US4558150A
Expired / Lapsed
US
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Intermediates for preparing amino thiol dipeptides
Assignee: ER Squibb and Sons LLC
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Filing: 1984-12-10
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Granted: 1985-12-10
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Expires: 2004-12-10
Abstract
Abstract Intermediates of the formula ##STR1## are disclosed. These compounds are useful in the preparation of amino thiol dipeptides possessing angiotensin converting enzyme inhibition activity and enkephalinase inhibition activity.
Inventors
- 👤 Eric M. Gordon
- 👤 Jollie D. Godfrey, Jr.
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 14:49
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; C07K5/0606; C07K5/06078; C07K5/06086; C07K5/06095; C07K5/06104; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 8
Claim 1
Independent Claim
125 words
A compound of the formula ##STR229## wherein R 2 is ##STR230## R 3 is hydrogen, lower alkyl, ##STR231## halo substituted lower alkyl, --(CH 2 ) m -cycloalkyl, ##STR232## --(CH 2 ) r --OH, ##STR233## --(CH 2 ) r --NH 2 , --(CH 2 ) r --SH, --(CH 2 ) r --S-lower alkyl, ##STR234## r is an integer from 1 to 4; R 14 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, or hydroxy; m is zero, one, two, three, or four; and p is one, two or three provided that p is more than one only if R 14 is hydrogen, methyl, methoxy, chloro, or fluoro.
Claim 2
Dependent Claim
125 words
A compound of the formula ##STR229## wherein R 2 is ##STR230## R 3 is hydrogen, lower alkyl, ##STR231## halo substituted lower alkyl, --(CH 2 ) m -cycloalkyl, ##STR232## --(CH 2 ) r --OH, ##STR233## --(CH 2 ) r --NH 2 , --(CH 2 ) r --SH, --(CH 2 ) r --S-lower alkyl, ##STR234## r is an integer from 1 to 4; R 14 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, or hydroxy; m is zero, one, two, three, or four; and p is one, two or three provided that p is more than one only if R 14 is hydrogen, methyl, methoxy, chloro, or fluoro.
Claim 3
Dependent Claim
125 words
A compound of the formula ##STR235## wherein R 2 is ##STR236## R 3 is hydrogen, lower alkyl, ##STR237## halo substituted lower alkyl, --(CH 2 ) m -cycloalkyl, ##STR238## --(CH 2 ) r --OH, ##STR239## --(CH 2 ) r --NH 2 , --(CH 2 ) r --SH, --(CH 2 ) r --S-lower alkyl, ##STR240## r is an integer from 1 to 4; R 14 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, or hydroxy; m is zero, one, two, three, or four; and p is one, two or three provided that p is more than one only if R 14 is hydrogen, methyl, methoxy, chloro, or fluoro.
Claim 4
Dependent Claim
125 words
A compound of the formula ##STR235## wherein R 2 is ##STR236## R 3 is hydrogen, lower alkyl, ##STR237## halo substituted lower alkyl, --(CH 2 ) m -cycloalkyl, ##STR238## --(CH 2 ) r --OH, ##STR239## --(CH 2 ) r --NH 2 , --(CH 2 ) r --SH, --(CH 2 ) r --S-lower alkyl, ##STR240## r is an integer from 1 to 4; R 14 is hydrogen, lower alkyl of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, or hydroxy; m is zero, one, two, three, or four; and p is one, two or three provided that p is more than one only if R 14 is hydrogen, methyl, methoxy, chloro, or fluoro.
Claim 5
Dependent Claim
59 words
A compound of claim 1 wherein: R 2 is ##STR241## R 3 is straight or branched chain lower alkyl of 1 to 4 carbons, --(CH 2 ) r --NH 2 , ##STR242## r is an integer from 1 to 4; R 14 is hydrogen, methyl, methoxy, methylthio, chloro, bromo, fluoro, or hydroxy; and m is zero, one, or two.
Claim 6
Dependent Claim
15 words
The compound of claim 3 wherein: R 2 is phenyl; and R 3 is ##STR243##
Claim 7
Dependent Claim
59 words
A compound of claim 2 wherein: R 2 is ##STR244## R 3 is straight or branched chain lower alkyl of 1 to 4 carbons, --(CH 2 ) r --NH 2 , ##STR245## r is an integer from 1 to 4; R 14 is hydrogen, methyl, methoxy, methylthio, chloro, bromo, fluoro, or hydroxy; and m is zero, one, or two.
Claim 8
Dependent Claim
15 words
The compound of claim 5 wherein: R 2 is phenyl; and R 3 is ##STR246##
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) | 1988-12-09 | 1989-06-10 | 1989-12-10 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-12-09 | 1993-06-10 | 1993-12-10 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-12-09 | 1997-06-10 | 1997-12-10 | $7700.00 | Window Closed / Lapsed |