US4560680A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Aminoalkyl and related substituted phosphinic acid angiotensin converting enzyme inhibitors
Assignee: ER Squibb and Sons LLC
•
Filing: 1984-05-10
•
Granted: 1985-12-24
•
Expires: 2004-05-10
Abstract
Abstract Compounds of the structure ##STR1## are provided which are inhibitors of angiotensin converting enzyme and are useful in the treatment of hypertension.
Inventors
- 👤 Denis E. Ryono
- 👤 Edward W. Petrillo, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 06:43
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/44; C07D209/48; C07F; C07F9/00; C07F9/02; C07F9/28; C07F9/30; C07F9/306; C07F9/32; C07F9/3205; C07F9/3211; C07F9/3223; C07F9/3241; C07F9/3258; C07F9/3288; C07F9/48; C07F9/4808; C07F9/4816; C07F9/547; C07F9/553; C07F9/5537; C07F9/572; C07F9/5728; C07F9/576; C07F9/59; C07F9/645; C07F9/6503; C07F9/6506; C07F9/655; C07F9/65515; C07F9/6558; C07F9/6561; C07F9/65615
Claims Analysis
Total Claims: 13
Claim 1
Independent Claim
162 words
A compound of the formula ##STR313## and pharmaceutically acceptable salts thereof, wherein R 1 is lower alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, aminoalkyl, furyl, furylalkyl, thienyl, thienylalkyl, pyridyl, pyridylalkyl or ##STR314## and R 5 and R 6 are independently selected from hydrogen, lower alkyl, haloalkyl, aryl, alkylaryl, cycloalkyl, cycloalkylalkyl, furyl, furylalkyl, thienyl, thienylalkyl, pyridyl or pyridylalkyl; R 2 and R 4 each is independently hydrogen, lower alkyl, arylalkyl, benzhydryl or ##STR315## wherein R 7 is hydrogen, lower alkyl or phenyl, R 8 is hydrogen, lower alkyl, lower alkoxy or phenyl or R 7 and R 8 taken together are --(CH 2 ) 2 --, --(CH 2 ) 3 --, --CH═CH--, or ##STR316## n is 0 or 1; R 3 is NH 2 (CH 2 ) m --, ##STR317## R 9 is hydrogen, lower alkyl, aryl or arylalkyl, and m is 0 or an integer of from 1 to 5, and --XOR 4 is an imino or amino acid derivative of the formula ##STR318##
Claim 2
Dependent Claim
162 words
A compound of the formula ##STR313## and pharmaceutically acceptable salts thereof, wherein R 1 is lower alkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, aminoalkyl, furyl, furylalkyl, thienyl, thienylalkyl, pyridyl, pyridylalkyl or ##STR314## and R 5 and R 6 are independently selected from hydrogen, lower alkyl, haloalkyl, aryl, alkylaryl, cycloalkyl, cycloalkylalkyl, furyl, furylalkyl, thienyl, thienylalkyl, pyridyl or pyridylalkyl; R 2 and R 4 each is independently hydrogen, lower alkyl, arylalkyl, benzhydryl or ##STR315## wherein R 7 is hydrogen, lower alkyl or phenyl, R 8 is hydrogen, lower alkyl, lower alkoxy or phenyl or R 7 and R 8 taken together are --(CH 2 ) 2 --, --(CH 2 ) 3 --, --CH═CH--, or ##STR316## n is 0 or 1; R 3 is NH 2 (CH 2 ) m --, ##STR317## R 9 is hydrogen, lower alkyl, aryl or arylalkyl, and m is 0 or an integer of from 1 to 5, and --XOR 4 is an imino or amino acid derivative of the formula ##STR318##
Claim 3
Dependent Claim
11 words
The compound as defined in claim 1 wherein n is 0.
Claim 4
Dependent Claim
11 words
The compound as defined in claim 1 wherein n is 1.
Claim 5
Dependent Claim
23 words
The compound as defined in claim 1 wherein R 3 is NH 2 (CH 2 ) m wherein m is 2 to 5.
Claim 6
Dependent Claim
12 words
The compound as defined in claim 1 wherein R 1 is arylalkyl.
Claim 7
Dependent Claim
14 words
The compound as defined in claim 1 wherein R 4 is H or benzyloxy.
Claim 8
Dependent Claim
9 words
The compound of claim 1 wherein X is ##STR319##
Claim 9
Dependent Claim
9 words
The compound of claim 1 wherein X is ##STR320##
Claim 10
Dependent Claim
9 words
The compound of claim 1 wherein X is ##STR321##
Claim 11
Dependent Claim
29 words
A composition useful for treating hypertension comprising a pharmaceutically acceptable carrier and an effective amount of a hypotensive agent as defined in claim 1 or pharmaceutically acceptable salt thereof.
Claim 12
Dependent Claim
9 words
The composition of claim 10 also including a diuretic.
Claim 13
Dependent Claim
21 words
The method of alleviating hypertension in a mammalian specie which comprises administering an effective amount of the composition of claim 10.
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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) | 1988-12-23 | 1989-06-24 | 1989-12-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-12-23 | 1993-06-24 | 1993-12-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-12-23 | 1997-06-24 | 1997-12-24 | $7700.00 | Window Closed / Lapsed |