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US 8,410,275 B2Granted
Bicyclic derivatives as CETP inhibitors
AssigneeNovartis AG
InventorsMasashi Kishida, Naoko Matsuura, Hidetomo Imase, Yuki Iwaki, Ichiro Umemura, Osamu Ohmori, Eiji Kawahara
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Abstract
The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.
Claims4
The compound of formula (I C)
- wherein X is N and Y is CH or N;
- R1 is 2-C1-C7-alkyl-2H-tetrazol-5-yl;
- the element —N(R4)(R5) is pyrrolidine-1-yl which is substituted by one or two substituents selected from the group consisting of C1-C7-alkyl-, C3-C7-cycloalkyl-, C3-C7-cycloalkyl-methyl-, C1-C7-alkoxy-methyl-, hydroxy-C1-C2-alkyl-C3-C7-cycloalkyl-, formyl-C3-C7-cycloalkyl-, formyl-C1-C2-alkyl-C3-C7-cycloalkyl-, HO2C—C3-C7-cycloalkyl-, HO2C—C1-C2-alkyl-C3-C7-cycloalkyl-, H2NC(═O)—C3-C7-cycloalkyl-, or H2NC(═O)—C1-C2-alkyl-C3-C7-cycloalkyl-;
- R9 is halogen;
- R12 and R13, independently of one another, is halo-C1-C7-alkyl or also halogen;
- wherein p is 1 or 2;
- or
- R4 is (C1-C4) alkyl- or (C3-C5) cycloalkyl-;
- and
- R5 is (C3-C7) cycloalkyl-(C1-C2) alkyl- which is optionally substituted by one to two substitutents selected from hydroxyl, alkoxy, HO2C—, HO2C—(C1-C3) alkyl-, hydroxy-(C1-C3) alkyl-, (C1-C6) alkoxy-carbonyl-, or (C1-C6) alkoxy-carbonyl-(C1-C3) alkyl-;
- or a salt thereof.
8 more elements
Dependencies are inferred from the claim text.