US4187216A
Expired / Lapsed
US
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Dipeptide derivatives
Assignee: Hoffmann La Roche Inc
•
Filing: 1977-06-08
•
Granted: 1980-02-05
•
Expires: 1997-06-08
Abstract
Abstract The present disclosure relates to dipeptide derivatives. These 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 17:55
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: 35
Claim 1
Independent Claim
93 words
Dipeptide derivatives of the formula ##STR7## wherein R is phenyl, substituted phenyl, lower cycloalkyl or n-(C 4 -C 6 )-alkyl; 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 alkanoyl, halo-alkanoyl, nitro-alkanoyl, cyano-alkanoyl, cycloalkylcarbonyl, cycloalkyl-alkanoyl, aroyl, aryl-alkanoyl, alkoxycarbonyl, aryloxycarbonyl, arylsulfonyl, alkylsulfonyl, cyclo-alkylsulfonyl, cycloalkylsulfinyl, cycloalkyl-alkylsulfonyl or cycloalkyl-alkylsulfinyl and the asterisk denotes that the configuration at the carbon atom so-marked is L when R 1 is other than hydrogen.
Claim 2
Dependent Claim
93 words
Dipeptide derivatives of the formula ##STR7## wherein R is phenyl, substituted phenyl, lower cycloalkyl or n-(C 4 -C 6 )-alkyl; 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 alkanoyl, halo-alkanoyl, nitro-alkanoyl, cyano-alkanoyl, cycloalkylcarbonyl, cycloalkyl-alkanoyl, aroyl, aryl-alkanoyl, alkoxycarbonyl, aryloxycarbonyl, arylsulfonyl, alkylsulfonyl, cyclo-alkylsulfonyl, cycloalkylsulfinyl, cycloalkyl-alkylsulfonyl or cycloalkyl-alkylsulfinyl and the asterisk denotes that 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
9 words
Dipeptide derivatives of claim 1 wherein R is phenyl.
Claim 5
Dependent Claim
9 words
The compound of claim 1 which is N-acetyl-L-alanyl-L-proline anilide.
Claim 6
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline anilide.
Claim 7
Dependent Claim
9 words
The compound of claim 1 which is N-benzoyl-L-alanyl-L-proline anilide.
Claim 8
Dependent Claim
9 words
The compound of claim 1 which is N-pivaloyl-L-alanyl-L-proline anilide.
Claim 9
Dependent Claim
9 words
The compound of claim 1 which is N-hexanoyl-L-alanyl-L-proline anilide.
Claim 10
Dependent Claim
9 words
The compound of claim 1 which is N-trifluoroacetyl-L-alanyl-L-proline anilide.
Claim 11
Dependent Claim
9 words
The compound of claim 1 which is N-cyanoacetyl-L-alanyl-L-proline anilide.
Claim 12
Dependent Claim
9 words
The compound of claim 1 which is N-(1-adamantylcarbonyl)-L-alanyl-L-proline anilide.
Claim 13
Dependent Claim
9 words
The compound of claim 1 which is N-(1-adamantylacetyl)-L-alanyl-L-proline anilide.
Claim 14
Dependent Claim
9 words
The compound of claim 1 which is N-(p-toluenesulfonyl)-L-alanyl-L-proline anilide.
Claim 15
Dependent Claim
9 words
The compound of claim 1 which is N-benzenesulfonyl-L-alanyl-L-proline anilide.
Claim 16
Dependent Claim
9 words
The compound of claim 1 which is N-(4-nitrobenzenesulfonyl)-L-alanyl-L-proline anilide.
Claim 17
Dependent Claim
9 words
The compound of claim 1 which is N-(1-naphthalenesulfonyl)-L-alanyl-L-proline anilide.
Claim 18
Dependent Claim
9 words
The compound of claim 1 which is N-(1-adamantylsulfinyl)-L-alanyl-L-proline anilide.
Claim 19
Dependent Claim
9 words
The compound of claim 1 which is N-(1-adamantylsulfonyl)-L-alanyl-L-proline anilide.
Claim 20
Dependent Claim
9 words
The compound of claim 1 which is N-(D-10-camphorsulfonyl)-L-alanyl-L-proline anilide.
Claim 21
Dependent Claim
9 words
The compound of claim 1 which is N-(4-acetylaminobenzenesulfonyl)-L-alanyl-L-proline anilide.
Claim 22
Dependent Claim
9 words
The compound of claim 1 which is N-(4-methoxybenzenesulfonyl)-L-alanyl-L-proline anilide.
Claim 23
Dependent Claim
9 words
The compound of claim 1 which is N-mesitylenesulfonyl-L-alanyl-L-proline anilide.
Claim 24
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline 2,4-dichloroanilide.
Claim 25
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline 4-nitroanilide.
Claim 26
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline 4-methoxyanilide.
Claim 27
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline cyclopentylamide.
Claim 28
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline cyclohexylamide.
Claim 29
Dependent Claim
9 words
The compound of claim 1 which is N-(p-toluenesulfonyl)-L-alanyl-L-proline cyclohexylamide.
Claim 30
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline cycloheptylamide.
Claim 31
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline cyclooctylamide.
Claim 32
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-alanine anilide.
Claim 33
Dependent Claim
9 words
The compound of claim 1 which is N-benzoyl-L-alanyl-L-alanine anilide.
Claim 34
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-alanine cyclohexylamide.
Claim 35
Dependent Claim
9 words
The compound of claim 1 which is N-propionyl-L-alanyl-L-proline n-pentylamide.
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) | 1983-02-04 | 1983-08-06 | 1984-02-05 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-02-04 | 1987-08-06 | 1988-02-05 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-02-04 | 1991-08-06 | 1992-02-05 | $7700.00 | Window Closed / Lapsed |