- CRYSTALLINE POLYMORPH OF N-(2,2,2-TRIFLUOROETHYL-9-[4-[R4-R[[[I4'- (TRIFLUOROMETHYL) [ 1,1 ' -BIPHENYL] -2-YL] CARBONYL] AMINO] -1 -PIPERIDINYL] BUTYL] -9H- FLUORENE-9-CARBOXAMIDE METHANESULFONATE AND PROCESS FOR PREPARATION THEREOF
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The present invention relates to? crystalline polymorph of N-(2,2.2-trifluoroethyl)-9- [4- [4- [ [[4,-(trifluoromethyl) [1,1 '-biphenyl] -2-yl] carbonyl] amino] - 1 -piperidinyl] butyl] -9H- fluorene-9-carboxamide methanesulfonate salt represented by the following structural formula- la and process for preparation thereof.
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- Method for synthesizing triglyceride transfer protease inhibitor
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The invention discloses a method for synthesizing the triglyceride transfer protease inhibitor Lomitapide. Specifically, based on improvement of an existing technique, the compounds 9-carboxyfluorene and 1,4-dibromobutane are used as raw materials, five-step reaction is conducted, and the defects of the prior art are overcome. Compared with the prior art, the method has the main advantage that column chromatography purification is avoided, and product purification is conducted with a recrystallization method which is economical and environment-friendly.
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- PROCESS FOR THE PREPARATION OF LOMITAPIDE
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The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities.
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- AMORPHOUS FORM OF LOMITAPIDE MESYLATE
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Provided is novel amorphous form of lomitapide mesylate salt and process for preparation thereof.
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- Crystal form III of lomitapide mesylate
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The invention provides a crystal form III of lomitapide mesylate. An X-ray diffraction pattern of the crystal form comprises diffraction peaks obtained when a diffraction angle 2theta is equal to 9.912 degrees, 11.584 degrees, 14.651 degrees, 15.444 degre
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Paragraph 0045; 0046; 0047
(2016/12/01)
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- COMPOUND IMPURITIES AND METHODS OF DETECTING SAME
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The present disclosure relates to compositions comprising impurities (e.g., carbamate and/or hydrolysis products) in a lomitapide sample and methods of detecting such impurities.
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Paragraph 0028
(2016/12/16)
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- New crystal forms of lomitapide mesylate and preparation method thereof
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The invention provides a new crystal form I and a new crystal form II of lomitapide mesylate and a preparation method thereof. An X-ray diffraction diagram of the crystallization form of the crystal form I contains diffraction peaks at the diffraction ang
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Paragraph 0048-0050
(2017/03/08)
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- PROCESS FOR MAKING LOMITAPIDE MESYLATE
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The present disclosure provides a process for lomitapide and its pharmaceutically acceptable salts. The present disclosure further provides pharmaceutically acceptable salts (e.g., 5 mesylate) of lomitapide in amorphous form.
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- Inhibitors of microsomal triglyceride transfer protein and method
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Compounds are provided which inhibit microsomal triglyceride transfer protein and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases. The compounds have the structure STR1 wherein Z, X1, X2, x and R5 are as defined herein.
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