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    Fimasartan

    ACTIVE PHARMA INGREDIENTS

    INTERMEDIATES

    MARKET PLACE

    PharmaCompass
    $ API Ref.Price (USD/KG) : 1,129Xls

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    2D Structure
    Also known as: 247257-48-3, Kanarb, Fimasartan [inn], 2-(1-((2'-(2h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-n,n-dimethylethanethioamide, Chembl1951143, Fimasartan (inn)
    Molecular Formula
    C27H31N7OS
    Molecular Weight
    501.6  g/mol
    InChI Key
    AMEROGPZOLAFBN-UHFFFAOYSA-N
    FDA UNII
    P58222188P
    Fimasartan is an angiotensin II receptor antagonist (ARB) drug employed in the treatment of both hypertension and heart failure. It has been found to be safe when administered with hydrochlorothiazide (a diuretic) in clinical trials. Fimasartan was initially approved September 9th, 2010 in South Korea and is marketed under the brand name Kanarb by Boryung Pharmaceuticals.
    1 2D Structure

    2D Structure

    2 Identification
    2.1 Computed Descriptors
    2.1.1 IUPAC Name
    2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-N,N-dimethylethanethioamide
    2.1.2 InChI
    InChI=1S/C27H31N7OS/c1-5-6-11-24-28-18(2)23(16-25(36)33(3)4)27(35)34(24)17-19-12-14-20(15-13-19)21-9-7-8-10-22(21)26-29-31-32-30-26/h7-10,12-15H,5-6,11,16-17H2,1-4H3,(H,29,30,31,32)
    2.1.3 InChI Key
    AMEROGPZOLAFBN-UHFFFAOYSA-N
    2.1.4 Canonical SMILES
    CCCCC1=NC(=C(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3C4=NNN=N4)CC(=S)N(C)C)C
    2.2 Other Identifiers
    2.2.1 UNII
    P58222188P
    2.3 Synonyms
    2.3.1 MeSH Synonyms

    1. Br-a657

    2.3.2 Depositor-Supplied Synonyms

    1. 247257-48-3

    2. Kanarb

    3. Fimasartan [inn]

    4. 2-(1-((2'-(2h-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-n,n-dimethylethanethioamide

    5. Chembl1951143

    6. Fimasartan (inn)

    7. P58222188p

    8. 2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]methyl]pyrimidin-5-yl]-n,n-dimethylethanethioamide

    9. 2-(2-butyl-4-methyl-6-oxo-1-{[2'-(1h-tetrazol-5-yl)-4-biphenylyl]methyl}-1,6-dihydro-5-pyrimidinyl)-n,n-dimethylethanethioamide

    10. Br-a657

    11. Br-a-657.k

    12. Unii-p58222188p

    13. 5-pyrimidineethanethioamide, 2-butyl-1,6-dihydro-n,n,4-trimethyl-6-oxo-1-((2'-(2h-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-

    14. 5-pyrimidineethanethioamide, 2-butyl-1,6-dihydro-n,n,4-trimethyl-6-oxo-1-[[2'-(2h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-

    15. Fimasartan [who-dd]

    16. Schembl2229436

    17. Schembl20126833

    18. Dtxsid80179460

    19. Chebi:136044

    20. Bcp11616

    21. Ex-a3997

    22. Hy-b0780

    23. Zinc3842872

    24. Bdbm50364573

    25. Mfcd13194795

    26. S4975

    27. Zb1816

    28. Akos016011331

    29. Akos037643761

    30. Ccg-269705

    31. Cs-3509

    32. Db09279

    33. Ncgc00390600-01

    34. Ac-30631

    35. As-35179

    36. D10556

    37. 257f483

    38. A919293

    39. L019170

    40. Q8563179

    41. 2-((2-butyl-4-methyl-6-oxo-1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-1,6-dihydropyrimidin-5-yl))-n,n-dimethylthioacetamide

    42. 2-(1-((2'-(1h-tetrazol-5-yl)biphenyl-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-n,n-dimethylethanethioamide

    43. 2-(1-((2-(2h-tetrazol-5-yl)-[1,1-biphenyl]-4-yl)methyl)-2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)-n,n-dimethylethanethioamide

    44. 2-[2-butyl-4-methyl-6-oxo-1-[[4-[2-(2h-tetrazol-5-yl)phenyl]phenyl]met Hyl]pyrimidin-5-yl]-n,n-dimethylethanethioamide

    45. 2-butyl-5-dimethylaminothiocarbonylmethyl-6-methyl-3-[[2'-(1h-tetrazol-5-yl)biphenyl-4-yl]methyl]pyrimidin-4(3h)-one

    2.4 Create Date
    2006-10-25
    3 Chemical and Physical Properties
    Molecular Weight 501.6 g/mol
    Molecular Formula C27H31N7OS
    XLogP33.5
    Hydrogen Bond Donor Count1
    Hydrogen Bond Acceptor Count6
    Rotatable Bond Count9
    Exact Mass501.23107981 g/mol
    Monoisotopic Mass501.23107981 g/mol
    Topological Polar Surface Area123 Ų
    Heavy Atom Count36
    Formal Charge0
    Complexity849
    Isotope Atom Count0
    Defined Atom Stereocenter Count0
    Undefined Atom Stereocenter Count0
    Defined Bond Stereocenter Count0
    Undefined Bond Stereocenter Count0
    Covalently Bonded Unit Count1
    4 Drug and Medication Information
    4.1 Drug Indication

    Used for the treatment of hypertension and heart failure.

    5 Pharmacology and Biochemistry
    5.1 Pharmacology

    Fimasartan is a selective angiotensin receptor 1 (AR1) inhibitor. It acts to lower blood pressure by inhibiting vasoconstriction

    5.2 ATC Code

    C - Cardiovascular system

    C09 - Agents acting on the renin-angiotensin system

    C09C - Angiotensin ii receptor blockers (arbs), plain

    C09CA - Angiotensin ii receptor blockers (arbs), plain

    C09CA10 - Fimasartan

    5.3 Absorption, Distribution and Excretion

    Absorption

    Tmax is 0.5-1.3 h.

    Route of Elimination

    Most is eliminated unchangd in bile with less than 3% in the urine.

    5.4 Biological Half-Life

    The half life of elimination is 7-10 h.

    5.5 Mechanism of Action

    Angiotensin II activates AR1 leading to vasoconstriction and increased noradrenaline release which further increases vasoconstriction via action at 1-adrenergic receptors. It also stimulates secretion of aldosterone which acts to increase sodium and water reabsorption in the renal tubules. Fimasartan bind to and antagonizes AR1 preventing vasoconstriction and reducing aldosterone secretion to increase natriuresis leading to a reduction in blood volume. Together these effects produce an anti-hypertensive effect.