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US4639434A Expired / Lapsed US ⏱️ 0.0 years remaining

Novel cyclosporins

Assignee: Novartis AG
•
Filing: 1985-03-19
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Granted: 1987-01-27
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Expires: 2005-03-19
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Abstract

Abstract Cyclosporins wherein the amino acid residue at the 8-position is a (D)-acyloxy- alpha -amino acid residue, typically of formula <IMAGE> wherein X=-MeBmt- or -dihydro-MeBmt-, Y=- alpha Abu-, -Ala-, -Thr-, -Val- or -Nva-, Z=-Val- or -Nva- and Q=R1-CO-O-CH(R2)-CH(CO-)-NH-wherein R1=H, C1-4alkyl or phenyl and R2=H or CH3, possess immunosuppressive, anti-inflammatory and anti-parasitic activity.

Inventors

  • 👤 Roland Wenger
  • 👤 Rene P. Traber
  • 👤 Hans Kobel
  • 👤 Hans Hofmann

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 06:58
CPC Classifications
C; C07; C07K; C07K7/00; C07K7/64; C07K7/645; A; A61; A61P; A61P29/00; A61P31/00; A61P31/04; A61P33/00; A61P37/00; A61P37/02; A61P37/06; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/19; Y10S930/27

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 95 words
A cyclosporin of formula IIIa, ##STR10## wherein Y' is -αAbu-, -Thr-, -Val- or -Nva-, Z' is -Val-, when Y' is -Thr-, or -Val- or Z' is -Val- or -Nva-, when Y' is -αAbu- or -Nva-, W' is -(D)Ser-, when Y' is -Thr-, -Val- or -Nva- and Z' is -Val-, or when Y' is -αAbu- or -Nva- and Z' is -Nva- or W' is -(D)Thr-, when Y' is -αAbu- and Z is -Val-, and X' is -MeBmt- or X' is -dihydro -MeBmt-, when Y' is -Thr-, -Val-, or -Nva-, Z' is -Val- and W' is -(D)Ser-.
Claim 2
Dependent Claim 95 words
A cyclosporin of formula IIIa, ##STR10## wherein Y' is -αAbu-, -Thr-, -Val- or -Nva-, Z' is -Val-, when Y' is -Thr-, or -Val- or Z' is -Val- or -Nva-, when Y' is -αAbu- or -Nva-, W' is -(D)Ser-, when Y' is -Thr-, -Val- or -Nva- and Z' is -Val-, or when Y' is -αAbu- or -Nva- and Z' is -Nva- or W' is -(D)Thr-, when Y' is -αAbu- and Z is -Val-, and X' is -MeBmt- or X' is -dihydro -MeBmt-, when Y' is -Thr-, -Val-, or -Nva-, Z' is -Val- and W' is -(D)Ser-.
Claim 3
Dependent Claim 11 words
A cyclosporin according to claim 1 which is [(D)Thr] 8 -Cyclosporine.
Claim 4
Dependent Claim 13 words
A cyclosporin according to claim 1 which is [Nva] 2 -[(D)Ser] 8 -Cyclosporine.
Claim 5
Dependent Claim 15 words
A cyclosporin according to claim 1 which is [Nva] 2 -[Nva] 5 [(D)Ser] 8 -Cyclosporine.
Claim 6
Dependent Claim 30 words
A pharmaceutical composition for inducing immuno suppression, treating inflammation, or treating parasitic infection comprising a cyclosporin as defined in claim 1 together with a pharmaceutically acceptable diluent or carrier therefor.
Claim 7
Dependent Claim 40 words
A method of inducing immuno suppression, 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)

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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) 1990-01-26 1990-07-28 1991-01-27 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-01-26 1994-07-28 1995-01-27 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-01-26 1998-07-28 1999-01-27 $7700.00 Window Closed / Lapsed

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