Inhibitors of meprin α and β
AssigneeVivoryon Therapeutics N.V.
InventorsMichael Wermann, Mirko Buchholz, Hans-Ulrich Demuth, Daniel Ramsbeck, Dagmar Schlenzig, Stephan Schilling
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Abstract
The present invention relates to novel hydroxamic acid derivatives as inhibitors of meprin β and/or α, pharmaceutical compositions comprising such compounds, methods for treatment or prophylaxis of diseases or conditions, especially such that are related to meprin β and/or α, and compounds and pharmaceutical compositions for use in such methods.
Claims19
A compound, its individual enantiomers, its individual diastereoisomers, its hydrates, its solvates, its crystal forms, its individual tautomers or a pharmaceutically acceptable salt thereof, which is represented by the following Formula V:
- wherein:
- R1 is joined together with R3 to form a heterocyclic ring;
- R2 is 3-carboxyphenyl;
- and
- R4 is H.
A compound represented by the following Formula I, its individual enantiomers, its individual diastereoisomers, its hydrates, its solvates, its crystal forms, its individual tautomers or a pharmaceutically acceptable salt thereof,
- wherein:
- n=1;
- R1 is selected from the group consisting of H and alkyl;
- R2 is selected the group consisting of 1,3-benzodioxol-5-yl, 3-carboxyphenyl, 4-carboxyphenyl, 3-carboxy-4-methoxyphenyl, 3,5-dichloro-4-hydroxyphenyl, 4-chlorophenyl, 4-cyanophenyl, 4-fluorophenyl, 2,6-difluoro-4-methoxyphenyl, 3-fluoro-4-methoxyphenyl, 3-methoxyphenyl, 4-methoxyphenyl, and 4-methylphenyl;
- Each R3 is H;
- Each R4 is H;
- and
- X is —CH2—.
A compound represented by the following Formula I, its individual enantiomers, its individual diastereoisomers, its hydrates, its solvates, its crystal forms, its individual tautomers or a pharmaceutically acceptable salt thereof,
- wherein:
- n=1;
- R1 is selected from the group consisting of H and alkyl;
- wherein said alkyl may be joined together with R3 to form a ring;
- R2 is 3-carboxyphenyl;
- R3 is independently selected from the group consisting of H, methyl, ethyl, 1-propyl, 2 propyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, and 2-carboxyethyl;
- and each of said arylalkyl, heteroaryl, and heteroarylalkyl can be optionally substituted;
- R4 is H;
- and
- X is —CH2—.
A compound, its individual enantiomers, its individual diastereoisomers, its hydrates, its solvates, its crystal forms, its individual tautomers or a pharmaceutically acceptable salt thereof, selected from the group consisting of:
A pharmaceutical composition comprising:
- a compound represented by the following Formula I, its individual diastereoisomers, its hydrates, its solvates, its crystal forms, its individual tautomers or a pharmaceutically acceptable salt thereof;
- and a pharmaceutically acceptable excipient;
- wherein:
- n=1;
- R1 is selected from the group consisting of H and alkyl;
- wherein said alkyl may be joined together with R3 to form a ring;
- R2 is 3-carboxyphenyl;
- R3 is independently selected from the group consisting of H, C1-4alkyl, aryl, arylalkyl, heteroaryl, and heteroarylalkyl;
- each of which can be optionally substituted;
- wherein said alkyl may be joined together with R1 to form a ring;
- R4 is H;
- and
- X is —CH2—.
Dependencies are inferred from the claim text.