BRUSH UP YOUR NMR, 4-(3,5-Dichloropyridin-4-yl)morpholine

New Drug Approvals

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3,5-Dichloro-4-morpholinopyridine

Preparation of 4-(3,5-Dichloropyridin-4-yl)morpholine (5).(Pichowicz, M.Crumpler, S.McDonald, E.Blagg, J. Tetrahedron 2010662398DOI: 10.1016/j.tet.2010.01.101)

 5 as a light-orange solid.
1H NMR (CDCl3, 400 MHz): δ = 8.35 (2H, s), 3.84 (4H, m), 3.37 (4H, m);
13C NMR (CDCl3, 101 MHz): δ = 150.8, 149.3, 128.4, 67.4, 50.4;
HRMS–ESI+m/z [M + H]+ calcd for C9H11Cl2N2O+: 233.02429; found: 233.02446.
 1H NMR PREDICT
13C NMR PREDICT
DEPT PREDICT
Org. Process Res. Dev., Article ASAP
DOI: 10.1021/acs.oprd.8b00009

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Clc2cncc(Cl)c2N1CCOCC1

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Fosravuconazole L-lysine ethanolate, ホスラブコナゾール L-リシンエタノール付加物

New Drug Approvals

Image result for Fosravuconazole L-lysine ethanolateImage result for Fosravuconazole L-lysine ethanolate

C23H2F2N5O5PS▪C6H14N2O2▪C2H6O : 739.73
[914361-45-8]

[(2R,3R)-3-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1,2,4-triazol-1-yl)butan-2-yl]oxymethyl dihydrogen phosphate;(2S)-2,6-diaminohexanoic acid;ethanol

L-Lysine [[(2R,3R)-3-[4-(4-cyanophenyl)-1,3-thiazol-2-yl]-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl)butan-2-yl]oxy]methyl dihydrogen phosphate ethanol

BFE-1224
BMS-379224
E-1224

ravuconazole prodrugs, ravuconazole methyl phosphate

fosravuconazole bis(L-lysine)

ホスラブコナゾール L-リシンエタノール付加物

Formula
C23H20F2N5O5PS. C6H14N2O2. C2H6O
CAS
914361-45-8
Mol weight
739.727

Antifungal, Ergosterol biosynthesis inhibitor

Fungal infection; Onychomycosis; Trypanosoma cruzi infection

PMDA JAPAN APPROVED

2018/1/19 PMDA APPROVED Fosravuconazole L-lysine ethanolate Nailin Sato Pharmaceutical

FOR

Tinea, nail (onychomycosis)

NOTE THIS STR

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  • 4-[2-[(1R,2R)-2-(2,4-Difluorophenyl)-1-methyl-2-[(phosphonooxy)methoxy]-3-(1H-1,2,4-triazol-1-yl)propyl]-4-thiazolyl]benzonitrile
  • E 1224
  • Fosravuconazole
  • CAS  351227-64-0

Drugs for Neglected Diseases initiative (DNDi), under license from Eisai, is developing fosravuconazole for CD  and eumycetoma 

In February 2013, the drug was in phase II/III development by Seren Pharmaceuticals for onychomycosis in North America, Europe and Asia, including Japan,

In 2010, the product was licensed exclusively to Brain Factory (now Seren Pharma) for development, commercialization and sublicense in Japan for the…

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ELECLAZINE, элеклазин , إيليكلازين , 依来克秦 , REVISITED

New Drug Approvals

Eleclazine.pngChemSpider 2D Image | eleclazine | C21H16F3N3O3

ELECLAZINE

GS-6615

Molecular Formula: C21H16F3N3O3
Molecular Weight: 415.372 g/mol

1443211-72-0

4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3-dihydro-1,4-benzoxazepin-5-one

4-(pyrimidin-2-ylmethyl)-7-[4-(trifluoromethoxy)phenyl]-2,3,4,5- tetrahydro-1,4- benzoxazepin-5-one

7-(4-(Trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one

1,4-Benzoxazepin-5(2H)-one, 3,4-dihydro-4-(2-pyrimidinylmethyl)-7-[4-(trifluoromethoxy)phenyl]-

Eleclazine; UNII-PUY08529FK; 1443211-72-0; GS-6615; PUY08529FK; 4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-on

элеклазин [Russian] [INN]
إيليكلازين [Arabic] [INN]
依来克秦 [Chinese] [INN]
  • Phase III Long QT syndrome
INGREDIENT UNII CAS
Eleclazine Hydrochloride 4R1JP3Q4HI 1448754-43-5

Eleclazine has been used in trials studying the treatment of LQT2 Syndrome, Long QT Syndrome, Ischemic Heart Disease, Ventricular Arrhythmia, and Long QT Syndrome Type 3, among others.

In 2015, orphan drug designation was assigned to the product by the FDA for the treatment of congenital long QT syndrome.

