I, 125 I and most preferably 64 Cu, 68Ga, 89 Zr, 99m Tc, 111 In, 18 F, 123 I and 124 I, wherein the therapeutically active nuclide is a therapeutically active radionuclide, more preferably selected from the group consisting of 47 Sc, 67 Cu, 89 Sr, 90 Y, 153 Sm, 149 Tb, 161 Tb, 177 Lu, 186 Re, 188 Re, 212 Pb, 213 Bi, 223 Ra, 225 Ac, 226 Th, 227 Th, 131 I, 211 At, preferably 47 Sc, 67 Cu, 90 Y, 177 Lu, 188 Re, 212 Pb, 213 Bi, 225 Ac, 227 Th, 131 I, 211 At and most preferably 90 Y, 177 Lu, 225 Ac, 227 Th, 131 I and 211 At.

5. The compound according to claim 4, wherein the compound is selected from the group including compound Hex-[Cys(tMeBn(InDOTA-PP))-Pro-Pro-Thr-Gln-Phe-Cys]-Asp-NH2 (3BP-3590) of the following formula , compound Hex-[Cys(tMeBn(LuDOTA-PP))-Pro-Pro-Thr-Gln-Phe-Cys]-Asp-NH2 (3BP-3591) of the following formula , compound Hex-[Cys(tMeBn(GaDOTA-PP))-Pro-Pro-Thr-Gln-Phe-Cys]-Asp-NH2 (3BP-3592) of the following formula , compound Hex-[Cys(tMeBn(EuDOTA-PP))-Pro-Pro-Thr-Gln-Phe-Cys]-Asp-NH2 (3BP-3661) of the following formula , the compound Hex-[Cys(tMeBn(InDOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-3623) of the following formula , the compound Hex-[Cys(tMeBn(LuDOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-3624) of the following formula , the compound Hex-[Cys(tMeBn(EuDOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-3662) of the following formula , the compound Hex-[Cys(tMeBn(GaDOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-3949) of the following formula , the compound Hex-[Cys-(tMeBn(CuDOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-4293) of the following formula And the compound Hex-[Cys-(tMeBn(ZnDOTA-AET))-Pro-Pro-Thr-Gln-Phe-Cys]-OH (3BP-4343) of the following formula .

6. The compound of any one of claims 1 to 5 for use in a method of diagnosing a disease, for use in a method of treating a disease, for use in a method of identifying a subject wherein the subject is likely to respond or likely not to respond to treatment for a disease, wherein the method of identifying a subject comprises carrying out the diagnostic method using the compound of any one of claims 1 to 5, preferably the method for diagnosing a disease described in any one of the preceding claims, or for use in a method of selecting a subject from a group of subjects wherein the subject is likely to respond or likely not to respond to treatment for a disease, wherein the method of selecting a subject from a group of subjects comprises carrying out the diagnostic method using the compound of any one of claims1-5, preferably a method for diagnosing a disease described in any one of the preceding paragraphs, or for use in a method for stratifying a group of subjects into subjects who are likely to respond to treatment for a disease and subjects who are likely not to respond to treatment for a disease, wherein the method for stratifying a group of subjects comprises performing a diagnostic method using a compound according to any one of paragraphs 1-5, preferably a method for diagnosing a disease described in any one of the preceding paragraphs.

7. A composition, preferably a pharmaceutical composition, wherein the composition comprises a compound according to any one of claims 1 to 5 and a pharmaceutically acceptable excipient.

8. A kit comprising a compound according to any one of claims 1-5, one or more optional excipients and optionally one or more devices, wherein the device(s) is(are) selected from the group consisting of a labeling device, a purification device, a processing device, a radioprotection device, an assay device or an administration device.

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