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Bortezomib CAS# 179324-69-7 硼替佐米
Bortezomib is a dipeptide boronic acid analogue with antineoplastic activity. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blockin...
Peuchmaur, Marine; Lacour, Marie-Agnes; Sevalle, Jean; Lisowski, Vincent; Touati-Jallabe, Youness; Rodier, Fabien; Martinez, Jean; Checler, Frederic; Hernandez, Jean-Francois. Further characterization of a putative serine protease contributing to the γ-secretase cleavage of β-amyloid precursor protein. Bioorganic & Medicinal Chemistry. Institut des Biomolecules Max Mousseron, UMR5247 CNRS, Faculte de Pharmacie. Universites Montpellier 1 and 2. Montpellier, Fr. 34093. Volume 21. Issue 4. Pages 1018-1029. 2013
Caspofungin Acetate CAS# 179463-17-3 醋酸卡泊芬净
Caspofungin acetate is a lipopeptide antifungal drug. It is a member of a new class of antifungals termed the echinocandins. It works by inhibiting the enzyme (1→3)-β-D-glucan synthase and thereby dis...
Leonard, William R., Jr.; Belyk, Kevin M.; Conlon, David A.; Bender, Dean R.; DiMichele, Lisa M.; Liu, Ji; Hughes, David L. Synthesis of the Antifungal β-1,3-Glucan Synthase Inhibitor CANCIDAS (Caspofungin Acetate) from Pneumocandin B0. Journal of Organic Chemistry. Process Research Department. Merck Research Laboratories. Rahway, USA 07065-0900. Volume 72. Issue 7. Pages 2335-2343. 2007
Prucalopride CAS# 179474-81-8 普芦卡必利
Prucalopride is a 5-HT4R agonist.
Reference: Yuan, Youzhi; Tang, Jiadeng; Cen, Junda. Synthesis of Prucalopride monosuccinate. Zhongguo Yiyao Gongye Zazhi. Volume 43. Issue 1. Pages 5-8. Journal. (2012).
Brensocatib CAS# 1802148-05-5
Brensocatib is a selective, orally active inhibitor of dipeptidyl peptidase-1 (DPP1), the enzyme responsible for activating neutrophil serine proteases. In preclinical biochemical assays, it inhibited...
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986)By: Doyle, Kevin; et alJournal of Medicinal Chemistry (2016), 59(20), 9457-9472
Repotrectinib CAS# 1802220-02-5
Repotrectinib (TPX-0005) is a compact, next-generation tyrosine kinase inhibitor targeting ROS1, ALK, and TRK with sub-nanomolar potency (IC₅₀ ~0.3–2.0 nM across ROS1/ALK/TRK) and broad activity again...
Preparation of fluorodimethyltetrahydroethenopyrazolobenzoxatriazacyclotridecinone derivatives for use as antitumor agentsAssignee: TP Therapeutics, Inc.Inventors: Cui, Jingrong J.; et alWorld Intellectual Property OrganizationPatent#WO2017007759 A1
Berotralstat CAS# 1809010-50-1 催乳药
Berotralstat (BCX7353) is a potent, selective, orally bioavailable small-molecule inhibitor of plasma kallikrein. In preclinical assays, it showed nanomolar potency (Ki ~1.0 nM) and effectively blocke...
Berotralstat (BCX7353): Structure-Guided Design of a Potent, Selective, and Oral Plasma Kallikrein Inhibitor to Prevent Attacks of Hereditary Angioedema (HAE)By: Kotian, Pravin L.; et alJournal of Medicinal Chemistry (2021), 64(17), 12453-12468
Remdesivir CAS# 1809249-37-3 瑞德西韦
Remdesivir (GS-5734) is a monophosphoramidate prodrug of an adenosine analog that inhibits viral RNA-dependent RNA polymerase. In preclinical assays, its active metabolite (GS-441524 triphosphate) sho...
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging VirusesBy: Siegel, Dustin; et alJournal of Medicinal Chemistry (2017), 60(5), 1648-1661
Almotriptan Malate CAS# 181183-52-8 依来曲普坦
Almotriptan Malate is a triptan drug discovered and developed by Almirall for the treatment of heavy migraine headache. Almotriptan is a Serotonin-1b and Serotonin-1d Receptor Agonist. Binding of the ...
Chen, Dongsheng; Chen, Yuanyuan; Ma, Zhilong; Zou, Lei; Li, Jianqi; Liu, Yu. One-Pot Synthesis of Indole-3-acetic Acid Derivatives through the Cascade Tsuji-Trost Reaction and Heck Coupling. Journal of Organic Chemistry. Volume 83. Issue 12. Pages 6805-6814. 2018.
Cabazitaxel CAS# 183133-96-2 卡巴他赛
Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity. Cabazitaxel binds to and stabilizes tubulin, resulting in the inhibitio...
Jing, Yun-rong; Zhou, Wei; Li, Wan-liang; Zhao, Lin-xiang; Wang, Yong-feng; Bioorganic & Medicinal Chemistry, Volume 22, Issue 1, Pages 194-203, Journal, 2014
Tipiracil HCl CAS# 183204-74-2 替吡嘧啶杂质
Tipiralacil, also known as TPI, is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials. ...
Ref: Maheta, Abhay Subodhbhai; Kaneria, Ankur Amrutlal; Bhesaniya, Kapil Dhanjibhai; Savaliya, Bhavesh Laljibhai; Koilpillai, Joseph Prabahar; Agarwal, Virendra Kumar; Chavan, Rahul Baburao; Arabiani, Mohsin Razakbhai; Hedapara, Kalpesh Ratilal; Katariya, Lalit Keshav; Patel, Vijay Premajibhai; Thummar, Mahesh Kurajibhai; Bhalodiya, Rahul Harsukhlal. Process for the preparation of tipiracil hydrochloride (Assignee Amneal Pharmaceuticals Company GmbH, Switz.). WO 2019002407 (2019).
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