US 2010/0144752 A1Published application

Heterocyclylamide-substituted thiazoles, pyrroles and thiophenes

AssigneeAiCuris GmbH & Co. KG

InventorsHolger Zimmermann, David Brückner, Kerstin Henninger, Martin Hendrix, Martin Radtke

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Abstract

The invention relates to heterocyclylamide-substituted thiazoles, pyrroles and thiophenes and to processes for preparing them, to their use for the treatment and/or prophylaxis of diseases, and to their use for the production of medicaments for the treatment and/or prophylaxis of diseases, particularly for use as antiviral agents, especially against cytomegaloviruses.

Claims11

Dependent claims

A compound of the formula

in which
R1 represents a group of the formula
where
* represents the point of attachment to the carbonyl group,
R3 represents phenyl or 5- or 6-membered heteroaryl,
where phenyl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
R4 represents phenyl or 5- or 6-membered heteroaryl,
where phenyl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
and
R5 and R6 independently of one another represent hydrogen, methyl or ethyl,
R2 represents phenyl,
where phenyl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl and C1-C6-alkoxy,
A represents a group of the formula
where
* represents the point of attachment to the carbonyl group,
# represents the point of attachment to the nitrogen atom of the urea,
R7 represents C1-C6-alkyl,
where alkyl may be substituted by one substituent, where the substituent is selected from the group consisting of C3-C6-cycloalkyl, C6-C10-aryl and 5- or 6-membered heteroaryl,
where cycloalkyl, aryl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
and
R8 and R9 represent, independently of one another, hydrogen, halogen or C1-C6-alkyl,
where alkyl may be substituted by one substituent, where the substituent is selected from the group consisting of C3-C6-cycloalkyl, C6-C10-aryl and 5- or 6-membered heteroaryl,
in which cycloalkyl, aryl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
or a salt, solvate, or solvate of a salt thereof.

21 more elements

Dependencies are inferred from the claim text.

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Abstract

A compound of the formula

in which
R1 represents a group of the formula
where
* represents the point of attachment to the carbonyl group,
R3 represents phenyl or 5- or 6-membered heteroaryl,
where phenyl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
R4 represents phenyl or 5- or 6-membered heteroaryl,
where phenyl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
and
R5 and R6 independently of one another represent hydrogen, methyl or ethyl,
R2 represents phenyl,
where phenyl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl and C1-C6-alkoxy,
A represents a group of the formula
where
* represents the point of attachment to the carbonyl group,
# represents the point of attachment to the nitrogen atom of the urea,
R7 represents C1-C6-alkyl,
where alkyl may be substituted by one substituent, where the substituent is selected from the group consisting of C3-C6-cycloalkyl, C6-C10-aryl and 5- or 6-membered heteroaryl,
where cycloalkyl, aryl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
and
R8 and R9 represent, independently of one another, hydrogen, halogen or C1-C6-alkyl,
where alkyl may be substituted by one substituent, where the substituent is selected from the group consisting of C3-C6-cycloalkyl, C6-C10-aryl and 5- or 6-membered heteroaryl,
in which cycloalkyl, aryl and heteroaryl may be substituted by 1 to 3 substituents, where the substituents independently of one another are selected from the group consisting of halogen, hydroxyl, oxo, nitro, cyano, trifluoromethyl, difluoromethyl, trifluoromethoxy, difluoromethoxy, monofluoromethoxy, trifluoromethylthio, C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, amino, C1-C6-alkylamino, aminocarbonyl and C1-C6-alkylaminocarbonyl,
or a salt, solvate, or solvate of a salt thereof.

21 more elements