- Amorphous metal-free roomerature phosphorescent small molecules with multicolor photoluminescence via a host-guest and dual-emission strategy
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Metal-free roomerature phosphorescence (RTP) materials offer unprecedented potentials for photoelectric and biochemical materials due to their unique advantages of long lifetime and low toxicity. However, the achievements of phosphorescence at ambient condition so far have been mainly focused on ordered crystal lattice or on embedding into rigid matrices, where the preparation process might bring out poor repeatability and limited application. In this research, a series of amorphous organic small molecular compounds were developed with efficient RTP emission through conveniently modifying phosphor moieties to β-cyclodextrin (β-CD). The hydrogen bonding between the cyclodextrin derivatives immobilizes the phosphors to suppress the nonradiative relaxation and shields phosphors from quenchers, which enables such molecules to emit efficient RTP emission with decent quantum yields. Furthermore, one such cyclodextrin derivative was utilized to construct a host-guest system incorporating a fluorescent guest molecule, exhibiting excellent RTP-fluorescence dual-emission properties and multicolor emission with a wide range from yellow to purple including white-light emission. This innovative and universal strategy opens up new research paths to construct amorphous metal-free small molecular RTP materials and to design organic white-light-emitting materials using a single supramolecular platform.
- Li, Dengfeng,Lu, Feifei,Wang, Jie,Hu, Wende,Cao, Xiao-Ming,Ma, Xiang,Tian, He
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Read Online
- Visible-Light-Excited Room-Temperature Phosphorescence in Water by Cucurbit[8]uril-Mediated Supramolecular Assembly
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Solid-state materials with efficient room-temperature phosphorescence (RTP) emissions have found widespread applications in materials science, while liquid or solution-phase pure organic RTP emission systems has been rarely reported, because of the nonradiative decay and quenchers from the liquid medium. Reported here is the first example of visible-light-excited pure organic RTP in aqueous solution by using a supramolecular host-guest assembly strategy. The unique cucurbit[8]uril-mediated quaternary stacking structure allows tunable photoluminescence and visible-light excitation, enabling the fabrication of multicolor hydrogels and cell imaging. The present assembly-induced emission approach, as a proof of concept, contributes to the construction of novel metal-free RTP systems with tunable photoluminescence in aqueous solution, providing broad opportunities for further applications in biological imaging, detection, optical sensors, and so forth.
- Huang, Zizhao,Ma, Xiang,Tian, He,Wang, Jie
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Read Online
- Tertiary amine derivatives and organic electroluminescent device including the same
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A UV-region high-energy external light source is effectively absorbed to minimize damage to organic materials in the organic electroluminescent device. 1 Is a cross-sectional view of an organic electroluminescence device according to the present invention. O-2 electrode 1 Or more organic material layers disposed between the (2) and (1) th electrodes. A capping layer is included. The organic material layer and/or the capping layer may include the 1 st amine derivative represented by Formula 3. Chemical Formula 1. Wherein each substituent in Formula 1 is as defined in the description of the invention.
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Paragraph 0152-0154
(2021/06/01)
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- Room-temperature phosphorescence of a water-soluble supramolecular organic framework
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A flexible porous water-soluble supramolecular organic framework was developed, which could efficiently exhibit phosphorescence both in an aqueous phase and in a film state at room-temperature.
- Lin, Xiaohan,Ma, Xiang,Wu, Wenjun,Xu, Chen
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supporting information
p. 10178 - 10181
(2021/10/12)
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- Dianthracene compound containing pyridyl at tail end and application thereof
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The invention provides dianthracene compounds shown in a general formula I in the specification. In the general formula I, L1 and L2 represent single bonds, substituted or unsubstituted heterocyclic aromatic groups of C2-C60 or substituted or unsubstituted hydrocarbon aromatic groups of C6-C60; L3 represents a substituted or unsubstituted heterocyclic aromatic group of C2-C60 or a substituted or unsubstituted hydrocarbon aromatic group of C6-C60; L1, L2 and L3 are shown in a formula in the specification at different time; R10, R18, R21 and R23-R28 represent hydrogen, halogen and substituted or unsubstituted alkyl or alkoxy of C1-C10. The compounds have good luminescence properties, high electron transport capacities and terrific solubility and can be used in luminescent materials, electron transport materials and hole-blocking materials in the electroluminescence field. The invention also provides an organic electroluminescence device at least comprising a pair of electrodes and organic luminescent media between the electrodes. The organic luminescent media at least comprise the dianthracene compounds.
