N-7-heterocyclyl pyrrolo[2,3-D]pyrimidines and the use thereof

Details N-7-heterocyclyl pyrrolo[2,3-D]pyrimidines and the use thereof N-7-heterocyclyl pyrrolo[2,3-D]pyrimidines and the use thereof

1998-09-10

2000-04-18

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

544280, A61K 31519, C07D48704

Patent

active

060515775

DESCRIPTION:

BRIEF SUMMARY
The invention relates to compounds of formula I ##STR2## wherein R.sub.1 is aryl; hydrogen, lower alkyl or halogen; lower alkoxy, lower alkoxy-lower alkenyl, unsubstituted or substituted lower alkoxycarbonyl, N-lower alkylaminocarbonyl or N,N-di-lower alkylaminocarbonyl; alkylcarbonyl or lower alkoxycarbonyl; acceptable salts; to processes for the preparation of those compounds, to pharmaceutical compositions comprising those compounds, to the use of those compounds in the therapeutic treatment of the human or animal body or in the preparation of pharmaceutical compositions.
Within the context of the present Application, the general terms used hereinbefore and hereinafter preferably have the following definitions:
The term "lower" denotes a radical having up to and including 7, and especially up to and including 6, carbon atoms.
Lower alkyl is, for example, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, neopentyl, n-hexyl or n-heptyl, preferably ethyl or methyl.
Lower alkylene is, for example, methylene, ethylene or propylene, preferably methylene or ethylene.
Alkyl and alkylene are straight-chained or branched. On their own, for example as lower alkyl, or as a constituent of other groups, for example lower alkoxy, lower alkylcarbonyl, lower alkoxycarbonyl, lower alkylaminocarbonyl, di-lower alkylaminocarbonyl, lower alkoxy-lower alkenyl, they may be unsubstituted or substituted, for example by halogen, hydroxy, lower alkoxy, trifluoromethyl or morpholin-4-yl; preferably they are unsubstituted or substituted by hydroxy or amino, N-lower alkylamino or N,N-di-lower alkylamino.
Halogen is, for example, chlorine, bromine or fluorine, but may also be iodine.
Lower alkoxy is, for example, n-propoxy, isopropoxy, n-butoxy, isobutoxy, sec-butoxy, tert-butoxy, n-amyloxy or isoamyloxy, preferably methoxy or ethoxy.
Lower alkoxycarbonyl denotes the radical lower alkyl--O--C(O)-- and is, for example, n-propoxycarbonyl, isopropoxycarbonyl, n-butoxycarbonyl, isobutoxycarbonyl, sec butoxycarbonyl, tert-butoxycarbonyl, n-amyloxycarbonyl or isoamyloxycarbonyl, preferably methoxycarbonyl or ethoxycarbonyl.
Lower alkylamino is, for example, n-propylamino, n-butylamino, isopropylamino or isobutyl-amino, preferably methylamino or ethylamino.
Di-lower alkylamino is, for example, dimethylamino, diethylamino, di-n-propylamino, n-butyl-amino, di-n-butylamino or n-propyl-n-butylamino, preferably dimethylamino, diethylamino or methylethylamino.
N-Lower alkylaminocarbonyl is, for example, N-methylcarbamoyl, N-ethylcarbamoyl, N-n-propylcarbamoyl or N-isopropylcarbamoyl, preferably N-methylcarbamoyl or N-ethyl-carbamoyl.
N,N-Di-lower alklaminocarbonyl is, for example, N,N-dimethylcarbamoyl, N,N-diethyl-carbamoyl, N-methyl-N-ethylcarbamoyl, N,N-di-n-propylcarbamoyl or N-methyl-N-isopropyl-carbamoyl, preferably N,N-dimethylcarbamoyl, N,N-diethylcarbamoyl or N-methyl-N-ethylcarbamoyl.
Aryl is, for example, phenyl or naphthyl, each of which is unsubstituted or substituted, for example as indicated hereinafter for phenyl. Aryl is preferably phenyl unsubstituted or substituted by one or more, for example from one to three, especially one or two, substituents from the group consisting of lower alkyl, halo-lower alkyl, (hydroxy or lower alkanoyloxy)-lower alkyl, lower alkoxy-lower alkyl, (hydroxy, lower alkoxy or lower alkanoyl-oxy)-lower alkoxy-lower alkyl, (amino, lower alkylamino, di-lower alkylamino or lower alkanoylamino)-lower alkoxy-lower alkyl, (amino or lower alkanoylamino)-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl; azacycloalkyl-lower alkyl, for example (piperidinyl, piperazinyl, morpholinyl or pyrrolidinyl)-lower alkyl; azaheteroaryl-lower alkyl, for example (imidazolyl, triazolyl, pyridyl, pyrimidinyl or pyrrolyl)-lower alkyl, (hydroxy, lower alkoxy or lower alkanoyloxy)-lower alkylamino-lower alkyl, (amino, lower alkylamino, di-lower alkylamino or lower alkanoylamino)-lower alkylamino-lower alkyl; azacycloalkyl-lower alkylamino-lower alkyl, for example (piperidinyl, piperaz

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