Cyclosporins and their use a pharmaceuticals

Details Cyclosporins and their use a pharmaceuticals Cyclosporins and their use a pharmaceuticals

C - Chemistry, Metallurgy

07

K

530/7.64, 167/10

C07K 7/64 (2006.01) A61K 38/13 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1338728

Cyclosporins wherein the residue at the 1-position (typically -MeBmt- or -dihydro-MeBmt-) is 3'0-acylated or 3'-oxo or -C1-4 alkoxyimino substituted, or wherein the residue at the 2-position is .beta.-0-acyl or .beta.-oxo substituted, or wherein the residue at the 2-position is -Ile-, or wherein the residue at the 11-position is -MeAla-, -MeIle- or -MealloIle- as well as various naturally occurring cyclosporins/dihydro-derivatives thereof, are useful in reversing resistance to chemotherapy, in particular resistance to cytostatic or anti-neoplastic therapy. Various of these cyclosporins and intermediates for their production are novel. Intermediates wherein the residue (e.g. -MeBmt-, -dihydro-MeBmt- etc.) at the 1-position is 8'-alkoxy or 7'-desmethyl-7'-hydrocarbyl substituted are novel and useful as immunosuppressants, anti-inflammatory and anti-parasitic agents.

569523

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