Indole derivatives, process for producing the same and medicinal

Details Indole derivatives, process for producing the same and medicinal Indole derivatives, process for producing the same and medicinal

1998-08-18

2000-07-11

Raymond, Richard L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546 31, A61K 3144, C07D48910

Patent

active

060873698

ABSTRACT:
A novel compound which is a .delta.-opioid antagonist having high selectivity and activity, that exhibits immunosuppressive action, antiallergic action, anti-inflammatory action and brain cell-protecting action is disclosed. The compound according to the present invention is an indole derivative represented by the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof. The present invention also provides an immunosuppressive agent, antiallergic agent, anti-inflammatory agent and brain cell-protecting agent comprising the derivative or the salt as an effective ingredient.

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patent: 5457208 (1995-10-01), Portghese et al.
patent: 5849731 (1998-12-01), Nagase et al.
Portoghese et al "Design of Peptidomimetic .delta. Opioid Receptor Antagonists Using the Message-Address Concept", J. Med. Chem. 1990, 33, 1714-1720.
Portoghese et al "Naltrindole 5'-Isothiocyanate: A Nonequilibrium, Highly Selective .delta. Opioid Receptor Antagonist", J. Med. Chem. 1990, 33, 1547-1548.
Portoghese ".delta. Opioid Antagonist Activity and Binding Studies of Regioisomeric Isothiocyanate Derivatives of Naltrindole: Evidence for .delta. Receptor Subtypes" J. Med. Chem. 1992, 35, 4086-4091.
Portoghese A Remarkable Change of Opioid Receptor Selectivity on the Attachment of a Peptidomimetic .kappa. Address Element to the .delta. Antagonist Natrindole: 5'-[N.sup.2 -Alkylamidino)methyl]naltrindole Derivatives as a Novel Class of .kappa. Opioid Receptor Antagonists, J. Med. Chem. 1993, 36, 179-180.
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