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Bazedoxifene is a third generation selective estrogen receptor modulator (SERM), developed by Pfizer following the completion of their takeover of Wyeth Pharmaceuticals. In late 2013, Pfizer received ...
Mylavarapu, Ravikumar; Kondaiah, G. C. M.; Reddy, L. Amaranth; Dubey, Manoj Kumar; Jasmine; Mukkanti, Kagga; Bandichhor, Rakeshwar. An improved synthesis of Bazedoxifene acetate. Chemistry & Biology Interface. Volume 5. Issue 2. Pages 137-150. Journal; Online Computer File. (2015).
Reference: Okamoto, Kazuya; Ueno, Tatsuhiko; Hato, Yoshio; Hakogi, Toshikazu; Majima, Shohei. Method for stereoselective preparation of substituted polycyclic pyridone derivative. Assignee Shionogi & Co., Ltd., Japan. WO 2019070059. (2019).
Atazanavir is an antiretroviral drug of the protease inhibitor (PI) class. It is sold under the trade name Reyataz. Like other antiretrovirals, it is used to treat infection of human immunodeficiency ...
Fan, Xing; Song, Yan-Li; Long, Ya-Qiu. An efficient and practical synthesis of the HIV protease inhibitor Atazanavir via a highly diastereoselective reduction approach. Organic Process Research & Development. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences. Volume 12. Issue 1. Pages 69-75. 2008.
Inavolisib, also known as GDC-0077, is a potent and selective PI3K inhibitor. Inavolisib is an extraordinarily potent and selective PI3Kα inhibitor (IC₅₀ ≈ 0.038 nM), exhibiting over 300-fold select...
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
Darunavir is a drug used to treat HIV infection. It is in the protease inhibitor class. Prezista is an OARAC recommended treatment option for treatment-naïve and treatment-experienced adults and adol...
Ghosh, Arun K.; Leshchenko, Sofiya; Noetzel, Marcus. Stereoselective Photochemical 1,3-Dioxolane Addition to 5-Alkoxymethyl-2(5H)-furanone: Synthesis of Bis-tetrahydrofuranyl Ligand for HIV Protease Inhibitor UIC-94017 (TMC-114). Journal of Organic Chemistry. Department of Chemistry. University of Illinois at Chicago. Chicago, USA 60607. Volume 69. Issue 23. Pages 7822-7829. 2004
Ceftobiprole is a broad-spectrum cephalosporin with potent in vitro and in vivo activity against a range of Gram-positive and Gram-negative pathogens. In vitro, it demonstrates strong activity against...
Patent#: WO2010136423
Pralsetinib (BLU-667) is a potent, selective, orally bioavailable RET kinase inhibitor. In preclinical biochemical assays, it inhibited wild-type RET with an IC50 of ~0.4 nM and retained strong activi...
Synthesis and intermediates in preparation of cis-N-[(1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)-3-pyridinyl]ethyl]-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]cyclohexanecarboxamideIP.com Journal (2021), 21(11A), 1-3
Pirtobrutinib, also known as LOXO-305 and LY 3527727, is a Bruton's tyrosine kinase (BTK) inhibitor and antineoplastic agent. Pirtobrutinib showed promising initial efficacy in pts with pretreated Ric...
Direct Multi-Deuterium Labelling of PirtobrutinibBy: Kriegelstein, Michal; et alJournal of Labelled Compounds and Radiopharmaceuticals (2024), 67(9), 314-323
Quemliclustat, also known as AB-680, is highly potent, reversible and selective CD73 inhibitor. Quemliclustat has been shown to block the production of adenosine. The reduction of adenosine restores i...
1.1Catalysts:Ammonium sulfateSolvents:Hexamethyldisilane;rt → reflux; 3 h, reflux1.2Solvents:Acetonitrile;reflux → 0 °C1.3Reagents:Trimethylsilyl triflate;0 °C; 1 h, 0 °C1.4Reagents:Sodium bicarbonateSolvents:Water;0 °C2.1Reagents:TriethylamineSolvents:Ethanol;overnight, rt → 110 °C; 110 °C → rt2.2Reagents:AmmoniaSolvents:Methanol;overnight, rt2.3Reagents:p-Toluenesulfonic acidSolvents:Acetone;overnight, rt3.1Reagents:Trimethyl phosphate;0 °C; 3 h, 0 °C3.2Reagents:Water;overnight, rt
Selpercatinib, also known as LOXO-292, is a potent and selective RET inhibitor with antineoplastic properties. LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion p...
Process for the preparation of 6-(2-hydroxy-2-methylpropoxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile and intermediates thereofBy: AnonymousIP.com Journal (2021), 21(2B), 1-10
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