  • Originator Gilead Sciences
  • Class Antiarrhythmics; Ischaemic heart disorder therapies; Pyrimidines; Small molecules; Vasodilators
  • Mechanism of Action Sodium channel antagonists

Highest Development Phases

  • Phase III  Long QT syndrome
  • Phase II/III Hypertrophic cardiomyopathy
  • Phase II Ventricular arrhythmias
  • No development reported 

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Baloxavir marboxil, バロキサビルマルボキシル , балоксавир марбоксил , بالوكسافير ماربوكسيل , 玛巴洛沙韦 ,

New Drug Approvals

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1985606-14-1.pngBaloxavir marboxil.pngImage result for XofluzaChemSpider 2D Image | baloxavir marboxil | C27H23F2N3O7S

Baloxavir marboxil

バロキサビルマルボキシル

балоксавир марбоксил [Russian] [INN]

بالوكسافير ماربوكسيل [Arabic] [INN]
玛巴洛沙韦 [Chinese] [INN]

Carbonic acid, [[(12aR)-12-[(11S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-3,4,6,8,12,12a-hexahydro-6,8-dioxo-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin-7-yl]oxy]methyl methyl ester

({(12aR)-12-[(11S)-7,8-Difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl]-6,8-dioxo-3,4,6,8,12,12a-hexahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazin-7-yl}oxy)methyl methyl carbonate

  1. (((12aR)-12-((11S)-7,8-Difluoro-6,11-dihydrodibenzo(b,E)thiepin-11-yl)-6,8-dioxo-3,4,6,8,12,12ahexahydro-1H-(1,4)oxazino(3,4-C)pyrido(2,1-F)(1,2,4)triazin-7-yl)oxy)methyl methyl carbonate
  2. Carbonic acid, (((12aR)-12-((11S)-7,8-difluoro-6,11-dihydrodibenzo(b,E)thiepin-11-yl)-3,4,6,8,12,12a-hexahydro-6,8-dioxo-1H-(1,4)oxazino(3,4-C)pyrido(2,1-F)(1,2,4)triazin-7-yl)oxy)methyl methyl ester

Antiviral

In Japan the product is indicated for treatment influenza types A and B in adults and children

RG-6152

UNII-505CXM6OHG

  • Originator Shionogi
  • Developer Roche; Shionogi
  • Class Antivirals; Dibenzothiepins; Esters; Pyridines; Small molecules; Triazines
  • Mechanism of Action Endonuclease inhibitors

Highest Development Phases

  • Marketed Influenza A virus infections; Influenza B virus infections
  • Phase III Influenza virus infections
  • Preclinical Influenza A virus H5N1 subtype
Xofluza (TN)
Antiviral
Formula
C27H23F2N3O7S
Cas
1985606-14-1
Mol weight
571.5492
2018/2/23 PMDA JAPAN APPROVED Baloxavir marboxil Xofluza Shionogi

Image result for japan animated flag

バロキサビル マルボキシル
Baloxavir Marboxil

C27H23F2N3O7S : 571.55
[1985606-14-1]

Image result for ShionogiImage result for Xofluza2D chemical structure of 1985606-14-1https://chem.nlm.nih.gov/chemidplus/sid/1985606141

Baloxavir marboxil (trade name Xofluza

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1,2 Diaminocyclohexane from Synthesis with Catalysts Pvt Ltd — All About Drugs

+91- 999-997-2051 info@synthesiswithcatalysts.com Website http://www.synthesiswithcatalysts.com/ bpk@synthesiswithcatalysts.com Axay Parmar Founder at Synthesis with Catalysts Pvt. Ltd, axayrp@gmail.com Basu Agarwal and Dr Razi Abdi shr@synthesiswithcatalysts.com, ba@synthesiswithcatalysts.com Synthesis with Catalysts Pvt Ltd was founded with an aim to help aromatic chemical, essential oil, pharmaceutical, API manufacturers to develop new products, increase productivity and improve production methodologies. We have an…

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ANTHONY M CRASTO GETS PHARMA EXCELLENCE AWARD AT THE GOLDEN GLOBE TIGER AWARDS 2018

New Drug Approvals

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Pic…. Shobha crasto, Lionel and Aishal collecting my award named The Golden Globe Tigers Awards 2018, for Excellence in Pharma, at kuala lumpur, Malaysia, 23 april 2018 at Pullman city centre hotel, Kuala lumpur, Malaysia. Dr Anthony could not travel as he is wheelchair bound and 90 percent paralysed

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DR ANTHONY M CRASTO

The Golden Globe Tigers Award 2018 is the highest recognition amongst individual and organizations who have achieved the highest levels of standards and benchmark in numerous areas such as CSR, Pharma, Social Media & Digital Marketing, Education Leadership Award and so on. The award ceremony took place in Pullman Kuala Lumpur City Centre Hotel & Residences on the 23rd of April, where a number of respectable attendees were present not only from Malaysia but from many different parts of the world such as Iceland, Saudi Arabia, India, China, South Africa and such!

The Golden Globe Tigers Award not only…

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