- Phosphorescent Pt(ii) complexes bearing a monoanionic C^N^N luminophore and tunable ancillary ligands
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A versatile design strategy is presented towards new monoanionic pincer luminophores, showing that cyclometallating C^N^N ligands can yield phosphorescent Pt(ii) complexes even if a neutral 1,2,3-triazole ring is inserted by click chemistry. The overall charge, intermolecular interactions and excited state properties can be manipulated and controlled by varying the nature of the ancillary ligand, and its effect on the structural and the triplet state characteristics can be thoroughly investigated and correlated by means of theory and spectroscopy.
- Hebenbrock, Marian,Stegemann, Linda,K?sters, Jutta,Doltsinis, Nikos L.,Müller, Jens,Strassert, Cristian A.
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Read Online
- Synthesis of 3,3′-di(2-pyridyl)-1,1′-bi-2-naphthol derivatives
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A new kind of (S)-3,3′-dipyridyl BINOLs (3a-d) with C 2-symmetry were synthesized in 79-84% yields by Suzuki coupling of the diboronic acid dipinacol ester (S)-1 containing a (S)-binaphthyl group with bromopyridine derivatives (2a-d) followed b
- Jin, Ri-Zhe,Bian, Zheng,Kang, Chuan-Qing,Guo, Hai-Quan,Gao, Lian-Xun
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Read Online
- Synthesis, Structure, and Chiroptical Properties of Indolo- and Pyridopyrrolo-Carbazole-Based C2-Symmetric Azahelicenes
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Treatment of 11,12-bis(1,1’-biphenyl-3-yl or 6-phenylpyridin-2-yl)-substituted 11,12-dihydro-indolo[2,3-a]carbazole with an oxidizing system of Pd(II)/Ag(I) induced effective double dehydrogenative cyclization to afford the corresponding π-extended azahelicenes. The optical resolutions were readily achieved by a preparative chiral HPLC. It was found that the pyridopyrrolo-carbazole-based azahelicene that contains four nitrogen atoms exhibits ca. 6 times larger dissymmetry factors both in circularly dichroism (CD) and circularly polarized luminescence (CPL), |gCD| and |gCPL| values being 1.1×10?2 and 4.4×10?3, respectively, as compared with the parent indolocarbazole-based azahelicene. Theoretical calculations at the RI-CC2 level were employed to rationalize the observed enhanced chiroptical responses. The (chir)optical properties of the former helicene was further tuned by a protonation leading to remarkable red-shift with a considerable enhancement of the |gCPL| value.
- Taniguchi, Taisei,Nishii, Yuji,Mori, Tadashi,Nakayama, Ken-ichi,Miura, Masahiro
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supporting information
p. 7356 - 7361
(2021/04/26)
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- Highly Active Fe3O4@SBA-15@NHC-Pd Catalyst for Suzuki–Miyaura Cross-Coupling Reaction
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A novel Pd-NHC functionalized magnetic Fe3O4@SBA-15@NHC-Pd was synthesized and used as an efficient heterogeneous catalyst in the Suzuki–Miyaura C–C bond formation reactions. The Fe3O4@SBA-15@NHC-Pd characterized by X-Ray Diffraction (XRD), X-ray Photoelectron Spectroscopy (XPS), Fourier Transform Infrared (FTIR) spectroscopy, Scanning Electron Microscopy (SEM), Transmission Electron Microscopy?(TEM), Energy Dispersive X-ray analysis (EDX), Thermogravimetric Analysis (TGA), Differential Thermal Analysis (DTA). The Inductively Coupled Plasma-Optical emission spectroscopy (ICP-OES)?analysis was used to determine the exact amount of Pd (0.33?wt%) in Fe3O4@SBA-15@NHC-Pd. The TEM images of the catalyst showed the existence of palladium nanoparticles immobilized in the catalyst's structure, while no reducing agent was used. The NHC moieties in the catalyst structure could be stabilize Pd(0) nanoparticles prevents agglomeration. The magnetic catalyst was effectively used in the Suzuki–Miyaura cross-coupling reaction of substituted phenylboronic acid derivatives with (hetero)aryl bromides in the presence of a K2CO3 at room temperature in aqueous media and magnetic catalyst could be simply extracted from the reaction mixture by an external magnet. Different aryl bromides were converted to coupled-products in excellent yields with spectacular TOFs values (up to 1,960,339?h?1); in the presence of 1?mg of Fe3O4@SBA-15@NHC-Pd catalyst (contains 3.1 × 10–6?mol% Pd) at room temperature in aqueous media. After reusability experiments, it is found that this catalyst was effectively used up to ten times in the reaction with almost consistent catalytic efficiency. A decrease in the activity of the 10th reused catalyst was found as 9%. Graphic Abstract: [Figure not available: see fulltext.]
