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HK1005741B - Cyclosporins - Google Patents

Cyclosporins Download PDF

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Publication number
HK1005741B
HK1005741B HK98104804.1A HK98104804A HK1005741B HK 1005741 B HK1005741 B HK 1005741B HK 98104804 A HK98104804 A HK 98104804A HK 1005741 B HK1005741 B HK 1005741B
Authority
HK
Hong Kong
Prior art keywords
ciclosporin
meleu
hydroxy
mebmt
meval
Prior art date
Application number
HK98104804.1A
Other languages
German (de)
English (en)
Chinese (zh)
Other versions
HK1005741A1 (en
Inventor
Young Ko Soo
Kobel Hans
Rosenwirth Brigitte
Seebach Dieter
P. Traber Rene
Wenger Roland
Bollinger Pietro
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB909023859A external-priority patent/GB9023859D0/en
Priority claimed from GB909023971A external-priority patent/GB9023971D0/en
Priority claimed from GB909023972A external-priority patent/GB9023972D0/en
Priority claimed from GB909023970A external-priority patent/GB9023970D0/en
Priority claimed from GB919116836A external-priority patent/GB9116836D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of HK1005741B publication Critical patent/HK1005741B/en
Publication of HK1005741A1 publication Critical patent/HK1005741A1/en

Links

Claims (13)

  1. L'utilisation d'une cyclosporine pour la préparation d'un médicament pour le traitement et la prévention du SIDA et des troubles liés au SIDA, caractérisée en ce que la cyclosporine
    (i) se lie à la cyclophiline humaine selon un rapport de liaison (RL) inférieur à 0,7, le RL étant le logarithme de la base 10 du rapport de la CI50 de la cyclosporine à la CI50 de la Ciclosporine telle que mesurée selon un essai ELISA compétitif, et
    (ii) a une activité dans la réaction lymphocytaire mixte ne dépassant pas 5% de celle de la Ciclosporine.
  2. Un procédé de préparation d'une composition pharmaceutique comprenant l'association d'un composé de formule I dans laquelle
    W   signifie MeBmt, dihydro-MeBmt ou 8'-hydroxy-MeBmt,
    X   signifie αAbu, Val, Thr, Nva ou MeOThr,
    R   signifie Sar ou (D)-MeAla,
    Y   signifie MeLeu, γ-hydroxy-MeLeu, MeIle, MeVal, MeThr, MeAla, MeaIle ou MeaThr,
    Z   sigifie Val, Leu, MeVal ou MeLeu, et
    Q   signifie MeLeu, γ-hydroxy-MeLeu ou MeAla,
    à condition que lorsque Y signifie MeLeu, Z signifie alors MeVal ou MeLeu ou bien W signifie 8'-hydroxy-MeBmt, avec un diluant ou véhicule pharmaceutiquement acceptable.
  3. Un procédé de préparation d'une composition pharmaceutique selon la revendication 2, dans lequel le composé de formule I est un composé de formule I' dans laquelle
    W'   signifie MeBmt ou dihydro-MeBmt,
    X'   signifie αAbu ou Nva,
    Y'   signifie γ-hydroxy-MeLeu, MeVal, MeThr ou MeIle, et
    Z'   signifie Val ou MeVal.
  4. Un procédé de préparation d'une composition pharmaceutique, comprenant l'association d'un composé choisi parmi
    la [dihydro-MeBmt]1-[γ-hydroxy-MeLeu]4-Ciclosporine,
    la [MeVal]4-Ciclosporine,
    la [MeIle]4-Ciclosporine,
    la [MeThr]4-Ciclosporine,
    la [γ-hydroxy-MeLeu]4-Ciclosporine,
    la [Nva]2-[γ-hydroxy-MeLeu]4-Ciclosporine,
    la [γ-hydroxy-MeLeu]4-[γ-hydroxy-MeLeu]6-Ciclosporine,
    la [MeVal]5-Ciclosporine,
    la [MeOThr]2-[(D)MeAla]3-[MeVal]5-Ciclosporine,
    la [8'-hydroxy-MeBmt]1-Ciclosporine, et
    la [γ-hydroxy-MeLeu]9-Ciclosporine,
    avec un diluant ou véhicule pharmaceutiquement acceptable.
  5. L'utilisation d'un composé de formule I ou I' tel que décrit à la revendication 2 ou 3 ou d'un composé choisi parmi les cyclosporines indiquées à la revendication 4, pour la préparation d'un médicament pour le traitement et la prévention du SIDA et des troubles liés au SIDA.
  6. Un procédé de préparation de la [MeIle]4-Ciclosporine, comprenant l'étape de culture dans un milieu nutritionnel d'une souche de Tolypocladium inflatum Gams produisant une [MeIle]4-Ciclosporine, et l'isolement du produit à partir du bouillon de fermentation.
  7. Le procédé selon la revendication 6, lorsque la souche de Tolypocladium inflatum Gams produisant une [MeIle]4-Ciclosporine est la souche de champignon DSM 6627.
  8. Une culture pure de la souche de champignon DSM 6627.
  9. Un procédé de préparation de cyclosporines qui comportent un ou plusieurs résidus γ-hydroxy-MeLeu, comprenant les étapes de culture de la souche de champignon DSM 6182 dans un milieu nutritionnel, l'addition d'une cyclosporine qui comporte un ou plusieurs résidus MeLeu, et l'isolement du produit à partir du bouillon de fermentation.
  10. Une culture pure de la souche de champignon DSM 6182.
HK98104804A 1990-11-02 1998-06-03 Cyclosporins HK1005741A1 (en)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
GB9023859 1990-11-02
GB909023859A GB9023859D0 (en) 1990-11-02 1990-11-02 Chemical products
GB9023972 1990-11-05
GB909023971A GB9023971D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB909023972A GB9023972D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB909023970A GB9023970D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB9023970 1990-11-05
GB9023971 1990-11-05
GB919116836A GB9116836D0 (en) 1991-08-05 1991-08-05 Organic compounds
GB9116836 1991-08-05

Publications (2)

Publication Number Publication Date
HK1005741B true HK1005741B (en) 1999-01-22
HK1005741A1 HK1005741A1 (en) 1999-01-22

Family

ID=27517009

Family Applications (1)

Application Number Title Priority Date Filing Date
HK98104804A HK1005741A1 (en) 1990-11-02 1998-06-03 Cyclosporins

Country Status (25)

Country Link
US (3) US5767069A (fr)
EP (1) EP0484281B2 (fr)
JP (1) JP2740775B2 (fr)
KR (1) KR100203556B1 (fr)
AT (1) ATE148469T1 (fr)
AU (1) AU649277B2 (fr)
CA (1) CA2054590C (fr)
CY (1) CY2159B1 (fr)
CZ (1) CZ280909B6 (fr)
DE (1) DE69124459T3 (fr)
DK (1) DK0484281T4 (fr)
ES (1) ES2095926T5 (fr)
FI (1) FI111730B (fr)
GR (2) GR3022592T3 (fr)
HK (1) HK1005741A1 (fr)
HU (1) HU212674B (fr)
IE (1) IE913824A1 (fr)
IL (1) IL99912A (fr)
MX (1) MX9101869A (fr)
MY (1) MY134806A (fr)
NZ (1) NZ240421A (fr)
PL (1) PL168609B1 (fr)
PT (1) PT99410B (fr)
SA (1) SA92120344B1 (fr)
SK (1) SK278808B6 (fr)

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