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US 8,138,179 B2Granted
Spiro-imidazo compounds
AssigneeNovartis AG
InventorsPeter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Stjepan Jelakovic, Bibia Bennacer, Stefan Stutz
Life of this patent
Estimating the term…
Abstract
Novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R1′, Q, m and n have the meanings explained in detail in the description, a process for their preparation and the use of these compounds as medicaments, in particular as aldosterone synthase inhibitors.
Claims11
A compound of the formula
- in which
- R is deuterium, halogen or hydrogen;
- a) R1 is in each case hydrogen, and R1′ and R1′ are together a radical of the formula
- or
- b) R1 and R1 are together a radical of the formula
- and R1′ is in each case hydrogen,
- and for both a) and b):
- A1 and A2 are two ortho ring atoms, and A is aryl or heterocyclyl, which radicals are unsubstituted or substituted by 1-4 C1-C8 alkoxy, C1-C8 alkoxycarbonyl, C1-C8 alkyl, C0-C8 alkylcarbonyl, C1-C8 alkylsulphonyl, optionally substituted aryl, aryl-C0-C4 alkoxycarbonyl, cyano, halogen, optionally substituted heterocyclyl, hydroxy, nitro, oxide, oxo, tri-C1-C4-alkylsilyl, trifluoromethoxy or trifluoromethyl;
- L1 is —CH2—, —CH2—CH2—, —CH═CH—, —CH═N—, —CH2—CH═N—, —CH═N—O—, —CH2—CH═N—O—, —CH2—O—, —CH2—CH2—O—, —CH═CH—O—, —CH2—S—, —CH2—CH2—S—, —CH═CH—S—, —CH2—NH—, —CH2—CH2—NH—, —CH═CH—NH—, —CH2—NH—O—, —CH2—CH2—NH—O—, —CH═CH—NH—O—, —CH2—O—NH—, —CH2—CH2—O—NH—, —CH═CH—O—NH—, —CH2—N═N—, —CH2—CH2—N═N—, —CH═CH—N═N—, —CH2—S(O)—, —CH2—CH2—S(O)—, —CH═CH—S(O)—, —CH2—SO2—, —CH2—CH2—SO2—, —CH═CH—SO2—, —O—, —S—, —NH—, —NH—O—, —O—NH—, —N═N—, —S(O)—or —SO2—, which radicals are unsubstituted or substituted by 1-3 R3;
- L2 is —CH2—, —CH2—CH2—, —CH═CH— or, if L1 is —CH2—, —CH2—CH2— or —CH═CH—, is also —N═CH—, —N═CH—CH2—, —O—N═CH—CH2 or —O—N═CH—, which radicals are unsubstituted or substituted by 1-3 R3 or, if L1 is not —O—, —S—, —NH—, —NH—O—, —O—NH—, —N═N—, —S(O)— or —SO2—, is also a bond;
- R3 is C1-C8 alkoxy, C1-C8 alkoxycarbonyl, C1-C8 alkyl, C0-C8 alkylcarbonyl or C1-C8 alkylsulphonyl;
- Q is oxygen or sulphur;
- m is a number 0, 1 or 2;
- n is a number 0, 1 or 2;
- p is a number 0, 1, 2, 3 or 4;
- where
- m and n are not simultaneously 0 and, if R1 is hydrogen, n is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.