- ?zdemir, ?smail,Akko?, Mitat,Alt?n, Serdar,Bu?day, Nesrin,Ya?ar, Sedat
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- Magnetite@MCM-41 nanoparticles as support material for Pd-N-heterocyclic carbene complex: A magnetically separable catalyst for Suzuki–Miyaura reaction
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The Magnetite@MCM-41@NHC@Pd catalyst was obtained with Pd metal bound to the NHC ligand anchored to the surface of Fe3O4@MCM-41. It was characterized by Fourier transform infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), X-ray diffraction (XRD), X-ray photoelectron spectroscopy (XPS), energy disperse X-ray analysis (EDX), thermogravimetric analysis (TGA), differential thermal analysis (DTA), and scanning electron microscopy (SEM). The amount of Pd in the Magnetite@MCM-41@NHC@Pd was measure by inductively coupled plasma–optical emission spectroscopy (ICP-OES) analysis. The catalytic activity of Magnetite@MCM-41@NHC@Pd heterogeneous catalyst done on Suzuki–Miyaura reactions of aryl halides with different substituted arylboronic acid derivatives. All coupling reactions afforded excellent yields and up to 408404 Turnover Frequency (TOF) h?1 in the presence of 2 mg of Magnetite@MCM-41@NHC@Pd catalyst (0.0564 mmol g?1, 0.01127 mmol% Pd) at room temperature in 2-propanol/H2O (1:2). Moreover, Magnetite@MCM-41@NHC@Pd catalyst was recover by applying the magnet and reused for another reaction. The catalyst showed excellent structural and chemical stability and reused ten times without a substantial loss in its catalytic performance.
- Akko?, Mitat,Bu?day, Nesrin,Alt?n, Serdar,Ya?ar, Sedat
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- N-heterocyclic carbene Pd(II) complex supported on Fe3O4@SiO2: Highly active, reusable and magnetically separable catalyst for Suzuki-Miyaura cross-coupling reactions in aqueous media
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A new type magnetic nano Fe3O4@SiO2@NHC@Pd-MNPs heterogeneous catalyst was fabricated and characterized by Fourier Transform Infrared (FTIR) spectroscopy, Transmission Electron Microscopy (TEM), X-Ray Diffraction (XRD), X-ray Photoelectron Spectroscopy (XPS), Energy Disperse X-ray analysis (EDX), Thermogravimetric Analysis (TGA), Differential Thermal Analysis (DTA), and Scanning Electron Microscopy (SEM). The loading amount of Palladium (Pd) to magnetic nano Fe3O4@SiO2@NHC@Pd-MNPs was measured by Inductively Coupled Plasma-Optical Emission Spectroscopy (ICP-OES) analysis. The catalytic activity of magnetic nano Fe3O4@SiO2@NHC@Pd-MNPs heterogeneous catalyst was examined on Suzuki-Miyaura cross-coupling reactions of aryl halides with different substituted arylboronic acid derivatives. All coupling reactions yielded excellent results and high TOF (up to 76528 h?1) in the presence of 2 mg of Fe3O4@SiO2@NHC@Pd-MNPs catalyst (0.0197 mmolg?1, 0.00394 mmol%Pd) at 80 °C in 2-propanol/H2O (1:2). In addition, the magnetic nano Fe3O4@SiO2@NHC@Pd-MNPs catalyst was easily recovered by using an external Nd-magnet and reused for the Suzuki cross-coupling reactions. The catalyst showed strong structural and chemical stability and was reused six times without losing its catalytic activity substantially.
