Sandoz Gmbh

Novartis Ag

Rene P Traber

Hans Hofmann

Roland M Wenger

Hans Kobel

Eugen Harri

Dieter Seebach

Pietro Bollinger

Max Kuhn

Soo Young Ko

Brigitte Besemer-Rosenwirth

Kuhn Max

It has been found that nonimmunosuppressive, cyclophilin-binding cyclosporins are useful in the treatment and prevention of AIDS and AIDS-related disorders. Such cyclosporins include novel Ciclosporin derivatives modified at the 4- and/or 5-positions.

Cyclosporins

Nonimmunosuppressant cyclosporin derivatives having cyclophilin-binding activity, for example, the compound, �MeIle!.sup.4 -ciclosporin, are useful in inhibiting HIV-1 replication in treating AIDS and AIDS related disorders.

Cyclosporins wherein the amino acid residue at the 8-position is a (D)-acyloxy-.alpha.-amino acid residue, typically of formula ##STR1## wherein X=-MeBmt- or -dihydro-MeBmt-, Y=-.alpha.Abu-, -Ala-, -Thr-, -Val- or -Nva-, Z=-Val- or -Nva- and Q=R.sub.1 --CO--O--CH(R.sub.2)--CH(CO--)--NH--wherein R.sub.1 =H, C.sub.1-4 alkyl or phenyl and R.sub.2 =H or CH.sub.3, possess immunosuppressive, anti-inflammatory and anti-parasitic activity.

Novel cyclosporins

The present invention relates to cyclosporin derivatives, especially compounds of formula I ##STR1## wherein A is ##STR2## useful as anti-arthritic agents.

Process for producing cyclosporin derivatives

Compounds of formula I ##STR1## selected from the group consisting of cyclosporin G, wherein A is ##STR2## dihydrocyclosporin G, wherein A is ##STR3## and isocyclosporin G, wherein A is ##STR4## are useful in treating inflammations and arthritis and as immuno-suppressant agents.

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Basel, Switzerland

Rene P Traber