专利号:US-12391725-B2 优先权日:2016-06-22 标题:Method for production of novel galeterone analogs and uses thereof 发明人:NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS 权利人:NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT 摘要:Galeterone and its C-3 analogs are of substantial interest because of their multi-target anticancer activities, including AR and Mnk degrading activities. Provided are novel procedures for gram-scale, high-yield synthesis of C-3 analogs of galeterone, including 3β-(1H-imidazole-1-yl)-17-(1H-benzimidazole-1-yl)-androsta-5,16-diene (galeterone 3β-imidazole) and 3β-(pyridine-4-ylmethoxy)-17-(1H-benzimidazol-1-yl)androsta-5,16-diene (galeterone 3β-pyridine methoxylate).
专利号:US-4500535-A 优先权日:1979-10-15 标 题:Method of regulating the immune response with pyridine derivatives 发明人:LOMBARDINO JOSEPH G; HARBERT CHARLES A 权利人:PFIZER 摘要:A series of 4-(2-carboxymethylthiomethyl)pyridines and related compounds, and their pharmaceutically acceptable salts, are disclosed as having immunoregulatory activity. Preferred compounds include 4-(2-carboxymethylthiomethyl)pyridine [alternatively named 2-(4-picolylthio)acetic acid] and (C 1 -C 4 )alkyl esters thereof, and 4-(1-formylmethylthiomethyl)-pyridine [alternatively named 2-(4-picolylthio)acetaldehyde] and bis(C 1 -C 4 )alkyl or cyclic acetals thereof. These acids, esters, aldehydes and acetals also have utility as intermediates in the synthesis of the corresponding 4-(2-hydroxyethylthiomethyl)pyridines.
专利号:US-10851059-B2 优先权日:2016-08-17 标题:Processes and intermediates for NEP inhibitor synthesis 发明人:KLEINBECK-RINIKER FLORIAN KARL; MAFLI IVES; MARTIN BENJAMIN; PENN GERHARD; SEDELMEIER GOTTFRIED; SEDELMEIER JOERG; VENTURONI FRANCESCO 权利人:NOVARTIS AG 摘要:The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril, inter alia via nitro 5 compounds. It further relates to new intermediate compounds and their use for said new chemical synthesis route, as well as a new catalyst ligand.
专利号:US-9562037-B2 优先权日:2014-02-26 标题:Synthesis and use of amine-containing flavonoids as potent anti-leishmanial agents 发明人:CHOW LARRY MING-CHEUNG; CHAN WILLIAM TAK HANG; CHAN KIN-FAI; WONG IRIS LAI KING; KAN WING-YIU 权利人:UNIV HONG KONG POLYTECHNIC 摘要:The present invention relates to novel series of amine-containing flavonoids and compositions containing the compounds, as well as the synthesis and the use of the same. The invention also relates to methods of treatment and prevention of diseases, in particular, parasitic infections including Leishmaniasis, comprising administration of the compounds.
专利号:US-10111854-B2 优先权日:2014-02-26 标题 :Synthesis and use of amine-containing flavonoids as potent anti-leishmanial agents 发明人:CHOW LARRY MING-CHEUNG; Chan Tak Hang William; CHAN KIN-FAI; WONG IRIS LAI KING; KAN WING-YIU 权利人:UNIV HONG KONG POLYTECHNIC 摘要:The present invention relates to novel series of amine-containing flavonoids and compositions containing the compounds, as well as the synthesis and the use of the same. The invention also relates to methods of treatment and prevention of diseases, in particular, parasitic infections including Leishmaniasis, comprising administration of the compounds.
专利号:US-8476313-B2 优先权日:2004-08-26 标 题:Heteroaryl-containing isoflavones as aromatase inhibitors 发明人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C 权利人:BRUEGGEMEIER ROBERT W; KIM YOUNG-WOO; HACKETT JOHN C; UNIV OHIO STATE RES FOUND 摘要:Compounds and methods useful for treating and prevention of cancer, particularly hormone-dependent breast cancer. Provided are compounds of formula I: n nwherein X is selected from O, N, S, SO, SO 2 , and S(CH 2 ) n , wherein n=1-10; R 1 and R 2 may be the same or different and are selected from H, OH, OCH 3 , OCH 2 CH 3 , OCH 2 C 6 H 5 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 2 CH 3 , CH 2 CH 2 CH 3 , CH(CH 3 ) 2 , C(CH 3 ) 3 , NO 2 , F, Cl, Br, CF 3 , SH, SCH 3 , SCH 2 CH 3 , OCOCH 3 , OCOC(CH 3 ) 3 , OCOCH 2 COOH, and CN; and R 3 is a nitrogen-containing heterocyclic ring. Also provided are method for treating or preventing cancer in a subject by administering a therapeutically effective amount of a heteroaryl-containing isoflavone, or a pharmaceutically acceptable salt or prodrug thereof, to a subject in need of treatment. Also provided is a method for the synthesis of 2-substituted isoflavones by first reacting deoxybenzoins with a phase transfer catalyst to provide a 2-(alkylthio)isoflavone; second deprotecting the 2-(alkylthio)isoflavone; and third applying selective debenzylation to form the final compound.
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合成参考文献
参考文献:10.1007/s11243-022-00518-3 摘要:González-Montiel S, Velázquez-Jiménez R, Segovia-Pérez R, Fragoso-Soto W, Martínez-Otero D, Andrade-López N, Salazar-Pereda V, Cruz-Borbolla J. η3-allyl-Pd(II) complexes of 2-, 3- and 4-pyridylmethyl-coumarin esters. Transition Metal Chemistry. 2022 Nov 30;():1–16. doi: 10.1007/s11243-022-00518-3.