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Paragraph 0086-0089; 0110-0113
(2021/03/03)
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- Dianthracene compound containing pyridyl at tail end and application thereof
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The invention provides dianthracene compounds shown in a general formula I in the specification. In the general formula I, L1 and L2 independently represent single bonds, substituted or unsubstituted heterocyclic aromatic groups of C2-C60 or substituted or unsubstituted hydrocarbon aromatic groups of C6-C60; L3 represents a substituted or unsubstituted heterocyclic aromatic group of C2-C60 or a substituted or unsubstituted hydrocarbon aromatic group of C6-C60; R10, R11, R12, R13, R14, R15, R16, R17, R18, R21, R23, R24, R25, R26, R27 and R28 independently represent hydrogen, halogen and substituted or unsubstituted alkyl or alkoxy of C1-C10. The compounds have good luminescence properties, high electron transport capacities and terrific solubility and can be used in luminescent materials, electron transport materials and hole-blocking materials in the electroluminescence field. The invention also provides an organic electroluminescence device at least comprising a pair of electrodes and organic luminescent media between the electrodes. The organic luminescent media at least comprise the dianthracene compounds.
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Paragraph 0096-0099; 0120-0123
(2021/03/03)
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- Two-photon fluorescent probe capable of targeting mitochondria and preparation method and application of probe
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The invention discloses a two-photon fluorescent probe capable of targeting mitochondria and a preparation method and application of the probe. The structure of the two-photon fluorescent probe is shown as a formula I, wherein R represents a conjugated structure, R' represents alkyl or aryl, R'' represents hydrogen, methyl or methoxy, X represents halogen anions or bi-trifluoromethane sulfonimideanions or hexafluoro-phosphoric acid anions or tetra-fluoroboric acid anions or trifluoromethanesulfonic acid anions. The compound has stronger two-photon excitation fluorescence, a good aggregation-induced luminescence effect, a great mitochondrial targeting function and excellent photoinduced singlet oxygen generation capability.
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Paragraph 0040-0043
(2019/07/16)
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- Diverse Multi-Functionalized Oligoarenes and Heteroarenes for Porous Crystalline Materials
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A modular synthesis of multi-functionalized biphenyl, terphenyl and higher linear oligophenylene dicarboxylic acids and pyridine-terminated oligoarenes by stepwise palladium–catalyzed borylation/Suzuki–Miyaura cross-coupling reactions is described. The presence of several distinct functional groups such as azide, hydroxy, and alkyne, as well as coordinative functional end groups (carboxylic acid or pyridine) combined in a single oligoarene molecular unit at strategic positions offer an advantageous dual-utility. First, these compounds can serve as useful molecular bricks (ditopic organic linkers) in the construction of complex porous crystalline materials. Second, after the assembly into the crystalline coordination networks, orthogonal functional sites within the linker-backbone offer tremendous potential from application perspectives as they can be modified by a wide range of post-synthetic modifications including azide–alkyne click chemistry. This allows further tailoring of the supramolecular assemblies to yield novel multifunctional materials.
- Grosjean, Sylvain,Hassan, Zahid,W?ll, Christof,Br?se, Stefan
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p. 1446 - 1460
(2018/10/24)
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- Monoamine Oxidase (MAO-N) Whole Cell Biocatalyzed Aromatization of 1,2,5,6-Tetrahydropyridines into Pyridines
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A sustainable MAO-N biocatalyzed process for the synthesis of pyridines from aliphatic tetrahydropyridines (THP) has been developed. Pyridine compounds were synthesized under mild reaction conditions and with high conversion, exploiting MAO-N whole cells as aromatizing biocatalysts. The kinetic profile of the whole cell biocatalytic transformation was finally investigated via in situ 19F NMR.
