US4963539A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Phosphonate and phosphonamide endopeptidase inhibitors
Assignee: ER Squibb and Sons LLC
•
Filing: 1989-01-17
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Granted: 1990-10-16
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Expires: 2009-01-17
Abstract
Abstract Compounds of the formula ##STR1## wherein Y is O or NH and X is ##STR2## will inhibit the action of neutral endopeptidase. As a result, such compounds produce diuresis, natriuresis, and lower blood pressure as well as being useful in the treatment of congestive heart failure, relieving pain, and diarrhea when administered to a mammalian host.
Inventors
- 👤 Norma G. Delaney
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 06:51
CPC Classifications
C; C07; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/6558; C07F9/65586; C07F9/28; C07F9/38; C07F9/40; C07F9/4071; C07F9/4075; C07F9/4087; C07F9/44; C07F9/4461; C07F9/4465; C07F9/448; C07F9/553; C07F9/572; C07F9/5728; C07F9/576; C07F9/58; C07F9/65583
Claims Analysis
Total Claims: 15
Claim 1
Independent Claim
85 words
A compound of the formula ##STR127## including a pharmaceutically acceptable salt thereof wherein: R 1 is straight or branched alkyl of 1 to 4 carbons or ##STR128## R 2 is straight or branched chain alkyl of 1 to 4 carbons, trifluoromethyl, or ##STR129## X is ##STR130## R 3 and R 5 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, and an alkali metal salt ion; and q is an integer from 1 to 4.
Claim 2
Dependent Claim
85 words
A compound of the formula ##STR127## including a pharmaceutically acceptable salt thereof wherein: R 1 is straight or branched alkyl of 1 to 4 carbons or ##STR128## R 2 is straight or branched chain alkyl of 1 to 4 carbons, trifluoromethyl, or ##STR129## X is ##STR130## R 3 and R 5 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, and an alkali metal salt ion; and q is an integer from 1 to 4.
Claim 3
Dependent Claim
91 words
A compound of the formula ##STR131## including a pharmaceutically acceptable salt thereof wherein: R 1 is straight or branched chain alkyl of 1 to 4 carbons or ##STR132## R 2 is straight or branched alkyl of 1 to 4 carbons, trifluoromethyl, or ##STR133## X is --NH--(CH 2 ) 2 --COOR 5 ; R 3 and R 5 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, and an alkali metal salt ion; and q is an integer from 1 to 4.
Claim 4
Dependent Claim
91 words
A compound of the formula ##STR131## including a pharmaceutically acceptable salt thereof wherein: R 1 is straight or branched chain alkyl of 1 to 4 carbons or ##STR132## R 2 is straight or branched alkyl of 1 to 4 carbons, trifluoromethyl, or ##STR133## X is --NH--(CH 2 ) 2 --COOR 5 ; R 3 and R 5 are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, and an alkali metal salt ion; and q is an integer from 1 to 4.
Claim 5
Dependent Claim
15 words
A compound of claim 2 wherein: R 1 is ##STR134## and R 2 is methyl.
Claim 6
Dependent Claim
9 words
The compound of claim 3, 4-[[(S)-2-[[hydroxy(2-phenylethyl)phosphinyl]amino]-1-oxo-propyl]amino]benzoic acid, dilithium salt.
Claim 7
Dependent Claim
15 words
A compound of claim 1 wherein: R 1 is methyl; and R 2 is ##STR135##
Claim 8
Dependent Claim
9 words
The compound of claim 5, 4-[[(S)-2-[(hydroxymethylphosphinyl)amino]-1-oxo-3-phenyl-propyl]amino]benzoic acid, dilithium salt.
Claim 9
Dependent Claim
9 words
The compound of claim 5, (S)-3-[[2-[(hydroxymethylphosphinyl)amino]-1-oxo-3-phenylpropyl]amino]benzoic acid, dilithium salt.
Claim 10
Dependent Claim
15 words
A compound of claim 5 wherein: R 1 is ##STR136## and R 2 is ##STR137##
Claim 11
Dependent Claim
9 words
The compound of claim 8, 3-[[(S)-2-[[hydroxy(2-phenylethyl)phosphinyl]amino]-1-oxo-3-phenylpropyl]amino]propanoic acid, dilithium salt.
Claim 12
Dependent Claim
15 words
A compound of claim 2 wherein: R 1 is ##STR138## and R 2 is methyl.
Claim 13
Dependent Claim
9 words
The compound of claim 10, 3-[[(S)-2-[[hydroxy(2-phenylethyl)phosphonyl]amino]-1-oxo-propyl]amino]propanoic acid, dilithium salt.
Claim 14
Dependent Claim
58 words
A pharmaceutical composition useful for reducing blood pressure and producing diuresis and natriuresis as well as treating congestive heart failure, pain, and/or diarrhea in a mammalian host comprising a pharmaceutically acceptable carrier and an endopeptidase inhibiting compound of the formula ##STR139## wherein X, R 1 , R 2 , and R 3 are as defined in claim 1.
Claim 15
Dependent Claim
57 words
A pharmaceutical composition useful for reducing blood pressure and producing diuresis and natriuresis as well as treating congestive heart failure, pain, and/or diarrhea in a mammalian host comprising a pharmaceutically acceptable carrier and an endopeptidase inhibiting compound of the formula ##STR140## wherein X, R 1 , R 2 and R 3 are as defined in claim 2.
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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) | 1993-10-15 | 1994-04-16 | 1994-10-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1997-10-15 | 1998-04-16 | 1998-10-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2001-10-15 | 2002-04-16 | 2002-10-16 | $7700.00 | Window Closed / Lapsed |