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Tafenoquine, also known as WR-238605, is an oral active antimalaria drug that is being investigated as a potential treatment for malaria, as well as for malaria prevention. Tafenoquine Shows Activity ...
Reference: Blumbergs, Peter; LaMontagne, Maurice P. 4-Methyl-5-[(un)substituted phenoxy]-2,6-dimethoxy-8-(aminoalkylamino)quinolones. Assignee United States Dept. of the Army, USA. US 4617394. (1986).
Cevimeline HCl is a cholinergic agonist that binds to muscarinic receptors. Muscarinic agonists in sufficient dosage can increase secretion of exocrine glands, such as salivary and sweat glands, and i...
Kovi, Ravishanker; Kannapan, Jayaraman; Chowdari, Talluri Buhshaiah; Shah, Chirag Vasantlal. Process for the preparation of cis-2-methylspiro(1,3-oxathiolane-5-3')quinuclidine. Assignee Apicore, LLC, USA. 2011. US 20110301352
Gepotidacin, also known as GSK-2140944, is a potent Type II DNA topoisomerase inhibitor. Gepotidacin is a novel antibacterial drug candidate. Gepotidacin Demonstrates Absence of Fluoroquinolone-Like A...
Reductive Amination Bicarbonate Quench: Gas-Evolving Waste Stream Near-Miss InvestigationBy: Dixon, Frank; et alOrganic Process Research & Development (2020), 24(6), 1063-1067
Migalastat is a potent inhibitor of glycolipid biosynthesis.
Reference: Kim, Jin-Seok; Lee, Yong-Taek; Lee, Kun-Hee; Myeong, In-Soo; Kang, Jong-Cheol; Jung, Changyoung; Park, Seok-Hwi; Ham, Won-Hun. Stereoselective Chirality Extension of syn,anti- and syn,syn-Oxazine and Stereochemical Analysis of Chiral 1,3-Oxazines: Stereoselective Total Syntheses of (+)-1-Deoxygalactonojirimycin and (-)-1-Deoxygulonojirimycin. Journal of Organic Chemistry. Volume 81. Issue 17. Pages 7432-7438. Journal; Online Computer File. (2016).
Teriflunomide, aslo known as A77 1726, is the active metabolite of leflunomide. Teriflunomide is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate ...
Subramaniam, Palaniraja; Ramasubbu, Chandrasekaran; Athiramu, Selvaraj. Exploiting intramolecular hydrogen bonding for the highly (Z)-selective & metal free synthesis of amide substituted β-aminoenones. Green Chemistry. Volume 19. Issue 11. Pages 2541-2545. Journal; Online Computer File. (2017).
Lanreotide is a a synthetic cyclic octapeptide analogue of somatostatin. Lanreotide inhibits the secretion of growth hormone (GH) by binding to pituitary somatostatin receptors, and may inhibit the re...
Gu, Hanhua; Zhou, Tianqiong. Process for preparation of lanreotide by combination of solid and liquid phase peptide synthesis methods. Assignee Hangzhou Huajin Pharmaceutical Co., Ltd., Peop. Rep. China. CN 104497130. (2015).
Glasdegib, also known as PF-04449913, is an orally bioavailable small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. Hedgehog inhibitor PF-04449913 a...
Peng, Zhihui; Wong, John W.; Hansen, Eric C.; Puchlopek-Dermenci, Angela L. A.; Clarke, Hugh J. Development of a Concise, Asymmetric Synthesis of a Smoothened Receptor (SMO) Inhibitor: Enzymatic Transamination of a 4-Piperidinone with Dynamic Kinetic Resolution. Hugh J. Organic Letters. Volume 16. Issue 3. Pages 860-863. Journal; Online Computer File. (2014).
Tovorafenib is a potent, oral type II RAF kinase inhibitor that in biochemical assays inhibits mutant BRAF V600E, wild-type BRAF and CRAF with low-nanomolar IC₅₀ values (≈7.1, 10.1 and 0.7 nM, respect...
New drugs on the pharmaceutical market containing fluorine and residues of tailor-made amino acidsBy: Han, Jianlin; et alUkrains'kii Khimichnii Zhurnal (Ukrainian Edition) (2024), 90(9), 31-56
Aprocitentan, also known as ACT-132577, is an endothelin receptor antagonist and an pharmacologically active metabolite of macitentan . Aprocitentan antagonized the specific binding of ET-1 on membr...
The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor AntagonistBy: Bolli, Martin H.; et alJournal of Medicinal Chemistry (2012), 55(17), 7849-7861
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity. RXDX-101 has demonstrated pote...
Reference: Menichincheri, Maria; Ardini, Elena; Magnaghi, Paola; Avanzi, Nilla; Banfi, Patrizia; Bossi, Roberto; Buffa, Laura; Canevari, Giulia; Ceriani, Lucio; Colombo, Maristella; Corti, Luca; Donati, Daniele; Fasolini, Marina; Felder, Eduard; Fiorelli, Claudio; Fiorentini, Francesco; Galvani, Arturo; Isacchi, Antonella; Borgia, Andrea Lombardi; Marchionni, Chiara; Nesi, Marcella; Orrenius, Christian; Panzeri, Achille; Pesenti, Enrico; Rusconi, Luisa; Saccardo, Maria Beatrice; Vanotti, Ermes; Perrone, Ettore; Orsini, Paolo. Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor. Journal of Medicinal Chemistry. Volume 59. Issue 7. Pages 3392-3408. Journal; Online Computer File. (2016).
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