US4537885A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Certain benzazocinone and benzazoninone derivatives
Assignee: Novartis Corp
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Filing: 1984-02-09
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Granted: 1985-08-27
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Expires: 2004-02-09
Abstract
Abstract Variously substituted 1-carboxymethyl-3-(carboxymethylamino)-benzazocin-2-one and benzazonin-2-one derivatives are disclosed as angiotensin converting enzyme inhibitors and anti-hypertensive agents. Synthesis of, pharmaceutical compositions and methods of treatment utilizing such compounds are included.
Inventors
- 👤 Jeffrey W. H. Watthey
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 19:16
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/022; C07K5/0222; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
72 words
A compound of the formula ##STR24## wherein S represents the chirality, n represents an integer from 1 to 4; p is the integer 3 or 4; R 8 is hydrogen, amino, benzyloxycarbonylamino, phenyl unsubstituted or monosubstituted by lower alkyl, lower alkoxy, lower alkanoyloxy, halogen, hydroxy, or trifluoromethyl; R 6 and R 7 independently represent hydroxy, lower alkoxy of up to 4 carbon atoms, benzyloxy or amino; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
72 words
A compound of the formula ##STR24## wherein S represents the chirality, n represents an integer from 1 to 4; p is the integer 3 or 4; R 8 is hydrogen, amino, benzyloxycarbonylamino, phenyl unsubstituted or monosubstituted by lower alkyl, lower alkoxy, lower alkanoyloxy, halogen, hydroxy, or trifluoromethyl; R 6 and R 7 independently represent hydroxy, lower alkoxy of up to 4 carbon atoms, benzyloxy or amino; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
12 words
A compound of claim 1 wherein (CH 2 ) p represents propylene.
Claim 4
Dependent Claim
13 words
A compound of claim 1 being 1-carboxymethyl-3-(1-carboxy-3-phenyl-(1S)-propylamino)-3,4,5,6-tetrahydro-(3S)-1-benzazocin-2-1H-one or a pharmaceutically acceptable salt thereof.
Claim 5
Dependent Claim
13 words
A compound of claim 1 being 1-carboxymethyl-3-(1-carboxy-3-phenyl-(1S)-propylamino)-1,3,4,5,6,7-hexahydro-(3S)-1-benzazonin-2-one or a pharmaceutically acceptable salt thereof.
Claim 6
Dependent Claim
13 words
A compound of claim 1 being 1-carboxymethyl-3-(1-ethoxycarbonyl-3-phenyl-(1S)-propylamino)-1,3,4,5,6,7-hexahydro-(3S)-1-benzazonin-2-one or a pharmaceutically acceptable salt thereof.
Claim 7
Dependent Claim
12 words
A compound of claim 1 being 3-[(5-benzyloxycarbonylamino-1-(S)-carboxypentyl)amino]-1-carboxymethol-3,4,5,6-tetrahydro-(3S)-benzazocin-2-1H-one or pharmaceutically acceptable salt thereof.
Claim 8
Dependent Claim
6 words
1-Carboxymethyl-3-(1-ethoxycarbonyl-3-phenyl-(1S)-propylamino)-3,4,5,6-tetrahydro-(3S)-1-benzazocin-2-1H-one or pharmaceutically acceptable salt thereof.
Claim 9
Dependent Claim
6 words
1-Carboxymethyl-3-(1-ethoxycarbonyl-3-phenyl-(1S)-propylamino)-3,4,5,6-tetrahydro-(3S)-1-benzazocin-2-1H-one or pharmaceutically acceptable salt thereof.
Claim 10
Dependent Claim
7 words
3-[(5-Amino-1-(S)-carboxypentyl)amino]-1-carboxymethyl-3,4,5,6-tetrahydro-(3S)-1-benzazocin-2-1H-one or a pharmaceutically acceptable salt thereof.
Claim 11
Dependent Claim
7 words
3-[(5-Amino-1-(S)-carboxypentyl)amino]-1-carboxymethyl-3,4,5,6-tetrahydro-(3S)-1-benzazocin-2-1H-one or a pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
43 words
A pharmaceutical composition suitable for oral or parenteral administration to mammals for the treatment or prevention of diseases responsive to inhibition of angiotensin-converting enzyme comprising an effective amount of a compound of claim 1 in combination with one or more pharmaceutically acceptable carriers.
Claim 13
Dependent Claim
28 words
A method of treating hypertensive or cardiac conditions in mammals which comprises administering to a mammal in need thereof an effective amount of a composition of claim 9.
Claim 14
Dependent Claim
24 words
A method of inhibiting angiotensin-converting enzyme which comprises administering to a mammal in need thereof an effective amount of a composition of claim 9.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-08-26 | 1989-02-25 | 1989-08-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-08-26 | 1993-02-25 | 1993-08-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-08-26 | 1997-02-25 | 1997-08-27 | $7700.00 | Window Closed / Lapsed |