- Novel synthesis method of 3-fluoropyridine-2-methanol
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The invention relates to the field of compound preparation, in particular to a novel synthesis method of 3-fluoropyridine-2-methanol. The 3-fluoropyridine-2-methanol has a structure as shown in a formula V. According to the synthesis method, cheap quinolinic acid is used as an initial raw material, the target product namely 3-fluoropyridine-2-methanol is obtained through the steps of anhydride, esterification, ammoniation, amino fluorination, ester group reduction, and the like, and the structure of the target product is characterized by 1HNMR and 13CNMR. The synthetic method is a brand new synthetic method of 3-fluoropyridine-2-methanol, and has the advantages of low cost, simple technology, high yield, good quality, and high industrialization value.
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- Compounds and Their Use in Treating Cancer
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The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts and prodrugs thereof, where R1, R4, R5, R6, R7, Linker, X, Y, A, G, D and E have any of the meanings defined herein. This specification also relates to the use of such compounds and pharmaceutically acceptable salts and prodrugs thereof in methods of treatment of the human or animal body, for example in prevention or treatment of cancer. This specification also relates to processes and intermediate compounds involved in the preparation of such compounds and to pharmaceutical compositions containing them.
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Paragraph 1652; 1653
(2019/07/10)
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- Three substituted naphthyridine compounds and its preparation and use
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The invention relates to 1,3,5-tri-substituted-1H-imidazo[4,5-h]1,6-diazanaphthalene-2(3H)-one compounds shown as the general formula I, isomers thereof and pharmaceutically acceptable salts thereof, a preparation method and applications thereof, and comp
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Paragraph 0061-0063
(2017/04/14)
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- BIOREVERSABLE PROMOIETIES FOR NITROGEN-CONTAINING AND HYDROXYL-CONTAINING DRUGS
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Disclosed are promoieties of the following formula which can be used to form prodrugs of nitrogen-containing or hydroxyl-containing drug or a pharmaceutically active agent: (I) and pharmaceutical compositions comprising the prodrugs.
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Page/Page column 129
(2015/06/18)
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- Repositioning HIV-1 integrase inhibitors for cancer therapeutics: 1,6-naphthyridine-7-carboxamide as a promising scaffold with drug-like properties
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Among a large number of HIV-1 integrase (IN) inhibitors, the 8-hydroxy-[1,6]naphthyridines (i.e., L-870,810) were one of the promising class of antiretroviral drugs developed by Merck Laboratories. In spite of its remarkable potency and efficacy, unfortun
- Zeng, Li-Fan,Wang, Yong,Kazemi, Roza,Xu, Shili,Xu, Zhong-Liang,Sanchez, Tino W.,Yang, Liu-Meng,Debnath, Bikash,Odde, Srinivas,Xie, Hua,Zheng, Yong-Tang,Ding, Jian,Neamati, Nouri,Long, Ya-Qiu
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p. 9492 - 9509
(2013/01/16)
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- Processes and intermediates useful for preparing integrase inhibitor compounds
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The invention provides processes and intermediates useful for preparing integrase inhibiting compounds.
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Page/Page column 16
(2010/11/30)
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- PHOSPHONATE ANALOGS OF HIV INTEGRASE INHIBITOR COMPOUNDS
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Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.
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Page/Page column 404-406
(2010/02/15)
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- PRE-ORGANIZED TRICYCLIC INTEGRASE INHIBITOR COMPOUNDS
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Tricyclic compounds according to the structure below, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed. Formula (I). Al and A2 are moieties forming a five, six, or seven membered ring. L is a bond or a linker connecting a ring atom of Ar to N. X is O, S, or substituted nitrogen. Ar is aryl or heteroaryl. Q is N, +NR, or CR4. The aryl carbons may be independently substituted with substituents other than hydrogen. The compounds may include prodrug moieties covalently attached at any site.
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- Synthesis and Pharmacology of a Series of 3- and 4-(Phosphonoalkyl)pyridine- and piperidine-2-carboxylic Acids. Potent N-Methyl-D-aspartate Receptor Antagonists
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We recently prepred a series of 3- and 4-(phosphonoalkyl)pyridine- and piperidine-2-carboxylic acids as antagonists of neurotransmission at N-methyl-D-aspartate (NMDA) preferring receptors.NMDA antagonists may prove to be useful therapeutic agents, for instance, as anticonvulsants, in the treatment of neurodegenerative disorders such as Alzheimer's disease and in the prevention of neuronal damage that occurs during cerebral ischemia.The compounds prepared were evaluated for their ability to displace CPP binding (an assay shown to be selective for compounds that bind at the NMDA receptor) and for their ability to block NMDA-induced lethality in mice (an assay that is also specific for competitive and noncompetitive NMDA antagonists).Two of the compounds, cis-4-(phosphonomethyl)piperidine-2-carboxylic acid (11a) and cis-4-(3-phosphonoprop-1-yl)piperidine-2-carboxylic acid (11c) proved to be potent NMDA antagonists. 11a and 11c displaced CPP binding with IC 50's of 95 and 120 nM, respectively, and both protected mice from NMDA-induced lethality, with MEDs (minimum effective dose, the dose at which three of the five animals tested survived) of 10 and 40 mg/kg ip, respectively.The rest of the compounds prepared were weakly active or inactive in these assays.The pattern of activity observed for this series parallels that observed for the acyclic series of ω-phosphono-α-amino acids, where AP5 and AP7 possessed NMDA antagonist activity while AP6 and AP8 were inactive.Reduction of conformational mobility by incorporation of the piperidine ring led to enhanced potency relative to the acyclic analogues.
- Ornstein, Paul L.,Schaus, John M.,Chambers, John W.,Huser, Diane L.,Leander, J. David,et al.
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p. 827 - 833
(2007/10/02)
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