Isoxazole-4-carboxamides and hydroxyalkylidenecyanoacetamides, pharmaceuticals containing these compounds and their use

A method for the treatment of leukemia, sarcomas, carcinoma, lymphoma, or skin cancer comprising the step of administrating a pharmaceutically effective amount of a compound of formula I, Ia, or Ib ##STR62## stereoisomeric forms thereof, or physiologically tolerable salts thereof, to a patient in need of such treatment, wherein

• R.sup.1 is
• a) hydrogen,
• b) alkyl having 1 to 6 carbon atoms,
• c) alkyl having 1 to 4 carbon atoms, mono- or polysubstituted by
• 1) halogen,
• d) phenyl,
• R.sup.2 is
• a) hydrogen,
• b) alkyl having 1 to 4 carbon atoms,
• c) phenyl-(C.sub.1 -C.sub.2)-alkyl,
• d) alkenyl having 2 to 3 carbon atoms,
• R.sup.3 is
• a) a mono-, di-, or trinuclear, unsaturated heterocyclic radical having 3 to 13 carbon atoms and 1 to 4 heteroatoms from the group comprising oxygen, sulfur, and nitrogen, of which a maximum of 1 is different from nitrogen, in the ring system, unsubstituted or mono- or polysubstituted by
• 1) halogen
• 2) alkyl having 1 to 3 carbon atoms,
• 3) alkyl having 1 to 3 carbon atoms, mono- or polysubstituted by
• 3.1 halogen,
• 4) alkoxy having 1 to 3 carbon atoms,
• 5) alkoxy having 1 to 3 carbon atoms, mono- or polysubstituted by
• 5.1 halogen,
• 6) nitro,
• 7) hydroxyl,
• 8) carboxyl,
• 9) carbamoyl,
• 10) an oxo group,
• b) a radical of the formula II, ##STR63## in which R.sup.4, R.sup.5, and R.sup.6 can be identical or different and are
• 1) hydrogen,
• 2) alkyl having 1 to 3 carbon atoms, mono- or polysubstituted by
• 2.1 halogen,
• 3) in which R.sup.4 is hydrogen and R.sup.5 and R.sup.6 together with the phenyl ring of formula II form a naphthalene ring,
• 4) in which R.sup.4 is hydrogen and R.sup.5 and R.sup.6 form a methylenedioxy radical,
• 5) alkoxy having 1 to 3 carbon atoms,
• 6) alkoxy having 1 to 3 carbon atoms, mono- or polysubstituted by
• 6.1 halogen,
• 7) (C.sub.1 -C.sub.3)-alkylmercapto,
• 8) (C.sub.1 -C.sub.3)-alkylmercapto, mono- or polysubstituted by
• 8.1 halogen,
• 9) halogen,
• 10) nitro,
• 11) cyano,
• 12) hydroxyl,
• 13) carboxyl,
• 14) (C.sub.1 -C.sub.3)-alkylsulfonyl,
• 15) carbalkoxy, having 1 to 3 carbon atoms in the alkyl chain,
• 16) benzoyl,
• 17) benzoyl, mono- or polysubstituted by
• 17.1 halogen,
• 17.2 (C.sub.1 -C.sub.3)-alkyl,
• 17.3 (C.sub.1 -C.sub.3)-alkoxy,
• 18) phenyl,
• 19) phenyl, mono- or polysubstituted by
• 19.1 (C.sub.1 -C.sub.3)-alkoxy,
• 19.2 halogen,
• 19.3 (C.sub.1 -C.sub.3)-alkyl,
• 20) phenoxy,
• 21) phenoxy, mono- or polysubstituted by
• 21.1 (C.sub.1 -C.sub.3)-alkoxy, mono- or polysubstituted by 21.1.1 halogen,
• 21.2 halogen,
• 21.3 (C.sub.1 -C.sub.3)-alkyl, mono- or polysubstituted by 21.3.1 halogen,
• c) a radical of the formula III,
• --(CH.sub.2).sub.n --COOR.sup.10 (III)
• in which R.sup.10 is
• 1) hydrogen
• 2) alkyl having 1 to 4 carbon atoms, n is an integer from 1 to 12,
• d) R.sup.2 and R.sup.3 together with the nitrogen to which they are bonded, form a 4- to 9-membered ring, substituted by
• 1) carbonyl on the carbon atom adjacent to the nitrogen atom,
• e) R.sup.2 and R.sup.3, together with the nitrogen to which they are bonded, form a 5- to 6-membered ring of the formula IV ##STR64## in which W is 1) --CH.sub.2 --,
• 2) --CH.sub.2 --CH.sub.2 --, ##STR65## 6) --CH.sub.2 --O-- or 7) --CH.sub.2 --S--
• R.sup.7 is
• a) hydrogen
• b) alkyl having 1 to 17 carbon atoms,
• c) alkyl having 1 to 3 carbon atoms, mono- or polysubstituted by halogen,
• d) phenyl-(C.sub.1 -C.sub.2)-alkyl;
• and
• R.sup.8 is
• a) hydrogen,
• b) methyl,
• c) alkenyl having 2 to 3 carbon atoms.