Patent ID: 6100271
Filing Date: 2000-08-08
Classification: A61P,C07D

Abstract:
A therapeutic compound, including resolved enantiomers, diastereomers, salts, or solvates thereof, having the formula:CORE MOIETY --(R).sub.jwherein:j is an integer from one to three;the core moiety is xanthinyl; andR is a member selected from the group consisting of hydrogen, hydroxyl, amino, C.sub.(1-10) alkyl, C.sub.(2-10) alkenyl, carbocyclic group and heterocyclic group and at least one R having formula I: ##STR8## with the proviso that the R having formula I is not attached at the N.sub.9 nitrogen atom of the xanthinyl;wherein:p is two;n is an integer from seven to twenty;(CH.sub.p).sub.n is unsubstituted or substituted by a member selected from the group consisting of halogen, hydroxyl, C.sub.(1-10) allyl, C.sub.(2-10) alkenyl, C.sub.(1-10) alkoxyl, C.sub.(1-10) alkanoyloxyl, C.sub.(1-10) oxoalkyl, carbocyclic group and heterocyclic group;R.sub.1 is a member selected from the group consisting of CH.sub.2 ; NR.sub.3, R.sub.3 being hydrogen, C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, or carbocyclic or heterocyclic group; O; --CHR.sub.4 O-- or --C(R.sub.4).sub.r O--, r being one or two, R.sub.4 being .dbd.O, hydrogen, C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, C.sub.(1-20) aminoalkyl, --(CH.sub.2).sub.q A(R.sub.5).sub.m, q being an integer from one to four, A being N or O, m being one or two and R.sub.5 being hydrogen, C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl, C.sub.(1-10) hydroxyalkyl, C.sub.(1-10) aminoalkyl, carbocyclic group or heterocyclic group;R.sub.2 is a member selected from the group consisting of hydrogen, halogen, C.sub.(1-10) alkyl, C.sub.(1-10) alkoxyl, C.sub.(2-10) alkenyl, C.sub.(1-10) hydroxyalkyl, C.sub.(1-20) aminoalkyl, --A(R.sub.5).sub.m and --CHR.sub.6 A(R.sub.5).sub.m ; wherein A, R.sub.5 and m are as defined above, R.sub.6 is a C.sub.(1-20) alkyl, C.sub.(1-20) alkoxyl, C.sub.(2-20) alkenyl, C.sub.(1-20) hydroxyalkyl, C.sub.(1-20) aminoalkyl, carbocyclic group or heterocyclic group, or A is N, m is two and the two R.sub.5 join together with the A to form a heterocycle having from four to seven ring atoms selected from the group consisting of N, C and O, the A comprising a heteroatom of the heterocycle;wherein at least one of: 1) R.sub.1 is NR.sub.3, O, or --CHR.sub.4 O-- or 2) R.sub.2 is --A(R.sub.5).sub.m ; andwherein said carbocyclic group or heterocyclic group is a member selected from the group consisting of: anthracenyl, bicyclo[4.4.0]decanyl, bicyclo[2.2.1]heptanyl, bicyclo[3.2.0]heptanyl, bicyclo[4.1.0]heptanyl, bicylo[2.2.1]hexanyl, bicyclo[4.3.0]nonanyl, bicyclo[2.2.2]octanyl, biphenyl, cyclopentadienyl, cyclopentanyl, cyclobutanyl, cyclobutenyl, cycloheptanyl, cyclohexanyl, cyclooctanyl, cyclopropanyl, fluorenyl, indenyl, phenyl, quinonyl, napthalenyl, phenanthrenyl, azetidinyl, benzofuranyl, benzothiophenyl, carbazolyl, furanyl, glutarimidyl, indolyl, isoquinolinyl, oxazolyl, oxetanyl, oxiranyl, pyrrolidinyl, pyranyl, piperidinyl, pyridinyl, pyrrolyl, quinolinyl, tetrahydrofuranyl, tetrahydropyranyl, tetrahydrothiophenyl and thiophenyl.