US4346089A
Expired / Lapsed
US
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1-Aza-4-oxa-bicyclo [4,4,0]decane derivatives
Assignee: Beecham Group PLC
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Filing: 1981-01-28
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Granted: 1982-08-24
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Expires: 2001-01-28
Abstract
Abstract Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and N-oxides thereof, wherein: R 1 is a C 1-6 alkoxy group; R 2 and R 3 are the same or different and are hydrogen, halogen, CF 3 , C 1-7 acyl, C 1-7 acylamino, C 1-6 alkyl-S(O) n wherein n is 0, 1 or 2, nitro, C 1-6 alkoxy, hydroxy, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C 1-6 alkyl groups; or R 1 and R 2 taken together are methylenedioxy or ethylenedioxy in which case R 3 is any one of the groups given for R 1 and R 2 above; R 4 is hydrogen, C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl; R 5 is hydrogen or C 1-4 alkyl; X is an oxygen or sulphur atom; or a sulphoxide group >S˜O; p is 1 or 2; and r is 1 or 2; are useful in the treatment of disorders related to imparied gastrointestinal motility.
Inventors
- 👤 Michael S. Hadley
- 👤 Francis D. King
- 👤 Roger T. Martin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 19:36
CPC Classifications
C; C07; C07D; C07D513/00; C07D513/02; C07D513/04; A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/535; A61K31/54; A61K31/60; C07D265/00; C07D265/28; C07D265/30; C07D265/32; C07D265/33; C07D279/00; C07D279/10; C07D279/12
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
140 words
A compound of the formula (I): ##STR71## and pharmaceutically acceptable salts and N-oxides thereof, wherein: R 1 is a C 1-6 alkoxy group; R 2 and R 3 are the same or different and are hydrogen, halogen, CF 3 , C 1-7 acyl, C 1-7 acylamino, C 1-6 alkyl-S(O) n wherein n is 0, 1 or 2, nitro, C 1-6 alkoxy, hydroxy, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C 1-6 alkyl groups; or R 1 and R 2 taken together are methylenedioxy or ethylenedioxy in which case R 3 is any one of the groups given for R 1 and R 2 above; R 4 is hydrogen, C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl; R 5 is hydrogen or C 1-4 alkyl; X is oxygen atom; p is 1; and r is 1.
Claim 2
Dependent Claim
140 words
A compound of the formula (I): ##STR71## and pharmaceutically acceptable salts and N-oxides thereof, wherein: R 1 is a C 1-6 alkoxy group; R 2 and R 3 are the same or different and are hydrogen, halogen, CF 3 , C 1-7 acyl, C 1-7 acylamino, C 1-6 alkyl-S(O) n wherein n is 0, 1 or 2, nitro, C 1-6 alkoxy, hydroxy, or amino, aminocarbonyl or aminosulphonyl optionally substituted by one or two C 1-6 alkyl groups; or R 1 and R 2 taken together are methylenedioxy or ethylenedioxy in which case R 3 is any one of the groups given for R 1 and R 2 above; R 4 is hydrogen, C 1-4 alkyl, phenyl or phenyl C 1-4 alkyl; R 5 is hydrogen or C 1-4 alkyl; X is oxygen atom; p is 1; and r is 1.
Claim 3
Dependent Claim
29 words
A compound according to claim 1, wherein R 2 and R 3 are as defined except that when alkyl-S(O) n , n must be 2, and X is oxygen.
Claim 4
Dependent Claim
15 words
A compound according to claim 1, wherein the benzamide moiety has the structure (III): ##STR72##
Claim 5
Dependent Claim
15 words
A compound according to claim 1, wherein the bicyclic moiety has the structure (V): ##STR73##
Claim 6
Dependent Claim
10 words
A compound according to claim 1, of formula (VI): ##STR74##
Claim 7
Dependent Claim
13 words
A compound according to claim 1, wherein R 4 is hydrogen or methyl.
Claim 8
Dependent Claim
23 words
A compound according to claim 1, having an axial bond between the amide nitrogen and the ring carbon to which it is bound.
Claim 9
Dependent Claim
30 words
A pharmaceutical composition comprising a compound according to claim 1 in an amount effective for the treatment of disorders related to impaired gastro-intestinal motility, together with a pharmaceutically acceptable carrier.
Claim 10
Dependent Claim
37 words
A compound according to claim 1, for use in the treatment of disorders related to impaired gastro-intestinal motility including retarded gastric emptying, dyspepsia, flatulence, oesophagal reflux, peptic ulser and emesis and which compound is a dopamine antagonist.
References Cited (Backward Citations)
DE2748260A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-08-23 | 1986-02-22 | 1986-08-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-08-23 | 1990-02-22 | 1990-08-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-08-23 | 1994-02-22 | 1994-08-24 | $7700.00 | Window Closed / Lapsed |