Immunosuppressive agent and process of producing the same
AssigneeToray Industries, Inc.
InventorsHiroshi Nagase, Koji Kawai, Shu Matsumoto, Takashi Endoh, Yoshiaki Katsura, Kohei Arakawa
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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.
Claims10
A method for effecting immunosuppression in a subject, which comprises administering to a subject in need of immunosuppression, an amount of a .delta.-opioid receptor antagonist, or a pharmaceutically acceptable salt thereof, in an amount sufficient to effect immunosuppression in said subject chlorine, bromine, amino, nitro, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or R.sub.4 and R.sub.5 together represent benzo.
- wherein said .delta.-opioid antagonist is a compound represented by the formula (1):
- ##STR7## wherein R.sub.1 represents C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.6 cycloalkylalkyl, C.sub.5 -C.sub.7 cycloalkenylalkyl, aryl, aralkyl, C.sub.4 -C.sub.5 trans-alkenyl, allyl or furan-2-ylalkyl, R.sub.2 represents hydrogen, hydroxy or C.sub.1 -C.sub.5 alkanoyloxy, R.sub.3 represents hydrogen, C.sub.1 -C.sub.5 alkyl or C.sub.1 -C.sub.5 alkanoyl, X represents oxygen, sulfur or nitrogen to which a radical Y is attached, wherein Y represents hydrogen or C.sub.1 -C.sub.5 alkyl, R.sub.4 and R.sub.5 individually represent hydrogen, fluorine,
Dependencies are inferred from the claim text.