Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist from Zydus Cadila

It’s only fair to share… Indian flag (S)-3-(4-((3-((isopropyl(thiophen-3- ylmethyl)amino)methyl)benzyl)oxy)phenyl)hex-4-ynoic acid Calcium (S)-3-(4-((3-((isopropyl(thiophen-3-yl methyl)amino)methyl)benzyl)oxy)phenyl)hex-4-ynoate Calcium (S)-3-(4-((3-((isopropyl(thiophen-3-yl methyl)amino)methyl)benzyl)oxy)phenyl)hex-4-ynoate   The compounds of theese type lower blood glucose, regulate peripheral satiety, lower or modulate triglyceride levels and/or cholesterol levels and/or low-density lipoproteins (LDL) and raises the high-density l ipoproteins (HDL) plasma levels and hence are useful in combating different …

Photoinduced Conversion of Antimelanoma Agent Dabrafenib to a Novel Fluorescent BRAFV600E Inhibitor

It’s only fair to share… N-(5-amino-2-tert-butyl)-11-fluorbenzol[f]thiazol-[4,5-h]-quinazolin-10-yl)-2,6-difluorbenzolsulfonamide = Dabrafenib_photo (2) C23H18F3N5O2S2 (Mr = 517.09) Solution of 5 mg (9.6 μmol) dabrafenib in 2 ml THF was irradiated at 365 nm with 5.4 W for 2 min. This procedure was repeated 18 times at room temperature. The reaction batches were combined. The total initial weight of dabrafenib …

Synthesis of 4-Heteroaryl–Quinazoline Derivatives as Potential Anti-breast Cancer Agents

It’s only fair to share… Ethyl 2-[(6,7-dimethoxyquinazolin-4-yl)amino]-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxylate (15b) Yield: 76%; mp: 254–256°C; IR (cm−1): 3200 (NH), 2974, 2854 (CH-aliphatic), 1656 (C=O); 1H NMR (DMSO-d6) δ ppm 1.03 (t, 3H, CH3CH2, J = 7.2 Hz), 1.21 (t, 2H, CH2, J = 6.9 Hz), 2.88 (t, 2H, CH2, J = 6.9 Hz), 3.40 (q, 2H, CH2, J = 6.9 Hz), 3.88 (s, 3H, OCH3), 3.91 (s, 3H, OCH3), 3.96 …

VT 1129

It’s only fair to share… VT 1129 1340593-70-5 CAS MF C22 H14 F7 N5 O2, MW 513.37 2-Pyridineethanol, α-(2,4-difluorophenyl)-β,β-difluoro-α-(1H-tetrazol-1-ylmethyl)-5-[4-(trifluoromethoxy)phenyl]-, (αR)- R ISOMER ROTATION + Originator Viamet Pharmaceuticals Class Antifungals; Small molecules Mechanism of Action 14-alpha demethylase inhibitors Orphan Drug Status Yes – Cryptococcosis On Fast track Cryptococcosis Phase I Cryptococcosis Most Recent Events 01 Jun 2016 VT 1129 receives Fast Track designation for Cryptococcosis …

Sanaria® PfSPZ Vaccine Against Malaria Receives FDA Fast Track Designation

It’s only fair to share… ROCKVILLE, Md., Sept. 22, 2016 /PRNewswire/ — Sanaria Inc. today announced it has received U.S. Food and Drug Administration (FDA) Fast Track designation for its preventative vaccine for malaria, Sanaria® PfSPZ Vaccine.  Sanaria believes its PfSPZ Vaccine is the only malaria vaccine to have ever received this distinction. According to the …

US FDA grants approval for Novartis’ Ilaris (canakinumab) to treat Periodic Fever Syndromes

It’s only fair to share… Ribbon diagram of canakinumab (blue) bound to IL-1β (yellow) from PDBentry 5bvp[1] US FDA grants approval for Novartis’ Ilaris to treat Periodic Fever Syndromes Novartis has received the US Food and Drug Administration’s (FDA) approval for Ilaris (canakinumab) to treat rare Periodic Fever Syndrome conditions. 26 September 2016 Read at http://www.pharmaceutical-technology.com/news/newsus-fda-grants-approval-for-novartis-ilaris-to-treat-periodic-fever-syndromes-5014453?WT.mc_id=DN_News …

WO 2016147120, AZILSARTAN, NEW PATENT, SMILAX Laboratories Ltd

It’s only fair to share… WO-2016147120, AZILSARTAN, NEW PATENT, SMILAX Laboratories Ltd SMILAX LABORATORIES LIMITED [IN/IN]; Plot No. 12/A, Phase – III, I.D.A. Jeedimetla, Hyderabad 500 055 (IN). The present invention relates to an improved process for the preparation of substantially pure compound of 2-Ethoxy-1-[[2′-(2,5-dihydro-5-oxo-1,2,4-oxadiazol- 3-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylic acid (Azilsartan) of Formula I, with a reduced content of …

WO 2016147197, DAPAGLIFLOZIN, NEW PATENT, HARMAN FINOCHEM LIMITED

It’s only fair to share…       WO 2016147197, DAPAGLIFLOZIN, NEW PATENT, HARMAN FINOCHEM LIMITED LINK>>> (WO2016147197) A NOVEL PROCESS FOR PREPARING (2S,3R,4R,5S,6R)-2-[4-CHLORO-3-(4-ETHOXYBENZYL)PHENY 1] -6-(HY DROXY METHYL)TETRAHYDRO-2H-PY RAN-3,4,5-TRIOL AND ITS AMORPHOUS FORM HARMAN FINOCHEM LIMITED [IN/IN]; 107, Vinay Bhavya Complex 159-A, C.S.T. Road Kalina, Mumbai 400098 Maharashtra (IN) KADAM, Vijay Trimbak; (IN). SAIKRISHNA; (IN). CHOUDHARE, …

WO 2016145990, Ledipasvir, New patent, SHANGHAI FOREFRONT PHARMACEUTICAL CO., LTD

It’s only fair to share… WO 2016145990, Ledipasvir, New patent, SHANGHAI FOREFRONT PHARMACEUTICAL CO., LTD (WO2016145990) METHOD OF PREPARATION FOR LEDIPASVIR AND DERIVATIVE THEREOF, AND INTERMEDIATE COMPOUND FOR PREPARATION OF LEDIPASVIR SHANGHAI FOREFRONT PHARMCEUTICAL CO., LTD [CN/CN]; Room 1306, No.781 Cailun Road China (Shanghai) Pilot Free Trade Zone, Pudong New Area Shanghai 201203 (CN) HUANG, Chengjun; …

2-Arylideneimidazo[1,2-a]pyridinones as Topoisomerase IIα-Inhibiting Anticancer Agents

It’s only fair to share… Scaffold-hopping of bioactive natural product aurones has been studied for the first time. 2-Arylideneimidazo[1,2-a]pyridinones as potential topoisomerase IIα (hTopoIIα)-targeting anticancer compounds were considered. A multifunctional activator, polyphosphoric acid, enabled to realize a cascade reaction of 2-aminopyridine with 2,3-epoxyesters toward synthesis of 2-arylideneimidazo[1,2-a]pyridinones. Most of the compounds exhibited hTopoIIα-selective poison activity …