Immunosuppressive agent and process of producing the same

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

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C07D72172

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053328183

ABSTRACT:
An immunosuppressive agent which has low toxicity and which exhibits excellent effectiveness even if it is orally administered is presented. The immunosuppressive agent of the present invention is characterized in that it contains .delta.-opioid antagonist having high selectivity to .delta.-opioid receptor. The present invention also provides a process of producing a naltrindole derivative characterized by reacting naltrexone or a salt thereof with a phenylhydrazine derivative in a solvent in the presence of methanesulfonic acid.

REFERENCES:
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patent: 4857533 (1989-08-01), Sherman et al.
Chemical Abstract vol. 108, #143295j 1988, Sultano et al, "Naltrindole, a highly selective and potent nonpeptide .delta. opioid receptor antagonist".
Science, pp. 62-72 (Jan. 1989).
Plotnikoff et al, Introduction: Ying-Yang Hypothesis of Immunomodulation, pp. 1-2. (1984).
Journal of Medicinal Chemistry, vol. 31, No. 2, pp. 281-282.
Carr et al., Life Sciences 47:1059 (1990).
P. S. Portoghese et al., Eur. J. Pharmacology 146:185 (1988).
Merck Index, 11th ed. pp. 6274-6274.

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