US4665193A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Amino acid ester renin inhibitors
Assignee: ER Squibb and Sons LLC
•
Filing: 1986-06-27
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Granted: 1987-05-12
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Expires: 2006-06-27
Abstract
Abstract Compounds of the formula <IMAGE> wherein A is <IMAGE> intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
Inventors
- 👤 Denis E. Ryono
- 👤 Edward W. Petrillo, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 13:57
CPC Classifications
C; C07; C07D; C07D233/00; C07D233/54; C07D233/64; C07K; C07K5/00; C07K5/02; C07K5/0227; Y; Y10; Y10S; Y10S530/00; Y10S530/86
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
318 words
A compound of the formula ##STR89## including a pharmaceutically acceptable salt thereof wherein: A is ##STR90## R 4 is --O--lower alkyl, --O--(CH 2 ) m --aryl, or --O--(CH 2 ) m --heterocyclo; m is zero, one, two, three or four; R 8 is hydrogen, ##STR91## R 10 is hydrogen, ##STR92## R 2 , R 3 , R 7 and R 9 are independently selected from the group consisting of hydrogen, lower alkyl, halo substituted lower alkyl, --(CH 2 ) n --aryl, --(CH 2 ) n --heterocyclo, --(CH 2 ) n --OH, --(CH 2 ) n --NH 2 , --(CH 2 ) n --SH, --(CH 2 ) n --S--lower alkyl, --(CH 2 ) 2 --S--(CH 2 ) 2 --NH 2 , ##STR93## and --(CH 2 ) n --cycloalkyl; n is an integer from 1 to 4; R 11 is ##STR94## R 1 is hydrogen, lower alkyl, --(CH 2 ) n --aryl, --(CH 2 ) n --cycloalkyl, ##STR95## the term lower alkyl refers to straight or branched chain radicals having up to seven carbon atoms; the term cycloalkyl refers to saturated rings of 4 to 7 carbon atoms; the term halogen refers to Cl, Br, and F; the term halo substituted lower alkyl refers to such lower alkyl groups in which one or more hydrogens have been replaced by Cl, Br, or F groups; the term aryl refers to phenyl, 1-naphthyl, 2-naphthyl, mono substituted phenyl, 1-naphthyl, or 2-naphthyl wherein said substituent is lower alkyl of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, halogen, hydroxy, amino, --NH--alkyl wherein alkyl is of 1 to 4 carbons, or --N(alkyl) 2 wherein alkyl is of 1 to 4 carbons, di or tri substituted phenyl, 1-naphthyl or 2-naphthyl wherein said substituents are methyl, methoxy, methylthio, halogen, or hydroxy; and the term heterocyclo refers to 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, imidazolyl, and indolyl.
Claim 2
Dependent Claim
318 words
A compound of the formula ##STR89## including a pharmaceutically acceptable salt thereof wherein: A is ##STR90## R 4 is --O--lower alkyl, --O--(CH 2 ) m --aryl, or --O--(CH 2 ) m --heterocyclo; m is zero, one, two, three or four; R 8 is hydrogen, ##STR91## R 10 is hydrogen, ##STR92## R 2 , R 3 , R 7 and R 9 are independently selected from the group consisting of hydrogen, lower alkyl, halo substituted lower alkyl, --(CH 2 ) n --aryl, --(CH 2 ) n --heterocyclo, --(CH 2 ) n --OH, --(CH 2 ) n --NH 2 , --(CH 2 ) n --SH, --(CH 2 ) n --S--lower alkyl, --(CH 2 ) 2 --S--(CH 2 ) 2 --NH 2 , ##STR93## and --(CH 2 ) n --cycloalkyl; n is an integer from 1 to 4; R 11 is ##STR94## R 1 is hydrogen, lower alkyl, --(CH 2 ) n --aryl, --(CH 2 ) n --cycloalkyl, ##STR95## the term lower alkyl refers to straight or branched chain radicals having up to seven carbon atoms; the term cycloalkyl refers to saturated rings of 4 to 7 carbon atoms; the term halogen refers to Cl, Br, and F; the term halo substituted lower alkyl refers to such lower alkyl groups in which one or more hydrogens have been replaced by Cl, Br, or F groups; the term aryl refers to phenyl, 1-naphthyl, 2-naphthyl, mono substituted phenyl, 1-naphthyl, or 2-naphthyl wherein said substituent is lower alkyl of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, halogen, hydroxy, amino, --NH--alkyl wherein alkyl is of 1 to 4 carbons, or --N(alkyl) 2 wherein alkyl is of 1 to 4 carbons, di or tri substituted phenyl, 1-naphthyl or 2-naphthyl wherein said substituents are methyl, methoxy, methylthio, halogen, or hydroxy; and the term heterocyclo refers to 2-thienyl, 3-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, imidazolyl, and indolyl.
Claim 3
Dependent Claim
9 words
A compound of claim 1 wherein: A is ##STR96##
Claim 4
Dependent Claim
9 words
A compound of claim 1 wherein: A is ##STR97##
Claim 5
Dependent Claim
80 words
A compound of claim 3 wherein: R 1 is hydrogen, ##STR98## R 2 is straight or branched chain lower alkyl of 1 to 4 carbons, benzyl, phenethyl or ##STR99## R 3 is hydrogen, straight or branched chain lower alkyl of 1 to 4 carbons, benzyl or phenethyl; R 7 is ##STR100## R 8 is ##STR101## R 9 is --(CH 2 ) n --aryl wherein aryl is phenyl or 1-naphthyl and n is one or two; and R 10 is ##STR102##
Claim 6
Dependent Claim
48 words
A compound of claim 4 wherein R 1 is hydrogen; R 2 is --CH 2 --CH(CH 3 ) 2 ; R 3 is --CH 2 --CH(CH 3 ) 2 or --CH(CH 3 ) 2 ; R 7 is ##STR103## R 9 is ##STR104## and R 10 is ##STR105##
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-05-11 | 1990-11-10 | 1991-05-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-05-11 | 1994-11-10 | 1995-05-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-05-11 | 1998-11-10 | 1999-05-12 | $7700.00 | Window Closed / Lapsed |