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Belumosudil CAS# 911417-87-3 2-[3-[4-[(1H-吲唑-5-基)氨基]喹唑啉-2-基]苯氧基]-N-异丙基乙酰胺
Belumosudil (SLx-2119, KD025) is a selective inhibitor of Rho-associated coiled-coil kinase-2 (ROCK2). In biochemical assays it inhibits ROCK2 with an IC₅₀ of ~60–105 nM and shows >200-fold selectivit...
A process for the preparation of 2-{3-[4-(1H-indazol-5-ylamino)-2-quinazolinyl]phenoxy}-N-(propan-2-yl) acetamide or its saltsBy: Rajan, Srinivasan Thirumalai; et alTechnical Disclosure Commons (2023), 6212, 1-19
Neratinib Maleate CAS# 915942-22-2 马来酸来那替尼
Neratinib, also known as HKI-272 or PB272, is an orally available, irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 rec...
Reference: Chew, Warren; Cheal, Gloria Karen; Lunetta, Jacqueline Francesca. Process for the preparation of substituted 3-cyanoquinolines and intermediates thereof. WO 2006127207. (Assignee Wyeth, John, and Brother Ltd., USA)
Naldemedine CAS# 916072-89-4
Naldemedine, also known as S 297995, is a peripherally-selective μ-opioid receptor antagonist under development by Shionogi for the treatment of opioid-induced adverse effects including constipation, ...
Reference: Inagaki M, Kume M, Tamura Y, Hara S, Goto Y, Haga N, Hasegawa T, Nakamura T, Koike K, Oonishi S, Kanemasa T, Kai H. Discovery of naldemedine: A potent and orally available opioid receptor antagonist for treatment of opioid-induced adverse effects. Bioorg Med Chem Lett. 2019 Jan 1;29(1):73-77. doi: 10.1016/j.bmcl.2018.11.007. Epub 2018 Nov 7. PubMed PMID: 30446313.
Opicapone CAS# 923287-50-7 奥匹帕酮
Opicapone (BIA 9-1067) is a potent, long-acting, reversible inhibitor of catechol-O-methyltransferase (COMT) developed to enhance levodopa bioavailability in Parkinson’s disease. In preclinical studie...
Discovery of a Long-Acting, Peripherally Selective Inhibitor of Catechol-O-methyltransferaseBy: Kiss, Laszlo E.; et alJournal of Medicinal Chemistry (2010), 53(8), 3396-3411
Elafibranor CAS# 923978-27-2 2-[2,6-二甲基-4-[(1E)-3-[4-(甲硫基)苯基]-3-氧代-1-丙烯-1-基]苯氧基]-2-甲基丙酸
Elafibranor, also known as GFT-505, is a dual PPARα/δ agonist. is an agonist of the peroxisome proliferator-activated receptor-α and peroxisome proliferator-activated receptor-δ. GFT505 has an active...
Design, synthesis and anti-NASH effect evaluation of novel GFT505 derivatives in vitro and in vivoBy: Xiang, Cen; et alEuropean Journal of Medicinal Chemistry (2023), 257, 115510
Milnacipran (HCl) CAS# 92623-85-3 / 101152-94-7 米那普仑
Milnacipran is a serotonin–norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. It is not approved for the clinical treatment of major depressive disorder in the US...
Coelho, Pedro S.; Brustad, Eric M.; Arnold, Frances H.; Wang, Zhan; Lewis, Jared C. In vivo and in vitro olefin cyclopropanation catalyzed by engineered and chimeric heme enzymes. Assignee California Institute of Technology, USA. WO 2014058744. (2014).
Fluorodopa F 18 CAS# 92812-82-3 (S)-2-氨基-3-(2-(氟-18F)-4,5-二羟基苯基)丙酸
Fluorodopa F 18 is radioactive agent.
Reference: Maisonial-Besset, Aurelie; Serre, Audrey; Ouadi, Ali; Schmitt, Sebastien; Canitrot, Damien; Leal, Fernand; Miot-Noirault, Elisabeth; Brasse, David; Marchand, Patrice; Chezal, Jean-Michel. Base/cryptand/metal-free automated nucleophilic radiofluorination of [18F]FDOPA from iodonium salts: Importance of hydrogen carbonate counterion. European Journal of Organic Chemistry. Volume 2018. Issue 48. Pages 7058-7065. Journal; Online Computer File. (2018).
Osilodrostat CAS# 928134-65-0 3-氟-4-[(5R)-5H,6H,7H-吡咯罗[1,2-c]吡唑-5-基]苯并腈
Osilodrostat, also known as LCI699, is a potent inhibitor of 11β-hydroxylase, the enzyme which catalyzes the final step of cortisol synthesis. LCI699 may thus be a potential new treatment for all form...
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 InhibitorsBy: Meredith, Erik L.; et alACS Medicinal Chemistry Letters (2013), 4(12), 1203-1207
Elinzanetant CAS# 929046-33-3
Elinzanetant is a potent, dual antagonist of the neurokinin-1 (NK-1) and neurokinin-3 (NK-3) receptors, with Kᵢ values reported at ~0.37 nM for NK-1 and ~3.0 nM for NK-3. In vitro studies show it bind...
Patent#: WO2011023733
Fedratinib CAS# 936091-26-8 N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-[2-(1-吡咯烷基)乙氧基]苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺
Fedratinib, also known as TG101348 and SAR302503, is a JAK2 inhibitor, is also an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential anti...
Reference: Tefferi, Ayalew. N-tert-butyl-3-[(5-methyl-2-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide for treating myelofibrosis. Assignee TargeGen, Inc., USA. WO 2012060847. (2012).
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