Toray Industries, Inc.

Shu Matsumoto

Hiroshi Nagase

Koji Kawai

Takashi Endo

Akira Mizusuna

Yoshihiro Onoda

Norio Kawabe

Takashi Endoh

Keijiro Takanishi

Katsuhiro Shibayama

Tetsuya Katou

Yoshiaki Katsura

Kohei Arakawa

Naoki Hirayama

This invention is directed to a indole derivative represented by the general formula (1) ##STR1## wherein R.sub.1 stands for alkyl of 1 to 5 carbon atoms, cycloalkylalkyl of 4 to 7 carbon atoms, cycloalkenylalkyl of 5 to 7 carbon atoms, aralkyl of 7 to 14 carbon atoms, trans-alkenyl of 4 or 5 carbon atoms, allyl, furanyl-2-ylalkyl of 1 to 5 carbon atoms, thienyl-2-ylalkyl of 1 to 5 carbon atoms, vinyloxycarbonyl, trichloroethoxycarbonyl, benzyloxycarbonyl, alkanoyl of 1 to 5 carbon atoms, aralkylcarbonyl of 7 to 14 carbon atoms, 2-furoyl, thiophene-2-carbonyl, cycloalkylcarbonyl of 4 to 7 carbon atoms, alkenylcarbonyl of 3 to 8 carbon atoms, or anisoyl, providing that said general formula (1) embraces a (+) form, a (-) form, and a (.+-.) form, or a pharmacologically acceptable salt thereof and to an immunorepressing agent having as an active component thereof the indole derivative or the pharmacologically acceptable salt thereof.

Indole derivatives

An agent for suppressing infiltration of eosinophils comprising as an effective ingredient a tricyclic triazolo derivative, which strongly suppresses infiltration of eosinophils into inflammatory regions, of the formula (I): ##STR1## wherein R.sup.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.5 cycloalkyl or substituted or non-substituted aryl; R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy or halogen; W represents C.dbd.O or CR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 independently represent hydrogen or lower alkyl; A represents C.sub.1 -C.sub.5 straight or branched saturated or unsaturated alkylene with the proviso that it may contain one or more hetero atoms; 1 represents 0 to 2, n represents 1 to 3, -- represents single bond or double bond; Y represents N or C; Z represents C(B)Ar.sup.1 Ar.sup.2 wherein B represents hydrogen, hydroxy or methoxy, Ar.sup.1 and Ar.sup.2 independently represent hydrogen or substituted or non-substituted aryl, CAr.sup.1 Ar.sup.2 wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above, O--CHAr.sup.1 Ar.sup.2 wherein Ar.sup.1 and Ar.sup.2 represent the same meanings as mentioned above or a condensed aromatic ring or a pharmaceutically acceptable salt thereof.

Composition for suppressing infiltration of eosinophils

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.

Immunosuppressive agent and process of producing the same

Methylenediphosphonic acid compounds and methods of use for the

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Kamakura, Japan

Shu Matsumoto