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New Drug Approvals

All about Patents and Intellectual property by DR ANTHONY MELVIN CRASTO, worlddrugtracker, Ph.D ( ICT, Mumbai) , INDIA 29Yrs Exp. in the feld of Organic Chemistry, Serving chemists around the world. THE VIEWS EXPRESSED ARE MY PERSONAL AND IN NO-WAY SUGGEST THE VIEWS OF THE PROFESSIONAL BODY OR THE COMPANY THAT I REPRESENT, amcrasto@gmail.com, +91 9323115463 India


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Besifovir, бесифовир , بيسيفوفير , 贝西福韦 ,

New Drug Approvals

Besifovir.svgChemSpider 2D Image | Besifovir | C10H14N5O4PBesifovir.pngBesifovir

  • Molecular FormulaC10H14N5O4P
  • Average mass299.223 Da
Phosphonic acid, [[[1-[(2-amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]- [ACD/Index Name]
бесифовир [Russian] [INN]
بيسيفوفير [Arabic] [INN]
贝西福韦 [Chinese] [INN]
((1-((2-Amino-9H-purin-9-yl)methyl)cyclopropoxy)methyl)phosphonic acid
[({1-[(2-Amino-9H-purin-9-yl)methyl]cyclopropyl}oxy)methyl]phosphonic acid
441785-25-7 [RN]

Besifovir (INN) is an investigational medication to treat hepatitis B virus (HBV) infection. It is a novel and potent acyclic nucleotide phosphonate with a similar chemical structure to adefovir and tenofovir.[2]Image result for BESIFOVIR

Besifovir dipivoxil maleate

CAS:1039623-01-2, Propanoic acid, 2,2-dimethyl-, 1,1′-[[[[[1-[(2-amino-9H-purin-9-yl)methyl]cyclopropyl]oxy]methyl]phosphinylidene]bis(oxymethylene)] ester, (2Z)-2-butenedioate (1:1)

Molecular Formula C22 H34 N5 O8 P . C4 H4 O4
 Molecular Weight 643.58
 Highest Phase Launched – 2017, korea

Besifovir dipivoxil maleate

Besifovir, also known as ANA-380; LB-80380; PMCDG dipivoxil, is a reverse transcriptase inhibitor potentially for treatment of hepatitis B infection. LB80380 is a prodrug and an oral nucleotide analogue that inhibits…

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Design, synthesis and biological evaluation of novel 5-hydroxy-2-methyl-4H-pyran-4-one derivatives as antiglioma agents

New Drug Approvals

Med. Chem. Commun., 2018, Advance Article
DOI: 10.1039/C7MD00551B, Research Article
Yi-Bin Li, Wen Hou, Hui Lin, Ping-Hua Sun, Jing Lin, Wei-Min Chen
Two series of 5-hydroxy-2-methyl-4H-pyran-4-one derivatives were synthesized and their antiglioma activities were evaluated.

Design, synthesis and biological evaluation of novel 5-hydroxy-2-methyl-4H-pyran-4-one derivatives as antiglioma agents

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D-2-Hydroxyglutarate (D-2HG) is frequently found in human brain cancers. Approximately 50–80% of grade II glioma patients have a high level…

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New Drug Approvals

SUDOTERB.pngFigure imgf000023_0002



CAS 676266-31-2;




Molecular Formula: C29H28F3N5O
Molecular Weight: 519.572 g/mol
  • Originator Lupin
  • Class Antituberculars; Isonicotinic acids; Pyrroles
  • Mechanism of Action Undefined mechanism
  • Orphan Drug Status No
  • New Molecular Entity Yes

Highest Development Phases

  • No development reported Tuberculosis

Most Recent Events

  • 23 Jul 2015 No recent reports on development identified – Phase-II for Tuberculosis in India (unspecified route)
  • 11 Dec 2013 Lupin completes a phase II trial in Tuberculosis in India prior to December 2013 (CTRI2009-091-000741)
  • 31 Jul 2010 Lupin completes enrolment in its phase II trial for Tuberculosis in India (CTRI2009-091-000741)


Sudoterb HCl
CAS: 1044503-04-9 (2HCl)
Chemical Formula: C29H30Cl2F3N5O
Molecular Weight: 592.4882

Image resultImage result for sudoterb


WO 2006109323

Tuberculosis (TB) is a contagious disease, which usually runs a protracted course, ending in death in majority of the cases, with relapse being a common feature of the disease. It is one…

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NNC 45-0781

New Drug Approvals

Image result for NNC 45-0781

NNC 45-0781

Molecular Formula C27H29NO3
Molecular Weight 415.5241

CAS 207277-66-5

  • 2H-1-Benzopyran-7-ol, 3,4-dihydro-3-phenyl-4-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-, cis-(-)-
  • (3S,4R)-3,4-Dihydro-3-phenyl-4-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2H-1-benzopyran-7-ol

