Bicyclic compounds with pharmaceutical activity

Details Bicyclic compounds with pharmaceutical activity Bicyclic compounds with pharmaceutical activity

1995-07-06

1999-06-01

Richter, Johann

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

549399, 549404, 549407, 549415, 549424, A61K 3135, C07D31106, C07D31500

Patent

active

059088605

DESCRIPTION:

BRIEF SUMMARY
This invention relates to a novel method of treatment, to novel compounds and to the preparation of compounds for use in such a method.
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-dimethyl-2H-1-benz opyran-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-415 065 (E. Merck) and EP-A-450415 (Squibb), EP-A-0 466 131 (Nissan Chemical Industries Ltd), EP-A-0339562 (Yoshitomi Pharmaceuticals), EP-A-0482934, EP-A-0296975, JO-2004-791 and WO.backslash.89.backslash.07103 also describe certain benzopyran derivatives which are believed to possess anti-hypertensive activity.
PCT/Application WO 92/22293 (SmithKline Beecham plc; unpublished at the priority date), describes certain fluorobenzoyl benzopyrans having inter alia anxiolytic and anti-convulsant activity.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-0 194 885 (E. Lilly) describes certain amino substituted benzopyran derivatives possessing anti-convulsant activity.
It has now been surprisingly found that certain compounds of formula (Ia) possess anxiolytic and anti-convulsant activity, and are also believed to have utility in the treatment or prevention of mania, depression and the effects associated with withdrawal from substances of abuse, and that compounds of formula (I) have utility in the treatment or prevention of disorders resulting from sub-arachnoid haemorrhage, neural shock, cerebral ischaemia, Parkinson's Disease, migraine and/or psychosis.
Accordingly, the present invention provides a method of treatment and/or prophylaxis of disorders resulting from sub-arachnoid haemorrhage, neural shock, cerebral ischaemia, Parkinson's Disease, migraine and/or psychosis, in mammals, especially humans which comprises administering to the sufferer in need thereof an effective or prophylactic amount of a compound of formula (I) or pharmaceutically acceptable salt thereof: ##STR2## 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 alkoxysulphonylamino, or ethylenyl terminally substituted by C.sub.1-6 alkylcarbonyl, nitro or cyano, or --C(C.sub.1-6 alkyl)NOH or --C(C.sub.1-6 alkyl)NNH.sub.2, or one of R .sub.1 and R.

REFERENCES:
patent: 5624954 (1997-04-01), Evans et al.

Affiliated with

Also associated with

Rating

Bicyclic compounds with pharmaceutical activity does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Bicyclic compounds with pharmaceutical activity, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Bicyclic compounds with pharmaceutical activity will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-955183