Claims
- 1. A method for treating neurodegenerative disease caused by glutamate receptor activity in a warm-blooded animal in need of said treatment which comprises administering to said animal a therapeutically effective amount of the benzomorphan derivative of formula ##STR5## wherein X is oxygen or sulphur;
- R.sup.1 is C.sub.1-8 -alkyl, C.sub.3-6 -alkenyl, or C.sub.2-8 -alkynyl, or aryl;
- R.sup.2 is hydrogen, C.sub.1-8 -alkyl, or C.sub.3-6 -alkenyl, C.sub.3-6 -alkynyl, aryl or aralkyl;
- R.sup.3 is hydrogen or C.sub.1-6 -alkyl;
- R.sup.4 is C.sub.1-8 -alkyl;
- R.sup.5 is C.sub.1-8 -alkyl;
- R.sup.6 is C.sub.1-8 -alkyl or aryl; and
- R.sup.7 and R.sup.8 independently of each other are hydrogen, halogen, C.sub.1-8 -alkyl, --C.sub.1-8 -alkoxy, --O-acyl, --CN, --NO.sub.2, --NH.sub.2, --NH(C.sub.1-8 -alkyl), --NH-acyl, --N(C.sub.1-8 -alkyl)-acyl--, or --N(C.sub.1-8 -alkyl).sub.2 wherein the alkyl groups may be identical or different,
- all racemic, enantiomeric and diastereomeric forms thereof or mixtures thereof, or pharmaceutically acceptable acid addition salts thereof;
- with the proviso that
- if
- X is oxygen
- R.sup.1 is C.sub.1-3 -alkyl, C.sub.3 -alkenyl or C.sub.3 -alkynyl;
- R.sup.2 is hydrogen, C.sub.1-4 -alkyl, C.sub.3 -alkenyl or C.sub.4 -alkenyl,
- R.sup.3 is hydrogen or C.sub.1-3 -alkyl
- R.sup.4 is methyl
- R.sup.5 is methyl
- R.sup.6 is C.sub.1-4 -alkyl or phenyl
- and one of the substituents R.sup.7 or R.sup.8 is hydrogen, the other of the substituents R.sup.7 or R.sup.8 is the 2'-position is not hydrogen, hydroxy, C.sub.1-3 -alkoxy or O-acyl.
- 2. A method for treating cerebral ischaemia in a warm-blooded animal in need of said treatment which comprises administering to said animal a therapeutically effective amount of a benzomorphan derivative ##STR6## wherein X is oxygen or sulphur;
- R.sup.1 is C.sub.1-8 -alkyl, C.sub.3-6 alkenyl, or C.sub.3-6 -alkynyl, aryl
- R.sup.2 is hydrogen, C.sub.1-8 -alkyl, or C.sub.3-6 -alkenyl, C.sub.3-6 -alkynyl, aryl, aralkyl;
- R.sup.3 is hydrogen, C.sub.1-6 -alkyl;
- R.sup.4 is C.sub.1-8 -alkyl;
- R.sup.5 is C.sub.1-8 -alkyl;
- R.sup.6 is C.sub.1-8 -alkyl, aryl;
- R.sup.7 and R.sup.8 independently of each other are hydrogen, C.sub.1-8 -alkyl, halogen, OH, C.sub.1-8 -alkoxy, --O-acyl, --CN, --NO.sub.2, NH.sub.2, --NH(C.sub.1-8 -alkyl), --N(C.sub.1-8 -alkyl).sub.2, wherein the alkyl groups may be identical or different, --NH-acyl or --N-acyl-(C.sub.1-8 -alkyl).
- 3. A method for treating epilepsy in a warm-blooded animal in need of said treatment which comprises administering to said animal a therapeutically effective amount of a benzomorphan derivative ##STR7## wherein X is oxygen or sulphur;
- R.sup.1 is C.sub.1-8 -alkyl, C.sub.3-6 alkenyl, or C.sub.3-6 -alkynyl, aryl
- R.sup.2 is hydrogen, C.sub.1-8 -alkyl, C.sub.3-6 -alkenyl, C.sub.3-6 -alkynyl, aryl, aralkyl;
- R.sup.3 is hydrogen, C.sub.1-6 -alkyl;
- R.sup.4 is C.sub.1-8 -alkyl;
- R.sup.5 is C.sub.1-8 -alkyl;
- R.sup.6 is C.sub.1-8 -alkyl, aryl;
- R.sup.7 and R.sup.8 independently of each other are hydrogen, C.sub.1-8 -alkyl, halogen, OH, C.sub.1-8 -alkoxy, --O-acyl, --CN, --NO.sub.2, NH.sub.2, --NH(C.sub.1-8 -alkyl), --N(C.sub.1-8 -alkyl).sub.2, wherein the alkyl groups may be identical or different, --NH-acyl or --N-acyl-(C.sub.1-8 -alkyl).
- 4. A benzomorphan derivative ##STR8## or a pharmaceutically acceptable acid addition salt thereof.
- 5. The benzomorphan derivative as recited in claim 4 which is the hydrochloride salt.
Parent Case Info
This is a continuation of application Ser. No. 08/217,540, filed Mar. 24, 1994, abandoned which is a continuation of application Ser. No. 07/904,738, filed Jun. 26, 1992, abandoned.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
4473576 |
Akkerman et al. |
Sep 1984 |
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Continuations (2)
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Number |
Date |
Country |
Parent |
217540 |
Mar 1994 |
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Parent |
904738 |
Jun 1992 |
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