초록

The invention relates to a novel cyclosporin, the pharmaceutical use thereof and a pharmaceutical composition containing it.

대표청구항 ▼

What is claimed is: 1. Synthesised cyclosporin having the formula: wherein: X is-MeBmt or 6,7-dihydro-MeBmt- U is-Abu, Nva, Val or Thr Y is Sar or (D)-MeSer or (D)-MeAla or (D)-MeSer (OAcyl) Z is (N-R)aa where aa={Val, Ile, Thr, Phe, Tyr, Thr (OAc), Thr (OG1), Phe (G2), PheCH2(G3) or Tyr (OG3)}

What is claimed is: 1. Synthesised cyclosporin having the formula: wherein: X is-MeBmt or 6,7-dihydro-MeBmt- U is-Abu, Nva, Val or Thr Y is Sar or (D)-MeSer or (D)-MeAla or (D)-MeSer (OAcyl) Z is (N-R)aa where aa={Val, Ile, Thr, Phe, Tyr, Thr (OAc), Thr (OG1), Phe (G2), PheCH2(G3) or Tyr (OG3)} with R={alkyl>CH3}; G1={phenyl-COOH, phenyl-COOMe or phenyl-COOEt}; G2={CH2COOH, CH2COOMe(Et), CH2PO(OMe)2 or CH2PO(OH)2}; G3={PO(OH)2, PO(OCH2CH═CH2)2, CH2COOH, CH2COOMe, or CH2COOEt} 2. Cyclosporin according to claim 1, wherein the residue Z in position 4 is (R)Val where R>CH3 and R<C10H11. 3. Cyclosporin according to claim 1, wherein the residue Z in position 4 is N-ethyl-Valine. 4. Pharmaceutical composition containing the compound having the formula: wherein: X is-MeBmt or 6,7-dihydro-MeBmt- U is-Abu, Nva, Val or Thr Y is Sar or (D)-MeSer or (D)-MeAla or (D)-MeSer (OAcyl) Z is (N-R)aa where aa={Val, Ile, Thr, Phe, Tyr, Thr (OAc), Thr (OG1), Phe (G2), PheCH2(G3) or Tyr (OG3)} with R={alkyl>CH3}; G1={phenyl-COOH, phenyl-COOMe or phenyl-COOEt}; G2={CH2COOH, CH2COOMe(Et), CH2PO(OMe)2 or CH2PO(OH)2}; G3={PO(OH)2, PO(OCH2CH═CH2)2, CH2COOH, CH2COOMe, or CH2COOEt} 5. Pharmaceutical composition according to claim 4, combined with a pharmaceutically acceptable solution. 6. A medicinal product for the treatment and prevention of acquired immunodeficiency syndrome (AIDS) containing the cyclosporin according to claim 1 or claim 4 . 7. A medicinal product for the treatment and prevention of AIDS containing the cyclosporin according to claim 3. 8. The pharmaceutical composition according to claim 4 for the treatment of acquired immunodeficiency syndrome AIDS.