BLU 554

It’s only fair to share… BLU 554 FGFR4 Inhibitor N-[(3S,4S)-3-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl]amino]tetrahydro-2H-pyran-4-yl]-2-propenamide N-[(3S,4S)-3-[[6-(2,6-Dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]tetrahydro-2H-pyran-4-yl]acrylamide CAS No. 1707289-21-1 Formula C24H24Cl2N4O4 MolWeight 503.378 PHASE 1 BLU-554 is a potent fibroblast growth factor receptor 4 (FGFR4) inhibitor. IC50 & Target: FGFR4[1] InVitro: Fibroblast growth factor receptor 4 (FGFR-4) is a protein that in humans is encoded by the FGFR-4 gene. This …

PF 06821497

It’s only fair to share…   PF 06821497 Cas 1844849-11-1 Designed to treat lymphoma 1(2H)-Isoquinolinone, 5,8-dichloro-2-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-3,4-dihydro-7-[(S)-methoxy-3-oxetanylmethyl]- MF C22 H24 Cl2 N2 O5,  MW 467.34 PF 06821497 5,8-Dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydro-3-pyridinyl)methyl]-7-[methoxy(3-oxetanyl)methyl]-3,4-dihydro-1(2H)-isoquinolinone 1(2H)-Isoquinolinone, 5,8-dichloro-2-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-3,4-dihydro-7-(methoxy-3-oxetanylmethyl)- Molecular Formula C22H24Cl2N2O5 Average mass 467.342 Da PF 06821497 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(S)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one US2015361067 Inventors Michael Raymond Collins, Robert Steven Kania, Robert Arnold Kumpf, Pei-Pei Kung, Daniel Tyler Richter, Scott Channing Sutton, …

ABBV 2222

It’s only fair to share… ABBV 2222 Benzoic acid, 4-[(2R,4R)-4-[[[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl]amino]-7-(difluoromethoxy)-3,4-dihydro-2H-1-benzopyran-2-yl]- 4-[(2R,4R)-4-({[1-(2,2-difluoro-1,3-benzodioxol-5-yl)cyclopropyl]carbonyl}- amino)-7-(difluoromethoxy)-3,4-dihydro-2H-chromen-2-yl]benzoic acid CAS  1918143-53-9 MF C28 H21 F4 N O7 MW 559.46 1H NMR (400 MHz, CDCl.sub.3) .delta. 8.17-8.03 (m, 2H), 7.49 (d, J=8.2 Hz, 2H), 7.16-6.99 (m, 4H), 6.73-6.67 (m, 2H), 6.38 (d, J=73.6 Hz, 1H), 5.48 (td, J=10.4, 6.1 Hz, 1H), 5.36 …

BMS 986158

It’s only fair to share… BMS 986158 MF C30H33N5O2, MW495.627 g/mol CAS 1800340-40-2 5H-Pyrido[3,2-b]indole-7-methanol, 3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-α,α-dimethyl-5-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- MOA:Bromodomain and extraterminal domain protein inhibitor Indication:Solid tumoursStatus: Phase II :Bristol-Myers Squibb (Originator) Phase I/IISolid tumours Originator Bristol-Myers Squibb Class Antineoplastics; Small molecules Mechanism of Action Bromodomain and extraterminal domain protein inhibitors 01 Jun 2015 Phase-I/II clinical trials for Solid tumours (Late-stage disease, Metastatic disease) …

GLGP 1837

It’s only fair to share… GLGP 1837 CAS 1654725-02-6 MF C16 H20 N4 O3 S, MW 348.42 For cystic fibrosis treatment N-(3-carbamoyl-5,5,7,7-tetramethyl-4H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-5-carboxamide 1H-Pyrazole-3-carboxamide, N-[3-(aminocarbonyl)-4,7-dihydro-5,5,7,7-tetramethyl-5H-thieno[2,3-c]pyran-2-yl]- Inventors Der Plas Steven Emiel Van, Sébastien Laurent Xavier MARTINA, Sébastien Jean-Jacques Cédric DROPSIT-MONTOVERT, Martin James Inglis Andrews, Hans KELGTERMANS Applicant Galapagos Nv SYNTHESIS GLGP 1837 ABC transporters are a family of …

EVP 4593

It’s only fair to share… EVP4593; EVP 4593; EVP-4593 M.Wt 356.42 545380-34-5; QNZ (EVP4593); QNZ; 6-Amino-4-(4-phenoxyphenylethylamino)quinazoline; N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine; Formula C₂₂H₂₀N₄O CAS No 545380-34-5 QNZ(EVP4593) is a derivative of 6-aminoquinazoline class that has been previously isolated as an inhibitor of PMA/PHA-induced NF-κB pathway activation in Jurkat cells (IC50= 9 nM). QNZ(EVP4593) is a derivative of 6-aminoquinazoline class …

The greening of peptide synthesis

It’s only fair to share…   The greening of peptide synthesis Stefan B. Lawrenson,a  Roy Arava  and  Michael North*a  *Corresponding authors aGreen Chemistry Centre of Excellence, Department of Chemistry, University of York, York, UK E-mail: Michael.north@york.ac.uk Abstract The synthesis of peptides by amide bond formation between suitably protected amino acids is a fundamental part of …

Process Development and Good Manufacturing Practice Production of a Tyrosinase Inhibitor via Titanium-Mediated Coupling between Unprotected Resorcinols and Ketones

It’s only fair to share…   (S)-4-(2,4-Dihydroxyphenyl)-N-(1-phenylethyl)piperidine-1-carboxamide (1) In a………………….. to yield crude 1 (3.51 kg, 77%, 97.7 A% purity). Recrystallization: In a 100 L double jacketed reactor were charged crude 1 (3.51 kg, 10.31 mol, 1.0 equiv), iPrOH (27.0 L, 7.5 vol), AcOH (74.1 g), and water (27.0 L, 7.5 vol). The suspension was warmed …

Debio-1452

It’s only fair to share… Debio-1452, AFN 1252 AFN-1252; UNII-T3O718IKKM; API-1252; CAS 620175-39-5; CHEMBL1652621; (E)-N-methyl-N-((3-methylbenzofuran-2-yl)methyl)-3-(7-oxo-5,6,7,8-tetrahydro-1,8-naphthyridin-3-yl)acrylamide MFC22 H21 N3 O3 2-Propenamide, N-methyl-N-[(3-methyl-2-benzofuranyl)methyl]-3-(5,6,7,8-tetrahydro-7-oxo-1,8-naphthyridin-3-yl)-, (2E)-  MW375.42 Phase 2, clinical trials for the oral treatment of staphylococcal infections, including hospital and community-acquired MRSA and acute bacterial skin and skin structure infections Qualified Infectious Disease Product designation GlaxoSmithKline plc INNOVATOR Debiopharm …