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US 2014/0349990 A1Published application
Pyrazolopyrrolidine Derivatives and their Use in the Treatment of Disease
AssigneeNovartis AG
InventorsJutta BLANK, Vincent BORDAS, Simona COTESTA, Vito GUAGNANO, Heinrich RUEEGER, Andrea VAUPEL
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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.
Claims16
A compound of formula (I), or a pharmaceutically acceptable salt thereof,
- wherein
- ring C is selected from
- i.
- and ii.
- A is selected from
- B is selected from
- R3 is selected from H, methyl, ethyl, —CH2F, —CF3, isopropyl, —OH, ethoxy, methoxy, cyclopropyl, —CH2OCH3 and —CH2OH;
- R4a is selected from H, (C1-C4)alkyl, (C3-C6)cycloalkyl, —(CH2)2—OH, —(CH2)2—O—CH3, —C(O)—NH(CH3), —C(O)—N(CH3)2,
- R4b is selected from H, (C1-C4)alkyl, (C3-C6)cycloalkyl, —(CH2)2—OH, —(CH2)2—O—CH3, —(CH2)2—O—CH2—CF3, —(CH2)—CH(OH)—CF3, —C(O)—NH(CH3), —C(O)—N(CH3)2,
- R5 is H;
- R1 is selected from H, methyl, chloro and fluoro;
- R2 is selected from bromo, chloro, fluoro, —O—CF3 and —CF3;
- R2a is fluoro;
- R8 is methyl;
- R15, R16, R18 and R33 are all methoxy;
- R17 is methyl or methoxy;
- R22, R23, R26, R27, R28, R30, R32 and R33 are all methyl;
- R24 is methyl or —CHF2;
- R25 is methyl or —NR9R10;
- R29 is H or methyl;
- R31 is H, methyl or methoxy;
- R34 is H or methyl;
- R9 is H or methyl;
- R10 is H, methyl or —C(O)—(C1-C3)alkyl;
- R35 is H, methyl, —C(O)CH3 or —C(O)OCH2CH3;
- and
- * indicates the point of attachment to the remainder of the molecule;
- with the proviso that
- when ring C is i:
- A is:
- R1 is selected from methyl, chloro and fluoro,
- B is:
- R2 is chloro, fluoro or —CF3,
- and the remaining substituents are as defined herein,
- then R3 is selected from H, methyl, ethyl, —CH2F, —CF3, —OH, ethoxy, methoxy, —CH2OCH3 and —CH2OH.
32 more elements
Dependencies are inferred from the claim text.