- Fluorinated Radicamine A and B: Synthesis and Glycosidase Inhibition
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Fluorinated derivatives of radicamine A and radicamine B have been synthesized from D-arabinose-derived cyclic nitrone. Structure-activity relationship studies showed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom. C-7 or C-11 fluorination of the aromatic ring decreased α-glucosidase inhibition of the derivatives, whereas C-8 or C-10 fluorination preserved glycosidase inhibitory activities. Fluorinated derivatives of radicamine A and B have been synthesized from D-arabinose-derived cyclic nitrone. Structure-activity relationship studies revealed that glycosidase inhibition of these fluorinated derivatives was significantly influenced by the position of the fluorine atom.
- Li, Yi-Xian,Iwaki, Ren,Kato, Atsushi,Jia, Yue-Mei,Fleet, George W. J.,Zhao, Xuan,Xiao, Min,Yu, Chu-Yi
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Read Online
- List fluoro Radicamine compounds and their use and preparation method
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The invention discloses a mono-fluorinated Radicamine compound which has a structure as shown in a formula (1), and further provides a preparation method for the mono-fluorinated Radicamine compound with the structure as shown in the formula (1) and an application of the mono-fluorinated Radicamine compound or the mono-fluorinated Radicamine compound prepared with the method to preparation of drugs for preventing and/or treating diabetes, drugs for preventing and/or treating Gaucher's diseases, drugs for preventing and/or treating tumors or antiviral drugs. The mono-fluorinated Radicamine compound provided by the invention is good in glycosidase inhibition activity.
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Paragraph 0076-0078
(2017/12/02)
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- TETRASUBSTITUTED ALKENE COMPOUNDS AND THEIR USE
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Disclosed herein are compounds, or pharmaceutically acceptable salts thereof, and methods of using the compounds for treating breast cancer by administration to a subject in need thereof a therapeutically effective amount of the compounds or pharmaceutically acceptable salts thereof. The breast cancer may be an ER-positive breast cancer and/or the subject in need of treatment may express a mutant ER-α protein.
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Page/Page column 124; 125
(2016/12/22)
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- NOVEL TETRAHYDROPYRIDOPYRIMIDINES AND TETRAHYDROPYRIDOPYRIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The invention provides novel compounds having the general formula (I): wherein R1, R2, R3, Q, U,W, Z, X and Y are as described herein, compositions including the compounds and methods of using the compounds. These compounds are HbsAg inhibitors and are useful as medicaments for the treatment or prophylaxis of HBV infection.
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Page/Page column 98
(2016/07/27)
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- [...] compd. mesogene medium
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The invention relates to bimesogenic compounds of formula I wherein R11, R12, MG11, MG12, X11, X12 and Sp1 have the meaning given in claim 1, to the use of bimesogenic compounds of formula I in liquid crystal media and particular to flexoelectric liquid crystal devices comprising a liquid crystal medium according to the present invention. Furthermore the invention relates to bimesogenic compounds of formula I inducing a second nematic phase in nematic mixtures that do not show this additional phase without compounds of formula I.
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Paragraph 0201; 0202
(2016/11/14)
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- THIOARYL DERIVATIVES AS GPR120 AGONISTS
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The present invention relates to thioaryl derivatives of Formula 1 as defined in the specification, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The thioaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in macrophages, pancreas cells, etc. due to anti-inflammatory action, and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, inflammation, obesity, non-alcoholic fatty liver, steatohepatitis or osteoporosis.
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Paragraph 373-374
(2014/05/24)
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- P-Hydroxyphenacyl photoremovable protecting groups Robust photochemistry despite substituent diversity
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A broadly based investigation of the effects of a diverse array of substituents on the photochemical rearrangement of p-hydroxyphenacyl esters has demonstrated that common substituents such as F, MeO, CN, CO2R, CONH2, and CH3 have little effect on the rate and quantum efficiencies for the photo-Favorskii rearrangement and the release of the acid leaving group or on the lifetimes of the reactive triplet state. A decrease in the quantum yields across all substituents was observed for the release and rearrangement when the photolyses were carried out in buffered aqueous media at pHs that exceeded the ground-state pKa of the chromophore where the conjugate base is the predominant form. Otherwise, substituents have only a very modest effect on the photoreaction of these robust chromophores.
- Givens, Richard S.,Stensrud, Kenneth,Conrad, Peter G.,Yousef, Abraham L.,Perera, Chamani,Senadheera, Sanjeewa N.,Heger, Dominik,Wirz, Jakob
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p. 364 - 384
(2011/06/22)
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- CYCLOALKYLAMINE DERIVATIVE
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Provided is a therapeutic agent for hyperparathyroidism, renal osteodystrophy, hypercalcemia and the like, which has a CaSR activating (agonist) action. A compound represented by the following general formula (1): [wherein, Ar which is a partial structure
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Page/Page column 64
(2011/07/30)
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- LIQUID-CRYSTALLINE COMPOUNDS AND LIQUID-CRYSTALLINE MEDIA
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The present invention relates to liquid-crystalline compounds having at least three fluorine-substituted benzene rings, a terminal trifluoromethyl group and at least one —CF2O— bridge. The invention also relates to liquid-crystalline media prep
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- [1,2,4] TRIAZOLO [4,3-B] PYRIDAZINES AS LIGANDS OF THE ANDROGEN RECEPTOR
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The invention concerns bicyclic compounds of Formula (I): wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
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Page/Page column 71
(2010/12/17)
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- HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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In one aspect, the present invention provides for a compound of Formula I; in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.