- Akko?, Mitat,Bu?day, Nesrin,Alt?n, Serdar,Kiraz, Nadir,Ya?ar, Sedat,?zdemir, ?smail
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- Palladium (II) complexes chelated by 1-substituted-4-pyridyl-1H-1,2,3-triazole ligands as catalyst precursors for selective ethylene dimerization
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A series of neutral as well as cationic palladium methyl complexes bearing 1-substituted-4-pyridyl-1H-1,2,3-triazole ligands were prepared and fully characterized by a range of analytical techniques. Conventional and 2D NMR spectroscopy as well as single-crystal X-ray diffraction analysis unambiguously determined the molecular structure of the complexes. The neutral complexes activated by methylaluminoxane were found to be effective catalysts in the ethylene dimerization reaction. The catalyst performance of the in-situ-generated active species was compared with the discrete cationic complexes of the same ligand scaffold. Activities and selectivities for the two systems were remarkably similar, pointing to similarities in the nature of the active species. Both catalytic systems showed a strong correlation of activity and selectivity with the nature of the ligand scaffold. Highest activities were attained when electron-withdrawing groups were incorporated into the triazole ring, while increasing steric bulk in the ortho-position on the pyridyl ring of the ligand led to the almost exclusive dimerization of ethylene with selectivities up to 94% observed toward 1-butene.
- Joseph, Mohammed Cassiem,Swarts, Andrew John,Mapolie, Selwyn Frank
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- Organic compound, polymer, mixture, composition, and organic electronic device
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The invention discloses an organic compound (1), and a polymer, a mixture, a composition and an organic electronic device which contain contain the organic compound. According to the invention, triphenylene, carbonyl and aza-aromatic ring groups are prope
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Paragraph 0220; 0224; 0227; 0263; 0267; 0270
(2020/02/14)
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- Group 4 Post-Metallocenes Supported by [OCH2 N,C(σ-aryl)] Auxiliaries Bearing a Seven-Membered Metallacycle: Synthesis, Characterization, and Catalysts for Olefin Polymerization
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A series of pyridine-2-phenolate-6-(σ-aryl) [OCH2 N,C] group 4 bis(benzyl) precatalysts, featuring a flexible O,N-donor chelate, have been prepared and characterized by multinuclear NMR spectroscopy. These complexes adopt C1/su
- Liu, Cham-Chuen,Liu, Qian,Yiu, Shek-Man,Chan, Michael C. W.
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supporting information
p. 2963 - 2971
(2019/08/22)
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- 1H-[1,2,4]Triazolo[4,3-a]pyridin-4-ium and 3H-[1,2,4]triazolo[4,3-a]quinolin-10-ium derivatives as new intercalating agents for DNA
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Two new cationic DNA intercalators, 3-phenyl-1-(6-phenylpyridin-2-yl)-1H-[1,2,4]triazolo[4,3-a]pyridin-4-ium (1a)+ and 1-phenyl-3-(6-phenylpyridin-2-yl)-3H-[1,2,4]triazolo[4,3-a]quinolin-10-ium (1b)+, were synthesized from 2-chloropyridine and 2-chloroquinoline, respectively, in a four-step procedure. Generation of the hydrazine, followed by condensation with an aldehyde to give a hydrazone and subsequent Buchwald-Hartwig amination gave a mixture of E- and Z-configured N,N-functionalized hydrazones. Finally, oxidative cyclisation gave rise to the formation of the cationic DNA intercalators, whose molecular structures were determined by single-crystal X-ray diffraction analysis of the hexafluorophosphate and tribromide salt of (1a)+ and (1b)+, respectively. The intercalative binding of (1a)PF6 and (1b)PF6 to ctDNA was confirmed by means of UV, CD and luminescence spectroscopy, determination of the DNA melting temperature and by rheology measurements.
- Hebenbrock, Marian,Müller, Jens
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p. 885 - 893
(2018/09/06)
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- Propionic Acid Derivatives and Methods of Use Thereof
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Provided herein are compounds and pharmaceutical compositions of formula I where R1, R2, R3, R4, R5 and R6 are as described herein. Also provided pharmaceutically acceptable salts or stereoisomers of these compounds. In addition methods are provided for inhibiting the binding of an integrin to treat various pathophysiological conditions.
