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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