- Toscani, Anita,Risi, Caterina,Black, Gary W.,Brown, Nicola L.,Shaaban, Ali,Turner, Nicholas J.,Castagnolo, Daniele
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p. 8781 - 8787
(2018/09/06)
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- Self-assembling molecular capsules based on α,γ-cyclic peptides
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A new capsule based on a β-sheet self-assembling cyclic peptide with the ability to recognize and release several guests is described. The host structure is composed of two self-complementary α,γ-cyclic peptides bearing a Zn porphyrin cap that is used for the selective recognition of the guest. The two components are linked through two dynamic covalent bonds. The combination of binding forces, including hydrogen bonding, metal coordination, and dynamic hydrazone bonds, allows the reversible recognition of long bipyridine guests. The affinity for these ligands showed a strong dependence on the guest length. Delivery of the encapsulated ligand can be achieved by hydrolysis of hydrazones to disrupt the sandwich complex structure.
- Ozores, Haxel Lionel,Amorín, Manuel,Granja, Juan R.
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supporting information
p. 776 - 784
(2017/05/17)
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- ONE STEP DIRECT ARYLATION OF COMMODITY CHEMICALS TO SPECIALTY CHEMICALS BY TANDEM CATALYTIC PLATFORM
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The present invention relates to a continuous direct arylation process based on a tandem catalyst for synthesizing specialty chemicals. A method for synthesizing an aryl-aryl structure from a substrate selected from the group consisting of benzyl alcohol, benzyl amine and toluene which are low value added compounds is developed using a silver ion-containing tandem catalyst. The method is applied for synthesizing hexaphenyl arylene and can be applied for synthesizing high value added compounds (not only natural substances and chemical compounds but pharmaceutical and agricultural pesticide relative fields) directly from primary raw materials through the reaction.COPYRIGHT KIPO 2017
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Paragraph 0044-0048; 0106
(2018/02/28)
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- Based on 4,4 the structure of the- [...][...] 9, the 9-bit [...] a main body material and its application (by machine translation)
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Based on 4,4 the structure of the- [...][...] 9, the 9-bit [...] a main body material and its application, the present invention discloses a kind HOMO line condition and at the same time has a high level and the main material with excellent performance, its to 4, the 4-bit connected [...][...] as the molecule skeleton structure, in its 9,9 the connecting substituent [...] -position, which can be connected with transmission performance of the cavity diphenylammonium unit Dn, but also can be connected with electronic transmission performance unit An: phosphorusoxychloride unit, sulfur and oxygen unit, in addition to the two special spiral ring-like structure can be formed. The main body material of the present invention synthetic method is simple and easy to operate, which is suitable to be widely used. Main body material by the present invention of the organic electroluminescent light-emitting device is phosphorescent blue light, has high efficiency, high brightness, low efficiency low starting voltage attenuation and electroluminescent performance, can be widely applied to the organic electroluminescent field. (by machine translation)
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- An electron transport material and an organic electroluminescence element using the same
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The compound represented by formula (1) is characterized in being stable in a thin film state even when voltage is applied, and in having a high charge- transporting capability. This compound is suitable for a charge transport material for an organic EL element, and by using this electron transport material in the electron transport layer and/or electron injection layer of an organic EL element, an organic EL element having a long life can be obtained. In formula (1), Py is pyridyl, any hydrogen of this pyridyl can be substituted by an alkyl, cycloalkyl, phenyl, 1-naphthyl, or 2-naphthyl, and the phenyl, 1-naphthyl, or 2-naphthyl can be further substituted by an alkyl or cycloalkyl; R is hydrogen, an alkyl, a cycloalkyl, or an aryl, and any hydrogen of this aryl can be substituted by an alkyl or cycloalkyl.