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Paragraph 1828; 1829
(2018/11/21)
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- A palladium catalyst system for the efficient cross-coupling reaction of aryl bromides and chlorides with phenylboronic acid: Synthesis and biological activity evaluation
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New benzimidazolium salts 1a-c and their palladium bis-N-heterocyclic carbene complexes 2a-c and palladium PEPPSI-type complexes 3a-c were designed, synthesized and structurally characterized by NMR (1H and 13C), IR, DART-TOF mass spectrometry and elemental analysis. Then these complexes 2-3 were employed in the Suzuki-Miyaura cross-coupling reaction of substituted arenes with phenylboronic acid under mild conditions in toluene and DMF/H2O (1/1) to afford functionalized biaryl derivatives in good to excellent yields. The antibacterial activity of palladium bis-N-heterocyclic carbene complexes 2a-c and palladium PEPPSI-type complexes 3a-c was measured by disc diffusion method against Gram positive and Gram negative bacteria. Compounds 2a, 2c and 3a-c exhibited potential antibacterial activity against four bacterial species among the five used indicator cells. The product 2b inhibits the growth of the all five tested microorganisms. Moreover, the antioxidant activity determination of these complexes 2-3, using 2.2-diphenyl-1-picrylhydrazyl (DPPH) as a reagent, showed that compounds 2a-c and 3b possess DPPH antiradical activity. The higher antioxidant activity was obtained from the product 2b which has radical scavenging activity comparable to that of the two used positive controls (gallic acid GA and tutylatedhydroxytoluene BHT ). Investigation of the anti-acetylcholinesterase activity of the studied complexes showed that compounds 2b, 3a, and 3b exhibited moderate activity at 100 μg/mL and product 2b is the most active.
- Lamia, Boubakri,Chakchouk-Mtibaa, Ahlem,Hallouma, Bilel,Mansour, Lamjed,Mellouli, Lotfi,?zdemir, Ismail,Ya?ar, Sedat,Hamdi, Naceur
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- Synthesis and catalytic applications of palladium N-heterocyclic carbene complexes as efficient pre-catalysts for Suzuki-Miyaura and Sonogashira coupling reactions
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A new palladium complex series with N-heterocyclic carbene (NHC), pyridine and phosphine ligands, PdCl2(L)NHC (2a-c)(L = NHC), PdCl2(L1)NHC(3a-c)(L1 = pyridine), PdCl2(L2)NHC(4a-c)(L2 = triphenylphosphine) was synthesised and fully characterized. The catalytic activities of these complexes were screened for the Sonogashira and Suzuki-Miyaura reactions between arylhalides and phenylacetylene, and phenylboronic acid, respectively. The results pointed out that the carbene/phosphine complexes 4a-c exhibited excellent catalytic activities as compared to 2a-c, 3a-c, and the well-known systems for the palladium-catalysed Sonogashira reaction. The reactivity of 4a-c in these preliminary Sonogashira coupling tests seems to be higher than that of previously reported catalytic systems based on Pd(NHC) moieties. These new palladium NHC complexes are among the first reported palladium catalysts that are efficient for catalysing the Sonogashira reaction from arylchloride substrates.
- Boubakri,Yasar,Dorcet,Roisnel,Bruneau,Hamdi,Ozdemir
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p. 5105 - 5113
(2017/07/11)
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- TRANSITION METAL COMPLEXES OF TRIDENTATE DIANIONIC CNN LIGANDS, PRODUCTION AND USE THEREOF
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New pyridylamide transition metal complex compositions for olefin polymerizations are described herein featuring a 7-membered chelate ring and a cyclometalated hydrocarbyl group. When activated using typical activators these compositions form active alkene polymerization catalysts. Theses novel catalyst compositions are shown herein to be active for olefin polymerization, especially for preparation of polymers containing ethylene.
