- High-Field Proton and Carbon-13 Nuclear Magnetic Resonance Studies of the Conformational Dynamic Properties of Seven-Membered Rings. 3-Substituted Derivatives of 1,5-Benzodioxepin
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The conformational and dynamic properties of the 3-methyl (6), 3-methoxy (7), and 3-methoxy-3-methyl (8) derivatives of 1,5-benzodioxepin 1 have been investigated by high-field 1H and 13C NMR methods.Analyses of the spectra at low temperatures (below coal
- Menard, D.,St-Jacques, M.
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Read Online
- SSAO INHIBITORS AND USE THEREOF
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Provided are a compound of formula (I') or (I), a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of SSAO, a pharmaceutical composition comprising a compound of formula (I') or (I), and a method of treating or preventing a disease in which SSAO plays a role.
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Paragraph 00630
(2021/05/07)
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- Synthesis and evaluation of novel potent TSPO PET ligands with 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamide
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Translocator protein (TSPO) expression is closely related with neuroinflammation and neuronal damage which might cause several central nervous system diseases. Herein, a series of TSPO ligands (11a–c and 13a–d) with a 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamide structure were prepared and evaluated via an in vitro binding assay. Most of the novel ligands exhibited a nano-molar affinity for TSPO, which was better than that of DPA-714. Particularly, 11a exhibited a subnano-molar TSPO binding affinity with suitable lipophilicity for in vivo brain studies. After radiolabeling with fluorine-18, [18F]11a was used for a dynamic positron emission tomography (PET) study in a rat LPS-induced neuroinflammation model; the inflammatory lesion was clearly visualized with a superior target-to-background ratio compared to [18F]DPA-714. An immunohistochemical examination of the dissected brains confirmed that the uptake location of [18F]11a in the PET study was consistent with a positively activated microglia region. This study proved that [18F]11a could be employed as a potential PET tracer for detecting neuroinflammation and could give possibility for diagnosis of other diseases, such as cancers related with TSPO expression.
- Hieu Tran, Van,Park, Hyunjun,Park, Jaekyung,Kwon, Young-Do,Kang, Shinwoo,Ho Jung, Jae,Chang, Keun-A,Chul Lee, Byung,Lee, Sang-Yoon,Kang, Soosung,Kim, Hee-Kwon
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p. 4069 - 4080
(2019/08/26)
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- HPK1 INHIBITORS, PREPARATION METHOD AND APPLICATION THEREOF
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Disclosed are HPK-1 inhibitors having a structure represented by Formula (X), pharmaceutical compositions comprising the HPK-1 inhibitors, methods of using the HPK-1 inhibitors, such as treating cancers, methods of preparing the HPK-1 inhibitors, and the synthetic intermediates.
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Page/Page column 153-154
(2019/11/12)
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- Novel potential pyrazolopyrimidine based translocator protein ligands for the evaluation of neuroinflammation with PET
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Translocator protein (TSPO) is an interesting biological target because TSPO overexpression is associated with microglial activation caused by neuronal damage or neuroinflammation, and these activated microglia are involved in several central nervous syst
- Kwon, Young-Do,Kang, Shinwoo,Park, Hyunjun,Cheong, Il-koo,Chang, Keun-A,Lee, Sang-Yoon,Jung, Jae Ho,Lee, Byung Chul,Lim, Seok Tae,Kim, Hee-Kwon
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p. 292 - 306
(2018/10/15)
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- NOVEL COMPOUND having VINYLPHENYLOXY moiety AND PHOTOSENSITIVE PHOTORESIST COMPOSITION INCLUDING THE SAME
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The present invention relates to a compound having a vinylphenyloxy group which is represented by chemical formula A, B, or C, and a photosensitive photoresist composition including the same. The chemical formula A, B, or C are as described in the detaile
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Paragraph 0123-0125
(2018/09/12)
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- NOVEL COMPOUND having VINYLPHENYLOXY moiety AND PHOTOSENSITIVE PHOTORESIST COMPOSITION INCLUDING THE SAME
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The present invention relates to a compound having a vinylphenyloxy group which is represented by chemical formula A, B, or C, and a photosensitive photoresist composition including the same. The chemical formula A, B, or C are as described in the detaile
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Paragraph 0123-0125
(2018/09/20)
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- Sweet switches: Azobenzene glycoconjugates synthesized by click chemistry
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Azobenzene glycoconjugates can be switched between two isomeric states, E and Z, to change the spatial orientation of the conjugated carbohydrate ligands. Mono-, di- and trivalent azobenzene glycoconjugates were synthesized using click chemistry and their
- Chandrasekaran, Vijayanand,Lindhorst, Thisbe K.
