US4428940A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Anti-hypertensive compounds and compositions
Assignee: Beecham Group PLC
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Filing: 1982-03-09
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Granted: 1984-01-31
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Expires: 2002-03-09
Abstract
Abstract Compounds of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein m is 0 to 3; n is 1 to 5; R 1 is hydrogen, or C 1-6 alkyl; R 2 is hydrogen, C 1-4 alkyl, --(CH 2 ) p --NH 2 wherein p is 1 to 4, or --NHCOR, wherein R 5 is C 1-4 alkyl; R 3 is hydrogen or C 1-6 alkyl; R 4 is C 1-4 alkyl, C 1-4 alkoxy, halogen or CF 3 ; and X is CH 2 or S. having useful pharmacological activity, compositions containing them, and a process for their preparation.
Inventors
- 👤 Roger E. Markwell
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 22:57
CPC Classifications
C; C07; C07D; C07D307/00; C07D307/77; C07D307/78; C07D307/79; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07D307/80; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; A61K; A61K38/00
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
89 words
A compound of formula (I), ##STR19## or a pharmaceutically acceptable salt thereof, wherein: m is 0 to 3; n is 1 to 5; R 1 is hydrogen or C 1-6 alkyl; R 2 is hydrogen, C 1-4 alkyl, --(CH 2 ) p -NH 2 wherein p is 1 to 4, or --NHCOR 5 wherein R 5 is C 1-4 alkyl; R 3 is hydrogen or C 1-6 alkyl R 4 is C 1-4 alkyl, C 1-4 alkoxy, halogen or CF 3 ; and x is CH 2 or S.
Claim 2
Dependent Claim
89 words
A compound of formula (I), ##STR19## or a pharmaceutically acceptable salt thereof, wherein: m is 0 to 3; n is 1 to 5; R 1 is hydrogen or C 1-6 alkyl; R 2 is hydrogen, C 1-4 alkyl, --(CH 2 ) p -NH 2 wherein p is 1 to 4, or --NHCOR 5 wherein R 5 is C 1-4 alkyl; R 3 is hydrogen or C 1-6 alkyl R 4 is C 1-4 alkyl, C 1-4 alkoxy, halogen or CF 3 ; and x is CH 2 or S.
Claim 3
Dependent Claim
21 words
A compound according to claim 1, wherein the dihydrobenzofuranyl moiety is bonded to the rest of the structure at the 2-position.
Claim 4
Dependent Claim
52 words
A compound according to claim 2, having the formula (I)' ##STR20## or a pharmaceutically acceptable salt thereof, wherein: n is 1 or 2 to 5 R 1 and R 3 are the same or different and each is hydrogen or C 1-4 alkyl; and R 2 is hydrogen or C 1-4 alkyl.
Claim 5
Dependent Claim
29 words
A compound according to claim 3, wherein: n is 2 to 5; R 1 is C 1-4 alkyl; R 2 is C 1-4 alkyl; and R 3 is hydrogen.
Claim 6
Dependent Claim
27 words
A compound according to claim 1 wherein the asymmetric centres of the part structures of formulae (A) and (B) (indicated *): ##STR21## are in the S configuration.
Claim 7
Dependent Claim
9 words
N-[N-[[2-(2,3-Dihydro-2-benzofuranyl)-1-(ethoxycarbonyl)]ethyl]-(S)-alanyl]-(S)-proline or N-[N-[[4-(2,3-Dihydro-2-benzofuranyl)-1-(ethoxycarbonyl)]butyl]-(S)-alanyl]-(S)-proline or a pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
9 words
N-[N-[[2-(2,3-Dihydro-2-benzofuranyl)-1-(ethoxycarbonyl)]ethyl]-(S)-alanyl]-(S)-proline or N-[N-[[4-(2,3-Dihydro-2-benzofuranyl)-1-(ethoxycarbonyl)]butyl]-(S)-alanyl]-(S)-proline or a pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
25 words
A pharmaceutical composition for the treatment of hypertension which comprises an effective amount of a compound according to claim 1 and a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
25 words
A method of treatment of hypertension in mammals including humans comprising administering to the sufferer a therapeutically effective amount of a composition of claim 7.
Claim 11
Dependent Claim
26 words
A compound of claim 1, wherein R 2 is hydrogen, C 1-4 alkyl or --(CH 2 ) p -NH 2 wherein p is 1 to 4.
Claim 12
Dependent Claim
84 words
A compound of the formula (II): ##STR22## wherein m is 0 to 3; n is 1 to 5; R 1 is hydrogen or C 1-6 alkyl; R 2 is hydrogen, C 1-4 alkyl, --(CH 2 ) p --NH 2 wherein p is 1 to 4, or --NHCOR 5 wherein R 5 is C 1-4 alkyl; R 3 is hydrogen or C 1-6 alkyl; R 4 is C 1-4 alkyl, C 1-4 alkoxy, halogen or CF 3 ; and X is CH 2 or S.
Claim 13
Dependent Claim
84 words
A compound of the formula (II): ##STR22## wherein m is 0 to 3; n is 1 to 5; R 1 is hydrogen or C 1-6 alkyl; R 2 is hydrogen, C 1-4 alkyl, --(CH 2 ) p --NH 2 wherein p is 1 to 4, or --NHCOR 5 wherein R 5 is C 1-4 alkyl; R 3 is hydrogen or C 1-6 alkyl; R 4 is C 1-4 alkyl, C 1-4 alkoxy, halogen or CF 3 ; and X is CH 2 or S.
Claim 14
Dependent Claim
21 words
A compound of the formula (III): ##STR23## wherein m, n, R 1 and R 4 are as defined in claim 10.
Claim 15
Dependent Claim
33 words
A compound of the formula (V): ##STR24## wherein R 1 is C 1-6 alkyl and m, n and R 4 are as defined in claim 10, and Q is a carbonyl protecting group.
Claim 16
Dependent Claim
16 words
A compound of claim 12, wherein the carbonyl protecting group Q is a ketal or thioketal.
References Cited (Backward Citations)
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