C.sub.4 -amide substituted compounds and their use as therapeuti

Details C.sub.4 -amide substituted compounds and their use as therapeuti C.sub.4 -amide substituted compounds and their use as therapeuti

1996-12-10

1998-12-01

Huang, Evelyn

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514456, 514302, 549389, 549399, 546116, A61K 3135, C07D31168, C07D31172

Patent

active

058439897

DESCRIPTION:

BRIEF SUMMARY
This application is the national phase of POT/EP95/02,149, filed Jun. 9,1995 issued as WO 95/34,547 on Dec. 21, 1995.
This invention relates to novel compounds, to processes for preparing them, and to their use as therapeutic agents.
European Published Patent Application No. 0126311 discloses substituted benzopyran compounds having blood pressure lowering activity, including 6-acetyl-trans-4-(4-fluorobenzoylamino)- 3,4-dihydro-2,2-dirmethyl-2H- 1 -benzopyran-3-ol.
Also EP-A-0 376 524, EP-A-0 205 292, EP-A-0 250 077, EP-A-0 093 535, EP-A-0 150 202, EP-A-0 076 075 and WO/89/05808 (Beecham Group plc) describe certain benzopyran derivatives which possess anti-hypertensive activity.
EP-A-0 350 805 (Biersdorf), EP-A-0 277 611, EP-A-0 277612, EP-A-0 337 179 and EP-A-0 355 565 (Hoechst Aktiengesellschaft); EP-A-0 466 131 (Nissan Chemical Industries Ltd), EP-A-0339562 (Yoshitomi Pharmaceuticals) EP-A-415 065 (E. Merck) EP-A-450415 (Squibb), EP-A-0482934, EP-A-0296975, EPA 571822 (Daiichi Pharm.), JO-2004-791 and WO.backslash.89.backslash.07103 also describe certain benzopyran derivatives which are believed to possess anti-hypertensive activity.
EP-A-0 430 621 and EP-A-0 385 584 (Beecham Group plc) describe the resolution of certain intermediates useful in the preparation of the compounds described in the above mentioned patent applications.
EP-A-0 139 992 (Beecham Group plc) describes certain benzopyran derivatives which have cis isomerism at position 3 and 4 which compounds are described as possessing anti-hypertensive activity.
PCT/GB92/01045 (SmithKline Beecham plc; unpublished at the priority date), which describes certain fluorobenzoylamino benzopyrans, pyranopyridines and tetrahydronaphthalenes in which the 3 and 4 position substituents are trans to each other. These compounds are described as possessing inter alia anxiolytic and anti-convulsant activity.
It has now been surprisingly found that certain compounds of formula (I) (below) possess anti-convulsant activity, and are therefore believed to be useful in the 30 treatment and/or prevention of epilepsy; the compounds of formula (I) are also believed to have utility in the treatment or prevention of anxiety, mania, depression, disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse, Parkinson's Disease, psychosis, migraine, cerebral ischaemia, Alzheimer's disease, schizophrenia, OCD (obsessive compulsive disorder), panic disorders and/or agression.
Accordingly, the present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof: ##STR1## wherein: either Y is N and R.sub.2 is hydrogen, or Y is C--R.sub.1 ; from the class of hydrogen, C.sub.3-8 cycloalkyl, C.sub.1-6 alkyl optionally interrupted by oxygen or substituted by hydroxy, C.sub.1-6 alkoxy or substituted aminocarbonyl, C.sub.1-6 alkylcarbonyl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 alkylcarbonyloxy, C.sub.1-6 alkoxy, nitro, cyano, halo, trifluoromethyl, CF.sub.3 S, or a group CF.sub.3 --A--, where A is --CF.sub.2 --, --CO--, --CH.sub.2 --, CH(OH), SO.sub.2, SO, CH.sub.2 --O, or CONH, or a group CF.sub.2 H--A'--where A' is oxygen, sulphur, SO, SO.sub.2, CF.sub.2 or CFH; trifluoromethoxy, C.sub.1-6 alkylsulphinyl, perfluoro C.sub.2-6 alkylsulphonyl, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkoxysulphinyl, C.sub.1-6 alkoxysulphonyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, phosphono, arylcarbonyloxy, heteroarylcarbonyloxy, arylsulphinyl, heteroarylsulphinyl, arylsulphonyl, heteroarylsulphonyl in which any aromatic moiety is optionally substituted, C.sub.1-6 alkylcarbonylamino, C.sub.1-6 alkoxycarbonylamino, C.sub.1-6 alkyl-thiocarbonyl, C.sub.1-6 alkoxy-thiocarbonyl, C.sub.1-6 alkyl-thiocarbonyloxy, 1-mercapto C.sub.2-7 alkyl, formyl, or aminosulphinyl, aminosulphonyl or aminocarbonyl, any amino moiety being optionally substituted by one or two C.sub.1-6 alkyl groups, or C.sub.1-6 alkylsulphinylamino, C.sub.1-6 alkylsulphonylamino,C.sub.1-6 alkoxysulphinylamino or C.sub.1-6 alkoxysulphonyla

REFERENCES:
patent: 3789056 (1974-01-01), Pfirrmann
patent: 4571406 (1986-02-01), Evans
patent: 5021432 (1991-06-01), Yamanaka
patent: 5624954 (1997-04-01), Evans

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