Category «Uncategorized»

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 …

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 …

Pimavanserin

It’s only fair to share… Pimavanserin MF C25H34FN3O2 MW 427.555 Pimavanserin, ACP 103, ACP-103; BVF-048 N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N’-(4-(2-methylpropyloxy)phenylmethyl)carbamide, 706779-91-1 (Pimavanserin ) 706782-28-7 (Pimavanserin Tartrate) for treatment of psychotic symptoms in patients with Parkinson’s disease WATCH OUT AS THIS POST IS UPDATED……….. Trade Name:Nuplazid® MOA:5-HT2A inverse agonist Indication:Hallucinations and delusions associated with Parkinson’s disease psychosis Company:Acadia (Originator) APPROVED US FDA 2016-04-29, ACADIA PHARMS INC, (NDA) …

Ranolazine, 雷诺嗪

It’s only fair to share… Ranolazine 雷诺嗪 MF C24H33N3O4 MW 427.536 Approvals FDA 2006, EMA 2008 for chronic angina Sponsor/Developer: Gilead Mechanism of action: Late sodium current inhibitor Indication (Phase): Type 2 diabetes (Phase III) A Phase 3 Study of Ranolazine in Subjects With Type 2 Diabetes Who Are Not Well Controlled on Metformin Alone (currently recruiting participants …

Imidafenacin, イミダフェナシン

It’s only fair to share… Imidafenacin イミダフェナシン Cas 170105-16-5 C20H21N3O, 319.408 APPROVED JAPAN 2015-07-29 4-(2-methyl-1H-imidazol-1-yl)-2,2-diphenylbutanamide 4-(2-methylimidazol-1-yl)-2,2-di(phenyl)butyramide D06273 KRP-197 KRP-197;ONO-8025 ONO-8025 UNII:XJR8Y07LJO Company:Kyorin (Originator), Ono (Originator)  4-(2-methyl-1-imidazolyl)- 2,2-diphenylbutyramide as a colorless needle: mp 189.0±190.0 C (from ethyl acetate:ethanol); High MS (EI+) m/z calcd for C20H21N3O 319.1685, found 319.1671; 1 H NMR (400 MHz, CDCl3) d 2.23 (3H, s), …

(3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol for the treatment of viral infections

It’s only fair to share… (3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol cas  1402802-45-2 JNJ ? WO 2012136834, WO 2014053595 for the treatment of viral infections Molecular Formula: C12H22N4O2 Molecular Weight: 254.32868 g/mol Inventors Gowan David Mc, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach,  Applicant Janssen R&D Ireland   (3S)-3-[(2-amino-5-methoxypyrimidin-4-yl)amino]heptan-1-ol Mark Hicken, …

ORM 10921

It’s only fair to share… ORM 10921 UNII-D26C95A960; D26C95A960; ORM-12741; ORM12741; ORM 12741; ORM-10921; (1S,12bS)-1-(Methoxymethyl)-1-methyl-2,3,4,6,7,12b-hexahydro-1H-[1]benzofuro[2,3-a]quinolizine (1S,12bS)-1-(methoxymethyl)-1-methyl-2,3,4,6,7,12b-hexahydro-[1]benzofuro[2,3-a]quinolizine 285.38, C18 H23 N O2 2H-Benzofuro[2,3-a]quinolizine, 1,3,4,6,7,12b-hexahydro-1-(methoxymethyl)-1-methyl-, (1S,12bS)- cas 610782-82-6 Belle David Din, Reija Jokela, Arto Tolvanen,Antti Haapalinna, Arto Karjalainen, Jukka Sallinen, Jari Ratilainen Applicant Orion Corporation David Din Belle Senior research scientist at Orion Corporation https://fi.linkedin.com/in/david-din-belle-a2594115 Jari Ratilainen https://fi.linkedin.com/in/jari-ratilainen-6a566218 Reija …

IPI-549

It’s only fair to share… IPI-549 CAS 1693758-51-8 MF : C30H24N8O2 Molecular Weight: 528.576 (S)-2-amino-N-(1-(8-((1-methyl-1H-pyrazol-4-yl)ethynyl)-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl)ethyl)pyrazolo[1,5-a]pyrimidine-3-carboxamide 2-amino-N-[(1S)-1-[8-[2-(1-methylpyrazol-4-yl)ethynyl]-1-oxo-2-phenylisoquinolin-3-yl]ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide Company Infinity Pharmaceuticals Inc. Description Small molecule inhibitor of phosphoinositide 3-kinase (PI3K) gamma Molecular Target Phosphoinositide 3-kinase (PI3K) gamma Mechanism of Action Phosphoinositide 3-kinase (PI3K) gamma inhibitor Therapeutic Modality Small molecule Latest Stage of Development Phase I Standard Indication Solid …