- Chiral Self-Discrimination and Guest Recognition in Helicene-Based Coordination Cages
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Chiral nanosized confinements play a major role for enantioselective recognition and reaction control in biological systems. Supramolecular self-assembly gives access to artificial mimics with tunable sizes and properties. Herein, a new family of [Pd2L4] coordination cages based on a chiral [6]helicene backbone is introduced. A racemic mixture of the bis-monodentate pyridyl ligand L1 selectively assembles with PdII cations under chiral self-discrimination to an achiral meso cage, cis-[Pd2L1P2L1M2]. Enantiopure L1 forms homochiral cages [Pd2L1P/M4]. A longer derivative L2 forms chiral cages [Pd2L2P/M4] with larger cavities, which bind optical isomers of chiral guests with different affinities. Owing to its distinct chiroptical properties, this cage can distinguish non-chiral guests of different lengths, as they were found to squeeze or elongate the cavity under modulation of the helical pitch of the helicenes. The CD spectroscopic results were supported by ion mobility mass spectrometry.
- Schulte, Thorben R.,Holstein, Julian J.,Clever, Guido H.
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Read Online
- 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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Read Online
- Catalytic Enantioselective Synthesis of Pyridyl Sulfoximines
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With unique chemical and biological activity, sulfoximines have attracted enormous attention in the past decades, whereas limited reports exist for their synthesis via asymmetric catalysis. We report the synthesis of chiral sulfoximines through the desymmetrizing N-oxidation of pyridyl sulfoximines using an aspartic acid-containing peptide catalyst. Various mono- and bis-pyridyl sulfoximine oxides are obtained with up to 99:1 er. The directing group introduced on the substrate highly enhances the enantioinduction and could be easily removed to give the free N-H sulfoximines. Additionally, peptides with methyl ester and the methyl amide C-terminal protecting group give the opposite enantiomers of the product. A binding model is proposed to explain this phenomenon.
- Miller, Scott J.,Tang, Yu
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supporting information
p. 9230 - 9235
(2021/07/01)
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- Compound with AMPK agonistic activity and preparation and application of prodrug thereof
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The invention relates to a compound with AMPK agonistic activity and a prodrug thereof, and as well as a preparation method and medical application of a prodrug thereof. The compound has the structure shown in the formula (I), and the prodrug of the compound has the structure shown in the formula (II), wherein each group and the substituent are as defined in the specification. The invention discloses a preparation method of the compound and application of the compound in prevention and treatment AMPK related diseases, and the AMPK related diseases include, but are not limited to, energy metabolism abnormality related diseases. Neurodegenerative diseases and inflammation-related diseases and the like.
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Paragraph 0145-0148; 0239-0242
(2021/10/27)
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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; 0114-0117
(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; 0124-0127
(2021/03/03)
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- INDOLO HEPTAMYL OXIME ANALOGUE AS PARP INHIBITOR
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Disclosed is a type of indolo heptamyl oxime compounds as a PARP inhibitor. Specifically disclosed are a compound as represented by formula (II) and a pharmaceutically acceptable salt thereof.
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Paragraph 0087; 0091
(2021/12/15)
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- Visible-Light-Photosensitized Aryl and Alkyl Decarboxylative Functionalization Reactions
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Despite significant progress in aliphatic decarboxylation, an efficient and general protocol for radical aromatic decarboxylation has lagged far behind. Herein, we describe a general strategy for rapid access to both aryl and alkyl radicals by photosensitized decarboxylation of the corresponding carboxylic acids esters followed by their successive use in divergent carbon–heteroatom and carbon–carbon bond-forming reactions. Identification of a suitable activator for carboxylic acids is the key to bypass a competing single-electron-transfer mechanism and “switch on” an energy-transfer-mediated homolysis of unsymmetrical σ-bonds for a concerted fragmentation/decarboxylation process.
- Patra, Tuhin,Mukherjee, Satobhisha,Ma, Jiajia,Strieth-Kalthoff, Felix,Glorius, Frank
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supporting information
p. 10514 - 10520
(2019/07/12)
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- Bipyridyl derivative and application thereof
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The present invention provides a novel compound, which has a structure general formula represented by a formula (I), wherein Ar1 and Ar2 are independently selected from an aromatic hydrocarbon derivative group containing benzimidazoyl, an aromatic hydrocarbon derivative group containing a pyridine group, substituted or unsubstituted C6-C30 aromatic hydrocarbon, and a substituted or unsubstituted C6-C30 fused ring aromatic hydrocarbon group, and R1 and R2 are independently and respectively selected from H, C1-C12 aliphatic hydrocarbon radical, phenyl, substituted phenyl, naphthyl, substituted naphthyl, biphenyl and substituted biphenyl. According to the present invention, the compound has characteristics of stable character, simple preparation process, high luminous efficiency and high carrier mobility, and can be used for the electron transport layer of the electroluminescent element, and the device applying the compound has characteristics of significant driving voltage reducing and current efficiency improving. The formula (I) is defined in the instruction.