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supporting information; experimental part
p. 7519 - 7521
(2012/10/07)
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- Structure guided P1′ modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer's disease
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The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off target toxicity, and improved micr
- Monenschein, Holger,Horne, Daniel B.,Bartberger, Michael D.,Hitchcock, Stephen A.,Nguyen, Thomas T.,Patel, Vinod F.,Pennington, Lewis D.,Zhong, Wenge
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scheme or table
p. 3607 - 3611
(2012/07/17)
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- Tandem Wittig-intramolecular Diels-Alder cycloaddition of ester-tethered 1,3,9-decatrienes under microwave heating
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Intramolecular Diels-Alder (IMDA) cycloaddition of the ester-tethered 1,3,9,-decatrienes possessing a carbonyl substituent at C10 has been investigated under controlled microwave heating (MeCN, 180 °C) to afford a variety of 3,4,4a,7,8,8a-hexahydroisochromen-1-ones in 53-89% yields and in 64:36-79:21 ratios for the cis and trans isomers. Under the same microwave heating conditions, a tandem Wittig-IMDA cycloaddition, starting from the α-bromoacetates of 3,5-hexadien-1-ols and glyoxalate/phenylglyoxal hydrates in the presence of PPh3 and 2,6-lutidine, has been demonstrated, furnishing 3,4,4a,7,8,8a-hexahydroisochromen-1-one adducts in 73-91% yields in favor of the cis isomers. During this tandem process, three consecutive carbon-carbon bonds in the end products were efficiently formed with the aid of microwave irradiation within short reaction times.
- Wu, Jinlong,Jiang, Xiuqing,Xu, Jingjing,Dai, Wei-Min
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experimental part
p. 179 - 192
(2011/02/28)
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- BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I); wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula (I), methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula (I), or compositions including them, to a subject. The invention also comprises further embodiments of Formulas (II) and (III), intermediates and processes useful for the preparation of compounds of the invention.
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Page/Page column 160
(2010/11/27)
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- Synthesis and Liquid Crystal Properties of Dimethylene Linked Compounds Incorporating the Cyclobutane or Spiroheptane Rings
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The preparation of sixteen dimethylene linked compounds is described heptane ring>, and a comparison is made between the transition temperatures of these compounds and those of the corresponding esters.This comparison once again highlights the fact that the cyclobutane ring should be regarded, in terms of its ability to promote nematic thermal stability, as a "chain stiffener rather than as a ring system.A comparison is also made of the nematic thermal stabilities of the trans-cyclobutane and the spiroheptane systems and of the trans-cyclohexane and the spiroundecane systems.
- Chan, L. K. M.,Gemmell, P. A.,Gray, G. W.,Lacey, D.,Toyne, K. J.
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p. 229 - 246
(2007/10/02)
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- Synthesis and liquid crystal properties of compounds incorporating cyclobutane, spiroheptane and dispirodecane rings
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A number of esters of structure (I) incorporating the cyclobutane, spiroheptane, or dispirodecane rings has been prepared using a diethyl malonate synthesis.Strict comparison of the liquid crystal behaviour amongst the three classes containing a terminal cyano-substituent was not possible because both the cyclobutanes and dispirodecanes are mixtures of cis- and trans-isomers; the spiroheptanes are racemic systems.Using preparative hplc, it was however possible to isolate the pure cis- and trans-isomers of two of the cyano-substituted cyclobutane esters (I; R = alkyl, -X- = --, Y = CN).From the physical data and the results for the corresponding spiroheptane esters, conclusions regarding the effects of these ring systems on liquid crystal behaviour were obtained.The pure cis- and trans-isomers of the cyclobutane ester (I, R = C3H7, -X- = --, Y = CN) have been assessed for the trends in both order parameter and viscosity with temperature; the results support the idea that idea that the trans-cyclobutane ring adopts a more planar conformation at higher temperatures.Keywords: cyclobutane- and related spiro-systems, cis-/trans-isomerism, order parameter, briefringence, viscosity, structure/property relations.
- Chain, L. K. M.,Gemmel, P. A.,Gray, G. W.,Lacey, D.,Toyne, K. J.
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p. 113 - 140
(2007/10/02)
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- LONG-ACTING CONTRACEPTIVE AGENTS: CYCLOPROPYL AND CYCLOBUTYL ESTERS OF NORETHISTERONE
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Several esters of norethisterone (17α-ethynyl-17β-hydroxyestr-4-en-3-one) with carboxylic acids containing a cyclopropyl or cyclobutyl ring have been synthesized and the stereochemistries of the side-chains determined.
- Shafiee, A.,Vossoghi, M.,Savabi, F.,Vlahov, R.,Tarpanov, V.,et al.
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p. 291 - 308
(2007/10/02)
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