- PROLINE DERIVATIVES USED AS PHARMACEUTICAL ACTIVE INGREDIENTS FOR THE TREATMENT OF TUMOURS
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The invention relates to proline derivatives and their salts, to pharmaceutical agents containing said derivatives and to the use of said agents for treating tumours. The invention also relates to methods for producing said compounds and pharmaceutical ag
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Page/Page column 39-40
(2008/06/13)
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- Peptide skeletal muscle relaxants
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Novel diquaternary polypeptides possessing skeletal muscle relaxation activity represented by the formulae: STR1 wherein: R is lower alkyl; R1 and R2 are lower alkyl or R1 and R2, together with the nitrogen to which they are attached form a heterocyclic ring having 5 to 7 member atoms; R3 is lower alkyl, [N,N-di(lower alkyl)-3-piperidinium](+), or [N,N-di(lower alkyl)-4-piperidinium](+) R4 is selected from the group consisting of t-butyl, benzyl or fluorenylmethyl; A1 is selected from the group consisting of trans-4-acetoxyproline, phenylalanine, glutamic acid-γ-methyl ester, or proline; AA2 is selected from the group consisting of phenylalanine, leucine, 3-(2-naphthyl)alanine, 3-(1-naphthyl)alanine, and 3-cyclohexylalanine; AA3 is proline when R3 is [N,N-di(lower alkyl)-3-piperidinium](+) or [N,N-di(lower alkyl)-4-piperidinium](+), and is Orn(δ-N(+) --R--R1 --R2) or Lys(ε-N(+) --R--R1 --R2) when R3 ia lower alkyl; AA4 is Orn(δ-N(+)--R--R1 --R2) or Lys(ε-N(+) --R--R1 --R2); Z(-) is a pharmaceutically acceptable anion; and (R)m R1 R2 N(+) represents the acceptable anion; (R)m R1 R2 N(+) -- represents the alpha amino group of AA1 ; and m represents an integer of 0 or 1 with the proviso that m is zero only when AA1 is trans-4-acetoxyproline or proline.
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- Enantioselective Solvent Extraction of Neutral DL-Amino Acids in Two-Phase Systems Containing N-n-Alkyl-L-proline Derivatives and Copper(II) Ion
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Distribution behavior of neutral amino acid enantiomers was examined in the aqueous and organic solvent of a two-phase system containing cupric ion and N-n-dodecyl-L-proline or N-n-alkyl-L-hydroxyproline.Significant enentioselectivity was observed when n-butyl, n-amyl, or n-octyl alcohol was used as the organic solvent.Equilibrium constants of ligand exchange reaction for several amino acid enantiomers were estimated for the n-butyl alcohol-water system.The enantioselectivity seems to depend primarily on the difference of the stability of mixed ligand complexes in the organic phase.
- Takeuchi, Toshifumi,Horikawa, Rikizo,Tanimura, Takenori
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p. 1152 - 1155
(2007/10/02)
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