US4384996A
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US
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Novel cyclosporins
Assignee: Novartis AG
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Filing: 1982-01-06
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Granted: 1983-05-24
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Expires: 2002-01-06
Abstract
Abstract Novel cyclosporins having an -Allylgly- residue in the 2-position and/or a -(D)-Ser- residue in the 8-position and process for their production. The novel cyclosporins are useful as pharmaceuticals, e.g. as immunosuppressive and anti-inflammatory agents.
Inventors
- 👤 Pietro Bollinger
- 👤 Johann J. Bolsterli
- 👤 Hans Kobel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 14:26
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/64; C07K7/645; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/27
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
18 words
A cyclosporin having a β-vinylene-α-amino acid residue at the 2-position and/or a β-hydroxy-α-amino acid residue at the 8-position.
Claim 2
Dependent Claim
18 words
A cyclosporin having a β-vinylene-α-amino acid residue at the 2-position and/or a β-hydroxy-α-amino acid residue at the 8-position.
Claim 3
Dependent Claim
42 words
A cyclosporin according to claim 1 of formula III, ##STR9## wherein Z 1 is allyl or ethyl, Z 2 is hydroxymethyl or, when Z 1 is allyl Z 2 is, methyl, and --X--Y-- is --CH═CH-- (trans) or --CH 2 --CH 2 --.
Claim 4
Dependent Claim
11 words
A cyclosporin according to claim 2, which is "(D)-Ser 8 -cyclosporin".
Claim 5
Dependent Claim
11 words
A cyclosporin according to claim 2, which is "(D)-Ser 8 -dihydrocyclosporin".
Claim 6
Dependent Claim
11 words
A cyclosporin according to claim 2, which is "Allylgly 2 -cyclosporin".
Claim 7
Dependent Claim
27 words
A pharmaceutical composition comprising an immunosuppressive effective amount of a cyclosporin according to claim 1 as active ingredient, together with a pharmaceutically acceptable diluent or carrier therefor.
Claim 8
Dependent Claim
35 words
A method of suppressing or reducing the immune response in a subject in need of such treatment, which method comprises administering to said subject an immunosuppressively effective amount of a cyclosporin according to claim 1.
Claim 9
Dependent Claim
23 words
A compound according to claim 1 in which the β-vinylene-α-amino acid residue is -Allylgly- and the β-hydroxy-α-amino acid residue is -(D)-Ser- or -(D)-Thr-.
Claim 10
Dependent Claim
69 words
A cyclosporin according to claim 1 of formula I ##STR10## where A is -Allylgly- or -α-Abu-, (D)-A is -(D)-Ala-, -(D)-Ser- or -(D)-Thr-, and MeC 9 is a residue of formula II ##STR11## in which the positions 2, 3 and 4 have the configurations S,R and R respectively, and --X--Y-- is --CH═CH-- (trans) or --CH 2 --CH 2 --, with the proviso that when (D)-A is -(D)-Ala, A is -Allylgly-.
References Cited (Backward Citations)
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Cited
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Cited
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Cited
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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) | 1986-05-23 | 1986-11-22 | 1987-05-24 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1990-05-23 | 1990-11-22 | 1991-05-24 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1994-05-23 | 1994-11-22 | 1995-05-24 | $7700.00 | Window Closed / Lapsed |