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US 8,575,158 B2Granted
1-phenyl-substituted heterocyclyl derivatives and their use as prostaglandin D2 receptor modulators
AssigneeActelion Pharmaceuticals Ltd.
InventorsHamed Aissaoui, Christoph Boss, Heinz Fretz, Julien Pothier, Sylvia Richard-Bildstein, Philippe Risch, Romain Siegrist
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Abstract
The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), wherein X, Y, Z, n, R1, R2, R3, R4, R5, R6, R7 and R10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.
Claims16
A compound of formula (I):
- wherein
- X represents —NH—, —O— or a bond;
- Y represents (C1-C4)alkandiyl;
- Z represents O or S;
- n represents 0 or 1;
- R1 represents
- (C4-C6)alkyl;
- (C1-C4)alkyl which is mono-substituted with (C3-C6)cycloalkyl, (C1-C4)alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted aryloxy, optionally substituted heteroaryloxy, optionally substituted aryl-(C1-C2)alkoxy, optionally substituted heteroaryl-(C1-C2)alkoxy, optionally substituted heteroarylsulfanyl or —NR8R9;
- (C2-C4)alkenyl which is mono-substituted with optionally substituted aryl;
- (C2-C4)alkynyl which is mono-substituted with optionally substituted aryl;
- (C3-C6)cycloalkyl which is mono- or di-substituted with (C1-C4)alkyl, mono-substituted with (C1-C4)alkoxy, mono-substituted with optionally substituted aryl or mono-substituted with optionally substituted heteroaryl;
- optionally substituted aryl;
- or
- a 10-membered partially unsaturated ring system;
- R2 represents hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)fluoroalkyl, halogen, (C1-C4)alkylsulfonyl, phenylsulfonyl or (C1-C4)alkylsulfonylamino;
- R3 represents hydrogen, (C1-C4)alkoxy or halogen;
- R4 represents hydrogen, (C1-C4)alkoxy, halogen, (C1-C4)alkylsulfonyl, optionally substituted aryl or optionally substituted heteroaryl;
- R5 represents hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)fluoroalkyl, halogen, cyano, —CONH2, optionally substituted aryl, optionally substituted heteroaryl, (C1-C4)alkylsulfonyl, phenylsulfonyl or dimethylamino-sulfonyl;
- and R6 represents hydrogen or halogen;
- or
- R5 and R6 together form a methylendioxy-group;
- R7 represents hydrogen or methyl;
- R8 represents hydrogen or methyl;
- R9 represents optionally substituted aryl, optionally substituted arylsulfonyl or optionally substituted heteroarylsulfonyl;
- and
- R10 represents —C(O)OH, —C(O)NH—CN, —C(O)NH—OH, —C(O)NH—S(O)2CF3 or optionally substituted heteroaryl;
- with the proviso that R1 is different from optionally substituted aryl if X represents —NH— or a bond;
- or a salt thereof.
25 more elements
Dependencies are inferred from the claim text.