Trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl] (2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid
AssigneeEli Lilly and Company
InventorsXinchao Chen, Scott Alan Frank, Steven Wayne Pedersen, David Michael Remick
Life of this patent
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Abstract
Abstract Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof, hydrate, and hydrate in crystalline form; pharmaceutical formulations; and methods of use are disclosed.
Claims21
A compound which is trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, a hydrate, or a pharmaceutically acceptable salt of said compound.
A composition comprising:
- trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, or a pharmaceutically acceptable salt thereof;
- and
- a solvate selected from:
- water, methanol, ethanol, isopropanol, formic acid, or acetic acid.
A method of preparing trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, or a pharmaceutically acceptable salt thereof, said method comprising de-esterifying a compound of formula II:
- where R is selected from a C1-4 alkyl, C1-4 haloalkyl, C3-6cycloalkyl, C1-4 alkyl-C3-6cycloalkyl, phenyl, or C1-5 alkylphenyl to provide a compound of formula I, or a pharmaceutically acceptable salt thereof
A compound having a structure illustrated below:
- wherein R is selected from:
- C1-4 alkyl, C1-4 haloalkyl, C3-6 cycloalkyl, C1-4 alkyl-C3-6cycloalkyl, phenyl, or C1-5 alkylphenyl.
A compound which is trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, or a pharmaceutically acceptable salt of said compound.
Dependencies are inferred from the claim text.