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US 8,575,160 B2Granted
Imidazole derivatives as aldosterone synthase inhibitors
AssigneeNovartis AG
InventorsRobert Sun, Lauren G. Monovich, Sylvie Chamoin, John Westbrook
Life of this patent
Estimating the term…
Abstract
The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to 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.
Claims15
A compound of Formula I:
- wherein:
- R1 and R2 are independently OH, C2-7alkenyloxy, C2-7alkoxy, C6-10aryl, aryl-C2-7alkenyl, C2-7alkenyl, C3-8cycloalkyl, C2-7alkynyl, C1-7cycloalkyl-C2-7alkynyl, heteroaryl, heteroaryl-C1-7alkyl, —CH2C(O)OH, —CH2C(O)O—C1-7alkyl, —CH2C(O)NH—C6-10aryl, —CH2C(O)NH-heteroaryl, —CH2C(O)-heterocyclyl, —CH2C(O)NH-heterocyclyl, —CH2C(O)NH—C1-7alkyl, —C(O)O—C1-7alkyl or —C(O)—C1-7alkyl;
- wherein aryl, heterocyclyl and heteroaryl are optionally substituted with one or more R6;
- with the proviso that one of R1 and R2 is other than C1-7alkyl;
- or
- R1 and R2 form together ═O, ═N(OH) or ═N(O—C1-7alkyl);
- and
- R3 and R4 are independently selected from the group consisting of H, hydroxy, aryl-C1-7alkyl or halo;
- wherein aryl is optionally substituted with one or more R8;
- and
- R5 is H, halo, hydroxy or C2-7alkenyl;
- and
- R6 and R8 for each occurrence, is independently C1-7alkyl, C3-7cycloalkyl, CN, OH, NH2, C1-7alkylamino, di-(C1-7alkyl)amino, C6-10aryl, heteroaryl, C1-7alkoxy, halo, heterocyclyl, benzyloxy, halo-C1-7alkoxy, —OS(O)2—C1-7alkyl or —OS(O)2-halo C1-7alkyl;
- wherein C8-10aryl, heterocyclyl and heteroaryl are optionally substituted with one or more R9;
- for each occurrence, R7 is independently hydrogen, C2-7alkenyl, C3-8cycloalkyl, halo, nitro, cyano, NH2, haloC1-7alkyl, C1-7alkoxy, C3-8cycloalkoxy, C8-10aryloxy, C8-10aryl, heteroaryl, heteroaryl-C1-7alkyl, heterocyclyl, heterocyclyl-C1-7alkyl, C(O)OR10 or N(R11R12), wherein said alkyl, alkenyl, alkoxy, aryl, heterocyclyl and heteroaryl each are optionally substituted with one or more substituent independently selected from C1-7hydroxy, halo, halo C1-7alkyl, C1-7alkoxy, nitro, cyano, C1-7alkylamino and C1-7alkoxy-C1-7alkyl;
- R9 for each occurrence, is independently C1-7alkyl, C1-7alkoxy, halo, haloC1-7alkyl, NH2, C1-7alkylamino, di-(C1-7alkyl)amino, haloC1-7alkoxy, CN, OH, C(O)O—C1-7alkyl, C(O)O-haloC1-7alkyl, carbamoyl, C1-7-alkylaminocarbonyl or di-C1-7alkylaminocarbonyl;
- R10, R11 and R12 for each occurrence are independently H, C3-8cycloalkyl, halo-C1-7alkyl, C6-10aryl, C6-10aryl-C1-7alkyl, heteroaryl, heteroaryl-C1-7alkyl, heterocyclyl, heterocyclyl-C1-7alkyl;
- or R11 and R13 taken together with the nitrogen to which they are attached form a 3 to 8-membered heterocyclyl ring or a 5-membered heteroaryl ring;
- n is 0 or 1;
- p is 0, 1, 2, 3, 4 and 5;
- or a pharmaceutically acceptable salt thereof.
18 more elements
Dependencies are inferred from the claim text.