![methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide](https://lh3.googleusercontent.com/blogger_img_proxy/AEn0k_tLgoCnjED_ssiJoUsxGAy3MnMp13Jwuzf4iKST9wGFHHdhjHYWu2v4-FztkieFF58DMHIZVRcPqQIVq1YiEhErB0BYc2yFdQMibNCDNAJmtTY3X0u-uUObQ_x5aA=s0-d)
LOMITAPIDE MESYLATE
| Methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide | |
| CAS No.: | 202914-84-9 |
|---|---|
| Synonyms: |
|
| Formula: | C40H41F6N3O5S |
| Exact Mass: | 789.26700 |
Lomitapide mesylate is a white to off-white powder that is slightly
soluble in aqueous solutions of pH 2 to 5. Lomitapide mesylate is freely soluble in acetone,ethanol and methanol; soluble in 2-butanol, methylene chloride andacetonitrile; sparingly soluble in 1-octanol and 2-propanol; slightly soluble in ethyl acetate; and insoluble in heptane.........https://www.cadth.ca/sites/default/files/cdr/monograph/Juxtapid_Product%20Monograph.pdf
他哌( INN，作为Juxtapid销售在美国和欧盟Lojuxta )是治疗家族性高胆固醇血症药物，由Aegerion药品开发。 它已作为单一治疗进行临床试验和与阿托伐他汀的复方，依泽替米贝和非诺贝特。 美国食品和药物管理局( fda ) 2012年12月21日批准了他哌，孤儿药物以降低LDL胆固醇、总胆固醇、载脂蛋白B，和乘坐吊盘上下密度脂蛋白(非HDL )胆固醇在同合子家族性高胆固醇血症患者( HoFH )。 2013年5月31日，欧洲人用医药产品委员会( CHMP )一个积极的意见，一致表决通过推荐营销授权他哌。 2013年7月31日，欧洲委员会批准他哌作为一个低脂肪饮食和其它降脂药物产品有或没有低密度脂蛋白( ldl )机在HoFH成年患者。
SEE NMR GIVEN BY MEDKOO
http://www.medkoo.com/Product-Data/LomitapideMesylate/QC-LomitapideMesylate-BBC41017web.pdf
Juxtapid (lomitapide) is developed and manufactured by Aegerion Pharmaceuticals for the treatment of patients with homozygous familial hypercholesterolemia (HoFH).
In December 2012, the US Food and Drug Administration (FDA) approved Juxtapid for lipoprotein cholesterol reduction in HoFH patients.
Lomitapide (Juxtapid® and Lojuxta®; Aegerion Pharmaceuticals, Inc., MA, USA), an orally administered inhibitor of the microsomal triglyceride transfer protein, inhibits the synthesis and secretion of ApoB-containing lipoproteins and, thus, reduces plasma levels of LDL cholesterol (LDL-C). Lomitapide has been approved for the therapy of homozygous familial hypercholesterolemia patients.
Homozygous Familial Hypercholesterolemia (HoFH)
"In
December 2012, the US Food and Drug Administration approved Juxtapid
for lipoprotein cholesterol reduction in HoFH patients."
HoFH is
an uncommon genetic disease that impairs the function of the receptor
responsible for removing lipoprotein cholesterol (LDL-C) and total
cholesterol from the body. The disease is inherited from parents and is
characterised by high levels of LDL cholesterol. It results in
developing premature and progressive atherosclerosis by narrowing or
blocking of the arteries.The disease is found in about one out of 1,000,000 persons internationally.
Juxtapid's mechanism of action
Juxtapid contains lomitapide, which inhibits the microsomal triglyceride transfer protein (MTTP). The MTTP is an important gene that is necessary for low-density lipoprotein (VLDL) assembly and secretion in the liver. The drug is available in capsule form for oral administration.1H NMR PREDICT OF MESYLATE
![methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide NMR spectra analysis, Chemical CAS NO. 202914-84-9 NMR spectral analysis, methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide H-NMR spectrum](https://lh3.googleusercontent.com/blogger_img_proxy/AEn0k_s3tVNbSry_vcVdDYenrdl3MeUZr-mtSH75gF1sifzOAA2jQooU94TUHWX6WUiiQarLckofHHAZHs4I3VHoJBZziN2wsEZRm4P3BryuGdxqhFc6VbcwfkTwJbRKT-ZHeC9cK2vmDQrQ8d10tw=s0-d)
13 C NMR PREDICT OF MESYLATE
![methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide NMR spectra analysis, Chemical CAS NO. 202914-84-9 NMR spectral analysis, methanesulfonic acid,N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide C-NMR spectrum](https://lh3.googleusercontent.com/blogger_img_proxy/AEn0k_uUayb1ahfdJ4sltJwd_4joTdi2bzNA3zui8RaVQO3AV-Ni3tnoDu_w9FpaoNd0Ka6QdJ59Zs9ajEQwaqIB_vBDroDUWe1rEO5c06J1Web8oho3D66UGx8FsplR3YQ_hWI5ZfzOTWnB958KfM8=s0-d)
COSY PREDICT
............
