Diagnostic and therapeutic alkylenediamine compounds and process

Drug – bio-affecting and body treating compositions – Radionuclide or intended radionuclide containing; adjuvant... – Attached to cyclopentano-hydrophenanthrene ; derivative thereof

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564305, 568579, 568924, 424 111, 424 91, 424 165, A61K 5100, A61M 3614

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active

060013303

ABSTRACT:
Diamine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided. The diamine compounds or serotonin are characterized by the formula: ##STR1## wherein: l, m and n can be the same or different and are an integer of 1 to 6; X, Y and Z can be the same or different and are hydrogen, halo, haloalkyl, (C.sub.1 -C.sub.6) alkyl, aryl, (C.sub.1 -C.sub.6) alkoxy, N-alkyl, (C.sub.2 -C.sub.6) acyloxy, N-alkylene, --SH, or --SR, wherein R is from the same group as R.sub.1 and R.sub.2 and can be the same or different than R.sub.1 and R.sub.2, amino, nitro, cyano, hydroxy, --C(.dbd.O) OR.sub.6, --C(.dbd.O) NR.sub.5 R.sub.4, NR.sub.3 R.sub.2, or S(.dbd.O).sub.k R.sub.1 wherein .sub.k is 1 or 2, and R.sub.4 to R.sub.6 are independently hydrogen or (C.sub.1 -C.sub.6) alkyl;

REFERENCES:
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Hanson et al (1997), Bioorganic & Medicinal Chemistry Letters, vol. 7, No. 20, pp. 2559-2564 (Oct. 21, 1997), Synthesis and Evaluation of Novel-N-L2-(Bis-aryl-methoxy)ethyl-N-aralkyl-.alpha.,.omega.-Alkanediamine s as Potent and Selective dopamine reuptake inhibitors: Seco analogs of GBR12935 and GBR12909.
Dorota Mateka, et al.
Development of Novel, Potent, and selective dopamine reuptake inhibitors through alterations of the piperazine ring of 1-[2(Diphenylmethoxy)Ethyl]-and 1-[2]BIS(4-Fluorophenyl)Methoxy[Ethyl]-4-(1-Phenylpropyl)Piperazines (GBR 12935 and GBR 12909).
Sanath Meegalla, et al., Tc-99m-Labeled Tropanes as Dopamine Transporter Imaging Agents, Biconjugate Chem., 1996,, 7, pp. 421-429.

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