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参考文献:喹诺酮类抗生素对分枝杆菌的构效关系:在n-1和c-7处结构变化的影响.
标题:喹诺酮类抗生素对分枝杆菌的构效关系:在n-1和c-7处结构变化的影响.
摘要:对常规药物治疗有抵抗力的结核感染的再次出现表明需要针对结核分枝杆菌的替代化学疗法.作为优化针对结核分枝杆菌的喹诺酮类抗菌药物研究的一部分,我们准备了一系列n-1-和c-7取代的喹诺酮类化合物,以研究这两个位置上喹诺酮类修饰物与活性之间的特定结构-活性关系.对抗分枝杆菌.通过文献方法合成的化合物被评估了对福分枝杆菌和耻垢分枝杆菌以及革兰氏阴性和革兰氏阳性细菌的活性.化合物对堡垒分枝杆菌的活性用作结核分枝杆菌活性的晴雨表.
DOI:10.1021/jm9507082
专利信息
专利号:US-9121110-B2
优先权日:2002-12-19
标 题 :Quasirandom structure and function guided synthesis methods
发明人:GOULIAEV ALEX HAAHR; HOLTMANN ANETTE; PEDERSEN HENRIK; FRANCH THOMAS
权利人:GOULIAEV ALEX HAAHR; HOLTMANN ANETTE; PEDERSEN HENRIK; FRANCH THOMAS; NUEVOLUTION AS
摘要:The present invention is directed to the synthesis of molecules guided by connector polynucleotides (CPNs) capable of hybridizing to complementary connector polynucleotides (CCPNs) harboring at least one functional entity comprising at least one reactive group. At least one of the CCPNs is capable of hybridizing to at least two CPNs. Each CPN will “callâ€? for one or more CCPNs capable of hybridization to the CPN. Following the formation of a supramolecular hybridization complex comprising a plurality of CPNs and a plurality of CCPNs, the reaction of reactive groups results in the formation of a molecule comprising covalently linked functional entities. The formation of the molecule involves the transfer of functional entities from one or more “donor CCPNsâ€? to at least one “acceptor CCPNâ€? with which the transferred functional entities were not associated prior to the transfer.
专利号:WO-2023086801-A1
优先权日:2021-11-09
标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use
发明人:HOUZE JONATHAN B; PANDYA BHAUMIK; KAPLAN ALAN P; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN
权利人:VIGIL NEUROSCIENCE INC
摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ('TREM2'). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
专利号:US-11008358-B2
优先权日:2015-03-25
标题:Synthesis of desosamines
发明人:MYERS ANDREW G; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof.
专利号:US-7981990-B2
优先权日:2007-08-31
标 题:Synthesis of a liquid polymer and a functionalized polymer
发明人:YAN YUAN-YONG
权利人:BRIDGESTONE CORP
摘要:A method comprising: (a) forming a living liquid polymer, wherein said living liquid polymer is anionically initiated and comprises a cation; (b) adding a functional initiator precursor of the formula FI-H, wherein H is hydrogen and FI is a functional group, said H terminates said living liquid polymer resulting in said liquid polymer having a number average molecular weight of about 20,000 (g/mole) to about 100,000 (g/mole), and said FI and said cation form a functional initiator; (c) adding monomer, wherein said functional initiator initiates anionic polymerization of said monomer; and (d) terminating the polymerization reaction initiated in step (c). Steps (a) through (c) may be conducted in a single reactor, allowing a liquid polymer to be dispersed in a functionalized polymer in a single polymerization step. Thus, the liquid polymer does not have to be handled separately and processing efficiency is improved.
专利号:US-9676783-B2
优先权日:2008-10-22
标 题:Method of treatment using substituted pyrazolo[1,5-A] pyrimidine compounds
发明人:HAAS JULIA; ANDREWS STEVEN W; JIANG YUTONG; ZHANG GAN
权利人:ARRAY BIOPHARMA INC
摘要:Compounds useful in the synthesis of compounds for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal.
专利号:US-8304410-B2
优先权日:2007-09-26
标题 :Pyrrole compounds as inhibitors of mycobacteria, synthesis thereof and intermediates thereto
发明人:BIAVA MARIANGELA; PORRETTA GIULIO CESARE; POMPEI RAFFAELLO; BOTTA MAURIZIO; MANETTI FABRIZIO; DE LOGU ALESSANDRO
权利人:BIAVA MARIANGELA; PORRETTA GIULIO CESARE; POMPEI RAFFAELLO; BOTTA MAURIZIO; MANETTI FABRIZIO; DE LOGU ALESSANDRO; UNIV ROMA; UNIV SIENA
摘要:The present invention relates to compounds having formula 3 n nas well as the synthesis, intermediates and methods of using the same.