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US 2012/0071512 A1Published application
5-pyridin-3-yl-1, 3-dihydro-indol-2-on derivatives and their use as modulators of aldosterone synthase and/or cyp11b1
AssigneeNovartis AG
InventorsQi-Ying Hu, Sylvie Chamoin, Christopher M. Adams, Chun Zhang
Life of this patent
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Abstract
The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Claims14
A compound of Formula I:
- a pharmaceutically acceptable salt thereof, wherein:
- X is CH2, O, S or —NR1;
- each R1 are independently C1-7alkyl or C3-8cycloalkyl;
- each of R2 and R6 are independently hydrogen, halogen, cyano, C1-7alkyl, hydroxy-C1-7alkyl, —OR7, C3-8cycloalkyl, halo-C1-7alkyl or —CH2—NR8—SO2—R10;
- R3 and R4 are independently hydrogen, halogen or cyano;
- R5 is hydrogen, C1-7alkyl, halogen, cyano, hydroxy, hydroxy-C1-7alkyl, hydroxy-C3-8cycloalkylalkyl, C1-7alkoxy-C3-8alkyl, —OR7, C6-10aryl, heteroaryl, heterocyclyl, C3-8cycloalkyl, halo-C1-7alkyl, —NR8R9, —CH2—NR8—C(O)NR8R9, —CH2—NR8—SO2—R70, —C(O)—R10, —SO2R10, —C(O)—NR8R9, —SO2—NR8R9, —NR8C(O)—R10, —CH2CN, or —NR8—SO2—R10;
- R7 is C1-7alkyl, C3-8cycloalkyl-C1-7alkyl, heterocyclyl-C1-7alkyl, C6-90aryl-C1-7alkyl, heteroaryl-C1-7alkyl or —C(O)—R10;
- in which C6-10aryl, heteroaryl, C1-7alkyl, heterocyclyl and C3-8cycloalkyl are optionally substituted with C1-7alkoxy, halo, halo-C3-8alkoxy, C1-7alkyl, OH or halo-C1-7alkyl;
- each of R8, R9 are independently hydrogen, C1-7alkyl, halo-C1-7alkyl, C6-10aryl-C1-7alkyl or heterocyclyl;
- or R8 and R9 can form together with the nitrogen atom to which they are attached a 5- or 6-membered ring heterocyclyl, wherein said heterocyclyl optionally contain an additional heteroatom selected from N, O or S and is optionally substituted with C1-7alkyl;
- and
- R10 is hydrogen, C1-7alkyl, halo-C1-7alkyl, C6-10aryl-C1-7alkyl, —NR8R9, or heterocyclyl;
- wherein each heteroaryl is a mono- or bicyclic aromatic moiety comprising 5-10 ring atoms selected from carbon atoms and 1 to 5 heteroatoms, and
- each heterocyclyl is a mono- or bicyclic saturated or partially saturated but non-aromatic moiety comprising 4-10 ring atoms selected from carbon atoms and 1 to 5 heteroatoms;
- and each heteroatoms being O, N or S;
- and with the proviso that when R5 is halogen or hydrogen than R2 is other than H;
- or a pharmaceutically acceptable salt thereof.
14 more elements
14-17. (canceled)
Dependencies are inferred from the claim text.