Unsaturated derivatives of hydroximino acid as inhibitors nadnad+- adp-ribosyltransferase

 

The invention relates to new unsaturated derivatives of hydroximino acid formulawhere R1means phenyl, optionally substituted by 1-3 substituents selected from the group comprising From1-2alkoxygroup, halogen, or represents a 6-membered unsaturated heterocyclic group containing one nitrogen atom as a heteroatom, and R2means hydrogen or R1together with R2form5-7-cycloalkyl group, Y represents hydrogen, a hydroxy-group,3-22-alkanoyloxy, X means halogen, a hydroxy-group or amino group, R3represents a group of formula-NR4R5where R4and R5mean independently from each other hydrogen, C1-5is an alkyl group, or R4and R5form with the adjacent nitrogen atom a 5 - or 6-membered saturated heterocyclic group which may contain an oxygen atom and may be condensed with a benzene ring, in addition, its geometrical and/or optical isomers and/or pharmaceutically acceptable acid salt additive. Compounds have inhibitory effects on NAD+-ADP-ribosyltransferase that lways;">

Description text in facsimile form (see graphic part)and

Claims

1. Unsaturated derivative of hydroximino acid of the formula (I)

where R1represents phenyl, optionally substituted by 1-3 substituents selected from the group comprising From1-2alkoxygroup, halogen, or represents a 6-membered unsaturated heterocyclic group containing one nitrogen atom as heteroatom;

R2means hydrogen

or R1together with R2forms With5-7-cycloalkyl group;

Y represents hydrogen, a hydroxy-group, With3-22-alkanoyloxy;

X means a halogen, a hydroxy-group or amino group;

R3represents a group of formula-NR4R5where R4and R5denote, independently of one another, hydrogen, C1-5is an alkyl group, or R4and R5form with the adjacent nitrogen atom a 5 - or 6-membered saturated heterocyclic group which may contain an oxygen atom and may be condensed with a benzene ring,

in addition, its geometrical and/or optical isomers and/or pharmaceutically when dstanley panelgroup, optionally substituted by 1-3 methoxypropane, or pyridium; R2means hydrogen; X is an amino group; Y represents hydrogen or a hydroxy-group; R3means pyrrolidino-, piperidino or morpholinopropan, in addition, its geometrical and/or optical isomers and/or pharmaceutically acceptable acid additive salt.

3. Pharmaceutical composition having inhibitory effect on NAD+-ADP-ribosyltransferase containing unsaturated derivative of hydroximino acid of the formula I

where R1represents phenyl, optionally substituted by 1-3 substituents selected from the group comprising From1-2alkoxygroup, halogen, or represents a 6-membered unsaturated heterocyclic group containing one nitrogen atom as heteroatom;

R2means hydrogen

or R1together with R2forms With5-7-cycloalkyl group;

Y represents hydrogen, a hydroxy-group, With3-22-alkanoyloxy;

X means a halogen, a hydroxy-group or amino group;

R3represents a group of formula-NR4R5where R4and R5signify, independently from each other, Simandou heterocyclic group, which may also contain an oxygen atom and may be condensed with benzene ring, or its geometric and/or optical isomers or pharmaceutically acceptable acid additive salt as an active ingredient and one or more traditional media.

4. The pharmaceutical composition according to p. 3 for the treatment of arrhythmia containing unsaturated derivative of hydroximino acid of the formula I, where R1represents phenyl, optionally substituted by 1-3 substituents selected from the group comprising From1-2alkoxygroup, halogen, or represents a 6-membered unsaturated heterocyclic group containing one nitrogen atom as heteroatom; R2means hydrogen or R1together with R2form a C5-7-cycloalkyl group; Y represents hydrogen, a hydroxy-group, With3-22-alkanoyloxy; X means a halogen, a hydroxy-group or amino group; R3represents a group of formula-NR4R5where R4and R5denote, independently of one another, hydrogen, C1-5is an alkyl group, or R4and R5form with the adjacent nitrogen atom a 5-or 6-membered saturated heterocyclic group, which may contain the Kie isomers or pharmaceutically acceptable acid additive salt as an active ingredient and one or more traditional media.

5. The pharmaceutical composition under item 3 or 4, containing the derived hydroximino acid of the formula I, where R1is panelgroup, optionally substituted by 1-3 methoxypropene, or pyridium; R2denotes a hydrogen atom; X is an amino group; Y is a hydrogen atom or a hydroxy-group; R3means pyrrolidino, piperidino or morpholinopropan, or its geometric isomers and/or optical isomer or pharmaceutically acceptable acid additive salt as an active ingredient.

 

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The invention relates to compounds of formula I:

< / BR>
where X represents CH2, CO, CS or SO2,

Y is selected from:

direct connection (i.e

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< / BR>
and their pharmaceutically acceptable salts,

where R1represents one or more substituents selected from H, halogen, hydroxy, alkyl with 1 to 3 carbon atoms (optionally substituted by hydroxyl), alkoxyl with 1 to 3 carbon atoms, alkylthio with 1 to 3 carbon atoms, alkylsulfonyl with 1 to 3 carbon atoms, alkylsulfonyl with 1 to 3 carbon atoms, nitro, cyano, Polygalaceae with 1 to 3 carbon atoms, polyalkyloxy with 1 to 3 carbon atoms, phenyl (optionally substituted by one or more substituents selected from halogen, alkyl with 1 to 3 carbon atoms, alkoxy with 1 to 3 carbon atoms), or R1is carbamoyl, optional alkilirovanny one or two alkyl groups, each independently from 1 to 3 carbon atoms;

R2represents an aliphatic group containing 1 to 3 carbon atoms, optionally substituted by hydroxy or alkoxy containing 1 to 3 carbon atoms;

E represents alkylenes chain containing 2 to 5 carbon atoms, optionally substituted by one or more alkyl groups containing 1 to 3 atom is dinasovymi or different and are independently an alkyl of 1 3 carbon atoms, alkoxy with 1 to 3 carbon atoms, halogen, hydroxy, polyaluminum with 1 to 3 carbon atoms, polyalkyloxy with 1 to 3 carbon atoms, cyano, alkylthio with 1 to 3 carbon atoms, alkylsulfonyl with 1 to 3 carbon atoms, alkylsulfonyl with 1 to 3 carbon atoms, phenyl (optionally substituted by one or more substituents selected from halogen, alkyl with 1 to 3 carbon atoms or alkoxy with 1 to 3 carbon atoms), carbamoyl, optional alkilirovanny one or two alkyl groups, each of which is independently from 1 to 3 carbon atoms, or G represents a phenyl ring having condensed with him heterocyclic or aromatic carbocyclic ring,

and O-acylated derivatives

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