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US 7,612,099 B2Granted
Vinylogous acid derivatives
AssigneeHoffmann-La Roche Inc.
InventorsDavid Banner, Hans Hilpert, Bernd Kuhn, Harald Mauser
Life of this patent
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Abstract
The invention is concerned with vinylogous acids derivatives of formula (I) wherein A and R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.
Claims23
A Compound of formula (I)
- wherein
- A is selected from the group consisting of —CH2—, —O— and —NR′—, wherein R′ is selected from the group consisting of hydrogen and C1-6 alkyl, or wherein R′ and R4 form C2-5 alkylene;
- R1 is selected from the group consisting of hydrogen, halogen, nitro, cyano, amino, C1-6 alkyl, heteroalkyl, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, hydroxy, C1-6 alkoxy, —NR′R″, —(C0-6 alkylene)-NR′R″, wherein R′ and R″ are independently selected from the group consisting of hydrogen, C1-6 alkyl, heteroalkyl, formyl, C1-6 alkylcarbonyl, optionally substituted C3-7 cycloalkylcarbonyl, optionally substituted arylcarbonyl, optionally substituted heteroarylcarbonyl, optionally substituted heterocyclylcarbonyl, C1-6 alkylsulfonyl, optionally substituted C3-7 cycloalkylsulfonyl, optionally substituted arylsulfonyl, optionally substituted heteroarylsulfonyl and optionally substituted heterocyclylsulfonyl, and —(C0-6 alkylene)-OR′, wherein R′ is selected from the group consisting of hydrogen, C1-6 alkyl, heteroalkyl, formyl and C1-6 alkylcarbonyl;
- R2, R2′ and R2″ are independently selected from the group consisting of hydrogen, halogen, cyano, nitro, amino, mono- or di-C1-6 alkyl substituted amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, hydroxy and C1-6 alkoxy;
- R3 is selected from the group consisting of hydrogen, halogen, cyano, nitro, amino, mono- or di-C1-6 alkyl substituted amino, C1-6 alky, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, hydroxy, C1-6 alkoxy, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C3-7 cycloalkyl-C1-6 alkyl, optionally substituted aryl-C1-6 alkyl, optionally substituted heteroaryl-C1-6 alkyl and optionally substituted heterocyclyl-C1-6 alkyl;
- R4 is selected from the group consisting of hydrogen, halogen, cyano, nitro, amino, mono- or di-C1-6 alkyl substituted amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, hydroxy, C1-6 alkoxy, optionally substituted C3-7 cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted C3-7 cycloalkyl-C1-6 alkyl, optionally substituted aryl-C1-6 alkyl, optionally substituted heteroaryl-C1-6 alkyl and optionally substituted heterocyclyl-C1-6 alkyl;
- R5 is selected from the group consisting of hydrogen and C1-6 alkyl;
- or
- R4 and R5, together with the carbon atom to which they are attached, form an optionally substituted C3-7 cycloalkyl ring or an optionally substituted heterocyclyl ring;
- R6 is selected from the group consisting of hydrogen and C1-6 alkyl;
- or a pharmaceutically acceptable salt thereof.
8 more elements
Dependencies are inferred from the claim text.