Patent ID: 6103910
Filing Date: 2000-08-15
Classification: A61P,C07D

Abstract:
A D-proline compound of the formula: ##STR101## wherein R.sup.1 is hydrogen or halogen;x is --(CH.sub.2).sub.n --; --CH(R.sup.2)(CH.sub.2).sub.n --; --CH.sub.2 O(CH.sub.2).sub.n --; --CH.sub.2 NH--; benzyl; --C(R.sup.2).dbd.CH--; --CH.sub.2 CH(OH)--; or thiazol-2,5-diyl;Y is --(CH.sub.2).sub.n --; --O--; --NH--; --N(R.sup.2)--; --CH.dbd.CH--; --NHC(O)NH--; --N(R.sup.2 )C(O)N(R.sup.2)--; --N[CH.sub.2 C.sub.6 H.sub.3 (OCH.sub.3).sub.2 ]--; --N(CH.sub.2 C.sub.6 H.sub.5)--; --N(CH.sub.2 C.sub.6 H.sub.5)C(O)N(CH.sub.2 C.sub.6 H.sub.5)--; --N(alkoxyalkyl)--; --N(cycloalkyl-methyl)--; 1,2-cyclohexyl; 1,3-cyclohexyl; 1,4-cyclohexyl; 1,2-naphthyl; 1,4-naphthyl; 1,5-naphthyl; 1,6-naphthyl; biphenyl; 1,2-phenylen;1,3-phenylen;1,4phenylen; 1,2-phenylen substituted by 1 to 4 substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, hydroxy, carboxy, --COO-lower alkyl, and nitrilo, 1,3-phenylen substituted by 1 to 4 substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy, hydroxy, carboxy, --COO-lower alkyl, and nitrilo; and 1,4-phenylen substituted by 1 to 4 substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, carboxy, --COO-lower alkyl, and nitrilo;X.sup.1 is --(CH.sub.2).sub.n --; --(CH.sub.2).sub.n CH(R.sup.2)--; --(CH.sub.2).sub.n OCH.sub.2 --; --NHCH.sub.2 --; benzyl; --CH.dbd.C(R.sup.2)--; --CH(OH)CH.sub.2 ; or thiazol-2,5-diyl;R.sup.2 is lower alkyl, lower alkoxy, or benzyl;--is a single or a double bond; andn is 0-3,or a pharmaceutically acceptable salt, monoester, or diester thereof.