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US 2007/0167457 A1Published application
N-aroyl piperazine derivatives as orexin receptor antagonists
AssigneeSmithKline Beecham Corporation
InventorsClive BRANCH, Christopher Johnson, David Nash, Geoffrey Stemp
Life of this patent
Estimating the term…
Abstract
This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.
Claims15
A compound of formula (I):
- wherein:
- Y represents NR2;
- m represents 1, 2, or 3;
- p represents 0 or 1;
- X is O, S, C═O, SO2, or —CH═CH—;
- Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S;
- any of which may be optionally substituted;
- Ar2 represents phenyl or a 5- or 6-membered heterocyclyl group containing 1 to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents;
- or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing 1 to 4 heteroatoms selected from N, O and S;
- R1 represents optionally substituted (C1-4)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S;
- R2 represents hydrogen, optionally substituted (C1-4)alkyl, optionally substituted (C1-6)alkanoyl, optionally substituted (C1-6)alkanoxycarbonyl or optionally substituted (C1-6)alkylaryloxycarbonyl;
- wherein the optional substituents for the groups Ar1, Ar2 and R1 are selected from the group consisting of halogen, hydroxy, oxo, cyano, nitro, (C1-4)alkyl, (C1-4)alkoxy, halo(C1-4)alkyl, halo(C1-4)alkoxy, aryl(C1-4)alkoxy, (C1-4)alkylthio, hydroxy(C1-4)alkyl, (C1-4)alkoxy(C1-4)alkyl, (C3-6)cycloalkyl(C1-4)alkoxy, (C1-4)alkanoyl, (C1-4)alkoxycarbonyl, (C1-4)alkylsulfonyl, (C1-4)alkylsulfonyloxy, (C1-4)alkylsulfonyl(C1-4)alkyl, arylsulfonyl, arylsulfonyloxy, arylsulfonyl(C1-4)alkyl, (C1-4)alkylsulfonamido, (C1-4)alkylamido, (C1-4)alkylsulfonamido(C1-4)alkyl, (C1-4)alkylamido(C1-4)alkyl, arylsulfonamido, arylcarboxamido, arylsulfonamido(C1-4)alkyl, arylcarboxamido(C1-4)alkyl, aroyl, aroyl(C1-4)alkyl, aryl(C1-4)alkanoyl, (C1-4)acyl, aryl, aryl(C1-4)alkyl, (C1-4)alkylamino(C1-4)alkyl, and
- R3 R4N—, R3OCO(CH2)r, R3CON(R4)(CH2)r, R3R4NCO(CH2)r, R3R4NSO2(CH2)r and R3SO2NR4(CH2)r wherein each of R3 and R4 independently represents a hydrogen atom or a (C1-4)alkyl group or where appropriate R3R4 forms part of a (C3-6)azacyloalkane or (C3-6)(2-oxo)azacycloalkane ring and r represents zero or an integer from 1 to 4, and
- R3R4N(CH2)n— and R3R4N(CH2)nO—, wherein n represents an integer from 1 to 4, wherein R3 with at least one CH2 of the (CH2)n portion of the group form a (C3-6)azacycloalkane and R4 represents hydrogen, a (C1-4)alkyl group or with the nitrogen to which it is attached forms a second (C3-6)azacycloalkane fused to the first (C3-6)azacycloalkane;
- or a pharmaceutically acceptable salt thereof.
12 more elements
Dependencies are inferred from the claim text.