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Anacetrapib

From Wikipedia, the free encyclopedia
Anacetrapib
Names
Preferred IUPAC name
(4S,5R)-5-[3,5-Bis(trifluoromethyl)phenyl]-3-{[4′-fluoro-2′-methoxy-5′-(propan-2-yl)-4-(trifluoromethyl)[1,1′-biphenyl]-2-yl]methyl}-4-methyl-1,3-oxazolidin-2-one
Other names
MK-0859
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
UNII
  • InChI=1S/C30H25F10NO3/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40/h5-12,14-15,26H,13H2,1-4H3/t15-,26-/m0/s1 checkY
    Key: MZZLGJHLQGUVPN-HAWMADMCSA-N checkY
  • InChI=1/C30H25F10NO3/c1-14(2)22-11-23(25(43-4)12-24(22)31)21-6-5-18(28(32,33)34)9-17(21)13-41-15(3)26(44-27(41)42)16-7-19(29(35,36)37)10-20(8-16)30(38,39)40/h5-12,14-15,26H,13H2,1-4H3/t15-,26-/m0/s1
    Key: MZZLGJHLQGUVPN-HAWMADMCBN
  • O=C2O[C@H](c1cc(cc(c1)C(F)(F)F)C(F)(F)F)[C@@H](N2Cc4c(c3cc(c(F)cc3OC)C(C)C)ccc(c4)C(F)(F)F)C
Properties
C30H25F10NO3
Molar mass637.51 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)
Chemical compound

Anacetrapib is aCETP inhibitor which was being developed to treatelevated cholesterol levels in an effort to preventcardiovascular disease.[1] In 2017 its development was abandoned byMerck.[2]

Evidence

[edit]

In 2017 REVEAL trial anacetrapib was shown to decrease the risk of repeat heart attacks in high-risk patients with previous acute coronary events.[3]

See also

[edit]

Other CETP inhibitors:[citation needed]

References

[edit]
  1. ^Gutstein DE, Krishna R, Johns D, et al. (2012)."Anacetrapib, a Novel CETP Inhibitor: Pursuing a New Approach to Cardiovascular Risk Reduction".Clinical Pharmacology & Therapeutics.91 (1):109–122.doi:10.1038/clpt.2011.271.PMID 22130116.S2CID 36510986.
  2. ^"Merck says will not seek approval of cholesterol treatment".Reuters. 2017. Retrieved18 October 2017.
  3. ^Filippatos, TD; Kei, A; Elisaf, MS (29 September 2017)."Anacetrapib, a New CETP Inhibitor: The New Tool for the Management of Dyslipidemias?".Diseases.5 (4): 21.doi:10.3390/diseases5040021.PMC 5750532.PMID 28961179.

Further reading

[edit]
  • WO 2007005572, Miller, Ross A. & Cote, Aaron S., "Process for synthesizing a CETP inhibitor", published 2007-01-11, assigned toMerck & Co. Inc. 
GI tract
Cholesterol absorption inhibitors,NPC1L1
Bile acid sequestrants/resins (LDL)
Liver
Statins (HMG-CoA reductase,LDL)
Niacin and derivatives (HDL andLDL)
MTTP inhibitors (VLDL)
ATP citrate lyase inhibitors (LDL)
Thyromimetics (VLDL)
Blood vessels
PPAR agonists (LDL)
Fibrates
Others
CETP inhibitors (HDL)
PCSK9 inhibitors (LDL)
ANGPTL3 inhibitors (LDL/HDL)
Combinations
Other
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