New water-soluble 2-(2,6-di:oxo-3-piperidinyl)-1H-iso-indole-1-di:one deriv. - may be administered parenterally and have comparable activity to thalidomide itself

摘要

Thalidomide derivs. of formula (I) and/or their salts, in racemic or optically active form, are new R1, R2 = 1-6C alkyl; or R1 + R2 = CH2CH2XCH2CH2; R3 = H or Me; X = O or NH. USE/ADVANTAGE - (I) have immunosuppresive and immunomodulating activity comparable, at least, to thalidomide itself. (I) are more water-soluble than thalidomide so that lower side effects are to be expected. Admin. is esp. parenteral. For example, for treatment of leprosy, colitis ulceroso or graft-versus-host diseases, medicaments contg. (I) can be administered intravenously, intradermally, intramuscularly or intranasally.