- Lipophilicity trends upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl groups
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A systematic comparison of lipophilicity modulations upon fluorination of isopropyl, cyclopropyl and 3-oxetanyl substituents, at a single carbon atom, is provided using directly comparable, and easily accessible model compounds. In addition, comparison with relevant linear chain derivatives is provided, as well as lipophilicity changes occurring upon chain extension of acyclic precursors to give cyclopropyl containing compounds. For the compounds investigated, fluorination of the isopropyl substituent led to larger lipophilicity modulation compared to fluorination of the cyclopropyl substituent.
- Jeffries, Benjamin,Wang, Zhong,Troup, Robert I.,Goupille, Ana?s,Le Questel, Jean-Yves,Fallan, Charlene,Scott, James S.,Chiarparin, Elisabetta,Graton, Jér?me,Linclau, Bruno
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supporting information
p. 2141 - 2150
(2021/02/05)
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- ION CHANNEL MODULATORS
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Provided, in part, are compounds of Formula I pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of conditions associated with the activity of sodium channels. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including neurological disorders (e.g., Dravet syndrome, epilepsy), pain, and neuromuscular disorders are also provided herein.
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Paragraph 0264-0266
(2020/12/13)
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- COMPOUNDS AND THEIR METHODS OF USE
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The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
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Page/Page column 150
(2018/09/08)
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- PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Page/Page column 97
(2016/07/05)
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- OXAZOLIDINONE HYDROXAMIC ACID COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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This invention pertains generally to treating bacterial infections using organic compounds of Formula I. In certain aspects, the invention pertains to treating infections caused by Gram-negative bacteria. (I) wherein X, Y, R1, R2, R3, R4 and R5 and defined herein.
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Page/Page column 124
(2015/05/19)
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- Reactivity and regiochemical behavior in the solvolysis reactions of (2,2-difluorocyclopyl)methyl tosylates
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The rate constants for acetolysis of (2,2-difluorocyclopropyl)methyl tosylate, and (2,2-difluoro-3-methylcyclopropyl)methyl tosylate at 92°C and of 1-(2,2-difluoropropyl)ethyl tosylate at 42°C are reported and the rectivities and regiochemistries of ring opening of these systems are discussed and compared with expectations based on computational results. The results are discussed in terms of the use of (2,2-difluorocyclopropyl)methyl systems as mechanistic probes.
- Battiste, Merle A.,Tian, Feng,Baker, John M.,Bautista, Olivia,Villalobos, Janette,Dolbier Jr., William R.
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