| abstract |
Cyclosporins in which the amino acid residue at position 1 is either derived from 2-carboxyazetidine, 2-carboxypyrrolidine (proline) or 2-carboxypiperidine, which may optionally be substituted on a ring carbon atom other than that at position 2 by an amino, methylamino, mercapto or hydroxy group, said group optionally being in derivative form, and/or by an acyclic aliphatic hydrocarbon group, or is an amino acid residuen wherein n is 0, 1 or 2, X represents an amino, methylamino, mercapto or hydroxy group which may optionally be in derivative form, R represents hydrogen or, when n is 1 or 2 and X represents an amino, methylamino, mercapto or hydroxy group, or when n is 0 and X represents an amino, methylamino or mercapto group, R represents an acyclic aliphatic hydrocarbon group, and R′ represents hydrogen or methyl; and/or the amino acid residue at position 2 is an amino acid residue n n-NH- -CO- wherein R₁ represents an acyclic aliphatic hydrocarbon group of four or more carbon atoms optionally substituted at the C₁ position by an amino, methylamino, mercapto or hydroxy group or such a group in derivative form, are of therapeutic value in various contexts in which the cyclosporins are used, for example as anti-bacterial agents and particularly as immunosuppressive and anti-inflammatory agents. |