Patent ID: 6200989
Filing Date: 2001-03-13
Classification: A61P,C07D

Abstract:
A method of antagonizing the urokinase plasminogen activator receptor in a patient suffering from a solid tumor, or metastases thereof, comprising administering to the patient in need thereof a urokinase plasminogen activator receptor antagonizing amount of a compound of the formula (I): ##STR21##wherein:R and R' are independently hydrogen, C.sub.1-6 -alkyl, styryl or C.sub.3 -cycloalkyl or, taken together with the carbon to which they are linked, form a C.sub.3-6 -cycloalkyl group;x is 0 or 1;A is --(CH.sub.2).sub.n --, --CH.sub.2 CH.dbd.CHCH.sub.2 --, --CH.sub.2 --CH.dbd.CH--CH.dbd.CH--CH.sub.2 --, --CH.sub.2 --CH.dbd.CH--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, --CH.sub.2 --CH.dbd.CH--CH.sub.2 --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.dbd.CH--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, --CH.sub.2 --CHOH--CHOH--CH.sub.2 --, --(CH.sub.2).sub.q --O--(CH.sub.2).sub.q, or --CH.sub.2 --A'--CH.sub.2 --,wherein q is an integer from 2 to 3 and n is an integer from 2 to 6, and A' is a C.sub.3-7 -cycloalkyl group;B is ##STR22##T is --CH.sub.2 --C.tbd.CH, --C.tbd.CH, --(CH.sub.2).sub.p --R.sup.3, --CH.dbd.CH--R.sup.3, --CH.sub.2 --NHCO--R.sup.3, --(CH.sub.2).sub.p --O--R.sup.3, or --CH(NH2)--CH.sub.2 R.sup.3, in which p is 0 or an integer from 1to 4, R.sup.3 is phenyl, naphthyl or biphenyl, unsubstituted or substituted by chlorine, bromine, iodine, fluorine, (C1-C6)alkyl, cyano, nitro, mono- or polyfluoroalkyl, --SO.sub.2 (C.sub.1-4 alkyl, --SO.sub.2 NH.sub.2, --SO.sub.2 NH(C.sub.1-4)alkyl, --SO.sub.2 N[(C.sub.1-4)alkyl].sub.2, --CONH.sub.2, --CONH(C.sub.1-4)alkyl, hydroxy, amino, carboxy, C.sub.1-4 -alkoxy, (C.sub.1-4) mono- or di-alkyl amino, (C.sub.1-4,)alkoxycarbonyl, mercapto, or C.sub.1-4 -alkylthio, or is a 5- or 6-membered heterocycle which contains 1or 2 heteroatom(s) selected from oxygen, sulfur or nitrogen and which is or is not benzocondensed, or an enantiomer, diastereoisomer, or racemate of a compound of formula I, or a mixture thereof, or a pharmaceutically acceptable salt of a compound of formula I.