EP0028064A1
Expired / Lapsed
EP
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Chromanol derivatives, a process for their preparation and a pharmaceutical composition comprising them
Assignee: Beecham Group PLC
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Filing: 1980-09-08
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Granted: —
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Expires: 2000-09-08
Abstract
Abstract Compounds of the formula (I): and salts and pro-drugs thereof, wherein: R 1 is a hydrogen atom or a lower alkyl group: R 2 is a hydrogen atom or a lower alkyl group: R 3 is a hydrogen atom or a lower alkyl group; R 4 is a hydrogen atom or an alkyl group; R 5 is a lower alkyl or a substituted alkyl group; or R 4 and R 5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom: R 6 is an electron donating group; R 7 is an electron withdrawing group; and the NR 4 R 5 and OR 3 moieties are trans having antihypertensive activity, pharmaceutical compositions containing them and processes for their preparation.
Inventors
- 👤 John Morris Evans
- 👤 Graham Andrew Showell
- 👤 Charles Sylvester Fake
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 18:08
CPC Classifications
C; C07; C07D; C07D493/00; C07D493/02; C07D493/04; C07D311/00; C07D311/02; C07D311/04; C07D311/22; C07D311/58; C07D311/68
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
127 words
A compound of the formula (I): and salts and pro-drugs thereof, wherein: R 1 is a hydrogen atom or a lower alkyl group; R 2 is a hydrogen atom or a lower alkyl group; R 3 is a hydrogen atom or a lower alkyl group; R 4 is a hydrogen atom or an alkyl group; R 5 is a lower alkyl or a substituted alkyl group; or R 4 and R 5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom; R 6 is an electron donating group; R 7 is an electron withdrawing group; and the NR 4 R 5 and OR 3 moieties are trans.
Claim 2
Dependent Claim
127 words
A compound of the formula (I): and salts and pro-drugs thereof, wherein: R 1 is a hydrogen atom or a lower alkyl group; R 2 is a hydrogen atom or a lower alkyl group; R 3 is a hydrogen atom or a lower alkyl group; R 4 is a hydrogen atom or an alkyl group; R 5 is a lower alkyl or a substituted alkyl group; or R 4 and R 5 are joined so that together with the nitrogen atom to which they are attached they form a 5-, 6- or 7-membered ring optionally containing an oxygen or sulphur atom; R 6 is an electron donating group; R 7 is an electron withdrawing group; and the NR 4 R 5 and OR 3 moieties are trans.
Claim 3
Dependent Claim
46 words
A compound according to claim 1 of the formula (II): and salts and pro-drugs thereof wherein R 3 , R 6 and R 7 have the values defined in claim 1 and n is 1 or 2, the cyclic amino and OR 3 moieties being trans.
Claim 4
Dependent Claim
22 words
A compound according to claim 2 of the formula (III): wherein R 6 and R 7 are as defined in claim 1.
Claim 5
Dependent Claim
21 words
A compound according to claim 2 of the formula (IV): wherein R 6 and R 7are as defined in claim 1.
Claim 6
Dependent Claim
44 words
5 . A compound according to any one of the claims 1 to 4 wherein R 6 is an amino, lower acylamino, lower alkylamino, lower dialkylamino, hydroxyl, lower alkoxyl or lower alkyl group wherein 'lower' means a group of up to 3 carbon atoms.
Claim 7
Dependent Claim
15 words
6 . A compound according to claim 5 wherein R 6 is amino or acetamido.
Claim 8
Dependent Claim
20 words
A compound according to any of the claims 1 to 6 wherein R 7 is nitro, cyano, carboxamido, or acetyl.
Claim 9
Dependent Claim
11 words
A compound according to claim 7 wherein R 7 is nitro.
Claim 10
Dependent Claim
130 words
9 . A process for the preparation of a compound according to claim 1 characterised by reaching a compound of the formula (VI): wherein R 1 , R 2 , R 6 and R 7 are as defined in claim 1 with the proviso that any amino group present in R 6 or R 7 is masked; with a compound of the formula (VII): wherein R 4 and R 5 are as defined in claim 1; and thereafter if desired or necessary converting R 3 , R 6 or R 7 in the thus formed compound to another group R 3 , R 6 or R 7 , removing the "masking" from any amino group present in R 6 or R 7 , or forming a salt of the compound.
Claim 11
Dependent Claim
18 words
10 . A pharmaceutical composition comprising a compound according to claim 1 together with a pharmaceutically acceptable carrier.
Claim 12
Dependent Claim
18 words
A compound according to any one of the claims 1 to 8 for use as an anti-hypertensive agent.
References Cited (Backward Citations)
GB1548221A
Cited
DE2713670A1
Cited
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