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, email@example.com, +91 9323115463 India
- Molecular FormulaC10H14N5O4P
- Average mass299.223 Da
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.
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|
|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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DOI: 10.1039/C7MD00551B, Research Article
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
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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LL 3858, SUDOTERB
|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)
CAS: 1044503-04-9 (2HCl)
Chemical Formula: C29H30Cl2F3N5O
Molecular Weight: 592.4882
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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- 2H-1-Benzopyran-7-ol, 3,4-dihydro-3-phenyl-4-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-, cis-(-)-
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
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
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.
- This article is part of the themed collection: Synthetic Approaches to Natural Products via Catalytic Processes
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DOI: 10.1039/C7GC01912B, Tutorial Review
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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