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Ceritinib CAS# 1032900-25-6 色瑞替尼
Ceritinib, also known as LDK378, is a selective inhibitor of ALK1, a target found in metastatic non-small cell lung cancer (NSCLC). In Phase I trials, LDK378 showed a marked clinical response in 78 pa...
Marsilje, Thomas H.; Pei, Wei; Chen, Bei; Lu, Wenshuo; Uno, Tetsuo; Jin, Yunho; Jiang, Tao; Kim, Sungjoon; Li, Nanxin; Warmuth, Markus; Sarkisova, Yelena; Sun, Frank; Steffy, Auzon; Pferdekamper, AnneMarie C.; Li, Allen G.; Joseph, Sean B.; Kim, Young; Liu, Bo; Tuntland, Tove; Cui, Xiaoming; Gray, Nathanael S.; Steensma, Ruo; Wan, Yongqin; Jiang, Jiqing; Chopiuk, Greg; Li, Jie; Gordon, W. Perry; Richmond, Wendy; Johnson, Kevin; Chang, Jonathan; Groessl, Todd; He, You-Qun; Phimister, Andrew; Aycinena, Alex; Lee, Christian C.; Bursulaya, Badry; Karanewsky, Donald S.; Seidel, H. Martin; Harris, Jennifer L.; Michellys, Pierre-Yves. Synthesis, Structure-Activity Relationships, and in Vivo Efficacy of the Novel Potent and Selective Anaplastic Lymphoma Kinase (ALK) Inhibitor 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) Currently in Phase 1 and Phase 2 Clinical Trials. Journal of Medicinal Chemistry. Volume 56. Issue 14. Pages 5675-5690. Journal; Online Computer File. (2013).
Telotristat ethyl CAS# 1033805-22-9 特罗司他乙酯
Telotristat ethyl, also known as LX 1032 or LX 1606, is an oral serotonin synthesis inhibitor or peripheral tryptophan hydroxylase (TPH) inhibitor . Telotristat etiprate has activity in controlling di...
Reference: Sands, Arthur Thomas. Preparation of multicyclic amino acid derivations as potent and selective THP1 inhibitors for treating metastatic bone disease. WO 2011100285. (Lexicon Pharmaceuticals, Inc., USA)
Sarecycline CAS# 1035654-66-0 沙茶碱
Sarecycline, also known as WC-3035 and P005672, is a novel, tetracycline-derived, narrow-spectrum antibiotic being developed for use as an oral once daily antibiotic treatment for patients suffering f...
Reference: Assefa, Haregewin; Bhatia, Beena; Draper, Michael; Honeyman, Laura; Molnar, Dennis P.; Kim, Oak K. Preparation of substituted tetracycline compounds for treatment of inflammatory skin disorders. Assignee Paratek Pharmaceuticals, Inc., USA. CA 2892739. (2008).
Niraparib CAS# 1038915-60-4 尼拉帕尼
Niraparib, also known as MK4827, is an orally active, potent and selective poly(ADP-Ribose) polymerase (PARP) inhibitor that radiosensitizes human lung and breast cancer cells. Niraparib inhibits PARP...
Reference: Jones, Philip; Ontoria Ontoria, Jesus Maria; Scarpelli, Rita; Schultz-Fademrecht, Carsten. Preparation of piperidinylphenylindazolylcarboxamide for use as poly(ADP-ribose)polymerase inhibitors. WO 2008084261. (Assignee Istituto Di Ricerche Di Biologia Molecolare P. Angeletti SpA, Italy)
Finerenone CAS# 1050477-31-0 (4S)-4-(4-氰基-2-甲氧基苯基)-5-乙氧基-1,4-二氢-2,8-二甲基-1,6-萘啶-3-甲酰胺(非奈利酮杂质)
Finerenone (BAY 94-8862) is a novel, selective non-steroidal mineralocorticoid receptor (MR) antagonist. In preclinical studies, it bound the MR with high affinity (Ki ~18 nM) and demonstrated greater...
Discovery of BAY 94-8862: A Nonsteroidal Antagonist of the Mineralocorticoid Receptor for the Treatment of Cardiorenal DiseasesBy: Baerfacker, Lars; et alChemMedChem (2012), 7(8), 1385-1403
Cabotegravir CAS# 1051375-10-0 卡替拉韦
Cabotegravir is a potent HIV-1 integrase strand transfer inhibitor (INSTI) that demonstrates strong in vitro activity, blocking viral DNA integration into host genomes at nanomolar concentrations with...
7-Step Flow Synthesis of the HIV Integrase Inhibitor DolutegravirBy: Ziegler, Robert E.; et alAngewandte Chemie, International Edition (2018), 57(24), 7181-7185
Dolutegravir CAS# 1051375-16-6 度鲁特韦
Dolutegravir, also known as GSK1349572, is a potent inhibitor of HIV integrase with an IC50 value of 2.7 nM for HIV-1 integrase-catalyzed strand transfer in vitro.1 It inhibits HIV-1 viral replication...
Aoyama, Yasunori; Hakogi, Toshikazu; Fukui, Yuki; Yamada, Daisuke; Ooyama, Takao; Nishino, Yutaka; Shinomoto, Shoji; Nagai, Masahiko; Miyake, Naoki; Taoda, Yoshiyuki; Yoshida, Hiroshi; Yasukata, Tatsuro. Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis. Organic Process Research & Development. Volume 23. Issue 4. Pages 558-564. Journal; Online Computer File. (2019).
Momelotinib CAS# 1056634-68-4 莫洛替尼
Momelotinib is a potent, selective inhibitor of Janus kinases JAK1 and JAK2, as well as activin A receptor type I (ACVR1/ALK2). In vitro, it inhibits JAK1, JAK2, and ACVR1 with IC₅₀ values of 11 nM, 1...
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitorBy: Desai, Jigar; et alBioorganic & Medicinal Chemistry Letters (2022), 66, 128728
Lefamulin CAS# 1061337-51-6 来法莫林
Lefamulin, also known as BC-3781, is a semi-synthetic compound that inhibits the synthesis of bacterial protein, which is required for bacteria to grow. Lefamulin acts by binding to the peptidyl trans...
Reference: Heilmayer, Werner; Mang, Rosemarie; Badegruber, Rudolf; Stickmann, Dirk; Novak, Rodger; Ferencic, Mathias; Bulusu, Atchyuta Rama Chandra Murty. Synthesis of pleuromutilin derivatives for the treatment of diseases mediated by microbes. MX 2010009451. (2012).
Rufinamide CAS# 106308-44-5 卢非酰胺
Rufinamide is a board spectrum anticonvulsant. It is used in combination with other medication and therapy to treat Lennox–Gastaut syndrome and various other seizure disorders. Rufinamide was approved...
Zhang, Ping; Russell, M. Grace; Jamison, Timothy F. Continuous Flow Total Synthesis of Rufinamide. Organic Process Research & Development. Volume 18. Issue 11. Pages 1567-1570. 2014.
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