Pteridine derivatives for the treatment of septic shock and tnf-a-related diseases
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Abstract
This invention relates to the use of a group of pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, for the manufacture of a medicament for the prevention or treatment of TNF-α related disorders.
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Citations
27 Claims
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1-7. -7. (canceled)
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8. A method of prevention or treatment of a disorder in a mammal, the said disorder being selected from the group consisting of toxic effects of TNF-α
- , alcohol-induced hepatitis, and cachexia, comprising administering to said mammal an effective amount of a pteridine derivative having the structural formula (I);
wherein X represents an oxygen atom or a group with the formula S(O)m wherein m is an integer from 0 to 2, or a group with the formula NZ and wherein;
R1 is selected from the group consisting of methyl, ethyl, isopropyl and pentyl;
Z is a group independently defined as R1 or Z is hydrogen or the group NZ together with R1 is either hydroxylamino or an optionally substituted heterocyclic group containing at least one nitrogen atom;
R2 is selected from the group consisting of amino;
acylamino;
R4 is an atom or a group selected from the group consisting of hydrogen;
halogen;
C1-7 alkyl;
C2-7 alkenyl;
C2-7 alkynyl;
halo C1-7 alkyl;
carboxy C1-7 alkyl;
acetoxy C1-7 alkyl;
carboxyaryl;
C1-7 alkoxy;
C3-10 cycloalkoxy;
aryloxy;
arylalkyloxy;
oxyheterocyclic;
heterocyclic-substituted alkyloxy;
thio C1-7 alkyl;
thio C3-10 cycloalkyl;
thioaryl;
thioheterocyclic;
arylalkylthio;
heterocyclic-substituted alkylthio;
amino;
hydroxylamino;
mercapto-amino;
acylamino;
thioacylamino;
alkoxyamino;
thioalkylamino;
acetal;
thioacetal;
carboxylic acid;
carboxylic acid esters, thioesters, halides, anhydrides, amides and thioamides;
thiocarboxylic acid;
thiocarboxylic acid esters, thioesters, halides, anhydrides, amides and thioamides;
hydroxyl;
sulfhydryl;
nitro;
cyano;
carbamoyl;
thiocarbamoyl, ureido;
thio-ureido;
alkylamino;
cycloalkylamino;
alkenylamino;
cycloalkenylamino;
alkynyl-amino;
arylamino;
arylalkylamino;
hydroxyalkylamino;
mercapto-alkylamino;
heterocyclic amino;
heterocyclic-substituted alkylamino;
oximino;
alkyloximino;
hydrazino;
alkylhydrazino;
phenylhydrazino;
cysteinyl acid, esters, thioesters, halides, anhydrides, amides and thioamides thereof;
aryl groups optionally substituted with one or more substituents selected from the group consisting of halogen, C1-7 alkyl, C1-7 alkoxy;
optionally substituted heterocyclic radicals;
aromatic or heterocyclic substituents substituted with an aliphatic spacer between the pteridine ring and the aromatic or heterocyclic substituent, whereby said aliphatic spacer is a branched or straight, saturated or unsaturated aliphatic chain of 1 to 4 carbon atoms;
branched or straight, saturated or unsaturated aliphatic chains of 1 to 7 carbon atoms; and
R3 is an atom or a group defined as R4, or R3 together with R4 forms a homocyclic or heterocyclic radical;
and/or being a pharmaceutically acceptable addition salt thereof and/or a stereoisomer thereof and/or a mono- or a di-N-oxide thereof and/or a solvate and/or a dihydro- or tetrahydropteridine derivative thereof. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27)
- , alcohol-induced hepatitis, and cachexia, comprising administering to said mammal an effective amount of a pteridine derivative having the structural formula (I);
Specification