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US 11,767,316 B2Granted
Non-fused thiophene derivatives and their uses
AssigneeEnyo Pharma
InventorsEric Meldrum, Benoît De Chassey, Peter Machin, Karine Fabienne Malagu, Paul Colin Michael Winship, Jean-Laurent Paparin, Mark Chambers, Jamie David Knight, Roberta Lanaro
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Abstract
The present invention relates to a new class of non-fused thiophene derivatives and their uses for treating diseases such as infection, cancer, metabolic diseases, cardiovascular diseases, iron storage disorders and inflammatory disorders.
Claims9
A compound of formula (I):
- wherein:
- R1 represents:
- a fused arylcycloalkyl selected from the group consisting of:
- R2 represents:
- a hydrogen,
- a halogen,
- a (C1-C6)alkyl optionally substituted by at least one halogen,
- an optionally substituted aryl, or
- an optionally substituted cycloalkyl;
- R3 represents:
- a 5-10 membered ring, saturated or unsaturated selected from the group consisting of:
- an aryl optionally fused to a heterocycloalkyl,
- a heteroaryl selected from the group consisting of a pyrimidinyl, a pyrazolyl, and a benzoisoxazolyl,
- and
- a 5-10 membered bridged carbocyclyl or heterocyclyl,
- said 5-10 membered ring is optionally substituted by at least one radical selected from the group consisting of:
- a halogen,
- a (C1-C6)alkyl optionally substituted by at least one halogen, or by an optionally bridged heterocycloalkyl optionally substituted by a (C1-C6)alkyl,
- a —NH—(C1-C6)alkyl or a —N—((C1-C6)alkyl)2, optionally substituted by at least one radical selected from the group consisting of a heterocycloalkyl, a cycloalkyl, a hydroxyl, a thiacycloalkyl-1,1dioxide and a (C1-C6)alkyloxy,
- a —NH-heterocycloalkyl, a —NH-cycloalkyl, a —N((C1-C6)alkyl)-heterocycloalkyl, or a —NH((C1-C6)alkyl)-thiacycloalkyl-1,1dioxide, optionally substituted by a hydroxyl, a (C1-C6)alkyl, a (C1-C6)alkyloxy or a —CO—R6 with R6 being a hydrogen or a (C1-C6)alkyl,
- a hydroxy, a —CN, a —CO—R6 or a —CO2R6 with R6 being a hydrogen or a (C1-C6)alkyl,
- a (C1-C6)alkyloxy optionally substituted by at least one radical selected from the group consisting of a halogen, a hydroxy, a (C1-C6)alkyloxy, a —NR7R8 with R7 and R8 are independently a hydrogen or a (C1-C6)alkyl, a —NHCOR9, a —NHCO2R9, with R9 being a (C1-C6)alkyl, a —CO2R6 with R6 being a hydrogen or a (C1-C6)alkyl, and a heterocycle,
- a —NHCOR9, a —NHCO2R9, or a —SO2R9, with R9 being a (C1-C6)alkyl, and
- a heterocycloalkyl, a bridged heterocycloalkyl, a heterocycloalkyloxy, a cycloalkyloxy, a thiaheterocycloalkyl-1,1-dioxide or a spiroheterocycloalkyl, optionally substituted by a (C1-C6)alkyl, a (C1-C6)alkyloxy, a hydroxy, a ketone, a halogen or a (C1-C6)alkyl optionally substituted by a (C1-C6)alkyloxy;
- R4 represents:
- a —CO2R10 with R10 being a hydrogen;
- and
- R5 represents:
- a hydrogen, or
- a (C1-C6)alkyl optionally substituted by at least one halogen
- and stereoisomers and pharmaceutical salts thereof.
28 more elements
Dependencies are inferred from the claim text.