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Paragraph 0082-0086
(2019/08/06)
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- Preparation method of niraparib tosilate monohydrate
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The invention discloses a preparation method of a compound 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide tosilate monohydrate. The method includes: carrying out Ulman reaction on 1H-indazole-7-methyl formate and (S)-3-(4-halogenophenyl)piperidine-1-tert-butyl formate to prepare 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-methyl formate, then under the conditions of ammonia gas and p-toluenesulfonic acid, preparing 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide tosilate monohydrate. The invention aims to avoid the disadvantages of existing methods, shortens the preparation route, and provides the preparation method of the 2-[4-((3S)-3-piperidyl)phenyl]-2H-indazole-7-formamide tosilate monohydrate with high chiral purity, and the method has the characteristics of mild reaction and easy operation.
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Paragraph 0034; 0035
(2017/07/21)
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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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- Octahedral [Pd6L8]12+ Metallosupramolecular Cages: Synthesis, Structures and Guest-Encapsulation Studies
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Four planar tripyridyl ligands (Ltripy), 1,3,5-tris(pyridin-3-ylethynyl)benzene 1 a, 1,3,5-tris[4-(3-pyridyl)phenyl]benzene 2 a, and the hexyloxy chain functionalized derivatives 1,3,5-tris[(3-hexyloxy-5-pyridyl)ethynyl]benzene 1 b, and 1,3,5-tris[4-(3-hexyloxy-5-pyridyl)phenyl]benzene 2 b, were synthesized and used to generate a family of [Pd6(Ltripy)8](BF4)12 octahedral cages (Ltripy=1 a, b or 2 a, b). The ligands and cages were characterized using a combination of 1H, 13C, and DOSY nuclear magnetic resonance (NMR) spectroscopy, high resolution electrospray mass spectrometry (HR-ESI-MS), infrared (IR) spectroscopy, elemental analysis, and in three cases, X-ray crystallography. The molecular recognition properties of the cages with neutral and anionic guests were examined, in dimethyl sulfoxide (DMSO), using NMR spectroscopy, mass spectrometry and molecular modeling. No binding was observed with simple aliphatic and aromatic guest molecules. However, anionic sulfonates were found to interact with the octahedral cages and the binding interaction was size selective. The smaller [Pd6(1 a, b)8]12+ cages were able to interact with three p-toluenesulfonate guest molecules while the larger [Pd6(2 a, b)8]12+ systems could host four of the anionic guest molecules. To probe the importance of the hydrophobic effect, a mixed water–DMSO (1:1) solvent system was used to reexamine the binding of the neutral organic guests adamantane, anthracene, pyrene and 1,8-naphthalimide within the cages. In this solvent system all the guests except adamantane were observed to bind within the cavities of the cages. NMR spectroscopy and molecular modeling indicated that the cages bind multiple copies of the individual guests (between 3–6 guest molecules per cage).
- Kim, Tae Y.,Digal, Lori,Gardiner, Michael G.,Lucas, Nigel T.,Crowley, James D.
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supporting information
p. 15089 - 15097
(2017/10/11)
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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 0093; 0094; 0095
(2016/10/08)
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- Compound containing quinoxaline and pyridine groups and organic electroluminescent device thereof
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The invention provides an organic electroluminescent compound containing quinoxaline and pyridine groups. The compound has better heat stability, high luminous efficiency and high luminous purity, can be used for manufacturing an organic electroluminescent device, and is applied to the field of organic solar cells, organic thin film transistors or organic photoreceptors. The invention also provides the organic electroluminescent device, which comprises an anode, a cathode and an organic layer, wherein the organic layer includes more than one layer in a luminous layer, a hole injection layer, a hole transporting layer, a hole blocking layer, and electron injection layer and an electron transporting layer; at least one layer in the organic layer contains a compound as shown by a structural formula I which is as shown in the description.
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Paragraph 0056; 0057
(2016/10/08)
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- Direct arylation of pyridines without the use of a transition metal catalyst
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A method for achieving the direct arylation of pyridines with phenylhydrazine hydrochloride was developed in this study. This new reaction proceeds readily at room temperature without the use of any transition metal catalysts. This method allows rapid access to various arylated heterocycles that are more difficult to access through traditional methods.
