RU94011565A - THIOXANTENONE COMPOUNDS, THEIR USE, ANTI-SMALL COMPOSITION - Google Patents

Claims (1)

Patented compounds with antitumor activity, structure:

where (1) n is 2 or 3; R ¹ and R ² are independently lower alkyl; Q is a residue selected from the group consisting of CH ₂ NHR ³ , CH ₂ N (R ⁴ ) SO ₂ R ⁷ , CH ₂ NHCHO, CH = N - AR, C (O) NR ⁵ R ⁶ , CH ₂ N ( P ⁴ ) C (O) R ⁷ , CH ₂ N (C ₂ H ₅ ) CHO, CH ₂ N (R ⁴ ) P (O) (O-lower alkyl) ₂ , CH ₂ N = CH - N (R ⁹ ) (R ^{1 0} ),
CH ₂ N (R ⁴ ) C (O) CF ₃ and CH ₂ N (R ⁴ ) C (O) OR ⁷ ; R ³ is hydrogen or lower alkyl; R ⁴ is hydrogen, lower alkyl or Ar; R ⁵ is hydrogen or lower alkyl; R ⁷ is lower alkyl or Ar; R ⁸ is hydroxyl; Ar is phenyl or phenyl substituted by methyl, methoxy, hydroxyl, halogen or nitro; and R ⁹ and R ^{1 0} - independently of each other, lower alkyl; (2) Q is a residue selected from the group consisting of CHN (R ⁴ ) SO ₂ R ⁷ , CH = N-AR, C (O) NR ⁵ R ⁶ , CH ₂ N (R ⁴ ) C (O) R ⁷ , CH ₂ N (R ⁴ ) P (O) (O-lower alkyl) ₂ , CH ₂ N (R ⁴ ) C (O) CF ₃ and CH ₂ N (R ⁴ ) C (O) OR ⁷ ; R ⁸ is hydrogen, lower alkyl, lower alkoxy or hydroxyl; Ar is phenyl substituted by hydroxyl and n, R ¹ , R ² , R ⁴ , R ⁵ , R ⁶ and R ⁷ take the values defined in part (1), provided that one or more of R ⁴ , R ⁵ or R ⁷ - Ar; or (3) Q is a residue selected from the group consisting of CH ₂ N = CHN (R ⁹ ) (R ^{1 0} ), CH ₂ N (R ⁴ ) C (O) CF ₃ and CH ₂ N (R ⁴ ) C (O) OR ⁷ ; R ⁸ is hydrogen, lower alkyl, lower alkoxy or hydroxyl; and n, R ¹ , R ² , R ⁴ , R ⁷ , Ar, R ⁹ and R ^{1 0} are as defined in paragraph (1), or their pharmaceutically acceptable acid addition salts or solvates. Thioxantenone-containing compositions and methods for treating tumors and cancer diseases in mammals using thioxantenones are also patented.