- Imidazolium-based protic ionic liquids with perfluorinated anions: Influence of chemical structure on thermal properties
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The influence of the cation chemical structure, namely its side chain, on the thermal properties of imidazolium-based protic ionic liquids (PILs) with different perfluorinated anions (trifluoromethanesulfonimide (TFSI), trifluoromethanesulfonic (TFS), and trifluoroacetic (TFA) acids) was studied. With that purpose, twenty-one PILs with various alkyl (methyl-, ethyl-, butyl- and vinyl-) and fluorinated (-CH2CF3, -CH2CHF2, and -CH2CH2F) side chains were successfully synthesized. Special attention was paid to an optimization of their synthesis conditions. The structure of synthesized fluorinated and alkyl-substituted PILs was confirmed by means of nuclear magnetic resonance (NMR) analysis (1D: 1H, 19F, 13C and 2D: 1H – 19F HOESY experiments) and Fourier transform infrared (FTIR) spectroscopy, while PILs thermal behavior was determined by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) in dynamic and isothermal modes. The correlation between the PILs chemical structure and their thermal stability was established. It has been found that an increase of the length of alkyl side chain (methyl- 2F 2 3) leads to a PIL with a higher crystallinity (a higher melting point temperature) and a lower thermal stability. Thus, the best performance in terms of the thermal stability was reached for monofluorinated- (-CH2F) and butyl-TFSI PILs in liquid state: 370 °C and 400 °C, respectively, while the lowest thermal stability was obtained for trifluorinated- (-CF3) and vinyl-TFA PILs in solid state: 145 °C and 129 °C, respectively.
- Fatyeyeva, K.,Kobzar, Ya. L.,Marais, S.,Martin, A.,Oulyadi, H.,Prykhodko, Y.
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- CHEMICAL COMPOUNDS
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The specification relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
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Page/Page column 53
(2019/01/17)
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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 0581; 0582
(2019/07/10)
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- ESTROGEN RECEPTOR MODULATORS
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The specification relates to compounds of Formula (I): (I) 5and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.
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Page/Page column 156; 157
(2018/08/20)
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- N-(2-(4-((1R,3R)-3-METHYL-2,3,4,9-TETRAHYDRO-1H-PYRIDO[3,4-B]INDOL-1-YL)PHENOXY)ETHYL)PROPAN-1-AMINE DERIVATIVES AND RELATED COMPOUNDS AS SELECTIVE DOWN-REGULATORS OF THE ESTROGEN RECEPTOR FOR TREATING CANCER
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The specification relates to compounds of Formula (I) and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, pharmaceutical compositions containing them and to the compounds of Formula (I) for use as selective down-regulators of the estrogen receptor in the treatment of cell proliferative disorders, such as cancer.
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Page/Page column 161
(2018/02/28)
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- OXADIAZEPINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF HEPATITIS B INFECTIONS
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Provided herein are compounds of formula (IA) and (III) useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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Page/Page column 146
(2018/02/28)
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- NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
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An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
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Paragraph 1028; 1029
(2018/09/08)
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- CHEMICAL COMPOUNDS
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The specification relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
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Paragraph 0705; 0706
(2017/11/11)
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- Preparation method of 2-(2',2'-difluoroethoxy)-6-(trifluoromethyl)benzene-1-sulfonyl chloride
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The invention discloses a preparation method of 2-(2',2'-difluoroethoxy)-6-(trifluoromethyl)benzene-1-sulfonyl chloride. The preparation method comprises following steps: (1) a sulfonyl chloride or a sulfonic anhydride is added into an organic solvent containing 2,2-difluoroethanol and an alkali, and a compound I is obtained via complete reaction, wherein the sulfonyl chloride is selected from alkyl sulfonyl chloride or benzene sulfonyl chloride, and the sulfonic anhydride is selected from alkyl sulfonic anhydride or benzene sulfonic anhydride; (2) m-trifluoromethylphenol, the compound I, and an alkali are added into an organic solvent, an obtained mixture is heated and stirred, and a compound II is obtained via complete reaction; and (3) an accelerant and the compound II are added into an organic solvent, a strong alkali is added, the sulfonyl chloride is added into an obtained reaction solution, and 2-(2',2'-difluoroethoxy)-6-(trifluoromethyl)benzene-1-sulfonyl chloride is obtained via complete reaction and purifying. The preparation method is simple, is high in efficiency, is safe and reliable, and is capable of increasing synthesis efficiency of penoxsulam greatly; and operation is simple and convenient.
