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US 2014/0371220 A1Published application
Substituted piperidinyl-pyridazinyl derivatives useful as scd 1 inhibitors
AssigneeJanssen Pharmaceutica NV
InventorsShyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
Life of this patent
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Abstract
The present invention is directed to novel piperidinyl-pyridazinyl derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.
Claims18
A compound of formula (I)
- wherein
- R1 is selected from the group consisting of
- a is an integer from 0 to 3;
- each R2 is independently selected from the group consisting of halogen, C1-4alkyl, C1-4alkoxy, halogenated C1-2alkyl, and halogenated C1-2alkoxy;
- R3 is selected from the group consisting of
- wherein R4 is selected from the group consisting of hydrogen, halogen, C1-4alkyl, halogenated C1-2alkyl, —C1-2alkyl-OH, C1-4alkoxy, halogenated C1-2alkoxy, —C1-2alkyl-O—C1-2alkyl, —CO2H, —C(O)O—C1-4alkyl, —C1-2alkyl-C(O)O—C1-2alkyl, —C1-2alkyl-OC(O)—C1-2alkyl, —NRARB, —C1-2alkyl-NRARB, —C(O)—NRARB, —C1-2alkyl-C(O)—NRARB and —NRA—C(O)—(C1-2alkyl);
- wherein R5 is selected from the group consisting of hydrogen, C1-4alkyl, —C2-4alkyl-OH, —C2-3alkyl-O—C1-2alkyl, —C1-2alkyl-C(O)O—C1-2alkyl, —C2-3alkyl-OC(O)—C1-2alkyl, —C2-4alkyl-NRARB and —C1-2alkyl-C(O)NRARB;
- and
- wherein b is an integer from 0 to 2;
- wherein each R6 is independently selected from the group consisting of halogen, C1-4alkyl, halogenated C1-4alkyl, —C1-2alkyl-OH, C1-4alkoxy, halogenated C1-4alkoxy, —C1-2alkyl-O—C1-2alkyl, —CO2H, —C(O)O—C1-4alkyl, —C1-2alkyl-C(O)O—C1-2alkyl, —C1-2alkyl-OC(O)—C1-2alkyl, —C(O)—NRARB, —C1-2alkyl-C(O)—NRARB, —NRARB, —C1-2alkyl-NRARB and —NRA—C(O)—C1-2alkyl;
- and wherein RA and RB are each independently selected from the group consisting of hydrogen and C1-2alkyl;
- alternatively RA and RB are taken together with the nitrogen atom to which they are bound to form piperidin-1-yl, piperazin-1-yl, morpholin-4-yl and pyrrolidin-1-yl;
- provided that when R3 is 3-methyl-1,2,4-thiadiazol-5-yl, then R1 is other than unsubstituted indoly-3-yl;
- or a pharmaceutically acceptable salt thereof.
11 more elements
-24. (canceled)
Dependencies are inferred from the claim text.