Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Patent
1994-11-10
1996-06-11
Russel, Jeffrey E.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
530321, A61K 3813, C07K 764
Patent
active
055255906
ABSTRACT:
Cyclosporins wherein the residue at the 1-position (typically -MeBmt- or -dihydro-MeBmt-) is 3'O-acylated or 3'-oxo or -C.sub.1-4 alkoxyimino substituted, or wherein the residue at the 2-position is .beta.-O-acyl or .beta.-oxo substituted, or wherein the residue at the 2-position is -Ile-, or wherein the residue at the 11-position is -MeAls-, -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.
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Bollinger Pietro
Bolsterli Johann J.
Payne Trevor G.
Honor Robert S.
Kassenoff Melvyn M.
McGovern Thomas O.
Russel Jeffrey E.
Sandoz Ltd.
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