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Paragraph 0184
(2016/10/08)
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- Space charge transfer compounds and the use of the compound of the organic light-emitting diode and the display device (by machine translation)
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The present invention relates to space charge transfer compounds and the use of the compound of the organic light-emitting diode and the display device, the space charge transfer compound comprises: naphthalene nucleus ; selected from diphenylenimine and phenyl carbazole electron donor portion; and is selected from pyridine, diazine, triazole and phenyl-and-dizole electron acceptor portion, wherein the electron donor portion and the electron acceptor moieties are bonded to the linker after benzene of states the naphthalene nucleus 1 and 8 bit. (by machine translation)
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Paragraph 0080; 0081; 0082
(2016/10/08)
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- COMPOUND, ORGANIC OPTOELECTRIC DEVICE AND DISPLAY DEVICE
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The present invention relates to a compound denoted by chemical formula 1, an organic photoelectron device including the compound and a display device including the organic photoelectron device. In chemical formula 1, L^1 to L^6 and R^1 to R^6 are described as the same as the patent specification.COPYRIGHT KIPO 2015
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Paragraph 0174; 0175; 0176; 0177
(2016/11/28)
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- Discovery of potent, orally bioavailable, small-molecule inhibitors of WNT signaling from a cell-based pathway screen
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WNT signaling is frequently deregulated in malignancy, particularly in colon cancer, and plays a key role in the generation and maintenance of cancer stem cells. We report the discovery and optimization of a 3,4,5-trisubstituted pyridine 9 using a high-throughput cell-based reporter assay of WNT pathway activity. We demonstrate a twisted conformation about the pyridine-piperidine bond of 9 by small-molecule X-ray crystallography. Medicinal chemistry optimization to maintain this twisted conformation, cognisant of physicochemical properties likely to maintain good cell permeability, led to 74 (CCT251545), a potent small-molecule inhibitor of WNT signaling with good oral pharmacokinetics. We demonstrate inhibition of WNT pathway activity in a solid human tumor xenograft model with evidence for tumor growth inhibition following oral dosing. This work provides a successful example of hypothesis-driven medicinal chemistry optimization from a singleton hit against a cell-based pathway assay without knowledge of the biochemical target.
- Adeniji-Popoola, Olajumoke,Aherne, Wynne,Blagg, Julian,Box, Gary,Clarke, Paul A.,Court, William,Crumpler, Simon,Dale, Trevor,De Haven Brandon, Alexis,Eccles, Suzanne A.,Esdar, Christina,Georgi, Katrin,Henley, Alan T.,Hobbs, Steve,Leuthner, Birgitta,Mallinger, Aurlie,Ortiz-Ruiz, Maria-Jesus,Pichowicz, Mark,Poeschke, Oliver,Raynaud, Florence,Rohdich, Felix,Schiemann, Kai,Smith, Elizabeth,Stieber, Frank,Stubbs, Mark,Tepoele, Robert,Thai, Ching,Valenti, Melanie,Waalboer, Dennis,Wienke, Dirk,Wood, Bozena,Workman, Paul
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supporting information
p. 1717 - 1735
(2015/04/27)
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- Phototautomerization in Pyrrolylphenylpyridine Terphenyl Systems
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[4-(2-Pyrrolyl)phenyl]pyridines 2-4 were synthesized and their photophysical properties and reactivity in phototautomerization reactions investigated by fluorescence spectroscopy and laser flash photolysis (LFP). The pKa for the protonation of the pyridine nitrogen in 2-4 was determined by UV-vis and fluorescence titration (pKa = 5.5 for 4). On excitation in polar protic solvents, 2-4 populate charge-transfer states leading to an enhanced basicity of the pyridine (pKa? ≈ 12) and enhanced acidity of pyrrole (pKa? ≈ 8-9) enabling excited-state proton transfer (ESPT). ESPT gives rise to phototautomers and significantly quenches the fluorescence of 2-4. Phototautomers 2-T and 4-T were detected by LFP with strong transient absorption maxima at 390 nm. Phototautomers 2-T and 4-T decayed by competing uni- and bimolecular reactions. However, at pH 11 the decay of 4-T followed exponential kinetics with a rate constant of 4.2 × 106 s-1. The pyridinium salt 4H+ forms a stable complex with cucurbit[7]uril (CB[7]) with 1:1 stoichiometry (β11 = (1.0 ± 0.2) × 105 M-1, [Na+] = 39 mM). Complexation to CB[7] increased the pKa for 4H+ (pKa = 6.9) and changed its photochemical reactivity. Homolytic cleavage of the pyrrole NH leads to the formation of an N-radical because of the decreased acidity of the pyrrole in the inclusion complex. (Figure Presented).
