It’s only fair to share… New Patent, Suzhou MiracPharma Technology Co Ltd, Brigatinib, WO 2017016410 WO-2017016410 Preparation method for antitumor drug AP26113 Suzhou MiracPharma Technology Co Ltd SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD [CN/CN]; Room 1305, Building 1,Lianfeng Commercial Plaza, Industrial District Suzhou, Jiangsu 215000 (CN) XU, Xuenong; (CN) Improved process for preparing brigatinib, useful for treating cancer …
1 (4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-4-ol)
It’s only fair to share… 1 (4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-4-ol) Examples Example 1 – Preparation Of Compound 1 (4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-4-ol) 4-(3-(methylthio)phenyl)-1 – 4-(3-(methylsulfonyl)phenyl)- propylpiperidin-4-ol 1 -propylpiperidin-4-ol To a suspension of 4-hydroxy-4-(3-(methylthio)phenyl)-l-propylpiperidin-l-ium chloride (140g, 348mmol) in 710mL water were added 1.5g sodium tungstate dihydrate, and the mixture was heated to 45°C. 102mL of 33%H202 were added in 20min at 45-55°C. …
Hoshinolactam, A new antitrypanosomal lactam
It’s only fair to share… Tropical diseases caused by parasitic protozoa are a threat to human health, mainly in developing countries. Trypanosomiasis (Chagas disease and sleeping sickness) and leishmaniasis, inter alia, are classified as neglected tropical diseases, and over 400 million people are at risk of contracting these diseases. In addition, a parasite of …
AMG-3969
It’s only fair to share… AMG-3969 M.Wt: 522.46 Cas : 1361224-53-4 , MF: C21H20F6N4O3S WO 2012027261 PRODUCT PATENT Inventors Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, Jean …
Pridopidine
It’s only fair to share… Pridopidine Molecular Formula C15H23NO2S Average mass 281.414 Da 346688-38-8 CAS FREE FORM 882737-42-0 (hydrochloride) 1440284-30-9 HBr 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidin 4- (3 -Methanesulfonyl-phenyl ) – 1-propyl -piperidine ACR16 Huntexil UNII-HD4TW8S2VK; 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine ACR 16 ASP 2314 FR 310826 Huntingtons chorea Dopamine D2 receptor antagonist; Opioid receptor sigma agonist 1 Neurosearch INNOVATORS, In 2012, the product was acquired by …
BMS-960
It’s only fair to share… BMS-960 PRECLINICAL (S)-1-((S)-2-Hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)piperidine-3-carboxylic Acid 3-Piperidinecarboxylic acid, 1-[(2S)-2-hydroxy-2-[4-[5-[3-phenyl-4-(trifluoromethyl)-5-isoxazolyl]-1,2,4-oxadiazol-3-yl]phenyl]ethyl]-, (3S)- (S)-1-((S)-2-Hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)piperidine-3-carboxylic Acid CAS 1265321-86-5 FREE FORM FREE FORM 528.48, C26 H23 F3 N4 O5 CAS 1265323-40-7 HCL SALT BASIC PATENT WO201117578, 2011, (US Patent 8399451) Inventors John L. Gilmore, James E. Sheppeck Applicant Bristol-Myers Squibb Company Sphingosine-1-phosphate (S1P) is the endogenous ligand for the …
Plinabulin
It’s only fair to share… Plinabulin Molecular FormulaC19H20N4O2 Average mass336.388 Da (3Z,6Z)-3-Benzylidène-6-{[4-(2-méthyl-2-propanyl)-1H-imidazol-5-yl]méthylène}-2,5-pipérazinedione 2,5-Piperazinedione, 3-[[5-(1,1-dimethylethyl)-1H-imidazol-4-yl]methylene]-6-(phenylmethylene)-, (3Z,6Z)- CAS 714272-27-2 NPI 2358 NPI-2358; NPI 2358 UNII:986FY7F8XR Phase 3 Clinical Tubulin antagonist Cancer; Febrile neutropenia; Non-small-cell lung cancer Plinabulin (chemical structure, BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and is in a world-wide Phase …
Telcagepant Revisited
It’s only fair to share… Telcagepant, MK-0974 Molecular FormulaC26H27F5N6O3 Average mass566.523 Da 1-piperidinecarboxamide, N-[(3R,6S)-6-(2,3-difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b]pyridin-1-yl)- CAS 781649-09-0 OriginatorMerck & Co ClassAntimigraines; Piperidines Mechanism of ActionCalcitonin gene-related peptide receptor antagonists Migraine is a neurovascular disorder characterized by severe, debilitating, and throbbing unilateral headache. Though a leading cause of disability, it is a highly prevalent disease with a clear unmet …
Nonsteroidal antiandrogens, (S)-N-(2-bromo-6-methoxypyridin-4-yl)-2-hydroxy-2,4-dimethylpentanamide
It’s only fair to share… C12 H17 Br N2 O3, 317.18 Butanamide, N-(2-bromo-6-methoxy-4-pyridinyl)-2-hydroxy-2,3-dimethyl-, (2S)- (S)-N-(2-bromo-6-methoxypyridin-4-yl)-2-hydroxy-2,4-dimethylpentanamide (S)-N-(2-Bromo-6-methoxypyridin-4-yl)-2-hydroxy-2,4-dimethylpentanamide CAS 1433905-44-2 Nonsteroidal antiandrogens HPLC (Daicel Chiralpak IC 250 × 4.6 mm, 5 μm, n-heptane/IPA/TFA 930:70:1, 1 mL·min–1, 25 °C, UV 210 nm): tr (minor) = 5.1 min, tr (major) = 5.9 min. NMR 1H (400 MHz, DMSO-d6): 10.0 …
Development of a concise, scalable synthesis of a CCR1 antagonist utilizing a continuous flow Curtius rearrangement
It’s only fair to share… Development of a concise, scalable synthesis of a CCR1 antagonist utilizing a continuous flow Curtius rearrangement Green Chem., 2017, Advance Article DOI: 10.1039/C6GC03123D, Paper Maurice A. Marsini, Frederic G. Buono, Jon C. Lorenz, Bing-Shiou Yang, Jonathan T. Reeves, Kanwar Sidhu, Max Sarvestani, Zhulin Tan, Yongda Zhang, Ning Li, Heewon Lee, …