LOMITAPIDE FREE BASE
1H NMR PREDICT
![N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide NMR spectra analysis, Chemical CAS NO. 182431-12-5 NMR spectral analysis, N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide H-NMR spectrum](https://lh3.googleusercontent.com/blogger_img_proxy/AEn0k_tGYdPEWghAwCIgF6P8KzxBcIwnBVlfQgE5mkp5-V_7o_zxALys851dprYSYJLzi1QGbOg0o4P5aM7Fj8zpkXkrwRAYM7962hF6PuiU4NqYRHXmtBS2a1rVb92jcr_5SEoL97xHiFQkt-EM=s0-d)
13C PREDICT OF BASE
![N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide NMR spectra analysis, Chemical CAS NO. 182431-12-5 NMR spectral analysis, N-(2,2,2-trifluoroethyl)-9-[4-[4-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]piperidin-1-yl]butyl]fluorene-9-carboxamide C-NMR spectrum](https://lh3.googleusercontent.com/blogger_img_proxy/AEn0k_uWjj1sa-pzla6GoJp7GrtkGt06xFjUPrUw3Fjvl-QD4WiHGXwlkYz74J4khRPoKJ4QNo_YMeZzMA8Dqe5Al7ThTAYEM2w-Oysg2WdR1JlQvF7paRl8VKgS_8FOdwb--9aClHLjNc2eliZG1w=s0-d)
Structure:
Spectrum Plot:
| Max ppm: | |
| Min ppm: | |
| Number of points: | |
| Line width (Hz): | |
| Annotate shifts: | |
| Display integral: | |
Cite:
| R.J. Abraham, M. Mobli Modelling 1H NMR Spectra of Organic Compounds: Theory, Applications and NMR Prediction Software, Wiley, Chichester, 2008. |
Shifts:
| Index | Name | Shift (ppm) |
|---|---|---|
| 6 | H28 | 4.172 |
| 7 | H29 | 4.172 |
| 9 | H23 | 6.800 |
| 15 | H1 | 2.647 |
| 16 | H2 | 2.647 |
| 19 | H19 | 7.546 |
| 21 | H25 | 7.479 |
| 24 | H22 | 7.809 |
| 26 | H27 | 7.567 |
| 29 | H21 | 7.809 |
| 31 | H26 | 7.567 |
| 33 | H24 | 7.479 |
| 35 | H18 | 7.546 |
| 37 | H3 | 1.059 |
| 38 | H4 | 1.059 |
| 40 | H6 | 1.677 |
| 41 | H7 | 1.677 |
| 43 | H8 | 2.163 |
| 44 | H9 | 2.163 |
| 47 | H10 | 2.264 |
| 48 | H11 | 2.264 |
| 50 | H14 | 1.554 |
| 51 | H15 | 1.554 |
| 53 | H5 | 2.607 |
| 55 | H20 | 5.687 |
| 60 | H30 | 7.438 |
| 62 | H32 | 7.422 |
| 64 | H33 | 7.542 |
| 66 | H31 | 7.781 |
| 70 | H34 | 8.175 |
| 72 | H36 | 7.663 |
| 75 | H37 | 7.663 |
| 77 | H35 | 8.175 |
| 83 | H12 | 2.264 |
| 84 | H13 | 2.264 |
| 86 | H16 | 1.554 |
| 87 | H17 | 1.554 |
Couplings:
| Index 1 | Index 2 | Coupling (Hz) |
|---|---|---|
| 1 | 3 | 160.00 |
| 1 | 4 | 160.00 |
| 1 | 6 | 9.58 |
| 1 | 7 | 9.58 |
| 3 | 4 | 160.00 |
| 3 | 6 | 9.58 |
| 3 | 7 | 9.58 |
| 4 | 6 | 9.58 |
| 4 | 7 | 9.58 |
| 6 | 7 | -12.50 |
| 6 | 9 | 2.56 |
| 7 | 9 | 7.98 |
| 15 | 16 | -13.20 |
| 15 | 37 | 2.51 |
| 15 | 38 | 13.21 |
| 16 | 37 | 13.21 |
| 16 | 38 | 2.65 |
| 19 | 21 | 7.50 |
| 19 | 24 | 0.60 |
| 19 | 26 | 1.10 |
| 21 | 24 | 1.10 |
| 21 | 26 | 7.50 |
| 24 | 26 | 7.50 |
| 24 | 29 | 0.60 |
| 29 | 31 | 7.50 |
| 29 | 33 | 1.10 |
| 29 | 35 | 0.60 |
| 31 | 33 | 7.50 |
| 31 | 35 | 1.10 |
