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专利信息
专利号:US-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人:ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
专利号:US-8399502-B2
优先权日:2008-09-17
标 题 :Analogs of indole-3-carbinol and their use as agents against infection
发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN
权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT
摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
专利号:US-11787803-B2
优先权日:2017-09-15
标 题 :Tetrahydro-imidazo quinoline compositions as CBP/P300 inhibitors
发明人:SCHILLER SHAWN E R; HERBERTZ TORSTEN; LI HONGBIN; GRAVES BRADFORD; MISCHKE STEVEN; WEST ANGELA V; DOWNING JENNIFER R; ERICSSON ANNA
权利人:FORMA THERAPEUTICS INC
摘要:The present disclosure is directed to inhibitors of the CBP/p300 family of bromodomains. The compounds can be useful in the treatment of disease or disorders associated with the inhibition of the CBP/p300 family of bromodomains. For instance, the disclosure is concerned with compounds and compositions for inhibition of the CBP/p300 family of bromodomains, methods of treating, preventing, or ameliorating diseases or disorders associated with the inhibition of CBP/p300 family of bromodomains, and methods of synthesis of these compounds.
专利号:WO-2023081730-A1
优先权日:2021-11-03
标 题:4-hydroxy-2-oxo-1,2-dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid cb2 receptor modulators for the treatment of cancer
发明人:ELZEIN ELFATIH; LIU JIWEN
权利人:TEON THERAPEUTICS INC
摘要:The present invention relates to 82 specific 4-hydroxy-2-oxo-1,2- dihydro-1,8-naphthyridine-3-carboxamide derivatives as cannabinoid CB2 receptor modulators for the treatment of cancer, e.g. to 6-(4- fluorophenyl)-4-hydroxy-1-(2-(4-methylpiperazin-1-yl)ethyl)-2-oxo-N- (spiro[2.3]hexan-5-yl)-1,2-dihydro-1,8-naphthyridine-3-carboxamide (example 1, compound 1) The present description discloses the synthesis and characterisation of the 82 claimed compounds as well as biological assays thereof.
专利号:ES-2794012-T3
优先权日:2008-10-27
标题 :Intermediaries for the synthesis of mTOR kinase inhibitors
专利号:US-9861636-B2
优先权日:2014-04-29
标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors
发明人:HE WEI
权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD
摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.