- Basari?, Nikola,Thomas, Suma S.,Bregovi?, Vesna Bla?ek,Cindro, Nikola,Bohne, Cornelia
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p. 4430 - 4442
(2015/05/13)
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- SPIRO-SUBSTITUTED OXINDOLE DERIVATIVES HAVING AMPK ACTIVITY
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The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 108; 109
(2015/01/07)
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- OLEFIN SUBSTITUTED OXINDOLES HAVING AMPK ACTIVITY
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The present invention relates to compounds of formula (I), which have valuable pharmacological properties, in particular are activators of AMPK and which are therefore useful in the treatment of certain disorders that can be prevented or treated by activation of this receptor. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
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Page/Page column 103; 104
(2015/01/07)
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- 3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
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The present application relates to novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.
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Page/Page column 42
(2014/01/18)
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- Long-lived charge separation in novel axial donor-porphyrin-acceptor triads based on tetrathiafulvalene, aluminum(III) porphyrin and naphthalenediimide
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Two self-assembled supramolecular donor-acceptor triads consisting of AlIII porphyrin (AlPor) with axially bound naphthalenediimide (NDI) as an acceptor and tetrathiafulvalene (TTF) as a secondary donor are reported. In the triads, the NDI and TTF units are attached to AlIII on opposite faces of the porphyrin, through covalent and coordination bonds, respectively. Fluorescence studies show that the lowest excited singlet state of the porphyrin is quenched through electron transfer to NDI and hole transfer to TTF. In dichloromethane hole transfer to TTF dominates, whereas in benzonitrile (BN) electron transfer to NDI is the main quenching pathway. In the nematic phase of the liquid crystalline solvent 4-(n-pentyl)-4′-cyanobiphenyl (5CB), a spin-polarized transient EPR spectrum that is readily assigned to the weakly coupled radical pair TTF.+NDI.- is obtained. The initial polarization pattern indicates that the charge separation occurs through the singlet channel and that singlet-triplet mixing occurs in the primary radical pair. At later time the polarization pattern inverts as a result of depopulation of the states with singlet character by recombination to the ground state. The singlet lifetime of TTF.+NDI.- is estimated to be 200-300 ns, whereas the triplet lifetime in the approximately 350 mT magnetic field of the X-band EPR spectrometer is about 10 μs. In contrast, in dichloromethane and BN the lifetime of the charge separation is III porphyrin to form axial covalent and coordination bonds with carboxylic acids and Lewis bases, respectively (see figure; NDI=naphthalenediimide, TTF=tetrathiafulvalene). Upon light excitation the triads undergo sequential electron transfer and by using a liquid-crystalline solvent and high magnetic field, the lifetime of the charge separation can be extended into the microsecond range. Copyright
- Poddutoori, Prashanth K.,Zarrabi, Niloofar,Moiseev, Andrey G.,Gumbau-Brisa, Roger,Vassiliev, Serguei,Van Der Est, Art
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p. 3148 - 3161
(2013/03/28)
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- Novel four-pyridylbenzene-armed biphenyls as electron-transport materials for phosphorescent OLEDs
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A series of four-pyridylbenzene-armed biphenyl derivatives were designed and synthesized as an electron-transport and exciton- and hole-block layer for the fac-tris(2-phenylpyridine)iridium (lr(PPy)3)-based green phosphorescent organic light-em
- Su, Shi-Jian,Tanaka, Daisaku,Li, Yan-Jun,Sasabe, Hisahiro,Takeda, Takashi,Kido, Junji
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supporting information; experimental part
p. 941 - 944
(2009/04/07)
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- Radical dearomatization of arenes and heteroarenes
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The stannane-mediated benzeneselenol-catalyzed addition of aryl iodides to a range of arenes and aromatic hetereocycles has been studied. With furan, thiophene, and several carbocyclic arenes, the addition takes place with quenching of the adduct radical by the catalytic selenol leading to moderate yields of aryl-dihydroarenes. With nitrogen heterocycles, on the other hand, it was not possible to suppress aromatization of the adduct radical and fully aromatized products were isolated. Aryl iodides bearing hydrogen bond donating groups in the ortho-position add to nitrogen heterocycles with high selectivity ortho- to the nitrogen, affording a simple one-step synthesis of potential chelating ligands. While 2-iodophenol is an excellent aryl radical source in these reactions, the homologous 1-iodo-2-naphthol fails owing to its reaction with diphenyl diselenide, which gives 1-phenylseleno-2-naphthol in high yield.
