US4176116A
Expired / Lapsed
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Dipeptide derivatives
Assignee: Hoffmann La Roche Inc
•
Filing: 1977-06-08
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Granted: 1979-11-27
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Expires: 1997-06-08
Abstract
Abstract The present disclosure relates to dipeptide derivatives. The novel compounds are useful as elastase inhibitors.
Inventors
- 👤 Cedric H. Hassall
- 👤 William H. Johnson
- 👤 Noel A. Roberts
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 14:24
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; A; A61; A61P; A61P29/00; A61K; A61K38/00
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
97 words
Dipeptide derivatives of the formula ##STR7## wherein R is methyl, ethyl, propyl or isopropyl; R 1 and R 2 each is hydrogen or methyl, with the proviso that R 1 and R 2 are not simultaneously hydrogen or R 1 and R 2 together are trimethylene; R 3 is selected from unsubstituted alkanoyl containing at least 3 carbon atoms or halo-alkanoyl, nitro-alkanoyl, cyano-alkanoyl, cycloalkylcarbonyl, cyclo-alkyl-alkanoyl, aroyl, aryl-alkanoyl, alkoxycarbonyl, aryloxycarbonyl, arylsulphonyl, alkylsulphonyl, cycloalkylsulphonyl, cyclo alkylsulphinyl, cyclo-alkyl-alkylsulphonyl or cycloalkyl-alkylsulphinyl and the asterisk denotes the configuration at the carbon atom so-marked is L when R 1 is other than hydrogen.
Claim 2
Dependent Claim
97 words
Dipeptide derivatives of the formula ##STR7## wherein R is methyl, ethyl, propyl or isopropyl; R 1 and R 2 each is hydrogen or methyl, with the proviso that R 1 and R 2 are not simultaneously hydrogen or R 1 and R 2 together are trimethylene; R 3 is selected from unsubstituted alkanoyl containing at least 3 carbon atoms or halo-alkanoyl, nitro-alkanoyl, cyano-alkanoyl, cycloalkylcarbonyl, cyclo-alkyl-alkanoyl, aroyl, aryl-alkanoyl, alkoxycarbonyl, aryloxycarbonyl, arylsulphonyl, alkylsulphonyl, cycloalkylsulphonyl, cyclo alkylsulphinyl, cyclo-alkyl-alkylsulphonyl or cycloalkyl-alkylsulphinyl and the asterisk denotes the configuration at the carbon atom so-marked is L when R 1 is other than hydrogen.
Claim 3
Dependent Claim
24 words
Dipeptide derivatives of claim 1, wherein R 1 is hydrogen and R 2 is methyl or R 1 and R 2 together are trimethylene.
Claim 4
Dependent Claim
10 words
Dipeptide derivatives of claim 1, wherein R 3 is aroyl.
Claim 5
Dependent Claim
10 words
Dipeptide derivatives of claim 3, wherein R 3 is benzoyl.
Claim 6
Dependent Claim
9 words
Dipeptide derivatives of claim 1 wherein R is ethyl.
Claim 7
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-L-proline methylamide.
Claim 8
Dependent Claim
9 words
The compound of claim 1 which is: N-pivaloyl-L-alanyl-L-proline ethylamide.
Claim 9
Dependent Claim
9 words
The compound of claim 1 which is: N-benzoyl-L-alanyl-L-proline ethylamide.
Claim 10
Dependent Claim
9 words
The compound of claim 1 which is: N-(n-valeryl)-L-alanyl-L-proline ethylamide.
Claim 11
Dependent Claim
9 words
The compound of claim 1 which is: N-ethoxycarbonyl-L-alanyl-L-proline ethylamide.
Claim 12
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-L-proline ethylamide.
Claim 13
Dependent Claim
9 words
The compound of claim 1 which is: N-phenacetyl-L-alanyl-L-proline ethylamide.
Claim 14
Dependent Claim
9 words
The compound of claim 1 which is: N-isobutanoyl-L-alanyl-L-proline ethylamide.
Claim 15
Dependent Claim
9 words
The compound of claim 1 which is: N-cyclohexylcarbonyl-L-alanyl-L-proline ethylamide.
Claim 16
Dependent Claim
9 words
The compound of claim 1 which is: N-(p-toluenesulphonyl)-L-alanyl-L-proline ethylamide.
Claim 17
Dependent Claim
9 words
The compound of claim 1 which is: N-(1-adamantylcarbonyl)-L-alanyl-L-proline ethylamide.
Claim 18
Dependent Claim
9 words
The compound of claim 1 which is: N-(D-10-camphorsulphonyl)-L-alanyl-L-proline ethylamide.
Claim 19
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-L-proline isopropylamide.
Claim 20
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-alanine ethylamide.
Claim 21
Dependent Claim
9 words
The compound of claim 1 which is: N-benzoyl-L-alanyl-L-alanine ethylamide.
Claim 22
Dependent Claim
9 words
The compound of claim 1 which is: N-pivaloyl-L-alanyl-L-alanine ethylamide.
Claim 23
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-L-alanine isopropylamide.
Claim 24
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-N-methyl-L-alanine ethylamide.
Claim 25
Dependent Claim
9 words
The compound of claim 1 which is: N-propionyl-L-alanyl-sarcosine ethylamide.
References Cited (Backward Citations)
DE2649171A1
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-11-26 | 1983-05-28 | 1983-11-27 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-11-26 | 1987-05-28 | 1987-11-27 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-11-26 | 1991-05-28 | 1991-11-27 | $7700.00 | Window Closed / Lapsed |