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Paragraph 0137
(2017/01/23)
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- Organometallic compound and organic light-emitting device including the same
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Organic metal compound and said organometallic compounds is disclosure is an organic light emitting device. (by machine translation)
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Paragraph 0490; 0518; 0519; 0520; 0521; 0522
(2016/10/07)
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- HETEROCYCLIC COMPOUNDS AND USE OF SAME
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Novel heterocyclic compounds are provided which display useful efficacy in the treatment of diseases caused by trypanosomatids. Particularly, the compounds of the invention are useful in the treatment of HAT and/or Chagas disease and/or Animal African trypanosomiasis (AAT).
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Paragraph 0033; 00179; 00200
(2016/01/08)
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- Methyl-D3 substd. organoiridium complex
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An organic light emitting device comprising an anode; a cathode; andan organic layer, disposed between the anode and the cathode, wherein the organic layer comprises a compound comprising a ligand having deuterium substitution, wherein deuterium is locate
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Paragraph 0139; 0140
(2016/10/07)
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- Fluoranthene derivative and organic electroluminescent device including the same
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Provided are a fluoranthene derivative represented by chemical formula 1 and an organic electroluminescent device comprising the same. In the chemical formula 1, definition of each substituent is as defined in the detailed description of the present invention. The organic electroluminescent device comprises: a first electrode; a second electrode; and one or more organic films disposed between the electrodes, wherein the organic films comprise the fluoranthene derivative.(AA) Negative electrode(BB) Electron injection layer(CC) Electron transport layer(DD) Light emitting layer(EE) Hole transport layer(FF) Hole injection layer(GG) Positive electrode(HH) Organic filmCOPYRIGHT KIPO 2016
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Paragraph 0113; 0114; 0115
(2016/10/07)
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- Synthesis and characterization of hydrophilic theophylline base compounds and their use as ligands in the microwave assisted Suzuki-Miyaura couplings of halopyridines in water Dedicated to the memory of Prof. Dr. Armando Cabrera Ortiz pioneer of Catalysis in Mexico. Great Researcher but above all a Great Human Being
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Xanthine derivatives, caffeine (L1), theobromine (L2), theophylline (L3), 7-(β-hydroxyethyltheophylline) (L4), (7-(2,3-dihydroxypropyl)theophylline) (L5), and theophylline 7-acetic acid (L6) and the acetylated derivatives of the later three (L7-L9) were employed as ligands for the in situ palladium catalyzed Suzuki-Miyaura cross couplings of a series of halogenated pyridines. Optimized conditions were found where the diacetylated ligand (L8) was determined to be the best for this process, producing good to excellent yields in the couplings of halogenated anilines with phenylboronic acid under mild reaction conditions in water using microwave irradiation.
- Conelly-Espinosa, Patricia,Toscano, Ruben A.,Morales-Morales, David
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p. 5841 - 5845
(2015/01/09)
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- Triarylbismuthanes as threefold aryl-transfer reagents in regioselective cross-coupling reactions with bromopyridines and quinolines
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Cross-coupling studies using bromopyridines and bromoquinolines with triarylbismuths as threefold coupling reagents in substoichiometric amounts under Pd-catalysed conditions are disclosed. The reactivity was high with both mono- and dibromopyridyl substrates, and mono- and bis-couplings were carried out regioselectively. A library of monoaryl and diaryl pyridines was formed in high yields. A one-pot strategy provided a simple and straightforward synthesis of both symmetrical and unsymmetrical diarylpyridines. Arylations of 2-bromo- and 3-bromoquinolines were achieved with triarylbismuth reagents. This study demonstrates that triarylbismuths may be used as threefold arylating reagents for the synthesis of aryl pyridines and quinolines through couplings with bromopyridines and bromoquinolines under Pd-catalysed conditions. Copyright
- Rao, Maddali L.N.,Dhanorkar, Ritesh J.
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p. 5214 - 5228
(2014/10/15)
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- POLYCYCLIC COMPOUNDS AS LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS
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Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
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Page/Page column 32
(2011/04/24)
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- EP2 RECEPTOR AGONISTS
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A compound of formula (III): or a salt, solvate and chemically protected form thereof, wherein: R5 is an optionally substituted C5-20 aryl or C4-20alkyl group; L′ is a single bond, —O— or —C(═O)—; A is selected from the group consisting of: formulae (i) (ii) (iii) wherein X and Y are selected from the group consisting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O, and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; D is selected from: formulae (i) (ii) (iii) (iv) (v) (vii) (viii) (ix) B is selected from the group consisting of: formulae (A) (B) where RP6 is selected from fluoro and chloro; and R2 is either: (i) —CO2H; (ii) —CONH2; (iii) —CH2—OH; or (iv) tetrazol-5-yl.