| 33 | 35 | 7.50 |
| 37 | 38 | -13.20 |
| 37 | 40 | 13.20 |
| 37 | 41 | 2.87 |
| 38 | 40 | 2.31 |
| 38 | 41 | 13.20 |
| 40 | 41 | -13.20 |
| 40 | 43 | 12.59 |
| 40 | 44 | 4.04 |
| 41 | 43 | 1.83 |
| 41 | 44 | 12.21 |
| 43 | 44 | -12.50 |
| 47 | 48 | -12.50 |
| 47 | 50 | 1.85 |
| 47 | 51 | 4.26 |
| 47 | 53 | 0.56 |
| 48 | 50 | 3.45 |
| 48 | 51 | 12.43 |
| 48 | 53 | -0.30 |
| 50 | 51 | -13.20 |
| 50 | 53 | 2.58 |
| 50 | 86 | 0.48 |
| 50 | 87 | 1.29 |
| 51 | 53 | 11.93 |
| 51 | 86 | -0.32 |
| 51 | 87 | 0.49 |
| 53 | 55 | 7.67 |
| 53 | 83 | -0.31 |
| 53 | 84 | 0.55 |
| 53 | 86 | 11.93 |
| 53 | 87 | 2.57 |
| 60 | 62 | 7.50 |
| 60 | 64 | 1.10 |
| 60 | 66 | 0.60 |
| 62 | 64 | 7.50 |
| 62 | 66 | 1.10 |
| 64 | 66 | 7.50 |
| 66 | 70 | 0.60 |
| 66 | 77 | 0.60 |
| 70 | 72 | 7.50 |
| 70 | 75 | 0.60 |
| 70 | 77 | 1.90 |
| 72 | 75 | 1.90 |
| 72 | 77 | 0.60 |
| 72 | 79 | -1.50 |
| 72 | 80 | -1.50 |
| 72 | 81 | -1.50 |
| 75 | 77 | 7.50 |
| 75 | 79 | -1.50 |
| 75 | 80 | -1.50 |
| 75 | 81 | -1.50 |
| 79 | 80 | 160.00 |
| 79 | 81 | 160.00 |
| 80 | 81 | 160.00 |
| 83 | 84 | -12.50 |
| 83 | 86 | 12.41 |
| 83 | 87 | 3.48 |
| 84 | 86 | 4.33 |
| 84 | 87 | 1.82 |
| 86 | 87 | -13.20 |
http://www.pharmadl.com/stmt-show_2babd0fa-723a-427d-96fe-cad4e2903f00_aeea1ded-3186-4f50-982f-01efab0779cc.html
Lomitapide
Common name: Lomitapide; AEGR 733; AEGR-733; BMS 201038; BMS-201038; Juxtapid; Lojuxta; Lomitapide
Mesylate
Trademarks: Juxtapid; Lojuxta
Molecular Formula: C39H37F6N3O2
CAS Registry Number: 182431-12-5; 202914-84-9 (Mesylate)
CAS Name: N-(2,2,2-trifluoroethyl)-9-[4-(4-{2-[4-(trifluoromethyl)phenyl]benzamido}piperidin-1-yl)butyl]-9H-fluorene-9-carboxamide
Molecular Weight: 693.720
SMILES:C1CN(CCC1NC(=O)C2=CC=CC=C2C3=CC=C(C=C3)C(F)(F)F)CCCCC4(C5=CC=CC=C5C6=CC=CC=C64)C(=O)NCC(F)(F)F
InChI Key: MBBCVAKAJPKAKM-UHFFFAOYSA-N
InChI: InChI=1S/C39H37F6N3O2/c40-38(41,42)25-46-36(50)37(33-13-5-3-10-30(33)31-11-4-6-14-34(31)37)21-7-8-22-48-23-19-28(20-24-48)47-35(49)32-12-2-1-9-29(32)26-15-17-27(18-16-26)39(43,44)45/h1-6,9-18,28H,7-8,19-25H2,(H,46,50)(H,47,49)
Activity: Treatment of Familial Hypercholesterolemia;
Microsomal Triglyceride Transfer Protein Inhibitor; MTP Inhibitor; Cholesterol
Lowering Drug; Hypolipidemic Agents
Status: Launched 2012 (US); 2013 (EU)
Originator: Aegerion Pharmaceuticals IncNASIK INDIA
Pandavleni_Caves_near_Nasik
P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.
P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.
P.S. : The views expressed are my personal and in no-way suggest the views of the professional body or the company that I represent.
COCK WILL TEACH YOU NMR
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