Patent US2730704A successfully refreshed from Google Patents.
US5227467A
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Immunosuppressive fluorinated cyclosporin analogs
Assignee: Merck and Co Inc
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Filing: 1991-04-29
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Granted: 1993-07-13
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Expires: 2011-04-29
Abstract
Abstract New immunosuppressive cyclosporin analogs are disclosed having one or more fluorinated amino acids. These analogs may also have a "C-9 amino acid" wherein the double bond is replaced by a heteroatom such as sulfur or oxygen.
Inventors
- 👤 Philippe L. Durette
- 👤 Arsenio A. Pessolano
- 👤 Janos Kollonitsch
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 09:26
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/64; C07K7/645; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
93 words
A compound of the formula I ##STR13## or a pharmaceutically acceptable salt thereof wherein R 1 is MeBmt or dihydroMeBmt; R 2 is Nva, Ser, Thr, or Val; R 3 is Sar, or N-methyl-D-alanyl; R 4 is MeLeu; R 5 is Val or 4-fluoro-Val; R 6 is MeLeu; R 7 is Ala; R 8 is D-alanyl; R 9 is MeLeu; R 10 is MeLeu; and R 11 is MeVal or 4-fluoro-MeVal; with the proviso that at least one of R 5 and R 11 is the amino acid residue with the 4-fluoro substituent.
Claim 2
Dependent Claim
93 words
A compound of the formula I ##STR13## or a pharmaceutically acceptable salt thereof wherein R 1 is MeBmt or dihydroMeBmt; R 2 is Nva, Ser, Thr, or Val; R 3 is Sar, or N-methyl-D-alanyl; R 4 is MeLeu; R 5 is Val or 4-fluoro-Val; R 6 is MeLeu; R 7 is Ala; R 8 is D-alanyl; R 9 is MeLeu; R 10 is MeLeu; and R 11 is MeVal or 4-fluoro-MeVal; with the proviso that at least one of R 5 and R 11 is the amino acid residue with the 4-fluoro substituent.
Claim 3
Dependent Claim
144 words
A compound of Formula I ##STR14## which is: (a) R 1 is MeBmt, R 2 is Abut, R 3 is Sar, R 4 is MeLeu, R 5 is 4-fluoro-Val, R 6 is MeLeu, R 7 is Ala, R 8 is D-Ala, R 9 is MeLeu, R 10 is MeLeu, R 11 is MeVal; (b) R 1 is dihydroMeBmt, R 2 is Abu, R 3 is Sar, R 4 is MeLeu, R 5 is 4-fluoro-Val, R 6 is MeLeu, R 7 is Ala, R 8 is D-Ala, R 9 is MeLeu, R 10 is MeLeu, R 11 is MeVal; or (c) R 1 is MeBmt, R 2 is Abu, R 3 is Sar, R 4 is MeLeu, R 5 is Val, R 6 is MeLeu, R 7 is Ala, R 8 is D-Ala, R 9 is MeLeu, R 10 is MeLeu, R 11 is 4-fluoro-MeVal.
Claim 4
Dependent Claim
144 words
A compound of Formula I ##STR14## which is: (a) R 1 is MeBmt, R 2 is Abut, R 3 is Sar, R 4 is MeLeu, R 5 is 4-fluoro-Val, R 6 is MeLeu, R 7 is Ala, R 8 is D-Ala, R 9 is MeLeu, R 10 is MeLeu, R 11 is MeVal; (b) R 1 is dihydroMeBmt, R 2 is Abu, R 3 is Sar, R 4 is MeLeu, R 5 is 4-fluoro-Val, R 6 is MeLeu, R 7 is Ala, R 8 is D-Ala, R 9 is MeLeu, R 10 is MeLeu, R 11 is MeVal; or (c) R 1 is MeBmt, R 2 is Abu, R 3 is Sar, R 4 is MeLeu, R 5 is Val, R 6 is MeLeu, R 7 is Ala, R 8 is D-Ala, R 9 is MeLeu, R 10 is MeLeu, R 11 is 4-fluoro-MeVal.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1996-07-12 | 1997-01-11 | 1997-07-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2000-07-12 | 2001-01-11 | 2001-07-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2004-07-12 | 2005-01-11 | 2005-07-13 | $7700.00 | Window Closed / Lapsed |