2H-1-Benzopyran-7-ol, 3,4-dihydro-3-phenyl-4-(4-(2-(1-pyrrolidinyl)ethoxy)phenyl)-, (3S,4R)-

  • OriginatorNovo Nordisk
  • ClassOsteoporosis therapies; Pyrrolidines; Small molecules
  • Mechanism of ActionSelective estrogen receptor modulators


WO 9818776

WO 9818771

WO 2003063859

A quantitative structure activity relationship study on cis-3,4-diaryl hydroxy chromones as high affinity partial agonists for the estrogen receptor
Chemistry: An Indian Journal (2003), 1, (3), 207-214


EP 0937057; WO 9818771, EP 0937060; WO 9818776


Coumarin (III) was prepared by condensation of benzophenone (I) with phenylacetic acid (II) in the presence of Ac2O and Et3N. Reduction of the lactone function of (III) with LiAlH4, followed by acidic treatment furnished diaryl chromene (IV). Subsequent hydrogenation of (IV) over Pd/C gave rise to the racemic cis chromane (V), which was O-alkylated with 1-(2-chloroethyl) pyrrolidine (VI) producing the corresponding (pyrrolidinyl)ethoxy derivative. Resolution by means of active ditoluoyl tartaric acid yielded the desired (-)-enantiomer (VII). Finally…

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Compound 7 Ethyl(1R,2S,3S,4S)-2-(furan-2-yl)-3-nitro-6-oxobicyclo[2.2.2]octane-1-carboxylate To a solution of CAT 10 (128 mg, 0.37 mmol) and the nitroolefin 9 (3.1 g, 22.3 mmol) in 10 mL anhydrous CH2Cl2 at room temperature was added enone 8 (1.8 g, 10.7 mmol). The resulting mixture was stirred at the same temperature until enone 8 is consumed as indicated by TLC. Then DBU (0.34 mL, 3.20 mmol) was added and the mixture was allowed to stir at ambient temperature until completion as indicated by TLC. The solution was concentrated in vacuo and purified by flash chromatography on silica gel (Hexane / EtOAc = 20 / 1) to give 7 (2 g, 61% yield) as a yellow solid. [α]D 23 28.0 (c = 1.0, CHCl3).

1H NMR (400 MHz, CDCl3): δ 7.29 (d, J = 0.8 Hz, 1H), 6.27 (dd, J = 2.0 Hz, J = 3.2 Hz, 1H), 6.14 (d, J = 4.0 Hz, 1H), 4.93 (m, 1H), 4.57 (d, J = 4.4 Hz, 1H), 4.11 (m, 2H), 3.04-3.02 (m, 1H), 2.80-2.75 (m, 1H), 2.60- 2.54 (m, 1H), 2.33-2.29 (m, 1H), 1.88-1.72 (m, 2H), 1.33-1.23 (m, 1H), 1.21 (t, J = 7.2 Hz, 3H).

13C NMR (100 MHz, CDCl3): δ 204.1, 168.7, 151.8, 142.5, 110.5, 108.1, 88.3, 61.3, 56.3, 42.0, 40.8, 33.7, 26.9, 19.2, 13.8.

IR (thin film): 3435, 3141, 3120, 2996, 2959, 1715, 1653, 1621, 1557, 1505, 1473, 1443, 1408, 1371, 1336, 1301, 1336, 1301, 1270, 1236, 1142, 1120, 1083, 1062, 1074, 1045, 1045, 1011, 996, 960, 930, 892, 884, 867, 803, 753, 628, 600, 508, 436 cm-1 .

LRMS (ESI): 308.0 (M+H)+ , 330.0 (M+Na)+ .

HRMS (ESI): calcd for C15H18O6N (M+H) + : 308.1129. Found: 308.1130.

Melting point: 117-118 oC.

Concise asymmetric total synthesis of (−)-patchouli alcohol

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The asymmetric total synthesis of (−)-patchouli alcohol was accomplished in a concise manner. Key reactions include a highly diastereo- and enantioselective formal organocatalytic [4 + 2] cycloaddition reaction, a radical denitration reaction, and an oxidative carboxylation reaction. The formal synthesis of norpatchoulenol was achieved as well.

Graphical abstract: Concise asymmetric total synthesis of (−)-patchouli alcohol


“ORG CHEM SELECT” CATERS TO EDUCATION GLOBALLY, No commercial exploits are done or advertisements added by me. This is a compilation for educational purposes only. 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

Synthesis of isosorbide: an overview of challenging reactions

New Drug Approvals

Green Chem., 2017, Advance Article
DOI: 10.1039/C7GC01912B, Tutorial Review
C. Dussenne, T. Delaunay, V. Wiatz, H. Wyart, I. Suisse, M. Sauthier
This review gives an overview of the catalysts and technologies developed for the synthesis of isosorbide, a platform molecule derived from biomass (sorbitol and cellulose).

Synthesis of isosorbide: an overview of challenging reactions

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