Patent US4764503A successfully refreshed from Google Patents.
US4764503A
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Novel cyclosporins
Assignee: Novartis AG
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Filing: 1987-05-13
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Granted: 1988-08-16
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Expires: 2007-05-13
Abstract
Abstract Cyclosporins wherein the amino acid residue at the 8-position is a (D)-acyloxy-α-amino acid residue, typically of formula ##STR1## wherein X=--MeBmt-- or --dihydro--MeBmt--, Y=--αAbu--, --Ala--, --Thr--, --Val-- or --Nva--, Z=--Val-- or --Nva-- and Q=R 1 --CO--O--CH(R 2 )--CH(CO--)--NH-- wherein R 1 =H, C 1-4 alkyl or phenyl and R 2 =H or CH 3 , possess immunosuppressive, anti-inflammatory and anti-parasitic activity.
Inventors
- 👤 Roland Wenger
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-07 17:56
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/64; C07K7/645; A; A61; A61K; A61K38/00; Y; Y02; Y02A; Y02A50/00; Y02A50/30; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/19; Y10S930/27
Claims Analysis
Total Claims: 7
Claim 1
Independent Claim
51 words
A cyclosporin of formula I ##STR10## wherein X is --MeBmt-- or --dihydro--MeBmt--, Y is --αAbu--, --Ala--, --Thr--, --Val-- or --Nva--, Z is --Val-- or --Nva--, and Q is a residue of formula II ##STR11## wherein R 1 is hydrogen, C 1-4 alkyl or phenyl and R 2 is hydrogen or methyl.
Claim 2
Dependent Claim
51 words
A cyclosporin of formula I ##STR10## wherein X is --MeBmt-- or --dihydro--MeBmt--, Y is --αAbu--, --Ala--, --Thr--, --Val-- or --Nva--, Z is --Val-- or --Nva--, and Q is a residue of formula II ##STR11## wherein R 1 is hydrogen, C 1-4 alkyl or phenyl and R 2 is hydrogen or methyl.
Claim 3
Dependent Claim
11 words
A cyclosporin according to claim 1 which is [O-acetyl-(D)-Ser] 8 -Cyclosporine.
Claim 4
Dependent Claim
13 words
A cyclosporine according to claim 1 which is [Nva] 2 -[O-acetyl-(D)Ser] 8 -Cyclosporine.
Claim 5
Dependent Claim
67 words
A cyclosporin according to claim 1 selected from the group consisting of: [Dihydro-MeBmt] 1 -[O-acetyl-(D)Ser] 8 -Cyclosporine; [O-benzoyl-(D)Ser] 8 -Cyclosporine; and [Dihydro-MeBmt] 1 -[Nva] 2 -[O-acetyl-(D)Ser] 8 -Cyclosporine;[Nva] 5 -[O-acetyl-(D)Ser] 8 -Cyclosporine; [O-acetyl-(D)Thr] 8 -Cyclosporine; [Val] 2 -[O-acetyl-(D)Ser] 8 -Cyclosporine; [Dihydro-MeBmt] 1 -[Val] 2 -[O-acetyl-(D)Ser] 8 -Cyclosporine; [Nva] 2 -[Nva] 5 -[O-acetyl-(D)Ser] 8 -Cyclosporine; [Thr] 2 -[O-acetyl-(D)Ser] 8 -Cyclosporine; and [Dihydro-MeBmt] 1 -[Thr] 2 -[O-acetyl-(D)Ser] 8 -Cyclosporine.
Claim 6
Dependent Claim
30 words
A pharmaceutical composition useful in inducing immunosuppression or treating inflammation or parasitic infection comprising a cyclosporin as defined in claim 1 together with a pharmaceutically acceptable diluent or carrier therefor.
Claim 7
Dependent Claim
39 words
A method of inducing immunosuppression, of treating inflammation or of treating parasitic infection in a subject in need of such treatment, which method comprises administering to said subject an effective amount of a cyclosporin as defined in claim 1.
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) | 1991-08-16 | 1992-02-15 | 1992-08-16 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-08-16 | 1996-02-15 | 1996-08-16 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-08-16 | 2000-02-15 | 2000-08-16 | $7700.00 | Window Closed / Lapsed |