US4146611A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Amino acid derivatives
Assignee: ER Squibb and Sons LLC
•
Filing: 1977-10-31
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Granted: 1979-03-27
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Expires: 1997-10-31
Abstract
Abstract A method for alleviating or reducing angiotensin related hypertension in hypertensive mammals comprises administering an effective amount of a compound having the general formula ##STR1## Intermediates for the preparation of such compounds are also included.
Inventors
- 👤 Miguel A. Ondetti
- 👤 Michael E. Condon
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-01 21:58
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/0606; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07C; C07C327/00; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D207/46; C07D209/00; C07D209/02; C07D209/04; C07D209/10; C07D209/18; C07D209/20; C07D211/00; C07D211/04; C07D211/06; C07D211/36; C07D211/60; C07D211/80; C07D211/84; C07D211/86; A61K; A61K38/00; Y; Y10; Y10S; Y10S530/00; Y10S530/80
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
142 words
A method for alleviating hypertension in hypertensive mammals which comprises administering an effective dose of a compound having the formula ##STR15## or salt thereof, wherein R is hydrogen or lower alkoxy R 1 is hydrogen, lower alkanoyl or amino(imino)methyl; R 2 is hydrogen, lower alkyl or phenyl-lower alkylene; R 3 is hydrogen; lower alkanoyl, benzoyl or ##STR16## A is hydrogen, lower alkyl or hydroxy-lower alkylene; B is hydrogen, lower alkyl, phenyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, imidazolyl-lower alkylene, indolyl-lower alkylene, mercapto-lower alkylene, lower alkylthio-lower alkylene, carbamoyl-lower alkylene or carboxy lower alkylene; or A and B together from a (CH 2 ) p bridge which completes an unsubstituted ring of 5 or 6 atoms with the nitrogen and carbon to which they are joined or said ring substituted with a hydroxy group; and p is 3 or 4.
Claim 2
Independent Claim
142 words
A method for alleviating hypertension in hypertensive mammals which comprises administering an effective dose of a compound having the formula ##STR15## or salt thereof, wherein R is hydrogen or lower alkoxy R 1 is hydrogen, lower alkanoyl or amino(imino)methyl; R 2 is hydrogen, lower alkyl or phenyl-lower alkylene; R 3 is hydrogen; lower alkanoyl, benzoyl or ##STR16## A is hydrogen, lower alkyl or hydroxy-lower alkylene; B is hydrogen, lower alkyl, phenyl, phenyl-lower alkylene, hydroxy-lower alkylene, hydroxyphenyl-lower alkylene, amino-lower alkylene, guanidino-lower alkylene, imidazolyl-lower alkylene, indolyl-lower alkylene, mercapto-lower alkylene, lower alkylthio-lower alkylene, carbamoyl-lower alkylene or carboxy lower alkylene; or A and B together from a (CH 2 ) p bridge which completes an unsubstituted ring of 5 or 6 atoms with the nitrogen and carbon to which they are joined or said ring substituted with a hydroxy group; and p is 3 or 4.
Claim 3
Dependent Claim
19 words
A method as in claim 1 wherein the compound has the L-configuration with respect to the carbon bearing B.
Claim 4
Dependent Claim
38 words
A method as in claim 1 wherein ##STR17## in the formula is the radical of glycine, alanine, leucine, threonine, phenylalanine, lysine, arginine, glutamine, histidine, methionine, serine, cysteine, tyrosine, valine, asparagine, glutamic acid, proline, hydroxyproline, phenylglycine, tryptophane or N-methylphenylalanine.
Claim 5
Dependent Claim
49 words
A method for alleviating hypertension in hypertensive mammals which comprises administering an effective dose of a compound having the formula ##STR18## or salt thereof, wherein R, R 1 , R 2 and R 3 have the same meaning as in claim 1, and R 4 is hydrogen or hydroxy.
Claim 6
Dependent Claim
27 words
A method as in claim 1 wherein the compound in the formula has A and B together as --(CH 2 ) 4 -- completing a six-membered ring.
Claim 7
Dependent Claim
55 words
A method as in claim 1 wherein the compound in the formula has R as hydroxy; R 1 as hydrogen; lower alkanoyl, or amino(imino)methyl; R 2 as hydrogen, lower alkyl or phenyl-lower alkylene; R 3 as hydrogen, lower alkanoyl or benzoyl; A as hydrogen; B as lower alkyl, guanidino-lower alkylene, amino-lower alkylene or phenyl-lower alkylene.
Claim 8
Dependent Claim
17 words
A method as in claim 1 wherein the compound in the formula has R 3 as ##STR19##
Claim 9
Dependent Claim
16 words
A method as in claim 1 wherein the compound in the formula has R as hydroxy.
Claim 10
Dependent Claim
21 words
A method as in claim 4 wherein the compound in the formula has R as hydroxy and R 4 as hydrogen.
Claim 11
Dependent Claim
31 words
A method as in claim 4 wherein the compound in the formula has R as hydroxy and R 1 , R 2 , R 3 and R 4 each as hydrogen.
Claim 12
Dependent Claim
24 words
A method as in claim 7 wherein the compound in the formula has R as hydroxy, each R 1 and R 2 as hydrogen.
Claim 13
Dependent Claim
16 words
A method as in claim 4 wherein the compound is cysteinylproline or acid addition salt thereof.
Claim 14
Dependent Claim
11 words
A method as in claim 4 wherein the compound is D-cysteinyl-L-proline.
Claim 15
Dependent Claim
42 words
A method as in claim 4 wherein the compound in the formula has R as hydroxy; R 1 as hydrogen, lower alkanoyl or amino(imino)methyl; R 2 as hydrogen, lower alkyl or phenyl-lower alkylene; and R 3 as hydrogen, lower alkanoyl or benzoyl.
Claim 16
Dependent Claim
57 words
A method as in claim 1 wherein the compound in the formula has R as hydroxy; R 1 as hydrogen, lower alkanoyl or amino(imino)methyl; R 1 as hydrogen, lower alkyl or phenyl-lower alkylene; R 3 as hydrogen, lower alkanoyl or benzoyl; A as hydrogen; and B as methyl, propyl, isopropyl, butyl, isobutyl, guanidinopropyl, aminopropyl, aminobutyl or phenylmethyl.
References Cited (Backward Citations)
US3857951A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-26 | 1982-09-25 | 1983-03-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-26 | 1986-09-25 | 1987-03-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-26 | 1990-09-25 | 1991-03-27 | $7700.00 | Window Closed / Lapsed |