- Li, Yahui,Liu, Wei,Kuang, Chunxiang
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supporting information
p. 7124 - 7127
(2014/07/07)
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- LINCOSAMIDE DERIVATIVE, AND ANTIBACTERIAL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT
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An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
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Page/Page column 24
(2010/04/24)
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- Quinoxaline derivate, and light-emitting element, light-emitting device, and electronic device using quinoxaline derivative
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An object is to provide a novel quinoxaline derivative. Another object is to provide a light-emitting element with low driving voltage. Still another object is to provide a light-emitting element with low power consumption. Yet another object is to provide a light-emitting device and an electronic device each having low power consumption by using such a light-emitting element. A quinoxaline derivative is provided which has a structure in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon of a pyridine ring are bound via an arylene group.
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Page/Page column 141
(2009/06/27)
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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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- METHOD OF PREPARING INHIBITORS OF PHOSPHODIESTERASE-4
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In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula
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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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- Alkyne-aryl phosphodiesterase-4 inhibitors
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Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.
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- 1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors
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Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.
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- Self-Assembly of 3-[4′-(Diethylboryl)phenyl]pyridine and 3-[3′-(Diethylboryl)phenyl]pyridine: Synthesis, Structural Features, and Stability in Solution
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The self-assembly of 3-[4′-(diethylboryl)phenyl]pyridine (3) and 3-[3′-(diethylboryl)phenyl]pyridine (4) was investigated by 1H and 11B NMR spectroscopies and vapor pressure osmometry. It can be seen that in solution 3 affords an equilibrium mixture of oligomers including a cyclic trimer as a major component via intermolecular boron-nitrogen coordination bonds, which is supported by temperature-, concentration-, and solvent-dependent behaviors of 3. In contrast, 4 seems to afford a mixture of oligomers including a cyclic dimer in solution. Judging from the low coalescence temperature in variable-temperature NMR in toluene-d8 and easy scrambling with the corresponding 3-[(diethylboryl)pheny]-5-methoxypyridines at ambient temperature, it is concluded that the intermolecular boron-nitrogen coordination bonds made by 3 or 4 are weaker than those formed by 3-(diethylboryl)pyridine (1) or 2-(diethylboryl)-5-methylpyridine (2). Poor thermal stability was supported by electrospray mass spectrometry and structural analyses utilizing a semi-empirical molecular orbital calculation AM1. It is noted that in the assembly of 4 there is a tendency to maintain high tetrahedral character at the boron atom in the complex at the expense of strain energy. Thus, these features of 3 and 4 in solution are in marked contrast to those of 1 and 2.
- Wakabayashi, Shigeharu,Sugihara, Yoshikazu,Takakura, Katsuto,Murata, Shigeru,Tomioka, Hideo,Ohnishi, Shiho,Tatsumi, Kazuyuki
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p. 6999 - 7008
(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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- 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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- Heterocyclic derivatives
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Quinuclidine derivatives of formula I, and their pharmaceutically acceptable salts, STR1 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; Ar1 is a phenylene moiety; Ar2 is a 6-membered heteroaryl moiety containing one or two nitrogen atoms; and wherein one or both of Ar1 and Ar2 may optionally bear one or more substituents such as halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and O-alkyl ethers of said oxime derivatives; inhibit squalene synthase and are therefore useful in treating treating diseases and medical conditions where inhibition of squalene synthase is desirable, for example in treating hypercholesterolemia and atherosclerosis. Processes for the preparation of these derivatives and pharmaceutical compositions containing them are also referred to as well as their use in medicine.
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- 11β-phenyl-14βH steroids
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New 11β-phenyl-14βH-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N?OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an α-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C1-8 alkoxy, mercapto or thioalkyl group, R2 is a methyl or ethyl residue, and R3 /R4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.
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- SYNTHESIS OF MESOMORPHIC 2-ALKYL-5-(p-CYANOPHENYL)PYRIDINES
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A new series of liquid-crystal derivatives of 2-alkyl-5-(p-cyanophenyl)pyridines were obtained by halogenation of 2-alkyl-5-phenylpyridines under the conditions of the Birckenbach-Gubo-Waters reaction with subsequent conversion of the 2-alkyl-5-(p-bromo- or iodophenyl)pyridines to the cyano derivatives.
- Pavlyuchenko, A. I.,Kovshev, E. I.,Titov, V. V.
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