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US 2016/0108047 A1Published application
Imidazopyrrolidine derivatives and their use in the treatment of disease
AssigneeNovartis AG
InventorsJutta BLANK, Guido BOLD, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
Life of this patent
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Abstract
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; 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.
Claims10
A compound of formula (I) or a pharmaceutically acceptable salt thereof,
- wherein
- A is selected from:
- B is selected from
- C is selected from:
- R1 is selected from H, halo and methyl;
- R2 is selected from halo, cyano, methyl, —CF3 and —O(C1-C4alkyl);
- R3 is selected from H, methyl, ethyl, n-propyl, iso-propyl, n-butyl, sec-butyl, iso-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, methoxyethyl-, and
- R4 is selected from:
- H;
- C1-C4alkyl;
- C3-C6cycloalkyl;
- pyridine, optionally substituted with one or two substituents selected from halo, cyano, —OH, —C1-C4alkyl, haloC1-C4alkyl, —O(haloC1-C4alkyl) and —C1-C4alkoxy;
- pyrimidin-5-yl, optionally substituted with one or two substituents selected from halo, cyano, —OH, —C1-C4alkyl, haloC1-C4alkyl, —O(haloC1-C4alkyl) and —C1-C4alkoxy;
- a 5- or 6-membered saturated or partially unsaturated heterocyclic ring containing 1 oxygen or 1 nitrogen atom or 1 oxygen and 1 nitrogen atom, and optionally substituted with one —C1-C6alkyl substituent, or optionally substituted with 1, 2, 3 or 4 methyl substituents, or optionally substituted with one substituent selected from —C(O) C1-C4alkyl, —C(O)OC1-C4alkyl, —C(O)NHC1-C4alkyl, and —S(O)2C1-C4alkyl;
- a 5-membered heteroaryl ring containing 1 or 2 nitrogen atoms, and optionally substituted with —C1-C4alkyl;
- a 5-membered heteroaryl ring containing 1 nitrogen atom and 1 oxygen or 1 sulphur atom, optionally substituted with one or two C1-C4alkyl;
- and
- R5 is H;
- R6 is selected from methyl and methoxy;
- and
- R7 is selected from methyl, —CH2F and —CHF2;
- provided that when
- A is
- B is
- C is
- R2 is selected from chloro, fluoro, trifluoromethyl, methyl and cyano;
- and
- R3 is isopropyl, isobutyl, cyclopropyl, cyclobutyl or cyclopentyl;
- then
- R4 is selected from:
- H;
- C1-C4alkyl;
- C3-C6cycloalkyl;
- a 5- or 6-membered saturated or partially unsaturated heterocyclic ring containing 1 or 2 heteroatoms selected from oxygen, sulphur and nitrogen, and optionally substituted with C1-C4alkyl;
- or a 5- or 6-membered saturated or partially unsaturated heterocyclic ring containing 1 oxygen or 1 nitrogen atom, and optionally substituted with one C1-C4alkyl substituent or optionally substituted with 1, 2, 3 or 4 methyl substituents;
- or a 5- or 6-membered saturated or partially unsaturated heterocyclic ring containing 1 oxygen or 1 nitrogen atom, or 1 oxygen and 1 nitrogen atom, and optionally substituted with one —C1-C6alkyl substituent, or optionally substituted with 1, 2, 3 or 4 methyl substituents, or optionally substituted with one substituent selected from —C(O) C1-C4alkyl, —C(O)OC1-C4alkyl, —C(O)NHC1-C4alkyl, and —S(O)2C1-C4alkyl;
- a 5-membered heteroaryl ring containing 1 or 2 nitrogen atoms, and optionally substituted with C1-C4alkyl;
- a 5-membered heteroaryl ring containing 1 nitrogen atom and 1 oxygen or 1 sulphur atom, optionally substituted with one or two C1-C4alkyl;
- wherein R8 is selected from OCH3, OH and OCF3;
- and R9 is halo;
- and wherein * indicates the point of attachment to the remainder of the molecule.
38 more elements
-12. (canceled)
Dependencies are inferred from the claim text.