Radioimaging and radiochemotherapy phenolic thioether amines...

C - Chemistry – Metallurgy – 07 – C

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C07C 323/41 (2006.01) A61K 31/135 (2006.01) A61K 31/22 (2006.01) A61K 51/00 (2006.01) C07C 323/25 (2006.01)

Patent

CA 2140293

Hydroxyphenylthioalkyl amines represented by formula (I), wherein R1 is H or C1-C8 alkyl; R2 is H or C1-C8 alkyl; R3 is H, C1-C8 alkyl or C1-C8 alkanoyl; R4 is H or C1-C8 alkanoyl; Ra is a radioactive material useful in radioimaging and/or radiochemotherapy where the dottet line (---) indicates: 1) Ra is covalently bound to the structure of formula (I); 2) Ra is ionically associated with the structure of formula (I); 3) Ra is radioactive carbon which is part of the structure of formula (I); and x is 1 to 5, with the provisos that when x is 1, one of R1, R2 or R3 is other than H, and that the sulphur containing group and the Ra group are in the 2, 4 or 6 positions of the phenyl ring, are useful in radioimaging and radiotherapy. Pre- ferred compounds for use in radioimaging are N-acetyl-4-S-cysteaminylphenol and N-[2-[(4'-acetoxyphenyl)thio]ethyl]acet- amide. The O-acylated derivatives are novel and are also useful in treatment of pigment disorders.

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