Novel derivatives of rapamycin, particularly 9-deoxorapamycins, 26-dihydro-rapamycins, and 40-0-substituted and 28,40-0,0-di-substituted rapamycins, are found to have pharmaceutical utility, particularly as an immunosuppressants.
This invention provides new antibiotics produced by cultivating a strain of the fungus species, Cylindrocarpon lucidum Booth or Tolypocladium inflatum Gams in contact with a nutrient medium, the antibiotics being useful anti-inflammatory and immunosuppressive agents.
The present invention relates to cyclosporin derivatives, especially compounds of formula I ##STR1## wherein A is ##STR2## useful as anti-arthritic agents.
Novel cyclosporins having an -Allylgly- residue in the 2-position and/or a -(D)-Ser- residue in the 8-position and process for their production. The novel cyclosporins are useful as pharmaceuticals, e.g. as immunosuppressive and anti-inflammatory agents.
Hydroxy-substituted [(D)Ser].sup.8 -Ciclosporin derivatives, particularly [O-(2-hydroxyethyl)(D)Ser].sup.8 -Ciclosporin, have advantageous pharmacological properties and are useful as immunosuppressants, for example in the treatment of transplant rejection and autoimmune diseases.
A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in t ...