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Rucaparib is a tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Rucaparib selectively binds to PARP1 and...
Reference: Belogi, Gianluca; Mazzoni, Andrea; Serra, Stefano; Novo, Barbara. Preparation of high-purity rucaparib via palladium-catalyzed regioselective coupling of a 4-alkoxycarbonyl-6-fluoroindole and an alkyl [(4-iodophenyl)methyl]methylcarbamate. WO 2019020508. (Olon S.p.A., Italy)
Fesoterodine is an antimuscarinic drug developed to treat overactive bladder syndrome (OAB). It was approved by the European Medicines Agency in April 2007, the US Food and Drug Administration on Octo...
Process for the preparation of fesoterodine fumarate; Dwivedi, Shriprakash Dhar; Prasad, Ashok; Jain, Kuldeep Natwarlal; Assignee Cadila Healthcare Limited, India; 2013; Patent Information; Sep 06, 2013; IN 2010MU02373; A
Treosulfan, a bifunctional alkylating agent and prodrug of a diepoxybutane derivative, shows potent cytotoxicity in vitro across various tumor cell lines. In leukemia and lymphoma cell models (e.g., H...
Chiroptical properties of 2,2'-bioxiraneBy: Daugey, N.; et alChirality (2018), 30(4), 342-350
Polidocanol is a local anaesthetic and antipruritic component of ointments and bath additives. It relieves itching caused by eczema and dry skin. It is formed by the ethoxylation of dodecanol. The sub...
Yu, Zeqiong; Bo, Shaowei; Wang, Huiyuan; Li, Yu; Yang, Zhigang; Huang, Yongzhuo; Jiang, Zhong-Xing. Application of Monodisperse PEGs in Pharmaceutics: Monodisperse Polidocanols. Molecular Pharmaceutics. Volume 14. Issue 10. Pages 3473-3479. 2017.
Deferiprone is a drug that chelates iron and is used to treat thalassaemia major. In 1994 was first approved for use in treating thalassaemia major in 1994 and had been licensed for use in Europe and ...
Dobbin, Paul S.; Hider, Robert C.; Hall, Adrian D.; Taylor, Paul D.; Sarpong, Patience; Porter, John B.; Xiao, Gaoyi; van der Helm, Dick. Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential. Journal of Medicinal Chemistry. Volume 36. Issue 17. Pages 2448-58. Journal. (1993).
Lofexidine reduces narcotic withdrawal symptoms.
Reference: Vartak, Ashish P.; Crooks, Peter A. A Scalable, Enantioselective Synthesis of the α2-Adrenergic Agonist, Lofexidine. Organic Process Research & Development. Volume 13. Issue 3. Pages 415-419. Journal. (2009).
Regadenoson is an A2A adenosine receptor agonist that is a coronary vasodilator that is commonly used in pharmacologic stress testing. It produces hyperemia quickly and maintains it for a duration tha...
Gao, Xihui; Qian, Jun; Zheng, Shuyan; Changyi, Yinzhi; Zhang, Jianping; Ju, Shenghong; Zhu, Jianhua; Li, Cong. Overcoming the Blood-Brain Barrier for Delivering Drugs into the Brain by Using Adenosine Receptor Nanoagonist. ACS Nano. Volume 8. Issue 4. Pages 3678-3689. 2014.
ITI-722 is a first-in-class dual 5HT2A receptor antagonist and dopamine receptor phosphoprotein modulator (DPPM).
Li, Peng; Zhang, Qiang; Robichaud, Albert J.; Lee, Taekyu; Tomesch, John; Yao, Wei; Beard, J. David; Snyder, Gretchen L.; Zhu, Hongwen; Peng, Youyi; Hendrick, Joseph P.; Vanover, Kimberly E.; Davis, Robert E.; Mates, Sharon; Wennogle, Lawrence P. Discovery of a Tetracyclic Quinoxaline Derivative as a Potent and Orally Active Multifunctional Drug Candidate for the Treatment of Neuropsychiatric and Neurological Disorders. Journal of Medicinal Chemistry. Intra-Cellular Therapies, Inc. New York, USA 10032Volume 57. Issue 6. Pages 2670-2682. 2014.
Axitinib, also known as AG013736, is an orally bioavailable tyrosine kinase inhibitor. Axitinib inhibits the proangiogenic cytokines vascular endothelial growth factor (VEGF) and platelet-derived grow...
Zhai, Li-Hai; Guo, Li-Hong; Luo, Yang-Hui; Ling, Yang; Sun, Bai-Wang. Effective Laboratory-Scale Preparation of Axitinib by Two CuI-Catalyzed Coupling Reactions. Organic Process Research & Development. Volume 19. Issue 7. Pages 849-857. Journal; Online Computer File. (2015).
Aclidinium bromide is a long-acting anticholinergic bronchodilator approved by the FDA in 2012 for use in the management of chronic obstructive pulmonary disease (COPD) which includes chronic bronchit...
Prat, Maria; Fernandez, Dolors; Buil, M. Antonia; Crespo, Maria I.; Casals, Gaspar; Ferrer, Manuel; Tort, Laia; Castro, Jordi; Monleon, Juan M.; Gavalda, Amadeu; Miralpeix, Montserrat; Ramos, Israel; Domenech, Teresa; Vilella, Dolors; Anton, Francisca; Huerta, Josep M.; Espinosa, Sonia; Lopez, Manuel; Sentellas, Sonia; Gonzalez, Marisa; Alberti, Joan; Segarra, Victor; Cardenas, Alvaro; Beleta, Jorge; Ryder, Hamish. Discovery of Novel Quaternary Ammonium Derivatives of (3R)-Quinuclidinol Esters as Potent and Long-Acting Muscarinic Antagonists with Potential for Minimal Systemic Exposure after Inhaled Administration: Identification of (3R)-3-{[Hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane Bromide (Aclidinium Bromide). Journal of Medicinal Chemistry. Volume 52. Issue 16. Pages 5076-5092. Journal. (2009).
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