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Page/Page column 21
(2010/06/14)
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- TRIDENTATE PLATINUM (II) COMPLEXES
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A platinum (II) complex of the general formula (I) or (II), in which Ar1, Ar2, and Ar3 are each independently aryl, heteroaryl, or heterocyclic. Ar1, Ar2, and Ar3 together form a tridentate ligand coordinated to the platinum through atoms X, Y, and Z, respectively, and X, Y, and Z are independently carbon or nitrogen. V is a bridging group or a covalent bond, and W is an anion. In general formula (I) in some cases, Ar1 is an anion and Ar2 and Ar3 are neutral; in other cases, Ar1 and Ar3 are neutral and Ar2 is an anion. In general formula (II), in some cases, Ar3 is an anion and Ar1 and Ar2 are neutral; in other cases, Ar1 and Ar3 are neutral and Ar2 is an anion. The complexes are asymmetric. The complexes emit in the UV to near IR range and are useful as emitters for organic light emitting devices.
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Page/Page column 23
(2009/10/22)
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- Practical routes to 2,6-disubstituted pyridine derivatives
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We report the synthesis of a series of 2,6-disubstituted pyridines in a straightforward manner starting from readily available 2-substituted pyridines. The main sequence involves a selective ?-lithiation reaction with halogen functionalization followed by
- Vandromme, Lucie,Reissig, Hans-Ulrich,Groeper, Susie,Rabe, Juergen P.
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experimental part
p. 2049 - 2055
(2009/04/04)
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- ANTHRACENE DERIVATIVE AND ORGANIC ELECTROLUMINESCENT ELEMENT USING THE SAME
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This invention provides an anthracene derivative, which has a heteroaryl group containing a nitrogen-containing six-membered ring and has a specific structure and comprises an organic thin film layer having a single or multilayer structure including at least a luminescent layer between a cathode and an anode. At least one of the organic thin film layers contains the anthracene derivative either solely or as a component of a mixture. The organic electroluminescent element can emit homogeneous luminscence for a long period of time and has a prolonged service life. The anthracene derivative can realize the above organic electroluminescent element.
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(2008/06/13)
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- PLATINUM COMPLEX AND LUMINESCENT ELEMENT
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Provision of a novel platinum complex which is useful as a material for a light-emitting device of good light emission characteristic and light emission efficiency, and a novel light-emitting material that may be utilized in various fields. A platinum complex represented by the following general formula (1): (in which two rings of ring A, ring B, ring C, and ring D represent nitrogen-containing heterocyclic rings which may have a substituent and the remaining two rings of them represent aryl rings or hetero aryl rings which may have a substituent, the ring A and the ring B, the ring A and the ring C or/and the ring B and the rind D may form condensed rings. Two of X1, X2, X3, and X4 represent nitrogen atoms coordination bonded to a platinum atom and the remaining two of them represent carbon atoms or nitrogen atoms. Q1, Q2, and Q3 each represents a bond, oxygen atom, sulfur atom or bivalent group, two of Z1, Z2, Z3, and Z4 represent coordination bonds, and the remaining two of them represent covalent bonds, oxygen atoms or sulfur atoms), and a light-emitting device containing the platinum complex.
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Page/Page column 24
(2008/06/13)
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- Novel gamma secretase inhibitors
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This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X—C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
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- PROCESS FOR PRODUCING BIARYL COMPOUND
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A process for producing a biaryl compound, characterized by reacting an arylhydrazine compound, hydrogen peroxide and an aryl compound. When the reaction is conducted in the presence of a given metal or a compound of the metal or in the presence of a metal oxide obtained by reacting the given metal or a compound of the metal with hydrogen peroxide, then the yield of the biaryl compound is improved.
