Adenosine derivatives, preparation methods and pharmaceutical co

Details Adenosine derivatives, preparation methods and pharmaceutical co Adenosine derivatives, preparation methods and pharmaceutical co

1994-06-29

1996-01-02

Nutter, Nathan M.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 2722, C07H 19167

Patent

active

054809835

DESCRIPTION:

BRIEF SUMMARY
The present invention relates, by way of novel products, to the adenosine derivatives of general formula (I) below and, if appropriate, their addition salts, in particular the pharmaceutically acceptable addition salts.
The compounds in question have a very valuable pharmacological profile insofar as they possess on the one hand, and in particular, analgesic properties, and on the other hand antihypertensive properties.
The present invention further relates to the method of preparing said products, to the synthesis intermediates and to the application of these products in therapeutics.
These adenosine derivatives have general formula (I): ##STR2## in which: R.sub.1 is a hydrogen atom, a halogen atom, a lower alkyl radical, a lower O-alkyl radical, a lower S-alkyl radical or a phenyl radical and can be located in the 2-, 4-, 5-, 6- or 7-position of the indole; radical, a C.sub.3 -C.sub.7 -cycloalkyl radical or a lower O-alkyl radical; to four identical or different substituents selected from a halogen atom, a nitro, lower alkyl, lower O-alkyl or lower S-alkyl group and a group --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 being the hydrogen atom or a lower alkyl radical; unsubstituted or substituted by one to four identical or different substituents selected from a halogen atom and a nitro, lower alkyl, lower O-alkyl or lower S-alkyl group; and R.sub.10 simultaneously being a lower alkyl radical or forming, together with the nitrogen atom to which they are attached, a heterocycle selected from morpholine, piperidine and pyrrolidine; atom or a lower alkyl radical; and C.sub.3 -C.sub.7 -cycloalkyl radical, a lower alkyl chain possessing an alcohol or ether functional group, or else a group --(CH.sub.2).sub.n --NR.sub.9 R.sub.10, n, R.sub.9 and R.sub.10 being as defined above.
Advantageously, the derivatives according to the invention are the derivatives of formula (I) given above in which: O-alkyl radical, a lower S-alkyl radical or a phenyl radical and can be located in the 2- or 5-position of the indole; radical, a C.sub.3 -C.sub.7 -cycloalkyl radical or a lower O-alkyl radical; or two identical or different substituents selected from a halogen atom, a nitro, lower alkyl or lower O-alkyl group and a group --NR.sub.7 R.sub.8, R.sub.7 and R.sub.8 being the hydrogen atom or a lower alkyl radical; 3 unsubstituted or substituted by a halogen atom; simultaneously being a lower alkyl radical or forming, together with the nitrogen atom to which they are attached, a heterocycle selected from morpholine, piperidine and pyrrolidine; atom or a lower alkyl radical; and C.sub.3 -C.sub.7 -cycloalkyl radical or a lower alkyl chain possessing an alcohol or ether functional group.
In the description and the claims, lower alkyl radical is understood as meaning a linear or branched hydrocarbon chain having from 1 to 6 carbon atoms. A lower alkyl radical is for example a methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, isopentyl, hexyl or isohexyl radical.
In the description and the claims, lower alkenyl radical is understood as meaning a linear or branched hydrocarbon chain having from 1 to 6 carbon atoms and possessing a double bond, such as, for example, an ethenyl group, and lower alkynyl radical is understood as meaning a linear or branched hydrocarbon chain having from 1 to 6 carbon atoms and possessing a triple bond, such as, for example, an ethynyl group.
C.sub.3 -C.sub.7 -Cycloalkyl radical is understood as meaning a saturated cyclic radical, preferably a cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl or cycloheptyl radical.
Halogen is understood as meaning a chlorine, bromine, iodine or fluorine atom.
Lower alkyl chain possessing an alcohol functional group is understood as meaning a lower alkyl chain in which one of the hydrogen atoms has been substituted by a hydroxyl group. Such a chain is for example the 1-hydroxy-2-methylpropan-2-yl chain.
Lower alkyl chain possessing an ether functional group is understood as meaning a lower alkyl chain in which one of the hydrogen atoms has been substituted by

REFERENCES:
patent: 5229505 (1993-07-01), Bru-Magniez et al.

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