CAS: 57186-25-1; 4B-Hydroxy-2-(2-Hydroxypropan-2-yl)-12B,12C-Dimethyl-5,6,6A,7,12,12B,12C,13,14,14A-Decahydro-2H-Chromeno[5',6':6,7]Indeno[1,2-B]Indol-3(4Bh)-One

该化合物是一种自然产生的藻类,主要源于真菌* Penciillum paxilli*,以其复杂的结构而著称,其中包括一个引信的四环环系统;和平线展示了重要的生物活动,特别是作为某些离子渠道(包括电压加钾渠道)的强大抑制剂;这种特性使它成为药物研究中的宝贵化合物,特别是在与...

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CAS号12627-35-9 青霉震颤素 A | CAS号121998-08-1 1'-O-Acetylpaxilline

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    专利号:US-2024343691-A1
    优先权日:2006-12-28
    标题:Compositions for modulating a kinase cascade and methods of use thereof
    发明人:HANGAUER JR DAVID G; PATRA DEBASIS; CODY JEREMY A; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
    权利人:ATNX SPV LLC
    摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl) pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

    专利号:US-8293739-B2
    优先权日:2006-12-28
    标题:Process for the preparation of compositions for modulating a kinase cascade and methods of use thereof
    发明人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON
    权利人:HANGAUER JR DAVID G; COUGHLIN DANIEL; GALE JONATHAN; CODY JEREMY A; PATRA DEBASIS; PALMER GRANT J; ISBESTER PAUL K; SALSBURY JONATHON; KINEX PHARMACEUTICALS LLC
    摘要:The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy) phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.

    专利号:US-2009270321-A1
    优先权日:2008-04-10
    标 题 :Over-expression of MPS-1 gene or its gene product(s) results in reduction in size of a variety of malignancies
    发明人:STACK JR BRENDAN CURRAN; DAI YUEMENG
    权利人:STACK JR BRENDAN CURRAN; DAI YUEMENG
    摘要:Metallopanstimulin-1 (MPS-1) is a multifunctional ribosomal protein. MPS-1 is a 10 kD zinc finger protein (ZFP) that is present in all tissues and expressed in increased quantities in a wide variety of proliferating tissues and malignancies. The ribosome is a ribonucleoprotein complex of ribosomal RNAs (rRNA) and proteins (r-protein). Conventionally, r-proteins are thought to be responsible for new protein synthesis, but emerging evidence has shown activity exists beyond this. Some extra-ribosomal functions of r-proteins have been observed in close relation to cancer pathology. MPS-1 is over-expressed in the serum and tissue of dozens of malignancies. However, it is unknown whether the enhanced expression of MPS-1 is the cause or result of tumor development and progression. Our preliminary observations show increased MPS-1 decreases paxillin. Recently, paxillin was found to have an important role in regulating both normal and tumor cell proliferation. n Elevation of MPS-1 in HNSCC samples and its structure/function as a ribosomal ZFP have led us to conclude that MPS-1 might be a subject of interest for malignant tumor therapy. Our data reveal that enhanced expression of MPS-1 protein can strongly suppress tumor cell proliferation. MPS-1 and significantly inhibits tumor growth both in vitro and in vivo in 3 distinct malignant cell lines. We have concluded that over-expression of MPS-1 might be used therapeutically in the treatment of some malignancies.

    专利号:CA-3111403-A1
    优先权日:2018-09-17
    标 题:Matter of composition, synthesis, formulation and application of fl118 platform positions 7 and 9-derived analogues for treatment of human disease

    专利号:WO-2020061106-A4
    优先权日:2018-09-17
    标题:Matter of composition, synthesis, formulation and application of fl118 platform positions 7 and 9-derived analogues for treatment of human disease

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    合成参考文献


    参考文献:10.1186/1471-2407-10-43
    摘要:Zhang S, Guo D, Luo W, Zhang Q, Zhang Y, Li C, Lu Y, Cui Z, Qiu X. TrkB is highly expressed in NSCLC and mediates BDNF-induced the activation of Pyk2 signaling and the invasion of A549 cells. BMC Cancer. 2010 Feb 16;10():43.
    参考文献:10.1016/j.mcn.2010.02.001
    摘要:Chacón MR, Fernández G, Rico B. Focal adhesion kinase functions downstream of Sema3A signaling during axonal remodeling. Molecular and Cellular Neuroscience. 2010 May;44(1):30–42. doi: 10.1016/j.mcn.2010.02.001.
    参考文献:10.1007/s10585-005-3733-6
    摘要:Hanada M, Tanaka K, Matsumoto Y, Nakatani F, Sakimura R, Matsunobu T, Li X, Okada T, Nakamura T, Takasaki M, Iwamoto Y. Focal Adhesion Kinase is Activated in Invading Fibrosarcoma Cells and Regulates Metastasis. Clinical & Experimental Metastasis. 2005 Nov;22(6):485–94. doi: 10.1007/s10585-005-3733-6.
    参考文献:10.1371/journal.pone.0021684
    摘要:Paron I, Berchtold S, Vörös J, Shamarla M, Erkan M, Höfler H, Esposito I. Tenascin-C Enhances Pancreatic Cancer Cell Growth and Motility and Affects Cell Adhesion through Activation of the Integrin Pathway. PLoS ONE. 2011 Jun 29;6(6):e21684. doi: 10.1371/journal.pone.0021684.
    参考文献:10.1007/978-1-61779-207-6_1
    摘要:Vicente-Manzanares M, Horwitz AR. Cell migration: an overview. Methods Mol Biol. 2011;769():1–24. doi: 10.1007/978-1-61779-207-6_1.
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