专利号:US-4440690-A 优先权日:1982-12-27 标题:Process for the synthesis of 6-bromo-17,21-dihydroxy 3,11,20-trioxo-1,4-pregnadienes 17,21-diesters 发明人:SHAPIRO ELLIOT L; FINKENOR LAWRENCE E 权利人:SCHERING CORP 摘要:Disclosed is an improved process for the synthesis of 6-bromo-17,21-dihydroxy-3,11,20-trioxo-1,4,-pregnadienes 17,21-diesters. In particular, this invention relates to the conversion of 17,21-dihydroxy-3,11,20-trioxo-1,4-pregnadienes 17,21-diesters to 6-borom-17,21-dihyroxy-3,11,20-trioxo-1,4-pregnadienes-17-21-diesters via bromination under ionic conditions, e.g. bromine in acetic acid.
专利号:US-2022265691-A1 优先权日:2019-07-12 标 题 :Methods for use of gene expression as an indicator of e-selectin inhibitor efficacy and clinical outcome for multiple tumor types 发明人:MAGNANI JOHN L; FOGLER WILLIAM E; THACKRAY HELEN M; FELDMAN ERIC J; STEWART DAVID 权利人:GLYCOMIMETICS INC 摘要:Cancer patients that express high levels of the E-selectin ligand (sialyl Lea/x) on their tumors have a poorer outcome. Interestingly, relapsed/refractory acute myeloid leukemia (AML) patients expressing high levels of sialyl Lex on their blasts show the greatest therapeutic response when treated with the E-selection inhibitor compound of Formula I. Transcriptome profiling of E-selectin ligand-forming glycosylation genes showed that ST3GAL4 and FUT7 were consistently expressed in the majority of cancers evaluated. Poor survival outcomes of FLT3-mutated AML patients that express high levels of ST3GAL4 and FUT7 implicated E-selectin in this disease state. These genes may be predictive biomarkers in AML patients. Methods of treatment of cancer comprising screening AML patients for expression of genes that contribute to the synthesis of the E-selectin ligand sialyl Lex, then treating those patients with an E-selection inhibitor, are disclosed.
专利号:US-4867914-A 优先权日:1982-02-26 标题:Pregnane derivatives and method of producing the same 发明人:BUNNO MASAYASU; HARADA HIDEMI; TSUJI MASAO; ICHIHARA YOSHIHIRO 权利人:KURARAY CO 摘要:There are provided 12-hydroxy- DELTA 4 or DELTA 1,4-pregnan-3-one-20-carbaldehyde and microbial method of producing the same. The compounds are novel and useful as starting materials for the synthesis of corticoids, typically prednisone, prednisolone and hydrocortisone, which have antiinflammatory activity.
专利号:US-4041055-A 优先权日:1975-11-17 标题:Process for the preparation of 17α-hydroxyprogesterones and corticoids from androstenes 发明人:SHEPHARD KENNETH PAUL; VAN RHEENEN VERLAN H 权利人:UPJOHN CO 摘要:This invention discloses a general process for the production of corticoids from androstenes. This invention provides an economically viable alternative synthesis of 17α-hydroxyprogesterones and the corticoids.
专利号:US-2019031650-A1 优先权日:2016-01-29 标 题 :Dna alkylation and cross-linking agents as compounds and payloads for targeted therapies 发明人:HERZON SETH; HEALY ALAN; CRAWFORD JASON; VIZCAINO MARIA; NIKOLAYEVSKIY HERMAN 权利人:UNIV YALE 摘要:The present invention is directed to compounds related to precolibactin pharmaceutical compositions based upon these compounds and methods of synthesis which are employed to provide intermediates and final compounds, which are principally alkylating agents and anticancer compounds. The chemical synthetic approach disclosed facilitates the synthesis of numerous precolibactin analogs which can be used in the treatment of cancer.
专利号:WO-9709067-A1 优先权日:1995-09-05 标 题 :Combination of 5-lipoxygenase and leukotriene synthesis inhibitors with glucocorticosteroids 发明人:BURCHARDT ELMAR-REINHOLD; MUELLER-PEDDINGHAUS REINER 权利人:BAYER AG; BURCHARDT ELMAR REINHOLD; MUELLER PEDDINGHAUS REINER 摘要:The combination is disclosed of 5-lipoxygenase inhibitors as direct action lipoxygenase inhibitors (LOI) or of leukotriene synthesis inhibitors (LSI) with glucocorticosteroids (GCS). This combination is suitable for treating and preventing various acute and chronic inflammatory processes, in particular of the respiratory tract, and may therefore be used as a medicament, in particular for treating asthma.
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