CAS: 891494-63-6; 6-Bromo-3-(1-Methyl-1H-Pyrazol-4-yl)-5-(3R)-3-Piperidinylpyrazolo[1,5-A]Pyrimidin-7-Amine

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CAS号1335211-24-9 (R)-tert-butyl ... | CAS号25016-11-9 1-甲基-1H-吡唑-4-甲醛 | CAS号754159-15-4 1-甲基-1H-吡唑-4-乙腈 | CAS号1039364-93-6 2-(1-methyl-1H-... | CAS号930286-91-2 [4,4'-Bi-1H-pyr... | CAS号163438-09-3 N-B°C-(R)-3-甲酸哌啶

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  • 1335211-24-9 = 891494-63-6
    反应条件:1.1 Reagents: Trifluoroacetic Acid Solvents: Dichloromethane
    标题:A Convergent Preparation Of The Chk1 Inhibitor Mk-8776 (Sch 900776)
    作者:Labroli,Marc A.; Dwyer,Michael P.; Poker,Cory; Keertikar,Kerry M.; Rossman,Randall; Et Al
    参考文献:Tetrahedron Letters 日期:2016 卷标:57(24) 页码:2601-2603
📜1-甲基-1H-吡唑-4-甲醛置于n-溴代丁二酰亚胺(Nbs),盐酸肼,Potassium Tert-Butylate,三氟乙酸体系中,用 乙二醇二甲醚,乙醇,二氯甲烷,乙腈 作为反应溶剂,化学反应生成 6-溴-3-(1-甲基-1H-吡唑-4-基)-5-(3R)-3-哌啶基吡唑并[1,5-A]嘧啶-7-胺
参考文献:Chk1抑制剂mk-8776(sch 900776)的收敛制剂
标题:Chk1抑制剂mk-8776(sch 900776)的收敛制剂
摘要:这封信描述了向chk1抑制剂mk-8776汇聚,高效途径的发展.该合成方法依赖于双吡唑加合物10与光学纯的β-酮腈9的环化,以一步构建吡唑并[1,5-A]嘧啶骨架.
DOI:10.1016/j.Tetlet.2016.04.102

海关参考信息

专利信息


专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人:ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.

专利号:WO-2022162606-A1
优先权日:2021-01-30
标 题:Heterocyclic compounds as kinase inhibitor and uses thereof
发明人:YAN ZHIYU; WANG XIAOHUI; LIU HANLAN; KHAN PASHA M; PANPATIL DAYANAND; PUJALA BRAHMAM; PENDHARKAR DHANANJAY; JADHAVAR PRADEEP S; SAEED UZMA; KUMAR VIVEK
权利人:SPEROGENIX THERAPEUTICS LTD; INTEGRAL BIOSCIENCES PRIVATE LTD
摘要:The present disclosure relates generally to compounds useful in treatment of conditions associated with Checkpoint kinase (CHK), particularly CHK-1 enzymes. Specifically, the present invention discloses compound of formula (J), which exhibits inhibitory activity against CHK-1 enzymes. Methods of treating conditions associated with excessive activity of CHK-1 enzymes such as cancer, idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) with such compounds is disclosed. Uses thereof, pharmaceutical compositions, kits and method of synthesis also disclosed. Formula (J)

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主要参考文献


1: Montano R, Chung I, Garner KM, Parry D, Eastman A. Preclinical development of the novel Chk1 inhibitor SCH900776 in combination with DNA-damaging agents and antimetabolites. Mol Cancer Ther. 2012 Feb;11(2):427-38. doi: 10.1158/1535-7163.MCT-11-0406. Epub 2011 Dec 27.
2: Lamore SD, Kamendi HW, Scott CW, Dragan YP, Peters MF. Cellular impedance assays for predictive preclinical drug screening of kinase inhibitor cardiovascular toxicity. Toxicol Sci. 2013 Oct;135(2):402-13. doi: 10.1093/toxsci/kft167. Epub 2013 Jul 28. 7(38):62091-62106. doi: 10.18632/oncotarget.11388.
4: David L, Fernandez-Vidal A, Bertoli S, Grgurevic S, Lepage B, Deshaies D, Prade N, Cartel M, Larrue C, Sarry JE, Delabesse E, Cazaux C, Didier C, Récher C, Manenti S, Hoffmann JS. CHK1 as a therapeutic target to bypass chemoresistance in AML. Sci Signal. 2016 Sep 13;9(445):ra90. doi: 10.1126/scisignal.aac9704. 16(9):1831-1842. doi: 10.1158/1535-7163.MCT-17-0018. Epub 2017 Jun 15. 19(10):830-841. doi: 10.1016/j.neo.2017.08.002. Epub 2017 Sep 6.

合成参考文献


摘要:S55 | ZINC15PHARMA | Pharmaceuticals from ZINC15 | DOI:10.5281/zenodo.3247749
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