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Lusutrombopag, also known as S-888711, is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombo...
Reference: Process for synthesizing lusutrombopag. Assignee Shanghai Wanquan Chemical Technology Co., Ltd., Peop. Rep. China. CN 106083759. (2016).
Dacomitinib, also known as PF-299 and PF-00299804 ; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EG...
Reference: Yu, Shu; Dirat, Olivier. Early and late stage process development for the manufacture of dacomitinib. ACS Symposium Series. Volume 1239. Issue Comprehensive Accounts of Pharmaceutical Research and Development: From Discovery to Late-Stage Process Development, Volume 1. Pages 235-252. Journal; Online Computer File. (2016).
Bexagliflozin is a potent, selective SGLT2 inhibitor designed to reduce renal glucose reabsorption. In preclinical enzyme assays, it showed high affinity for human SGLT2 (IC₅₀ ~1–2 nM) with >300-fold ...
C-Aryl glucosides substituted at the 4'-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetesBy: Xu, Baihua; et alBioorganic & Medicinal Chemistry Letters (2011), 21(15), 4465-4470
Dasabuvir, also known as ABT-333, is a non-nucleoside polymerase inhibitor currently under clinical trials for the treatment of Hepatitis C. In the United States, it is approved by the Food and Drug A...
Barnes, David M.; Shekhar, Shashank; Dunn, Travis B.; Barkalow, Jufang H.; Chan, Vincent S.; Franczyk, Thaddeus S.; Haight, Anthony R.; Hengeveld, John E.; Kolaczkowski, Lawrence; Kotecki, Brian J.; Liang, Guangxin; Marek, James C.; McLaughlin, Maureen A.; Montavon, Donna K.; Napier, James J. Discovery and Development of Metal-Catalyzed Coupling Reactions in the Synthesis of Dasabuvir, an HCV-Polymerase Inhibitor. Journal of Organic Chemistry. Volume 84. Issue 8. Pages 4873-4892. Journal; Online Computer File. (2019).
Moxidectin is an anthelmintic drug which kills parasitic worms (helminths), and is used for the prevention and control of heartworm and intestinal worms. Moxidectin is a semisynthetic derivative of ne...
Reference: Beddall, Nicola E.; Howes, Peter D.; Ramsay, Michael V. J.; Roberts, Stanley M.; Slawin, Alexandra M. Z.; Sutherland, Derek R.; Tiley, Edward P.; Williams, David J. Chemical transformations of S541 factors (A)-(D): preparation and reactions of the 23-ketones. Tetrahedron Letters. Volume 29. Issue 21. Pages 2595-8. Journal. (1988).
Cedazuridine (E7727) is an oral cytidine deaminase (CDA) inhibitor developed to enhance the bioavailability of the hypomethylating agent decitabine. In preclinical studies, cedazuridine potently inhib...
Design, Synthesis, and Pharmacological Evaluation of Fluorinated Tetrahydrouridine Derivatives as Inhibitors of Cytidine DeaminaseBy: Ferraris, Dana; et alJournal of Medicinal Chemistry (2014), 57(6), 2582-2588
Capivasertib (AZD5363) is a potent, selective pan-AKT inhibitor with preclinical efficacy across multiple tumor models. It inhibited AKT1/2/3 with IC₅₀ values of 0.04–0.08 μM and suppressed downstream...
Crystalline forms of 4-(tert-butoxycarbonylamino)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxylic acid and tert-butyl (S)-(4-((1-(4-chlorophenyl)-3-hydroxypropyl)carbamoyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-yl)carbamateBy: AnonymousIP.com Journal (2024), 24(4B), 1-7
Tezacaftor, also known asVX-661, is CFTR modulator. VX-661 is potentially useful for treatment of cystic fibrosis disease. Cystic fibrosis (CF) is a genetic disease caused by defects in the CF transme...
Reference: Dhamankar, Varsha; Dinehart, Kirk Raymond; Dokou, Eleni; Ferris, Lori Ann; Gopinathan, Nishanth; McCarty, Katie; Metzler, Catherine; Zhang, Beili. Preparation of cystalline forms and pharmaceutical compositions comprising them as CFTR modulators for the treatment of cystic fibrosis. Assignee Vertex Pharmaceuticals Incorporated, USA. WO 2019079760. (2019).
Plazomicin is a next-generation aminoglycoside that has been designed as an antibiotic to avoid resistance through aminoglycoside-modifying enzymes. Plazomicin demonstrates high activity against the E...
Reference: Ma, Shutao; Cai, Xiaokang. Method for preparing plazomicin antibiotic for bacterial infection. Assignee Shandong University, Peop. Rep. China. CN 108948107. (2018).
Relebactam, also known as MK-7655, a potent and selective β-lactamase inhibitor. At a concentration of 4 mg/L, MK-7655 reduced imipenem MICs for Enterobacteriaceae with KPC carbapenemases from 16-64 m...
Reference: Mangion, Ian K.; Ruck, Rebecca T.; Rivera, Nelo; Huffman, Mark A.; Shevlin, Michael. A concise synthesis of a β-lactamase inhibitor. Organic Letters. Volume 13. Issue 20. Pages 5480-5483. Journal; Online Computer File. (2011).
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