摘要 |
<p>The invention relates to a DGAT inhibitor of formula (I): including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents—C(═O)—;—O—C(═O)—; C(═O)—C(═O)—;—NRx—C(═O)—;—Z1—C(O)—;—Z1—NRx—C(═O)—;—C(═O)—Z1—;—NRx—C(═O)—Z1—;—S(═O)p-;—C(═S)—;—NRx—C(═S)—;—Z1—C(═S)—;—Z1—NRx—C(═S)—;—C(═S)—Z1-; NRx—C(═S)—Z—; Y represents NRx—C(=0)-Z2—;—NRx—C(=0)-Z2—NRy—;—NRx—C(=0)-Z 2—NRy—C(=0)—;—NRx—C(=0)-Z2—NRy—C(=0)-; O—;—NRx—C(=0)-Z2-0-;—NRx—C(=0)-Z2-0-C(=0)-;—NRx—C(=0)-Z2—C(=0)-;—NRx—C(=0)-Z2—C(=0)-;—NRx—C(=0)-0-Z2—C(=0)-;—NRx—C(=0)-0-Z2—C(=0)-0-;—NRx—C(═O)—O—Z2—O—C(═O)—;—NRx—C(═O)—Z2—C(═O)—NRy—;—NRx—C(═O)—Z2—NRy—C(=0)-NRy—;—C(═O)—Z2—;—C(═O)—Z2—O—;—C(=0)-NRx—Z2—;—C(=0)-NRx—Z2-0-;—C(=0)-NRx—Z2—C(=0)-0-;—C(=0)-NRx—Z2-0-C(=0)-;—C(=0)-NRx—Z2—NRy—;—C(=0)—NRx—Z2—NRy—C(=0)-;—C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkyloxy, C3-6Cycloalkyl or aryl; C2-6alkenyl; C2-6alkynyl; C3-6cycloalkyl; adamantanyl; aryl1; aryl1C1-6alkyl; Het1; or Het1C1-6alkyl; provided that when Y represents—NRx—C(═O)—Z2—;—NRx—C(=0)-Z2—NRy;—NRx—C(═O)—Z2—C(═O)—NRy—;—C(═O)—Z2—;—NRx—C(=0)-Z2—NRy—C(=0)—NRy—;—C(═O)—NR—Z2—;—C(═O)—NR—O—Z2—; or—C(=0)-NRx—Z2—NRy—; then R1 may also represent hydrogen; R2 represents hydrogen, C1-12alkyl, C2-6alkenyl or R3; provided that if X represents—O—C(═O)—; the R2 O represents R3; and provided that (A) is excluded; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use as a medicine of said compounds.</p> |
申请人 |
JANSSEN PHARMACEUTICA, N.V. |
发明人 |
BONGARTZ, JEAN-PIERRE, ANDRE, MARC;LINDERS, JOANNES, THEODORUS, MARIA;MEERPOEL, LIEVEN;VAN LOMMEN, GUY, ROSALIA, EUGEEN;COESEMANS, ERWIN;BRAEKEN, MIRIELLE;BUYCK, CHRISTOPHE, FRANCIS, ROBERT, NESTOR;BERWAER, MONIQUE, JENNY, MARIE;DE WAEPENAERT, KATHARINA, ANTONIA, GERMANIA, J.M.;ROEVENS, PETER, WALTER, MARIA;BOECKX, GUSTAAF, MARIA;DAVIDENKO, PETR, VLADIMIRIVICH |