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Page/Page column 197
(2010/08/04)
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- SUBSTITUTED BICYCLOLACTAM COMPOUNDS
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The invention provides compounds of formula (1), and the pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5a, R5b, R5c, R5d, Q, A, Z, and R7 /s
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Page/Page column 16
(2009/03/07)
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- SPIRO SUBSTITUTED CYCLOPROPANE COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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A compound of the Formula I: or a pharmaceutically acceptable salt, solvate or isomer thereof, can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-alpha or combinations thereof.
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Page/Page column 19; 22
(2009/10/01)
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- Regioselectivity of fluorine substitution by alkoxides on unsymmetrical difluoroarenes
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An efficient approach to unsymmetrical halogenated resorcinol diethers has been developed. This synthesis consists of two subsequent nucleophilic aromatic substitutions (SNAr) of unsymmetrical difluoroarenes by alkoxides. The novelty of this ap
- Dirr, Ronan,Anthaume, Cyril,Désaubry, Laurent
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p. 4588 - 4590
(2008/09/21)
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- PESTICIDAL SUBSTITUTED PHENYLETHERS
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The invention relates to the use of phenylether derivatives of formula (I), to compositions thereof for the control of pests, including arthropods and helminths.
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Page/Page column 42; 46
(2008/06/13)
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- 2-AMINO- AND 2-THIO-SUBSTITUTED 1,3-DIAMINOPROPANES
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Disclosed are compounds of the formula: where variables Q, Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer’s disease and other diseases characterized by deposition of A beta peptide in a mammal.
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Page/Page column 180
(2008/06/13)
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- BENZOCHROMENE DERIVATIVES
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The invention relates to benzochromene derivatives of formula (I), in which the different parameters have the meanings as cited in the text, to liquid crystal media, which contain these compounds, and to the use of these media in electro-optical displays,
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Page/Page column 129
(2010/02/08)
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- The synthesis and mesomorphic properties of some novel antiferroelectric liquid crystals
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Several esters have been synthesised that exhibit the antiferroelectric smectic C phase. The core structures, like virtually all antiferroelectric materials, are very similar to that of MHPOBC. Lateral fluoro substituents have been used to reduce melting points and to investigate their effect on mesomorphic properties, spontaneous polarisation and tilt angle. A new device format reported by Lagerwall requires antiferroelectric liquid crystals with a 45° tilt angle. Novel antiferroelectric materials were prepared with fluoro substituents in lateral positions and in a terminal chain to provide low melting points, high antiferroelectric phase stability, high spontaneous polarisation and tilt angles of up to 45°. The synthetic routes to the novel materials are discussed, and the transition temperatures, tilt angles and spontaneous polarisations are compared to those of known materials.
- Hird, Michael,Goodby, John W.,Toyne, Kenneth J.,Gleeson, Helen F.,Peter Buxton,Seed, Alexander J.,Herbert, Mark R.
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p. 213 - 220
(2007/10/03)
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- Cyclobutanecarboxylic acid derivatives and liquid crystalline compositions containing them
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An optically inactive cyclobutanecarboxylic acid derivative of the general formula STR1 wherein R1 is a hydrogen atom or a straight or branched chain alkyl group having 1-14 carbon atoms, R2 is a straight or branched chain alkyl grou
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- Electroclinic and antiferroelectric properties of (R)-(-)-nonan-3-yl 4-(4′-dodecyloxybiphenyl-4-ylcarbonyloxy)-3-fluorobenzoate
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The synthesis of the novel chiral mesogen (R)-(-)-nonan-3-yl 4-(4′-dodecyloxybiphenyl-4-ylcarbonyloxy)-3-fluorobenzoate and a discussion of its various liquid-crystalline properties are reported. Initial optical microscopy studies revealed the presence of a smectic A* phase and what was at first thought to be a smectic C* phase; further examination of this compound as thin film preparations revealed the presence of s±1/2 disclinations suggesting that the phase is an antiferroelectric subphase. Furthermore, these observations were supported by results from both differential scanning calorimetry and contact miscibility studies using known smectic C*A standards. The antiferroelectric nature of the phase was confirmed by obtaining sharp threshold characteristic curves during electrical switching studies from the antiferroelectric to an induced ferroelectric phase. Additionally, the chirality of the compound results in a reduction in the environmental symmetry for the smectic A* phase, and this allows electroclinic switching in the pretransitional region of the smectic A* phase close to the smectic C*A transition to take place under suitable conditions.
- Booth, Christopher J.,Dunmur, David A.,Goodby, John W.,Toyne, Kenneth J.,Watson, Marcus J.
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p. 919 - 926
(2007/10/03)
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- Ferroelectric liquid crystal device
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A ferroelectric liquid crystal device having a pair of substrates each provided with voltage appli-cation means, an orientation control layer formed on at least one of the substrates, and a layer of ferro-electric liquid crystal composition formed between the pair of substrates, the device being characterized in that the ferroelectric liquid crystal composition comprises at least one compound (a) having an optically active group of the formula (I): and at least one compound (b) which is reverse to the compound (a) in the direction of a helical pitch induced in a nematic phase, the liquid crystal composi-tion exhibiting at least a smectic C phase, smectic A phase and nematic phase at least 20μm in helical pitch.
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