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- Novel gamma secretase inhibitors
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This invention discloses novel gamma secretase inhibitors of the formula: wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —XC(O)Y, alkylene-XC(O)Y, cycloalkylene-X-C(O)—Y, —CH—X—C(O)—NR3—Y or —CH—X—C(O)—Y, wherein X and Y are as defined herein; each R3 and each R3A are independently H, or alkyl; R11 is aryl, heteroaryl, alkyl, cycloalkyl, arylalkyl, arylcycloalkyl, heteroarylalkyl, heteroarylcycloalkyl, arylheterocycloalkyl, or alkoxyalkyl. Also disclosed is a method of treating Alzheimer's Disease using one or more compounds of the invention.
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- Synthesis of novel halopyridinylboronic acids and esters. Part 4: Halopyridin-2-yl-boronic acids and esters are stable, crystalline partners for classical Suzuki cross-coupling
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This paper describes some methods for the synthesis and the isolation of novel 5 or 6-halopyridin-2-yl-boronic acids and esters 3, 4, 7. These compounds are prepared via a regioselective halogen-metal exchange using n-butyllithium and subsequent quenching with triisopropylborate starting from appropriate dihalopyridines. All substrates studied to date provided a single regioisomeric boronic acid or ester product. Additionally, these compounds have been found to undergo Pd-catalysed coupling with arylhalides and authorise a strategy to produce new pyridines libraries.
- Bouillon, Alexandre,Lancelot, Jean-Charles,Santos, Jana Sopkova De Oliveira,Collot, Valérie,Bovy, Philipppe R.,Rault, Sylvain
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p. 10043 - 10049
(2007/10/03)
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- Aminoalkoxide-mediated formation and stabilization of phenylpyridyllithium: Straightforward access to phenylpyridine derivatives
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It is shown that lithium aggregates promoted the efficient metalation of phenylpyridines and stabilization of phenylpyridyllithium. The BuLi-LiDMAE superbase prevented dimerization or nucleophilic addition encountered with t-BuLi or n-BuLi. The reported s
- Gros, Philippe,Fort, Yves
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p. 2028 - 2029
(2007/10/03)
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- Syntheses of substituted pyridines, quinolines and diazines via palladium-catalyzed cross-coupling of aryl Grignard reagents
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The palladium-catalyzed cross-coupling reactions between arylmagnesium halides (phenylmagnesium chloride, mesitylmagnesium bromide, 4-(methoxycarbonyl)phenylmagnesium chloride and 4-cyanophenylmagnesium chloride) and halopyridines allowed the synthesis of substituted pyridines. Owing to the remarkably mild conditions used (often below 0°C), the reaction could be extended to the use of functionalized halopyridines, haloquinolines and halodiazines.
- Bonnet, Véronique,Mongin, Florence,Trécourt, Fran?ois,Quéguiner, Guy,Knochel, Paul
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p. 4429 - 4438
(2007/10/03)
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- Herbicidal 2-(hectero)aryloxy-6-arypyridines and 2-aryl-4-(hetero)aryloxypyrimidines
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New herbicidal pyridine and pyrimidine derivatives of general formula (I), STR1 wherein Z represents a nitrogen atom or a C--H group; A represents an optionally substituted aryl group or an optionally substituted 5- or 6-membered nitrogen-containing heteroaromatic group; n represents an integer from 0 to 2 and R1 or each R1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R2 or each R2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.
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- Herbicidal 2, 6-disubstituted pyridines and 2, 4-disubstituted pyrimidines
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New herbicidal pyrimidine derivatives of general formula (I), STR1 wherein Z represents a nitrogen atom; A represents a substituted aryl group or an optionally substituted pyridyl or pyrazolyl group; n represents an integer from 0 to 2 and R1 or each R1 independently represents a hydrogen atom or an optionally substituted alkyl, alkoxy, alkylthio or dialkylamino group; m represents an integer from 0 to 5 and R2 or each R2 independently represents a hydrogen or a halogen atom or an optionally substituted alkyl, haloalkyl, haloalkoxy, alkoxy, alkylthio group or a nitro, cyano or a halosulphonyl group; and X represents an oxygen or sulphur atom.
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- Bis (biaryl) compounds as inhibitors of leukotriene biosynthesis
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Compounds having the Formula I: STR1 are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection and in preventing the formation of atherosclerotic plaques.
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