BC-3781……A Pleuromutilin by Nabriva (Austria) in phase 2

New Drug Approvals

Antibiotics 02 00500 i025

BC-3781

Topical pleuromutilin antibiotic agent

Gram-positive, including MRSA, PHASE 2 COMPLETED

Nabriva (Austria)

BC-3781
The pleuromutilin BC-3781 belongs to the first generation of pleuromutilins to combine excellent oral
bioavailability with substantial activity against Gram-positive pathogens and atypicals as well as some
Gram-negative pathogens. In particular, BC-3781 is highly active against multi-drug resistant (MDR)
pathogens including methicillin resistant Staphylococcus aureus (MRSA), MDR Streptococcus pneumonia
(i.e. macrolide and quinolone resistance), and vancomycin resistant Enterococcus faecium. It is
characterized by excellent in vivo activities (e.g. pneumonia model), outstanding PK/PD parameters,
allowing once a day dosing, and a novel mode of action. BC-3781 is being developed for both oral and IV
administration and is intended for the treatment of serious multi-drug resistant skin & skin structure
infections (CSSI) and moderate to severe pneumonia (CAP, HAP etc).

Pleuromutilins have been known since 1951, but only entered the market in 2007 with the approval of retapamulin for…

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Cabazitaxel

New Drug Approvals

Cabazitaxel.png

Cabazitaxel

For treatment of patients with hormone-refractory metastatic prostate cancer previously treated with a docetaxel-containing treatment regimen.

4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-7β,10β-dimethoxy-9-oxotax-11-en-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenyl-propionate

(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(Acetyloxy)-15-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-ene-2-yl benzoate

183133-96-2

Jevtana, Taxoid XRP6258, Cabazitaxelum, 183133-96-2, Xrp6258, CHEBI:63584, XRP-6258, TXD 258, XRP 6258
Molecular Formula: C45H57NO14   Molecular Weight: 835.93238

EMA:LinkUS FDA:link

Cabazitaxel is prepared by semi-synthesis from 10-deacetylbaccatin III (10-DAB) which is extracted from yew tree needles. The chemical name of cabazitaxel is (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxy-tax-11-en-2-yl benzoate and is marketed as a 1:1 acetone solvate (propan-2-one),

Cabazitaxel is an anti-neoplastic used with the steroid medicine prednisone. Cabazitaxel is used to treat people with prostate cancer that has progressed despite treatment with docetaxel. Cabazitaxel is prepared by semi-synthesis with a precursor extracted from yew needles (10-deacetylbaccatin III). It was approved…

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NEW DRUG APPROVALS bY DR ANTHONY CRASTO WILL TOUCH 2 LAKH VIEWS THIS MONTH

A highly water-dispersible/magnetically separable palladium catalyst based on a Fe3O4@SiO2 anchored TEG-imidazolium ionic liquid for the Suzuki-Miyaura coupling reaction in water

A highly water-dispersible/magnetically separable palladium catalyst based on a Fe3O4@SiO2 anchored TEG-imidazolium ionic liquid for the Suzuki-Miyaura coupling reaction in water

Green Chem., 2014, Advance Article
DOI: 10.1039/C3GC42311E, Paper
Babak Karimi, Fariborz Mansouri, Hojatollah Vali
*
Corresponding authors
a
Department of Chemistry, Institute for Advanced Studies in Basic Sciences (IASBS), P.O. Box 45137-66731, Gava Zang, Zanjan, Iran
b
Anatomy and Cell Biology and Facility for Electron Microscopy Research, McGill University, 3450 University St, Montreal, Canada

A novel ionic liquid functionalized magnetic nanoparticle was prepared by anchoring an imidazolium ionic liquid bearing triethylene glycol moieties on the surface of silica-coated iron oxide nanoparticles.

A novel ionic liquid functionalized magnetic nanoparticle was prepared by anchoring an imidazolium ionic liquid bearing triethylene glycol moieties on the surface of silica-coated iron oxide nanoparticles. The material proved to be an effective host for the immobilization of a Pd catalyst through a subsequent simple ion-exchange process giving a highly water dispersible, active and yet magnetically recoverable Pd catalyst (Mag-IL-Pd) in the Suzuki–Miyaura coupling reaction in water. The as-prepared catalyst displayed remarkable activity toward challenging substrates such as heteroaryl halides and ortho-substituted aryl halides as well as aryl chlorides using very low Pd loading in excellent yields and demonstrating high TONs. Since the catalyst exhibited extremely low solubility in organic solvent, the recovered aqueous phase containing the catalyst can be simply and efficiently used in ten consecutive runs without significant decrease in activity and at the end of the process can be easily separated from the aqueous phase by applying an external magnetic field. This novel double-separation strategywith negligible leaching makes Mag-IL-Pd an eco-friendly and economical catalyst to perform this transformation

CHEMDRAW PRO 8.0

CHEMDRAW PRO 8.0

 

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General procedure of the production of nano and microparticles by the aerosol flow reactor method

The general procedure of the production of nano and microparticles by the aerosol flow reactor method is presented in Figure 1. Materials such as drug, polymer, and/or other excipients are dissolved in a solvent like water and ethanol that are most commonly used solvents. This starting solution is atomized with an appropriate droplet generator. The droplets are carried to a heated tubular laminar flow reactor with the aid of a dry gas or saturated gas. Allowing to use variable flow rates as well as temperatures in the reactor the droplet drying and residence time in the reactor can be fixed. Possible molecular rearrangements such as self-assembling and crystallization occur in this section. Dry aerosols are diluted by large volume of dry gas downstream the reactor to avoid solvent recondensation and wall deposition. Subsequently, the particles are collected by a collector that is suitable for the particular size of the particles.

Particle size and size distribution are determined directly from a gas phase with low-pressure impactors and a differential mobility analyzer (DMA). Particle morphology is observed by a scanning electron microscopy (SEM) and transmission electron microscopy (TEM). Moreover, the crystallinity of the materials can be detected by TEM.

Umirolimus, Biolimus

New Drug Approvals

Biolimus A9.png

Umirolimus, Biolimus

Biosensors (Originator)

40 -O-[(2′-ethoxy) ethyl]rapamycin

(1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-12-{(2R)-1-[(1S,3R,4R)-4-(2-Ethoxyethoxy)-3-methoxycyclohexyl]-2-propanyl}-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36 -dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone

Umirolimus [INN], Umirolimus [USAN:INN], UNII-U36PGF65JH, TRM-986, 42-O-(2-ethoxyethyl) rapamycin, cas no 851536-75-9
Molecular Formula: C55H87NO14   Molecular Weight: 986.27758
Umirolimus (INN/USAN), is a macrocyclic lactone, a highly lipophilic derivative of sirolimus, an immunosuppressant. This drug is proprietary toBiosensors International, which uses it in its own drug-eluting stents, and licenses it to partners such as Terumo.
Biosensors had been developing a Biolimus A9(R)-eluting coronary stent for the treatment of arterial restenosis. No recent development has been reported. The product candidate was developed with BioMatrix(R), the company’s low-profile, rapid-exchange delivery system. Specifically engineered for use on stents, Biolimus A9(R), a new rapamycin derivative, readily attaches to and enters smooth muscle cell membranes and binds to immunophilins inside the cell, causing cell cycle arrest at G0. Animal and in vitro studies suggest potency and…

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