New alkyl-ketone compounds are histone deacetylase inhibitors, useful to treat e.g. cancer, hematologic or solid tumors, non-Hodgkins tumors, T-cell lymphoma, type I diabetes or Hashimoto's thyroiditis, and to modulate e.g. cell cycle

摘要

Alkyl-ketone compounds (I), are new. Alkyl-ketone compounds of formula (Ar1-[CH 2] m-Z 1-N(Z 2-R 2)-Z 3-[CO] r-[CH 2] n-Y 1-[CO] s-Y 2-R 1) (I), are new. Ar1 : benzyl, aryl- or heteroaryl (all containing 1-3 substituents of -F, -Cl, -1-4C alkyl, -OH, -O-1-4C alkyl, -CF 3or -NH 2); Z 1-Z 3a direct bond, O or S; Y 1, Y 2a direct bond, N(-R 2), - N(-R 2)-O-, -O-N(-R 2), O or S; n : 1-10; m : 0-4; r, s : 0 or 1; R 1benzyl- or (hetero)aryl residue (both containing 1-3 substituents of -F, -Cl, 1-4C alkyl, -OH, -O-1-4C alkyl, -CF 3- or -NH 2); and R 2H or 1-4C alkyl. ACTIVITY : Cytostatic; Antianemic; Antiapoptotic; Apoptotic; Angiogenesis Modulator; Antiinflammatory; Antiasthmatic; Antiallergic; Ophthalmological; Dermatological; Antiarthritic; Osteopathic; Vasotropic; Antirheumatic; Gastrointestinal-Gen; Antibacterial; Immunosuppressive; Antidiabetic; Hemostatic; Neuroprotective; Muscular-Gen; Antipsoriatic; Nephrotropic; Respiratory-Gen; Immunomodulator; Anabolic; Cardiant; Nootropic; Tranquilizer; Anticonvulsant; Neuroleptic. MECHANISM OF ACTION : Histone deacetylase inhibitor; Dipeptidyl peptidase IV inhibitor.