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Venetoclax CAS# 1257044-40-8 维纳妥拉(ABT-199)
Venetoclax, also known as ABT-199 or GDC0199, is an orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. Venetoclax mimi...
Reference: Ku, Yi-Yin; Chan, Vincent S.; Christesen, Alan; Grieme, Timothy; Mulhern, Mathew; Pu, Yu-Ming; Wendt, Michael D. Development of a Convergent Large-Scale Synthesis for Venetoclax, a First-in-Class BCL-2 Selective Inhibitor. Journal of Organic Chemistry. Volume 84. Issue 8. Pages 4814-4829. Journal; Online Computer File. (2019).
Mitapivat CAS# 1260075-17-9 PKR抑制剂(MITAPIVAT)
Mitapivat (AG-348) is an oral, allosteric activator of red blood cell pyruvate kinase (PKR). In preclinical biochemical assays, it increased PKR activity with an EC50 of ~0.5 µM and stabilized the tet...
An Improved and commercially viable process for preparationof N-[4-[[4-(cyclopropylmethyl)-1-piperazinyl]carbonyl]phenyl]-8-quinolinesulfonamide and its intermediatesIP.com Journal (2023), 23(3A), 1-8
Delgocitinib CAS# 1263774-59-9 迪高替尼
Delgocitinib is a pan-JAK inhibitor targeting JAK1, JAK2, JAK3, and TYK2 with nanomolar potency (IC₅₀ values generally 2–30 nM across isoforms). In cellular assays, it suppressed cytokine-induced STAT...
Stereocontrolled Synthesis of Delgocitinib, a JAK Inhibitor for the Treatment of Atopic DermatitisBy: Takiguchi, Hiromu ; et alOrganic Process Research & Development (2021), 25(2), 342-348
Ciclesonide CAS# 126544-47-6 环索奈德
Ciclesonide is an inhaled corticosteroids, used to ameliorate symptoms of airway inflammatory diseases, such as asthma, allergic rhinitis, and chronic obstructive pulmonary disease. Ciclesonide is a c...
Chen, Yingjiang; Ding, Yan; Wang, Erhua. Synthesis of ciclesonide. Huagong Shikan. Medicinal Chemical Engineering Institute. China Pharmaceutical University. Nanjing, Peop. Rep. China 210009. Volume 20. Issue 5. Pages 30-32. 2006
Acoziborole CAS# 1266084-51-8 4-氟-N-(1-羟基-3,3-二甲基-1,3-二氢苯并[C][1,2]噁硼戊环-6-基)-2-(三氟甲基)苯甲酰胺
Acoziborole, also known as SCYX-7158 is an orally-active compound with potent antitrypanosoma activity for the potent treatment of stage 2 human African trypanosomiasis. Human African trypanosomiasis ...
Benzoxaboroles: a new class of potential drugs for human African trypanosomiasisBy: Jacobs, Robert T.; et alFuture Medicinal Chemistry (2011), 3(10), 1259-1278
Encorafenib CAS# 1269440-17-6 康奈非尼
Encorafenib, also known as LGX-818, is an orally available Raf kinase inhibitor with potential antineoplastic activity. LGX818 specifically inhibits Raf kinase, a serine/threonine enzyme in the RAF/mi...
Reference: Huang, Shenlin; Jin, Xianming; Liu, Zuosheng; Poon, Daniel; Tellew, John; Wan, Yongqin; Wang, Xing; Xie, Yongping. Preparation of sulfonamidophenylimidazolylpyrimidine derivatives and analogs for use as protein kinase inhibitors. Assignee IRM LLC, Bermuda; Novartis A.-G. WO 2011025927. (2011).
Bivalirudin CAS# 128270-60-0 比伐卢定
Bivalirudin, also known as BG-8967, is a specific and reversible direct thrombin inhibitor (DTI). Chemically, it is a synthetic congener of the naturally occurring drug hirudin (found in the saliva of...
Okada, Yohei; Suzuki, Hideaki; Nakae, Takashi; Fujita, Shuji; Abe, Hitoshi; Nagano, Kazuo; Yamada, Toshihide; Ebata, Nobuyoshi; Kim, Shokaku; Chiba, Kazuhiro. Tag-assisted liquid-phase peptide synthesis using hydrophobic benzyl alcohols as supports. Journal of Organic Chemistry. Department of Applied Biological Science. Tokyo University of Agriculture and Technology. 3-5-8 Saiwai-cho, Fuchu, Tokyo, Japan 183-8509. Volume 78. Issue 2. Pages 320-327. 2013
Romidepsin CAS# 128517-07-7 罗米地辛
Romidepsin, also known as FK228; is a bicyclic depsipeptide antibiotic isolated from the bacterium Chromobacterium violaceum with antineoplastic activity. After intracellular activation, romidepsin bi...
Li, Khan W.; Wu, Jerry; Xing, Wenning; Simon, Julian A. Total Synthesis of the Antitumor Depsipeptide FR-901,228. Journal of the American Chemical Society. Volume 118. Issue 30. Pages 7237-7238. 1996.
Rimegepant CAS# 1289023-67-1
Rimegepant (BMS-927711) is a potent, orally bioavailable small-molecule antagonist of the calcitonin gene–related peptide (CGRP) receptor. In preclinical binding assays, it inhibited human CGRP recept...
Discovery of (5S,6S,9R)-5-Amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): An Oral Calcitonin Gene-Related Peptide (CGRP) Antagonist in Clinical Trials for Treating MigraineBy: Luo, Guanglin; et alJournal of Medicinal Chemistry (2012), 55(23), 10644-10651
Nirogacestat CAS# 1290543-63-3
Nirogacestat (PF-03084014) is a potent, selective, orally bioavailable γ-secretase inhibitor that blocks Notch receptor activation. In in vitro assays, Nirogacestat inhibits Notch signaling with an IC...
Bioorganic & Medicinal Chemistry Letters (2011), 21(9), 2637-2640
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