- Crich, David,Patel, Mitesh
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p. 7824 - 7837
(2007/10/03)
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- CATHEPSIN CYSTEINE PROTEASE INHIBITORS
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This invention relates to class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis. They have the following structure: Formula (I).
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- Direct synthesis of heterobiaryls by radical addition to pyridine: Expeditious synthesis of chelating ligands
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The addition of aryl radicals to pyridine may be affected in moderate yield on exposure of aryl iodides to tributyltin hydride, AIBN, and diphenyl diselenide in hot pyridine. Mixtures of ortho-, meta-, and para-aryl substituted pyridines are typically obtained. When the iodide is ortho-substituted with a hydrogen bond donor, such as o-iodophenol, significantly improved selectivity for ortho-substituted pyridines, with potential as bidentate chelating ligands, is obtained.
- Crich, David,Patel, Mitesh
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p. 499 - 504
(2007/10/03)
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- Sulfonamidopyrrolidinone factor Xa inhibitors: Potency and selectivity enhancements via P-1 and P-4 optimization
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Sulfonamidopyrrolidinones were previously disclosed as a selective class of factor Xa (fXa) inhibitors, culminating in the identification of RPR120844 as a potent member with efficacy in vivo. Recognizing the usefulness of the central pyrrolidinone template for the presentation of ligands to the S-1 and S-4 subsites of fXa, studies to optimize the P-1 and P-4 groups were initiated. Sulfonamidopyrrolidinones containing 4-hydroxy- and 4- aminobenzamidines were discovered to be effective inhibitors of fXa. X-ray crystallographic experiments in trypsin and molecular modeling studies suggest that our inhibitors bind by insertion of the 4-hydroxybenzamidine moiety into the S-1 subsite of the fXa active site. Of the P-4 groups examined, the pyridylthienyl sulfonamides were found to confer excellent potency and selectivity especially in combination with 4-hydroxybenzamidine. Compound 20b (RPR130737) was shown to be a potent fXa inhibitor (K1 = 2 nM) with selectivity against structurally related serine proteinases (> 1000 times). Preliminary biological evaluation demonstrates the effectiveness of this inhibitor in common assays of thrombosis in vitro (e.g. activated partial thromboplastin time) and in vivo (e.g. rat FeCl2-induced carotid artery thrombosis model).
- Choi-Sledeski, Yong Mi,McGarry, Daniel G.,Green, Daniel M.,Mason, Helen J.,Becker, Michael R.,Davis, Roderick S.,Ewing, William R.,Dankulich, William P.,Manetta, Vincent E.,Morris, Robert L.,Spada, Alfred P.,Cheney, Daniel L.,Brown, Karen D.,Colussi, Dennis J.,Valeria, Chu,Heran, Christopher L.,Morgan, Suzanne R.,Bentley, Ross G.,Leadley, Robert J.,Maignan, Sebastien,Guilloteau, Jean-Pierre,Dunwiddie, Christopher T.,Pauls, Henry W.
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p. 3572 - 3587
(2007/10/03)
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- Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use
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The present invention is directed to compound of the formula I: STR1 wherein R1, R2, R3, R4, R5, X, Y, and STR2 are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
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- Quinuclidine derivatives as squalene synthase inhibitors
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Compounds of formula (I) and their pharmaceutically acceptable salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1 -CR2 is a double bond; X is selected from --CH2 CH2 --, --CH=CH--, --C C--, --CH2 O--, --CH2 NH--, --NHCH2 --, --CH2 CO--, --COCH2 --, --CH2 S-- and --SCH2 --; Ar1 is a phenylene moiety; Ar2 is a heteroaryl moiety; and wherein one or both of Ar1 and Ar2 may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, carboxyalkyl and alkanoylamino; provided that when R1 is hydroxy, X is not selected from --NHCH2 -- and --SCH2 --; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial, such as hypercholesterolemia and atherosclerosis. Processes for preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medicine.
