Category «Uncategorized»

Tedatioxetine Revisited

It’s only fair to share… Tedatioxetine TEDATIOXETINE; UNII-5H681S8O3S; Lu AA24530; 508233-95-2; Molecular Formula: C18H21NS Molecular Weight: 283.43104 g/mol 4-{2-[(4-Méthylphényl)sulfanyl]phényl}pipéridine 508233-95-2 [RN] Lu AA24530 Piperidine, 4-[2-[(4-methylphenyl)thio]phenyl] OriginatorLundbeck A/S DeveloperLundbeck A/S; Takeda ClassAntidepressants; Anxiolytics; Piperidines Mechanism of ActionBiogenic monoamine uptake inhibitors; Serotonin 2C receptor antagonists; Serotonin 3 receptor antagonists Generalised anxiety disorder; Major depressive disorder Most Recent …

GNE-272

It’s only fair to share… GNE-272 (S)-1-(3-((2-fluoro-4-(1-methyl-1H-pyrazol-4- yl)phenyl)amino)-1-(tetrahydrofuran-3-yl)-6,7-dihydro-1H-pyrazolo[4,3-c]pyridin- 5(4H)-yl)ethanone 1-[3-[2-fluoro-4-(1-methylpyrazol-4-yl)anilino]-1-[(3S)-oxolan-3-yl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-5-yl]ethanone CAS 1936428-93-1 Molecular Formula: C22H25FN6O2 Molecular Weight: 424.471303 g/mol GENENTECH, INC. [US/US]; 1 DNA Way South San Francisco, California 94080-4990 (US). CONSTELLATION PHARMACEUTICALS, INC. [US/US]; 215 First Street Suite 200 Cambridge, Massachusetts 02142 (US) ROMERO, F. Anthony; (US). MAGNUSON, Steven; (US). PASTOR, Richard; (US). TSUI, Vickie …

Consumption of a bioactive compound from Neem plant could significantly suppress development of prostate cancer

It’s only fair to share… (From left to right) Principal Investigator Associate Professor Gautam Sethi and NUS PhD candidate Ms Zhang Jingwen from the Department of Pharmacology at the NUS Yong Loo Lin School of Medicine led a research which found that a bioactive compound from the neem plant could significantly suppress development of prostate …

Novel Autotaxin Inhibitors for the Treatment of Osteoarthritis Pain from Lilly Research Laboratories

It’s only fair to share… 2-(2-(1H-1,2,3-triazol-5-yl)ethoxy)-1-(2-((2,3-dihydro-1H-inden-2-yl)amino)-5,7-dihydro-6Hpyrrolo[3,4-d]pyrimidin-6-yl)ethan-1-one l-[2-(2,3-dihydro- lH-inden-2-ylamino)-5,7-dihydro-6H-pyrrolo[3,4- d]pyrimidin-6-yl]-2-[2-(lH- l ,2,3-triazol-4-yl)ethoxy]ethanone. CAS 1619971-30-0 1-[2-(2,3-dihydro-1H-inden-2-ylamino)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidin-6-yl]-2-[2-(1H-1,2,3-triazol-4-yl)ethoxy]ethanone; Molecular Formula: C21H23N7O2 Molecular Weight: 405.45302 g/mol US2014200231 Scheme A     Scheme B   Scheme C VI   Scheme E Autotaxin is an enzyme reported to be the source of lysophosphatidic acid (LPA) which up-regulates pain-related proteins through one if its …

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 …