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Adefovir dipivoxil (trade names Preveon and Hepsera) is an antiviral acyclic nucleoside phosphonate (ANP) analog. It is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibito...
Roux, Loic; Priet, Stephane; Payrot, Nadine; Weck, Clement; Fournier, Maelenn; Zoulim, Fabien; Balzarini, Jan; Canard, Bruno; Alvarez, Karine. Ester prodrugs of acyclic nucleoside thiophosphonates compared to phosphonates: Synthesis, antiviral activity and decomposition study. European Journal of Medicinal Chemistry. Volume 63. Pages 869-881. 2013.
Nerandomilast, also known as BI-1015550, is a potent PDE4 inhibitor that displays anti-inflammatory activity. BI 1015550 shows a preferential enzymatic inhibition of PDE4B. In vitro, BI 1015550 inhibi...
Development of a Scalable Asymmetric Process for the Synthesis of Selective PDE4B Inhibitor Nerandomilast (BI 1015550)By: Frutos, Rogelio P.; et alOrganic Process Research & Development (2024), 28(9), 3745-3751
Piflufolastat F19 (DCFPyL, non-radioactive analog of ^18F-DCFPyL) is a high-affinity ligand for prostate-specific membrane antigen (PSMA) used to characterize binding and pharmacologic properties inde...
18F-LABELED PEPTIDE LIGANDS USEFUL IN PET AND CERENKOV LUMINESCENCE IMAGINGAssignee: Cornell UniversityInventor: Babich, John W.World Intellectual Property OrganizationPatent#WO2019126497
Febuxostat, also known as Uloric and TMX-67, is a xanthine oxidase inhibitor used to treat_x000D_ hyperuricemia and chronic gout.
Process for the preparation of febuxostat and salts thereof; Birari, Dilip Ramdas; Rao, Dharmaraj Ramachandra; Kankan, Rajendra Narayanrao; Assignee Cipla Limited, India; Curtis, Philip Anthony 2011; Patent Information; Jun 23, 2011; WO 2011073617 A1
Voxelotor, also known as GBT-440, is a hemoglobin S allosteric modulator. GBT440 Inhibits Sickling of Sickle Cell Trait Blood Under In Vitro Conditions Mimicking Strenuous Exercise. GBT440 increases h...
Reference: Metcalf, Brian; Chuang, Chihyuan; Dufu, Kobina; Patel, Mira P.; Silva-Garcia, Abel; Johnson, Carl; Lu, Qing; Partridge, James R.; Patskovska, Larysa; Patskovsky, Yury; Almo, Steven C.; Jacobson, Matthew P.; Hua, Lan; Xu, Qing; Gwaltney, Stephen L.; Yee, Calvin; Harris, Jason, Morgan, Bradley P.; James, Joyce; Xu, Donghong; Hutchaleelaha, Athiwat; Paulvannan, Kumar; Oksenberg, Donna; Li, Zhe. Discovery of GBT440, an Orally Bioavailable R-State Stabilizer of Sickle Cell Hemoglobin. ACS Medicinal Chemistry Letters. Volume 8. Issue 3. Pages 321-326. Journal; Online Computer File. (2017).
Acoramidis (AG10) is a potent, selective, orally bioavailable stabilizer of transthyretin (TTR). In preclinical biochemical assays, it bound TTR with high affinity (Kd₁ ~5 nM) and prevented dissociati...
AG10 inhibits amyloidogenesis and cellular toxicity of the familial amyloid cardiomyopathy-associated V122I transthyretinBy: Penchala, Sravan C.; et alProceedings of the National Academy of Sciences of the United States of America (2013), 110(24), 9992-9997, S9992/1-S9992/23
Futibatinib, also known as TAS-120 is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor TAS-120 selectively and ir...
This synthetic route was from WO2015008844
Ivosidenib, also known as AG-120 and RG-120, is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a muta...
Reference: Popovici-Muller, Janeta; Lemieux, Rene M.; Artin, Erin; Saunders, Jeffrey O.; Salituro, Francesco G.; Travins, Jeremy; Cianchetta, Giovanni; Cai, Zhenwei; Zhou, Ding; Cui, Dawei; Chen, Ping; Straley, Kimberly; Tobin, Erica; Wang, Fang; David, Muriel D.; Penard-Lacronique, Virginie; Quivoron, Cyril; Saada, Veronique; de Botton, Stephane; Gross, Stefan; Dang, Lenny; Yang, Hua; Utley, Luke; Chen, Yue; Kim, Hyeryun; Jin, Shengfang; Gu, Zhiwei; Yao, Gui; Luo, Zhiyong; Lv, Xiaobing; Fang, Cheng; Yan, Liping; Olaharski, Andrew; Silverman, Lee; Biller, Scott; Su, Shin-San M.; Yen, Katharine. Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers. ACS Medicinal Chemistry Letters. Volume 9. Issue 4. Pages 300-305. Journal; Online Computer File. (2018).
Loratinib, also known as PF-06463922, is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential a...
Reference: Johnson, Ted W.; Richardson, Paul F.; Bailey, Simon; Brooun, Alexei; Burke, Benjamin J.; Collins, Michael R.; Cui, J. Jean; Deal, Judith G.; Deng, Ya-Li; Dinh, Dac; Engstrom, Lars D.; He, Mingying; Hoffman, Jacqui; Hoffman, Robert L.; Huang, Qinhua; Kania, Robert S.; Kath, John C.; Lam, Hieu; Lam, Justine L.; Le, Phuong T.; Lingardo, Laura; Liu, Wei; McTigue, Michele; Palmer, Cynthia L.; Sach, Neal W.; Smeal, Tod; Smith, Graham L.; Stewart, Albert E.; Timofeevski, Sergei; Zhu, Huichun; Zhu, Jinjiang; Zou, Helen Y.; Edwards, Martin P. Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations. Journal of Medicinal Chemistry. Volume 57. Issue 11. Pages 4720-4744. Journal; Online Computer File. (2014).
Cetrorelix acetate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity used in infertility treatment.
Lu, Zhixian; Chen, Weiguang; Zheng, Fanna; Yang, Hui; Ding, Yanwei. Process for preparation of cetrorelix acetate by solid phase peptide synthesis method. Assignee Qingdao Beitaike Biotechnology Co., Ltd., Peop. Rep. China. CN 104277093. 2015
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