Iodotamoxifen derivatives and use for estrogen receptor-positive

Details Iodotamoxifen derivatives and use for estrogen receptor-positive Iodotamoxifen derivatives and use for estrogen receptor-positive

1987-09-09

1989-06-13

Maples, John S.

Drug, bio-affecting and body treating compositions

Radionuclide or intended radionuclide containing; adjuvant...

564324, 548575, 514428, 514651, 5142392, 514317, 514648, 544174, 546236, A61K 4902, C07D20704, C07C 9306

Patent

active

048391557

ABSTRACT:
Iodotamoxifen derivatives which are compounds of formula (3) ##STR1## wherein X represents 3- or 4- iodo and R.sup.1 and R.sup.2, which may be the same or different, represent C.sub.1-3 alkyl, especially methyl or ethyl, groups or R.sup.1 represents a hydrogen atom and R.sup.2 a C.sub.1-3 alkyl group or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group, especially a pyrrolidino, piperidino, 4-methylpiperidino or morpholino group, and their pharmaceutically acceptable acid addition salts are potent anti-estrogenic compounds useful for treatment of estrogen receptor-positive (hormone-dependent) breast cancers.
Radioisotopic iodotamoxifen derivatives of formula (3) are useful in radiotherapy or gamma ray imaging of these cancers.

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