Claims
- 1. A compound of the following formula ##STR7## and a salt thereof wherein A is hydrogen, hydroxy or OY wherein Y is a hydroxy protecting group selected from benzyl, triphenylmethyl, tetrahydropyrandyl, methoxymethyl and Si, R.sup.1, r.sup.2, R.sup.3 wherein R.sup.1, R.sup.2 and R.sup.3 are each C.sub.1 -C.sub.6 alkyl or phenyl;
- Ar is phenyl optionally substituted with one or more substituent selected from halo, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, CF.sub.3, C.sub.1 -C.sub.4 alkoxy-C.sub.1 -C.sub.4 alkyloxy and carboxy-C.sub.1 -C.sub.4 alkyloxy;
- X is benzofuranyl, benzothiophenyl, and pyridyl, these groups optionally being substituted with up to three substituents selected from halo, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, NO.sub.2, CF.sub.3 and SO.sub.2 CH.sub.3 ; and
- R is hydrogen, C.sub.1 -C.sub.4 alkyl or a hydroxy protecting group selected from benzyl, triphenylmethyl, tetrahydropyranyl, methoxymethyl and Si, R', R.sup.2, R.sup.3 wherein R', R.sup.2, R.sup.3 are each C.sub.1 -C.sub.6 alkyl or phenyl.
- 2. A compound according to claim 1, wherein A is hydrogen or hydroxy, and R is hydrogen or C.sub.1 -C.sub.4 alkyl.
- 3. A compound according to claim 2, wherein Ar is phenyl.
- 4. A compound according to claim 1, wherein A is OY, and R is a hydroxy protecting group, and wherein the hydroxy protecting groups are selected from benzyl, triphenylmethyl, tetrahydropyranyl, methoxymethyl and R.sup.1 R.sup.2 R.sup.3 Si, wherein R.sup.1, R.sup.2 and R.sup.3 are each C.sub.1 -C.sub.6 alkyl or phenyl.
- 5. A pharmaceutical composition useful as an analgesic, or an agent for treatment of stroke or abdominal pain which comprises a compound according to claim 1, and a pharmaceutically inert carrier.
- 6. A method for the treatment of a medical condition for which agonist activity toward opioid Kappa receptor is needed in a mammalian subject, the method comprises administering to said subject a therapeutically effective amount of a compound according to claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
PCTJP9500631 |
Mar 1995 |
JPX |
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CROSS REFERENCE TO RELATED APPLICATIONS
This application is a divisional of U.S. application Ser. No. 08/913,823 filed on Sep. 26, 1997, now U.S. Pat. No. 5,952,369, which is the national stage of International Application No. PCT/JP96/00820 having an international filing date of Mar. 28, 1996, designating inter alia the United States claiming priority from PCT/JP95/00631 filed on Mar. 31, 1995.
Divisions (1)
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Number |
Date |
Country |
Parent |
913823 |
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