- Fluorinations of unsymmetrical diaryliodonium salts containing: Ortho -sidearms; Influence of sidearm on selectivity
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Activated aromatics were reacted with two different fluoroidoane reagents 1 and 2 in the presence of triflic acid to prepare only the para-substituted diaryliodonium salts. With fluoroiodane 1 the unsymmetrical diaryliodonium salts contained an ortho-propan-2-ol sidearm, whereas the alcohol sidearm was eliminated to form an ortho-styrene sidearm in the reaction with fluoroiodane 2. Only the diaryliodonium salts containing a styrene sidearm were fluorinated successfully to deliver para-fluorinated aromatics in good yields.
- Abudken, Ahmed M. H.,Hope, Eric G.,Singh, Kuldip,Stuart, Alison M.
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p. 6140 - 6146
(2020/10/30)
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- Synthesis and Biological Evaluation of N-((1-(4-(Sulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide Inhibitors of Glycine Transporter-1
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We previously disclosed the discovery of rationally designed N-((1-(4-(propylsulfonyl)piperazin-1-yl)cycloalkyl)methyl)benzamide inhibitors of glycine transporter-1 (GlyT-1), represented by analogues 10 and 11. We describe herein further structure-activit
- Cioffi, Christopher L.,Liu, Shuang,Wolf, Mark A.,Guzzo, Peter R.,Sadalapure, Kashinath,Parthasarathy, Visweswaran,Loong, David T. J.,Maeng, Jun-Ho,Carulli, Edmund,Fang, Xiao,Karunakaran, Kalesh,Matta, Lakshman,Choo, Sok Hui,Panduga, Shailijia,Buckle, Ronald N.,Davis, Randall N.,Sakwa, Samuel A.,Gupta, Priya,Sargent, Bruce J.,Moore, Nicholas A.,Luche, Michele M.,Carr, Grant J.,Khmelnitsky, Yuri L.,Ismail, Jiffry,Chung, Mark,Bai, Mei,Leong, Wei Yee,Sachdev, Nidhi,Swaminathan, Srividya,Mhyre, Andrew J.
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p. 8473 - 8494
(2016/10/03)
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- Pyrazolo [3,4 - the b] pyridine and [...] composition preparation method and use of (by machine translation)
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The present invention provides a pyrazolo [3,4 - the b] pyridine and [...] compound of preparation and use, in particular, the present invention provides a following formula (I) compounds are shown, wherein the definition of each group as described in the specification. The compounds of the invention has excellent tyrosine kinase inhibiting activity, so can be used for preparing a series of treating diseases associated with the tyrosine kinase activity of the drug. (by machine translation)
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Paragraph 0534; 0535; 0536; 0537
(2017/07/22)
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- PHARMACEUTICAL COMPOUNDS
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This invention relates to compounds that inhibit or modulate the activity of Chk-1 kinase. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds.
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Page/Page column 93; 147
(2015/09/23)
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- Modulators of methyl modifying enzymes, compositions and uses thereof
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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Page/Page column 135; 136
(2015/12/26)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein
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Paragraph 00254; 00255
(2013/06/05)
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- Ortho-selectivity in SNAr substitutions of 2,4-dihaloaromatic compounds. Reactions with anionic nucleophiles
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The nucleophilic addition of organic anions to aromatic compounds with halogens positioned both ortho and para to activating groups was studied in a variety of solvents. Substrates showed strong preferences for ortho substitution in most cases. Evidence is presented for activating group-dependent coordination, which contributes to very high ortho-selectivity in nonpolar solvents. This also drives the overall reaction rate in these solvents, and is of close to the same magnitude of rate increase derived from polar solvents. para-Products are maximized by using crown ethers in protic solvents. Solvent effects overall are very different from corresponding reactions with amine nucleophiles due primarily to the different charges present in the transition states, and to solvation of the nucleophile.
- Wendt, Michael D.,Kunzer, Aaron R.
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scheme or table
p. 3041 - 3044
(2010/07/18)
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- Regioselective SNAr reactions of substituted difluorobenzene derivatives: practical synthesis of fluoroaryl ethers and substituted resorcinols
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In this Letter, we describe a practical and highly selective method for the preparation of fluoroaryl ethers and differentially substituted resorcinol derivatives. This synthetic strategy relies on a selective SNAr of substituted difluorobenzen
- Ouellet, Stéphane G.,Bernardi, Anna,Angelaud, Remy,O'Shea, Paul D.
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supporting information; experimental part
p. 3776 - 3779
(2009/10/11)
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- Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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Page/Page column 30
(2008/06/13)
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- 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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- Nitrone derivatives
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A compound represented by the figure (1) or a pharmaceutically acceptable salt thereof is useful as medicament for treating retinal degenerative disorders: wherein Ar is optionally substitued phenyl or optionally substituted heteroaryl;. n is 0, 1 or 2; W
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- Synthesis and preliminary data on new selective and potent gastric prokinetic substituted benzamides
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A series of amino-halogen-N- benzamides was synthesized and evaluated for enhancing gastric emptying.Compared to metoclopramide, domperidone and bromopride, a number of compounds were shown to be more active in enhancing gastric motility (rat stomach emptying), devoid of dopaminergic D2-receptor antagonism (rat apomorphine test) and to be less toxic. substituted benzamides / gastrokinetic activity
- Corona, L Del,Signorelli, G,Pinzetta, A,Coppi, G
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p. 419 - 425
(2007/10/02)
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