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Paragraph 0043; 0044
(2016/10/08)
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- Solvent-free synthesis of alkyl and fluoroalkyl sulfonium salts from sulfides and fluoroalkyl trifluoromethanesulfonates
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A series of diaryl(fluoroalkyl)sulfonium salts were synthesized from electron-rich diaryl sulfides and fluoroalkyl trifluoromethanesulfonates under solvent-free conditions. Unlike diaryl sulfides, dialkyl and alkyl(aryl) sulfides reacted with fluoroalkyl
- Song, Hai-Xia,Wang, Shi-Meng,Wang, Xiao-Yan,Han, Jia-Bin,Gao, Ying,Jia, Su-Jiao,Zhang, Cheng-Pan
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p. 131 - 140
(2016/11/19)
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- Substituted Oxopyridine Derivatives and Use Thereof in the Treatment of Cardiovascular Disorders
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The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
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Paragraph 1360-1362
(2016/05/02)
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- DGAT1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
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The present invention discloses a novel DGAT1 inhibitor, especially the compound of formula (I) or a pharmaceutically acceptable salt thereof, preparation and pharmaceutical composition thereof, as well as their uses in the preparation of a medicament for the prevention and treatment of Familial hyperchylomicronemia (FCS), obesity, hyperlipoproteinemia or hypertriglyceridemia.
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Paragraph 0268; 0269
(2016/08/23)
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- A solvent-free facile synthesis of (E)-bis(phosphonium)ethylenes from organo-phosphines and TfOCH2CF2H reagent
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(E)-Bis(phosphonium)ethylenes were synthesized from aryl-, alkyl-, and arylalkylphosphines under solvent-free conditions using TfOCH2CF2H as reagent. The reaction allows for a convenient access to vinylenebis(trialkylphosphonium) sal
- Wang, Shi-Meng,Han, Jia-Bin,Zhang, Cheng-Pan,Qin, Hua-Li
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p. 6219 - 6222
(2015/10/20)
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- SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF CARDIOVASCULAR DISORDERS
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The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.
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Paragraph 1971-1974
(2016/10/07)
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- NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF
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The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.
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Paragraph 0441; 0442
(2014/10/29)
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- 3-AMINOCYCLOPENTANECARBOXAMIDES AS CHEMOKINE RECEPTOR MODULATORS
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There is provided a compound of Formula I(a) or I(b) or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
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Page/Page column 75-76
(2010/06/17)
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- BICYCLOANILINE DERIVATIVE
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The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of =NH or =O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
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Page/Page column 48
(2010/04/25)
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- Peptide inhibitors of hepatitis C virus NS3 protease
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Fluorinated oligopeptides, especially those having 4,4-difluoro-2-amino butyric acid at the C terminus, may be effective inhibitors of hepatitis C virus NS3 protease. Examples of hexapeptides of the invention, optimized for binding in the S1 specificity p
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Page/Page column 29
(2008/06/13)
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- Synthesis and Biological Activity of Fluoroalkylamine Derivatives of Narcotic Analgesics
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N-Ethyl-, N-(2-fluoroethyl)-, N-(2,2-difluoroethyl)-, and N-(2,2,2-trifluoroethyl)-substituted normeperidine (1b-e) and normetazocine (2b-e) derivatives were prepared.The analgesic activities of the compounds were determined in mice.Opiate receptor binding studies, in the presence and absence of sodium ion, were carried out.The antagonist activities of normetazocine derivatives were studied in monkeys.These were further examined in the isolated guinea pig ileum for agonist activity.These pKa values were measured in vivo agonist activity was lost with the weakly bas ic derivatives.For the normetazocine derivatives, opiate receptor binding data were consistent with guinea pig ileum agonist potency and mouse vas deferens antagonist potency but not in vivo data.Opiate receptor binding was reduced for the less basic normetazocine derivatives.In the normeperidine series, there was no apparent direct relationship between pKa and opiate receptor binding.However, a relationship involving the hydrophobic character of the N-substituent is discussed.The N-(2-fluoroethyl) derivatives in both series were found to cause convulsions in rats at doses of 40-45 mg/kg ip.Elevated serum citrate levels were found in these rats, implicating in vivo oxidative deamination of the N-(fluoroalkyl) substituent to fluoroacetate.
- Reifenrath, William G.,Roche, Edward B.,Al-Turk, Walid A.,Johnson, Howard L.
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p. 985 - 990
(2007/10/02)
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