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- Electrosynthesis of Unsymmetrical Polyaryls by a SRN1-Type Reaction
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Unsymmetrical polyaryls are electrosynthesized in liquid ammonia by a single-step SRN1 reaction in the presence of a redox mediator starting from aromatic halides and 2,6-di-tert-butyl phenoxide.With monoaryl halides activated by electron-withdrawing substituents (N of pyridyl or quinolyl, trifluoromethyl, cyano, sulfone, ester, ketone, alkyl sulfide, N(1+) of anilinium), biaryls are obtained in good yields (between 50 and 95percent).The yields of ter- and quateraryls are lower (40percent maximum).The reaction is extended to other ortho-disubstituted phenols.Elimination reactions of the tert-butyl groups from the products are achieved by a Friedel-Crafts reaction using either trifluoromethanesulfonic acid or aluminum trichloride as catalysts.
- Boy, P.,Combellas, C.,Suba, C.,Thiebault, A.
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p. 4482 - 4489
(2007/10/02)
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- Electrosynthesis of unsymmetrical donor-acceptor polyaryls
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Unsymmetrical Donor-Acceptor Polyaryls are synthesized by an electrochemically induced SRN1 reaction using 2,6-ditertbutyl phenoxide as nucleophile and acceptor substituted polyarylbromides The latter are synthesized by a cross coupling reaction of aromatic organometallic reagents and aromatic halides catalyzed by palladium complexes.
- Boy,Combellas,Thiebault,Amatore,Jutand
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p. 491 - 494
(2007/10/02)
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- Preparation of 1-alkyl-1,4-dihydro-4-oxo-7-(4-pyridyl)-3-quinolinecarboxylic acid
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4-(Bromophenyl)pyridines, useful in preparing bactericides, are prepared by reacting a 4-phenylpyridine with bromine in the presence of an excess of a Lewis acid catalyst, preferably aluminum chloride.
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- A NOVEL BASE-CATALYZED TRANSFORMATION OF α-AZOBENZYL HYDROPEROXIDE INTO BENZOIC ACID. A POSTULATED OXENOID INTERMEDIATE OF THE REACTION.
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α-Azobenzyl hydroperoxide (1) gives benzoic acid, 4-bromophenyl-pyridines (2 and 3) in addition to benzoyldiazene (4) and benzohydrazide (5) in the reaction catalyzed by pyridine; dioxirane (9) or carbonyl oxide (10) is proposed as an intermediate.
- Tezuka, T.,Iwaki, M.
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p. 3109 - 3112
(2007/10/02)
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- SYNTHESIS OF ALKYL-SUBSTITUTED ARYLPYRIDINES IN THE VAPOR PHASE BY THE CHICHIBABIN METHOD
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An industrial cadmium calcium phosphate catalyst was used in the syntheses of pyridine bases in the vapor phase by the Chichibabin method (condensation of carbonyl compounds with ammonia).Alkyl-substituted arylpyridines with the aryl radical at C2, C3, or C4 are formed during the condensation of aromatic aldehydes and ammonia with saturated and unsaturated aldehydes and also with methyl alkyl ketones.
- Soldatenkov, A. T.,Fedorov, V. O.,Chandra, R.,Polosin, V. M.,Mikaya, A. I.,Prostakov, N. S.
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p. 179 - 185
(2007/10/02)
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- Synthetic Applications of N-N Linked Heterocycles. Part 7. The Preparation of 4-Alkyl- and 4-Aryl-pyridines by Regiospecific Attack of Grignard Reagents γ to Quaternary Nitrogen in N-(2,6-Dimethyl-4-oxopyridin-1-yl)pyridinium Salts
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N-(2,6-Dimethyl-4-oxopyridin-1-yl)pyridinium salts (4), new reagents for the regiospecific synthesis of 4-substituted pyridines, give moderate to high yields of 4-alkyl- and 4-aryl-pyridines (8) - (10) on reaction with Grignard reagents.The scope and limitations on the reaction, which proceeds via 1,4-dihydro-intermediates (5) - (7), are explored.No 2-substituted pyridines were detected.Some reactions with organolithium compounds are also described.
- Katritzky, Alan R.,Beltrami, Hector,Sammes, Michael P.
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p. 2480 - 2484
(2007/10/02)
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