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Ponesimod CAS# 854107-55-4 珀奈莫德
Ponesimod (ACT-128800) is a selective, orally active sphingosine-1-phosphate receptor 1 (S1P₁) modulator. In preclinical studies, it bound human S1P₁ with high affinity (Ki ~2.5 nM) and showed >10,000...
2-Imino-thiazolidin-4-one Derivatives as Potent, Orally Active S1P1Receptor AgonistsBy: Bolli, Martin H.; et alJournal of Medicinal Chemistry (2010), 53(10), 4198-4211
Azilsartan medoxomil CAS# 863031-21-4 阿齐沙坦奥美沙坦酯
Azilsartan medoxomil also known as TAK-491, is an orally administered angiotensin II receptor type 1 antagonist (blocker) used in the treatment of adults with essential hypertension. Azilsartan medoxo...
Garaga, Srinivas; Misra, Nimesh C.; Raghava Reddy, Ambati V.; Prabahar, Koilpillai Joseph; Takshinamoorthy, Chandiran; Sanasi, Paul Douglas; Babu, Korupolu Raghu. Commercial Synthesis of Azilsartan Kamedoxomil: An Angiotensin II Receptor Blocker. Organic Process Research & Development. Volume 19. Issue 4. Pages 514-519. Journal; Online Computer File. (2015).
Dasatinib CAS# 863127-77-9 达沙替尼(一水合物)
Dasatinib, also known as BMS-354825, is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activitie...
Balaji, N.; Sultana, Sayeeda. Trace level determination and quantification of potential genotoxic impurities in dasatinib drug substance by UHPLC/infinity LC. International Journal of Pharmacy and Pharmaceutical Sciences. Department of Chemistry. St. Peter's University. Tamil Nadu, India 600054. Volume 8. Issue 10. Pages 209-216. 2016
Flurpiridaz-nonradiolabeled CAS# 863888-33-9 2-叔丁基-4-氯-5-[[4-(2-氟乙氧基甲基)苯基]甲氧基]哒嗪-3-酮
Flurpiridaz (also known as ¹⁸F-flurpiridaz) is a radiolabeled myocardial perfusion imaging agent targeting mitochondrial complex I.. ¹⁸F-Flurpiridaz demonstrated high affinity for mitochondrial comple...
Synthesis and Biological Evaluation of Pyridazinone Analogues as Potential Cardiac Positron Emission Tomography TracersBy: Purohit, Ajay; et alJournal of Medicinal Chemistry (2008), 51(10), 2954-2970
Revefenacin CAS# 864750-70-9 瑞维那新
Revefenacin, also known as TD-4208; GSK-1160724, is a long-acting muscarinic receptor antagonist and may be potentially useful for the treatment of respiratory disease.
Reference: Colson, Pierre-Jean. Process for preparing a biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl) benzoyl]methylamino}ethyl)piperidin-4-yl ester. Assignee Theravance, Inc., USA. WO 2012009166. (2012).
Fostemsavir CAS# 864953-29-7
Fostemsavir is an oral prodrug of temsavir, a first-in-class HIV-1 attachment inhibitor that selectively binds to the viral envelope glycoprotein gp120. In vitro, it prevents conformational changes re...
Wang T, Ueda Y, Zhang ZX, et al. Discovery of the Human Immunodeficiency Virus Type 1 (HIV-1) Attachment Inhibitor Temsavir and Its Phosphonooxymethyl Prodrug Fostemsavir.J. Med. Chem 2018, 61(14):6308-6327
Belinostat CAS# 866323-14-0 贝利司他
Belinostat is a novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apo...
Bao, Xuefei; Song, Dake; Qiao, Xuejun; Zhao, Xuan; Chen, Guoliang. The development of an effective synthetic route of belinostat. Organic Process Research & Development. Volume 20. Issue 8. Pages 1482-1488. Journal; Online Computer File. (2016).
Carfilzomib CAS# 868540-17-4 卡非佐米
Carfilzomib, also known as PR-171, is a tetrapeptide epoxyketone and an epoxomicin derivate with potential antineoplastic activity. Carfilzomib irreversibly binds to and inhibits the chymotrypsin-like...
Screen, Michael; Britton, Matthew; Downey, Sondra L.; Verdoes, Martijn; Voges, Mathias J.; Blom, Annet E. M.; Geurink, Paul P.; Risseeuw, Martijn D. P.; Florea, Bogdan I.; van der Linden, Wouter A.; Pletnev, Alexandre A.; Overkleeft, Herman S.; Kisselev, Alexei F. Nature of Pharmacophore Influences Active Site Specificity of Proteasome Inhibitors. Journal of Biological Chemistry. Volume 285. Issue 51. Pages 40125-40134. Journal. (2010).
Tecovirimat CAS# 869572-92-9
Tecovirimat was discontinued
Reference: Dong, Ming-xin; Li, Hai-tao; Wang, Xiao-hua; Mao, Wen-xiang; Zhou, Shang-min; Dai, Qiu-yun. Preparation and structural determination of tecovirimat monohydrate crystal. Zhongguo Xinyao Zazhi. Volume 21. Issue 23. Pages 2736-2739. (2012).
Infigratinib CAS# 872511-34-7 FGFR抑制剂(NVP-BGJ398)
Infigratinib is a selective, oral small-molecule inhibitor of fibroblast growth factor receptors (FGFR) 1–3, designed to block aberrant FGFR signaling implicated in tumor growth and survival. In vitro...
Discovery of 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), A Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine KinaseBy: Guagnano, Vito; et alJournal of Medicinal Chemistry (2011), 54(20), 7066-7083
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