US4288431A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Cyclosporin derivatives, their production and pharmaceutical compositions containing them
Assignee: Novartis AG
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Filing: 1979-10-12
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Granted: 1981-09-08
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Expires: 1999-10-12
Abstract
Abstract Compounds of formula I ##STR1## selected from the group consisting of cyclosporin G, wherein A is ##STR2## dihydrocyclosporin G, wherein A is ##STR3## and isocyclosporin G, wherein A is ##STR4## are useful in treating inflammations and arthritis and as immuno-suppressant agents.
Inventors
- 👤 Rene P. Traber
- 👤 Hans Hofmann
- 👤 Eugen Harri
- 👤 Kuhn Max
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-24 16:54
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/64; C07K7/645; C12; C12N; C12N1/00; C12N1/14; C12N1/145; A; A61; A61K; A61K38/00; C12R; C12R2001/00; C12R2001/645; C12R2001/885; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/19; Y10S930/27
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
31 words
A compound of formula I ##STR6## selected from the group consisting of cyclosporin G, wherein A is ##STR7## dihydrocyclosporin G, wherein A is ##STR8## and isocyclosporin G, wherein A is ##STR9##
Claim 2
Dependent Claim
31 words
A compound of formula I ##STR6## selected from the group consisting of cyclosporin G, wherein A is ##STR7## dihydrocyclosporin G, wherein A is ##STR8## and isocyclosporin G, wherein A is ##STR9##
Claim 3
Dependent Claim
83 words
The compound of claim 1 which is cyclosporin G which has the following approximate characteristics: ##EQU3## UV spectrum in CH 3 OH: end absorption IR spectrum in CH 2 Cl 2 : see FIG. 1 IH.N.M.R. spectrum in CDCl 3 90 MH z (Tetramethylsilane as internal standard): see FIG. 2 Formula: C 63 H 113 N 11 O 12 and when in crystalline form a m.pt. of about 193°-194° C., and being more polar than cyclosporin D and less polar than cyclosporin A.
Claim 4
Dependent Claim
14 words
The compound of claim 1 which is cyclosporin G substantially free from cyclosporin D.
Claim 5
Dependent Claim
14 words
The compound of claim 1 which is cyclosporin G in greater than 95% purity.
Claim 6
Dependent Claim
89 words
The compound of claim 1 which is dihydrocyclosporin G having the following approximate characteristics: [α] D 20 =-232° (c=0.64 in CHCl 3 ) UV spectrum in CH 3 OH: end absorption IR spectrum in CH 2 Cl 2 : see FIG. 3 IH.N.M.R. spectrum in CDCl 3 , 90 MH z (Tetramethylsilane as internal standard): see FIG. 4 Formula: C 63 H 115 N 11 O 12 and when in amorphous powder form a m.pt. of 150°-153° C. and obtainable by hydrogenating cyclosporin G as defined in claim 1.
Claim 7
Dependent Claim
9 words
The compound of claim 1 which is isocyclosporin G.
Claim 8
Dependent Claim
72 words
A process for the production of a compound of claim 1 which comprises, (a) cultivating a cyclosporin G-producing strain of the fungal species Tolypocladium under aerobic conditions in the presence of a nutrient medium until a sufficient amount of cyclosporin G is produced and thereafter isolating cyclosporin G, or (b) reducing cyclosporin G by catalytic hydrogenation to produce dihydrocyclosporin G, or (c) rearranging cyclosporin G under acidic conditions to produce isocyclosporin G.
Claim 9
Dependent Claim
30 words
A pharmaceutical composition useful in treating chronic inflammations or immunosuppressant disorders comprising a therapeutically effective amount of a compound of claim 1 in association with a pharmaceutical carrier or diluent.
Claim 10
Dependent Claim
32 words
A method of treating chronic inflammations or immunosuppressant disorders in animals, which comprises administering a therapeutically effective amount of a compound of claim 1 to an animal in need of said treatment.
References Cited (Backward Citations)
US4108985A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1984-09-07 | 1985-03-09 | 1985-09-08 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-09-07 | 1989-03-09 | 1989-09-08 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-09-07 | 1993-03-09 | 1993-09-08 | $7700.00 | Window Closed / Lapsed |