- 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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Page/Page column 18; 19; 24; 25
(2017/07/06)
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- Polymorphs of Lomitapide and its Salts
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The present invention provides novel polymorphs of Lomitapide, process for their preparation and pharmaceutical compositions comprising them. The present invention also provides a novel polymorph of Lomitapide mesylate, process for its preparation and pharmaceutical compositions comprising it.
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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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Page/Page column 19
(2016/06/01)
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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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Paragraph 0037; 0038
(2016/12/26)
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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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Paragraph 0124; 0133
(2016/05/02)
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- CONFORMATIONALLY RESTRICTED AROMATIC INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND METHOD
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Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable salts thereof or prodrug esters thereof, wherein q is 0,1 or 2; R is H, alkyl, aryl or halogen; A is (1) a bond; (2) -O-; or (3) (i); B is: (ii) or (iii) or (iv) or (v) (wherein (a = 2, 3 or 4)) or (vi) or (vii) or (viii); and wherein L, L, R, R, R, R, R, R, R, R, R, X, (ix), (x) and (xi) are as defined herein.
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- 5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP
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5-Carboxamido-1,3,2-dioxaphosphorinanes have been identified as potent inhibitors of microsomal triglyceride-transfer protein. The 1,3,2- dioxaphosphorine functionality acted as a neutral and stable replacement for piperidine and piperidine N-oxide.
- Sulsky, Richard,Robl, Jeffrey A.,Biller, Scott A.,Harrity, Thomas W.,Wetterau, John,Connolly, Fergal,Jolibois, Kern,Kunselman, Lori
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p. 5067 - 5070
(2007/10/03)
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- Substituted piperazine derivatives, the preparation thereof and their use as medicaments
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The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, RcRf, Rgand m, n and X are defined as in claim 1, the isomers and salts thereof, particularly the
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- Substituted piperazine derivatives, the preparation thereofand their use as medicaments
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The present invention relates to substituted piperazine derivatives of general formula , (I wherein Ra, Rb, Rc, Rf, Rg, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
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- Substituted piperazine derivatives as mtp inhibitors
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The present invention relates to substituted piperazine derivatives of general formula wherein Ra to Rc, Ya, Yb, X and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
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- A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors
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A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in place of a piperidine group afforded potent inhibitors of MTP in vitro which were weakly active in vivo. Appropriate substitution on the benzimidazole ring, especially with small alkyl groups, led to dramatic increases in potency, both in a cellular assay of apoB secretion and especially in animal models of cholesterol lowering. The most potent in this series, 3g (BMS-212122), was significantly more potent than BMS-201038 in reducing plasma lipids (cholesterol, VLDL/LDL, TG) in both hamsters and cynomolgus monkeys.
- Robl,Sulsky,Sun,Simpkins,Wang,Dickson Jr.,Chen,Magnin,Taunk,Slusarchyk,Biller,Lan,Connolly,Kunselman,Sabrah,Jamil,Gordon,Harrity,Wetterau
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p. 851 - 856
(2007/10/03)
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