2,3,4-三氟苯甲酸置于n,N'-二环己基碳二亚胺,Lithium Diisopropyl Amide体系中,用 四氢呋喃,正庚烷,乙基苯,N,N-二甲基甲酰胺 用作溶剂,化学反应 146.0H,反应生成4-辛基酚乙氧基化物 参考文献:Improved Experimental Procedure For The Synthesis Of The Potent Mek Inhibitor Pd184352 标题:Improved Experimental Procedure For The Synthesis Of The Potent Mek Inhibitor Pd184352 摘要:An Improved Synthesis Of The Potent Mek Inhibitor Pd184352 (2-(2-Chloro-4-Iodo-Phenylamino)-N-Cyclopropylmethoxy-3,4-Difluoro-Benzamide)) Is Herein Reported. This New And Reproducible Protocol Provides A Simple And Efficient Way Of Generating Gram Quantities Of Pd 184352 With Minimal Purification. Doi:10.1080/00397910500184909
专利号:US-2025206743-A1 优先权日:2022-03-25 标 题:Tyk2 inhibitor synthesis and intermediates thereof 发明人:MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG 权利人:TAKEDA PHARMACEUTICALS CO 摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-9365532-B1 优先权日:2011-02-14 标题:Synthesis, composition and use of novel therapeutic and cosmetic Schiff base products formed by reaction of a carbonyl containing moeity with a transimination nucleophilic catalyst and the use of transimination nucleophilic catalysts to increase the rate at which carbonyl containing therapeutic and cosmetic actives form Schiff base products with biological amines 发明人:ISAACMAN STEVEN 权利人:ISAACMAN STEVEN; NANOMETICS LLC 摘要:The present invention relates to the synthesis, composition and use of novel moieties formed by reacting a transimination nucleophilic catalyst, molecular or polymeric, with carbonyl-containing therapeutic or cosmetic moieties. The resultant Schiff base product is highly reactive towards transimination with a biological amine. The catalyst and carbonyl-containing moiety can be molecular or polymeric, and the resultant chemical and physical properties of the Schiff base products can be engineered by appropriate selection of said catalyst. The present invention also relates to the synthesis, composition and use of novel moieties that are used as actives in sunless tanning preparations. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate at which a carbonyl-containing moiety reacts with a biological amine. The present invention also relates to the use of transimination nucleophilic catalysts to increase the rate and efficacy of commercial sunless tanning preparations. Improvements on stability and efficacy of said preparations are disclosed. While the invention has been described in terms of its preferred embodiments, those skilled in the art will recognize that the invention can be practiced with modification within the spirit and scope of the appended claims. Accordingly, the present invention should not be limited to the embodiments as described above, but should further include all modifications and equivalents thereof within the spirit and scope of the description provided herein.
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:US-2022143183-A1 优先权日:2019-02-23 标题:Photoswitchable protacs and synthesis and uses thereof 发明人:TRAUNER DIRK; REYNDERS MARTIN; MATSUURA BRYAN; BEROUTI MARLEEN; PAGANO MICHELE 权利人:UNIV NEW YORK 摘要:Provided are compounds, which may be referred to as PHOTACs (photoswitchable proteolysis targeting chimeras), and compositions, kits, and methods of making and using PHOTACs. PHOTACs have one or more E3 ligase ligand(s), one or more photoswitchable group(s), optionally, one or more linker(s), and one or more ligand(s) for a target protein. PHOTACs may be suitable for use in methods to treat diseases, such as, for example, cancer. PHOTACs may also be suitable for use in methods to induce selective degradation of a target protein.
专利号:CN-118922420-A 优先权日:2022-03-25 标题 :Synthesis of TYK2 inhibitors and their intermediates
参考文献:10.4161/cbt.4.11.2286 摘要:Hawkins W, Mitchell C, McKinstry R, Gilfor D, Starkey J, Dai Y, Dawson K, Ramakrishnan V, Roberts JD, Yacoub A, Grant S, Dent P. Transient exposure of mammary tumors to PD184352 and UCN-01 causes tumor cell death in vivo and prolonged suppression of tumor regrowth. Cancer Biol Ther. 2005 Nov;4(11):1275–84. doi: 10.4161/cbt.4.11.2286. 参考文献:10.1186/1471-2202-12-69 摘要:Hughes R, Gilley J, Kristiansen M, Ham J. The MEK-ERK pathway negatively regulates bim expression through the 3' UTR in sympathetic neurons. BMC Neuroscience. 2011 Jul 15;12(1):69. doi: 10.1186/1471-2202-12-69. 参考文献:10.4161/cbt.4.11.2335 摘要:Franklin RA, Libra M, Stivala F, McCubrey JA. Two targets are better than one. Promising combination therapy to treat breast cancer. Cancer Biol Ther. 2005 Nov;4(11):1190–1. doi: 10.4161/cbt.4.11.2335.