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Vorasidenib CAS# 1644545-52-7 PVM/MA共聚物
Vorasidenib, also known as AG-881, is a potent and selective orally available inhibitor of mutated forms of both isocitrate dehydrogenase type 1 (IDH1, IDH1 [NADP+] soluble) in the cytoplasm and type ...
Vorasidenib (AG-881): A First-in-Class, Brain-Penetrant Dual Inhibitor of Mutant IDH1 and 2 for Treatment of GliomaBy: Konteatis, Zenon; et alACS Medicinal Chemistry Letters (2020), 11(2), 101-107
Iptacopan CAS# 1644670-37-0
Iptacopan, also known as LNP023, is a complement Factor B Inhibitor (IC50=10 nM). LNP023 improves LN in MRL/lpr mice. The mechanism is as follows: LNP023 binds to CFB to inhibit the activation of the ...
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated DiseasesBy: Mainolfi, Nello; et alJournal of Medicinal Chemistry (2020), 63(11), 5697-5722
Efinaconazole CAS# 164650-44-6 艾氟康唑
Efinaconazole is a triazole antifungal. It is approved for use in Canada and the USA as a 10% topical solution for the treatment of onychomycosis (fungal infection of the nail). Efinaconazole acts as ...
Tamura, Keiji; Kumagai, Naoya; Shibasaki, Masakatsu. An Enantioselective Synthesis of the Key Intermediate for Triazole Antifungal Agents; Application to the Catalytic Asymmetric Synthesis of Efinaconazole (Jublia). ournal of Organic Chemistry. Volume 79. Issue 7. Pages 3272-3278. Journal; Online Computer File. (2014).
Bendamustine CAS# 16506-27-7 宾达氮芥
Bendamustine is a bifunctional mechlorethamine derivative with alkylator and antimetabolite activities. Bendamustine possesses three active moieties: an alkylating group; a benzimidazole ring, which m...
Shrawat, Vimal Kumar; Purohit, Prashant; Singh, Vinod Kumar; Unnam, Seshachalam. Process for preparing bendamustine hydrochloride monohydrate. Assignee Shilpa Medicare Limited, India. IN 2010CH03261 (2012).
Anidulafungin CAS# 166663-25-8 阿尼芬净
Anidulafungin, also known as LY303366, is a semisynthetic echinocandin used as an antifungal drug. Anidulafungin was approved on 2/21/2006. Anidulafungin has proven efficacy against esophageal candidi...
Norris, Timothy; VanAlsten, John; Hubbs, Stephen; Ewing, Marcus; Cai, Weiling; Jorgensen, Matthew L.; Bordner, Jon; Jensen, Grace O. Commercialization and Late-Stage Development of a Semisynthetic Antifungal API: Anidulafungin/D-Fructose (Eraxis). Organic Process Research & Development. Volume 12. Issue 3. Pages 447-455. 2008.
Clevidipine CAS# 167221-71-8 丁酸氯维地平
Clevidipine is a dihydropyridine L-type calcium channel blocker, highly selective for vascular, as opposed to myocardial, smooth muscle and, therefore, has little or no effect on myocardial contractil...
Sun, Hua-jun; Huang, Lu; Yang, Shang-jin Xiandai Yaowu Yu Linchuang Volume 26 Issue 1 Pages 40-42 Journal 2011
Belzutifan CAS# 1672668-24-4 3-[[(1S,2S,3R)-2,3-二氟-2,3-二氢-1-羟基-7-(甲基磺酰基)-1H-茚-4-基]氧基]-5-氟苄腈
Belzutifan (MK-6482, PT2977) is a selective, orally bioavailable inhibitor of hypoxia-inducible factor-2α (HIF-2α). In preclinical studies, belzutifan bound HIF-2α with high affinity (Kd ~50 nM) and d...
Reference: Enantio- and Diastereoselective Total Synthesis of Belzutifan Enabled by Rh-Catalyzed HydrogenationBy: Le, Diane N., Johnson, Heather C., Lam, Yu-hong, Sun, Chunrui, Cheng, Lili,Belyk, Kevin M.Organic Letters (2024), 26(19), 4059-4064
Flibanserin CAS# 167933-07-5 氟立班丝氨
Flibanserin is a full agonist of the 5-HT1A receptor (Ki = 1 nM) and, with lower affinity, as an antagonist of the 5-HT2A receptor (Ki = 49 nM) and antagonist or very weak partial agonist of the D4 re...
Reference: Yang, Feipu & Wu, Chunhui & Li, Zhiqiang & Tian, Guanghui & Wu, Jianzhong & He, Yang & Shen, Jingshan. (2016). A Facile Route of Synthesis for Making Flibanserin. Organic Process Research & Development. 20. 10.1021/acs.oprd.6b00108.
Conivaptan Hydrochloride CAS# 168626-94-6 盐酸考尼伐坦
Conivaptan hydrochloride is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist).
Tsunoda, Takashi; Yamazaki, Atsuki; Iwamoto, Hidenori; Sakamoto, Shuichi. Practical Synthesis of N-{4-[(2-Methyl-4,5-dihydroimidazo[4,5-d][1]benzazepin-6(1H)-yl)carbonyl]phenyl}biphenyl-2-carboxamide Monohydrochloride: an Arginine Vasopressin Antagonist. Organic Process Research & Development. Chemical Technology Labs. Yamanouchi Pharmaceutical Co., Ltd. Takahagi-shi, Ibaraki, Japan 318-0001. Volume 7. Issue 6. Pages 883-887. 2003
Zanubrutinib CAS# 1691249-45-2 扎努布鲁替尼
Zanubrutinib (BGB-3111) is a potent, selective, and irreversible Bruton's tyrosine kinase (BTK) inhibitor with demonstrated efficacy both in vitro and in vivo. In vitro, it effectively inhibits BTK ac...
Highly Enantioselective Ir-catalyzed Hydrogenation of Pyrazolo[1,5-a]pyrimidine for the Synthesis of ZanubrutinibBy: Yuan, Haohuan; et alJournal of Organic Chemistry (2024), 89(3), 1748-1752
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