| 摘要 |
Non-peptidic compounds characterized by containing a segment condensed from pipecolic acid, aspartic acid, proline and threonine, or derivatives thereof, are useful to treat autoimmune diseases and inflammatory conditions. Compounds of particular interest are those of formula (I), wherein R<1> is phenyl or cyclohexyl; wherein R<2> is hydrido or methyl; wherein R<3> is selected from hydrido, hydroxy, acetylamino, acetyl (Lys/Tyr/Thr)NH-, propionylamino and benzyloxycarbonylamino; wherein R<5> is selected from isopropyl, isobutyl, n-propyl, n-butyl, aminopropyl, aminobutyl, phenyl, benzyl, hydroxyphenyl, hydroxybenzyl, morpholinocarbonylethyl, morpholinocarbonylpropyl, piperazinocarbonylethyl, piperazinocarbonylpropyl, pyridinylcarbonylethyl, pyridinylcarbonylpropyl, oxazolylcarbonylethyl, oxazolylcarbonylpropyl, azepinylcarbonylethyl and azepinylcarbonylpropyl; wherein R<6> is selected from hydrido, methyl, hydroxy, methoxy, phenyl and aminocarbonyl; wherein R<7> is carboxyl or methylthiomethyl; wherein R<9> is selected from hydrido, hydroxy, methoxy and phenyl; wherein R<12> is selected from methyl, ethyl, propyl, butyl, isobutyl, -CH(iBu)CH2OH and -CH(iBu)CONH2; or a pharmaceutically-acceptable amide, ester or salt thereof. A disease state of particular interest for use of the compounds would be rheumatoid arthritis.
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