Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-06-25
1998-05-19
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544263, A01N 4354, C07D48700
Patent
active
057536651
DESCRIPTION:
BRIEF SUMMARY
This is a 371 application of PCT/EP 94/03364 filed on Oct. 12, 1994. to pharmaceutical compositions containing them, to processes for their preparation and to their use in the treatment and/or prophylaxis of seizures, neurological disorders such as epilepsy and/or conditions in which there is neurological damage such as stroke, brain trauma, head injuries and haemorrhage.
In particular the present invention provides compounds of formula I ##STR2## which includes pharmaceutically acceptable salts thereof and stereoisomers thereof with one or more of halo, cyano, hydroxy or amino): C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkanoyl; groups (optionally substituted with one or more of halo, cyano, hydroxy or amino): C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkanoyl, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphinyl or C.sub.1-6 alkylsulphonyl; and R.sub.5 combined together with the carbon atom to which they are attached represent C.sub.3-6 cycloalkylidene (each alkyl or cycloalkylidene being optionally substituted with one or more of halo, cyano, hydroxy, amino or C.sub.1-6 alkyl); and mercapto, cyano or one of the following groups (optionally substituted with one or more of halo, cyano, hydroxy or amino; and any nitrogen atom being optionally substituted with one or more C.sub.1-6 alkyl): C.sub.1-6 alkyl, C.sub.1-6 alkanoyl, C.sub.1-6 alkoxy, C.sub.2-6 alkoxycarbonyl, carboxy, C.sub.1-6 alkanoyloxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphinyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphonylamino, sulphamoyl, carbamoyl, C.sub.2-6 alkylcarbamoyl or C.sub.1-6 alkanoylamino; neurological disorders such as epilepsy and/or conditions in which there is neurological damage such as stroke, brain trauma, head injuries and haemorrhage.
It will be understood that any group mentioned herein which contains a chain of three or more atoms signifies a group in which the chain may be straight or branched. For example, an alkyl group may comprise propyl which includes n-propyl and isopropyl and butyl which includes n-butyl, sec-butyl, isobutyl and tert-butyl. The total number of carbon atoms is specified herein for certain substituents, for example C.sub.1-6 alkyl signifies an alkyl group having from 1 to 6 carbon atoms. The term `halo` as used herein signifies fluoro, chloro, bromo and iodo. The term `optionally substituted` as used herein, unless immediately followed by a list of one or more substituent group or groups, means optionally substituted with one or more of halo, cyano, hydroxy, amino or C.sub.1-6 alkyl. When the phenyl ring substituents R.sub.6, R.sub.7 and R.sub.8 are other than H, the substituent may replace any H attached to a carbon atom in the ring and may be located at any such position of the ring, ie up to three of positions 2, 3, 4, 5 and/or 6.
Pharmaceutically acceptable compounds of formula I or II may comprise those compounds which, if administered to an animal in a therapeutically effective dose, may be non-toxic and/or may be associated with limited effects in the animal to be treated that would be acceptable in the light of the nature of the therapy and/or condition to be treated; and those compounds which may be compatible with pharmaceutical carriers and/or diluents suitable for formulating the pharmaceutical compositions of the present invention described herein.
Racemic compounds of formula I in which:
Therefore the present invention provides novel compounds of formula II ##STR3## which includes pharmaceutically acceptable salts thereof and stereoisomers thereof with one or more of halo, cyano, hydroxy or amino): C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkanoyl; groups (optionally substituted with one or more of halo, cyano, hydroxy or amino): C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkanoyl, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphinyl or C.sub.1-6 alkylsulphonyl; and R.sub.5 combined together with the carbon atom to which they are attached represent C.sub.3-6 cycloalkylidene (each alkyl or cycloalkylidene being optionally substituted with one or more of halo, cyano, hydr
REFERENCES:
patent: 4269820 (1981-05-01), Davies et al.
patent: 5387747 (1995-02-01), Bru-Magniez et al.
Fernandez Fernandez Maria Isabel
Heal David John
Sargent Bruce Jeremy
Knoll Aktiengesellschaft
Ngo Tamthom T.
Shah Mukund J.
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