New tubulysin analogs, useful for treating tumor or cancer diseases, immunologically induced or autoimmune diseases, inflammatory diseases or rheumatoid arthritis or for surface modification of implants

摘要

Analogs (I) of tubulysins (natural cytotoxic tetrapeptides) are new. Tubulysin analogs of formula (I) (with the exception of the natural tubulysins of formula (I')) and their salts, solvates and hydrates are new. [Image] A : optionally substituted 5- or 6-membered heteroarylene; X : O, S, NR 1 3 or CR 1 4R 1 5; Y : O, S or NR 1 6; R 1 - R 1 6H, alkyl, alkenyl, alkynyl, heteroalkyl, aryl, heteroaryl, cycloalkyl, alkylcycloalkyl, heteroalkylcycloalkyl, heterocycloalkyl, aralkyl or heteroaralkyl; or two groups together form part of a cycloalkyl or heterocycloalkyl ring system; Ra : H, alkyl, alkenyl, aryl or heteroaryl; Rb : H, OH, alkyl, aryl or heteroaryl. ACTIVITY : Cytostatic; immunosuppressive; antiinflammatory; antirheumatic; antiarthritic; antidiabetic; fungicide. MECHANISM OF ACTION : None given in the source material.