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专利信息
专利号:US-9242998-B2
优先权日:2013-02-07
标题 :Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis C
发明人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; DAI XING; PALANI ANANDAN; NARGUND RAVI; LAI ZHONG; ZORN NICOLAS; XIAO DONG; DANG QUN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-12304912-B2
优先权日:2020-07-28
标 题 :Fused bicyclic RAF inhibitors and methods for use thereof
发明人:BELFIELD ANDREW; JONES CLIFFORD DAVID; MARGATHE JEAN-FRANÇOIS; COLLETTO CHIARA
权利人:JAZZ PHARMACEUTICALS IRELAND LTD
摘要:The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
专利号:US-7485725-B1
优先权日:2004-11-12
标 题:Substituted pyridines
发明人:CEFALO DUSTIN R; HENDERSON JASON I; MOKRI HOMAYOUN H
权利人:FRONTIER SCIENT INC
摘要:A class of 2,4-; 2,3,4-; 2,4,6-; 2,3,4,5,6-substituted pyridines is provided which include novel compounds. The substitutions are achieved according to methods disclosed herein in which a metallated pyridine is reacted with an electrophile. Suitable electrophiles include CO 2 , SO 2 , dialkylcarbonates, ureas, formamides, amides, carboxylic acid esters, mono- and dihaloalkyls, halogens such as chlorine, fluorine, bromine, and iodine, metallic salts, sulfones, sulfonyls, aldehydes, ketones, anhydrides, nitriles, and electrophilic boron compounds including, but not limited to, boron trialkoxides and boron trihalides. The subject invention more specifically discloses a process for the synthesis of 2,6-difluoropyridin-4-ylboronic acid which comprises: (1) reacting 2,4,6-trifluoropyridine with hydrazine monohydrate to produce 2,6-difluoro-4-hydrazinopyridine, (2) reacting the 2,6-difluoro-4-hydrazinopyridine with elemental bromine to produce 4-bromo-2,6-difluoropyridine, and (3) reacting the 4-bromo-2,6-difluoropyridine with an organolithium compound and a borate at a temperature of less than 0° C. to produce the 2,6-difluoropyridin-4-ylboronic acid, wherein said process is conducted in an organic solvent.
专利号:US-7087755-B1
优先权日:2004-11-12
标 题 :Substituted pyridines
发明人:CEFALO DUSTIN R; HENDERSON JASON I; MOKRI HOMAYOUN H
权利人:FRONTIER SCIENT INC
摘要:A class of 2,4-; 2,3,4-; 2,4,6-; 2,3,4,5,6-substituted pyridines is provided which include novel compounds. The substitutions are achieved according to methods disclosed herein in which a metallated pyridine is reacted with an electrophile. Suitable electrophiles include CO 2 , SO 2 , dialkylcarbonates, ureas, formamides, amides, carboxylic acid esters, mono- and dihaloalkyls, halogens such as chlorine, fluorine, bromine, and iodine, metallic salts, sulfones, sulfonyls, aldehydes, ketones, anhydrides, nitrites, and electrophilic boron compounds including, but not limited to, boron trialkoxides and boron trihalides. The subject invention more specifically discloses a process for the synthesis of 2,6-difluoropyridin-4-ylboronic acid which comprises: (1) reacting 2,4,6-trifluoropyridine with hydrazine monohydrate to produce 2,6-difluoro-4-hydrazinopyridine, (2) reacting the 2,6-difluoro-4-hydrazinopyridine with elemental bromine to produce 4-bromo-2,6-difluoropyridine, and (3) reacting the 4-bromo-2,6-difluoropyridine with an organolithium compound and a borate at a temperature of less than about 0° C. to produce the 2,6-difluoropyridin-4-ylboronic acid, wherein said process is conducted in an organic solvent.
专利号:US-2025276972-A1
优先权日:2020-12-15
标 题:Compounds as casein kinase inhibitors
发明人:Zhou Enxing; LIU YUAN; WANG HANPING; WU GUANGLONG; SHAO NING
权利人:GRITSCIENCE BIOPHARMACEUTICALS CO LTD
摘要:Provided are casein kinase inhibitors, or pharmaceutically acceptable salts thereof. Corresponding pharmaceutical compositions, methods of synthesis, and intermediates are also provided.