Benzyl sulfonamide derivatives useful as MOGAT-2 inhibitors
AssigneeEli Lilly and Company
InventorsMaria Carmen Fernandez, Lance Allen Pfeifer, Maria Rosario Gonzalez-Garcia
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds of Formula below: and analogues thereof where the various substituent groups, R1, R2, R3, R4, R5 A, and X are described herein; or a pharmaceutical salt thereof; a method of treating a condition such as hypertriglyceridemia and a process for preparing the compounds.
Claims27
A compound of the formula below:
- wherein
- R1 is selected from:
- —CH3 and —CF3;
- R2 is selected from:
- H, —CH3, —CH2OCH3, and —CH2OCH2CH3;
- R3 is selected from:
- H, —C1-2 alkyl, —CH2OCH3, —CH2OCH2CH3;
- R4 is selected from:
- H, halo, and —OCH3;
- R5 is selected from H and halo;
- A is selected from:
- CH, CF, C—CN, and N;
- X is selected from:
- CH, CF, COCH3, and N;
- and
- provided that only one of X and A is N,
- or a pharmaceutically acceptable salt thereof.
A compound of the formula below:
- or a pharmaceutically acceptable salt thereof.
A compound which is N-[(1S)-2,2,2-Trifluoro-1-{4-[({(2S)-2-[(5-fluoropyridin-2-yl)oxy]-3-methoxypropyl}amino)methyl]phenyl}ethyl]methanesulfonamide hydrochloride.
A pharmaceutical composition comprising N-[(1S)-2,2,2-Trifluoro-1-{4-[({(2S)-2-[(5-fluoropyridin-2-yl)oxy]-3-ethoxypropyl}amino)methyl]phenyl}ethyl]methanesulfonamide, or a pharmaceutically acceptable salt thereof, and at least one of a pharmaceutically acceptable carrier, diluent, or excipient.
A compound which is N-[(1S)-2,2,2-Trifluoro-1-{4-[({(2S)-2-[(5-fluoropyridin-2-yl)oxy]-3-ethoxypropyl}amino)methyl]phenyl}ethyl]methanesulfonamide hydrochloride salt in crystalline form characterized by an X-ray powder diffraction pattern obtained from a CuKα source λ=1.54056 Å), which comprises peaks at:
- a) 12.71°, 14.95°, 18.13°, 18.67°, 21.14° and 27.76°±/−0.2 in 2θ or
- b) 5.46°, 11.10°, 12.71°, 13.97°, 14.95°, 18.13°, 18.67°, 21.14°, and 27.76°±/−0.2° in 2θ.
Dependencies are inferred from the claim text.