Patent US1902648A successfully refreshed from Google Patents.
Patent US4185096A successfully refreshed from Google Patents.
US4185096A
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Novel derivatives of pepstatin, their preparation and compositions containing them
Assignee: Bpifrance Financement SA
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Filing: 1978-07-31
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Granted: 1980-01-22
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Expires: 1998-07-31
Abstract
Abstract The novel derivatives of pepstatin have the general formula (I) below in which X, Y and Z, are identical or different, and each represent an amino-acid selected from arginine, glutamic acid, aspartic acid, lysine, histidine and valine, the carboxyl function of the terminal amino-acid being esterifiable. The indices a, b and c are each equal to zero or 1, the sum a+b+c being equal to 1, 2 or 3. The invention also includes the water soluble salts and their preparation, and the compositions containing them. ##STR1## These novel products are particularly useful in the diagnosis and treatment of arterial hypertension due to the action of renine.
Inventors
- 👤 Bertrand Castro
- 👤 Joel Menard
- 👤 Genevieve Evin
- 👤 Pierre Corvol
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 22:32
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/02; A; A61; A61P; A61P9/00; A61P9/12; C07K5/00; C07K5/02; C07K5/0205; A61K; A61K38/00; Y; Y10; Y10S; Y10S530/00; Y10S530/86
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
77 words
A pepstatin derivative having the formula ##STR4## wherein R 1 , R 2 and R 3 are each a side chain from an amino-acid selected from the group consisting of arginine, glutamic acid, aspartic acid, lysine, histidine and valine; R 4 is H or C 1 -C 4 alkyl; and a and b are each zero or 1, the sum of a plus b being equal to 0, 1 or 2; and their salts with solubilizing bases.
Claim 2
Dependent Claim
77 words
A pepstatin derivative having the formula ##STR4## wherein R 1 , R 2 and R 3 are each a side chain from an amino-acid selected from the group consisting of arginine, glutamic acid, aspartic acid, lysine, histidine and valine; R 4 is H or C 1 -C 4 alkyl; and a and b are each zero or 1, the sum of a plus b being equal to 0, 1 or 2; and their salts with solubilizing bases.
Claim 3
Dependent Claim
61 words
The pepstatin derivative of claim 1, comprising the methyl ester of pepstatin-arginine whose characteristics are as follows: melting point ("Kofler" bank)=262°-263° C. rotatory power: [α] D 20 =40.1° (c=0.18; methanol) analysis (amino-acids) after hydrolysis with 6 N hydrochloric acid for 24 hours at 110° C.: arginine: 0.95 alanine: 1 valine: 2.10 infrared spectrum: characteristic "ester" band at 1740 cm -1 .
Claim 4
Dependent Claim
43 words
The pepstatin derivative of claim 1, comprising pepstatin-arginine whose characteristics are as follows: melting point ("Kofler" bank) higher than 250° C. (decomposition) analysis (amino-acids) after hydrolysis with 6 N hydrochloric acid for 24 hours at 110° C.: alanine: 1 valine: 1.96 arginine: 1.
Claim 5
Dependent Claim
50 words
The pepstatin derivative of claim 1, comprising pepstatin-glutamic acid whose characteristics are as follows: melting point ("Kofler" bank): 230° C. rotatory power: [α] D 20 =-79.0° (c=0.55; methanol) analysis (amino-acids) after hydrolysis with 6 N hydrochloric acid for 24 hours at 110° C.: alanine: 1 valine: 1.97 glutamic acid: 0.99.
Claim 6
Dependent Claim
50 words
The pepstatin derivative of claim 1, comprising pepstatin-aspartic acid whose characteristics are as follows: melting point ("Kofler" bank): 238°-240° C. rotatory power: [α] D 25 =-67.6° (c=0.51 methanol) analysis (amino-acids) after hydrolysis with 6 N hydrochloric acid for 24 hours at 110° C.: aspartic acid: 0.92 alanine: 1.12 valine: 2.
Claim 7
Dependent Claim
31 words
An antihypertensive composition, comprising an amount effective to reduce hypertension of, a pepstatin derivative according to claim 1, in association with one or several compatible and pharmaceutically acceptable diluents or adjuvants.
Claim 8
Dependent Claim
25 words
A method of treatment of hypertension associated with an excessive secretion of renin, which comprises administering to a hypertensive patient the composition of claim 6.
Claim 9
Dependent Claim
15 words
The antihypertensive composition of claim 6, wherein said amount is from 1 to 30 mg/kg.
Claim 10
Dependent Claim
39 words
A method of diagnosing hypertension associated with an excessive secretion of renin, which comprises administering to a hypertensive patient a diagnostically effective amount of a pepstatin derivative according to claim 1, and observing the resultant change in blood pressure.
Claim 11
Dependent Claim
23 words
The pepstatin derivatives of claim 1, wherein said solubilizing bases are selected from the group consisting of arginine, lysine and α,γ-diamino butyric acid.
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) | 1983-01-21 | 1983-07-23 | 1984-01-22 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-01-21 | 1987-07-23 | 1988-01-22 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-01-21 | 1991-07-23 | 1992-01-22 | $7700.00 | Window Closed / Lapsed |