(radio) labelled biotin derivatives

Details (radio) labelled biotin derivatives (radio) labelled biotin derivatives

C - Chemistry, Metallurgy

07

F

C07F 13/00 (2006.01) A61K 49/00 (2006.01) A61K 49/08 (2006.01) A61K 51/04 (2006.01) C07D 495/04 (2006.01) C07F 1/00 (2006.01) C07F 5/00 (2006.01) C07F 7/22 (2006.01) C07F 7/24 (2006.01) C07F 9/66 (2006.01) C07F 11/00 (2006.01) C07F 15/00 (2006.01) C07K 5/08 (2006.01)

Patent

CA 2232411

The invention relates to a labelled biotin compound, wherein said biotin compound is represented by general formula (I) wherein: n is 1 or 2, R is a chelating group for chelating a metal atom, and Sp is a spacing group having at least 4 atoms spacing NH from R; and wherein said biotin compound is labelled with a metal atom selected from (a) the group consisting of the radioactive isotopes 99mTc, 203Pb, 66Ga, 67Ga, 68Ga, 72As, 111In, 113mIn, 114mIn, 97Ru, 62Cu, 64Cu, 52Fe, 52mMn, 51Cr, 186Re, 188Re, 77As, 90Y, 67Cu, 169Er, 117mSn, 121Sn, 127Te, 142Pr, 143Pr, 198Au, 199Au, 149Tb, 161Tb, 109Pd, 165Dy, 149Pm, 151Pm, 153Sm, 157Gd, 166Ho, 172Tm, 169Yb, 175Yb, 177Lu, 105Rh and 111Ag or (b) the group consisting of the paramagnetic metal atoms Cr, Mn, Fe, Co, Ni, Cu, Pr, Nd, Sm, Yb, Gd, Tb, Dy, Ho and Er; said metal atom being attached to the biotin compound by means of said chelating group. The invention further relates to a pharmaceutical composition comprising said labelled biotin compound, to the use of said composition for diagnosis and therapy, and to a kit for preparing a radiopharmaceutical composition.

Composé de biotine marqué dans lequel ledit composé de biotine est représenté par la formule générale (I). Dans la formule, n vaut 1 ou 2, R représente un groupe de chélateur servant à chélater un atome métallique, et Sp représente un groupe d'espacement comprenant au moins 4 atomes qui écartent NH de R; ledit composé de biotine étant marqué avec un atome métallique sélectionné dans (a) le groupe formé par les isotopes radioactifs ?99m¿Tc, ?203¿Pb, ?66¿Ga, ?67¿Ga, ?68¿Ga, ?72¿As, ?111¿In, ?113m¿In, ?114m¿In, ?97¿Ru, ?62¿Cu, ?64¿Cu, ?52¿Fe, ?52m¿Mn, ?51¿Cr, ?186¿Re, ?188¿Re, ?77¿As, ?90¿Y, ?67¿Cu, ?169¿Er, ?117m¿Sn, ?121¿Sn, ?127¿Te, ?142¿Pr, ?143¿Pr, ?198¿Au, ?199¿Au, ?149¿Tb, ?161¿Tb, ?109¿Pd, ?165¿Dy, ?149¿Pm, ?151¿Pm, ?153¿Sm, ?157¿Gd, ?166¿Ho, ?172¿Tm, ?169¿Yb, ?175¿Yb, ?177¿Lu, ?105¿Rh and ?111¿Ag ou dans (b) le groupe formé par les atomes métalliques paramagnétiques Cr, Mn, Fe, Co, Ni, Cu, Pr, Nd, Sm, Yb, Gd, Tb, Dy, Ho et Er; ledit atome métallique étant attaché au composé de biotine par ledit groupe chélateur. Cette invention concerne également une composition pharmaceutique comprenant ledit composé de biotine marqué, l'utilisation de cette même composition pour le diagnostic et la thérapie, et un nécessaire servant à préparer une composition pharmaceutique radiomarquée.

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