- Characteristics of polymer light emitting diode using a phosphorescent terpolymer containing perylene, triazine and ir(ppy)3 moieties in the polymer side chain
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We have synthesized a novel nonconjugated phosphorescent terpolymer, PPPMA-co-DTPM-co-Ir(ppy)3, containing perylene and Ir complex moieties as lightemitting units and a triazine moiety as electron transporting unit in the polymer side chain. Th
- Oh, Se Young,Jang, Kyoungmi,Lee, Chang Ho
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Read Online
- Introducing of a New Bio-inspired Hierarchical Porous Silica as an Inorganic Host for Ni–Pd Alloy Nanoparticles for the Synthesis of Aminobiphenyls from the One-Pot Suzuki–Miyaura Coupling-Nitro Reduction
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This work reports a facial way to synthesize of an efficient catalyst based Ni–Pd alloy nanoparticles which supported on a new bio-inspired hierarchical porous silica and its catalytic activity in the one-pot Suzuki–Miyaura cross coupling-nitro reduction. The synthesized catalyst was fully characterized by FT-IR, XRD, FESEM–EDX, elemental mapping, TEM, ICP-AES, N2 adsorption–desorption, DRS–UV–Vis and XPS techniques. Use of inexpensive catalyst, high yields of the products and reusability of the catalyst are some of the advantages of our procedure. Graphical Abstract: [Figure not available: see fulltext.].
- Beigbaghlou, Somayyeh Sarvi,Javad Kalbasi, Roozbeh,Marjani, Katayoun,Habibi, Azizollah
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Read Online
- The two isomers of a cyclometallated palladium sensitizer show different photodynamic properties in cancer cells
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This report demonstrates that changing the position of the carbon-metal bond in a polypyridyl cyclopalladated complex, i.e. going from PdL1 (N^N^C^N) to PdL2 (N^N^N^C), dramatically influences the photodynamic properties of the compl
- Zhou, Xue-Quan,Busemann, Anja,Meijer, Michael S.,Siegler, Maxime A.,Bonnet, Sylvestre
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Read Online
- ARYL AND HETEROARYL COMPOUNDS, AND THERAPEUTIC USES THEREOF IN CONDITIONS ASSOCIATED WITH THE ALTERATION OF THE ACTIVITY OF GALACTOCEREBROSIDASE
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The application is directed to compounds of formulae (IA) and (IB): (IA) and (IB), and their salts and solvates, wherein R1a, R2a, A1, A2, A3, A4, R1b, R2b, B1, B2, B3, and G are as set forth in the specification, as well as to methods for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of, e.g., lysosomal storage diseases, such as Krabbe's disease, and α-synucleinopathies, such as Parkinson's disease.
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Page/Page column 87
(2021/06/04)
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- Preparation methods of Vismodegib and intermediate of Vismodegib
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The invention provides preparation methods of Vismodegib and an intermediate of the Vismodegib, namely, preparation methods of 2-chloro-N-(4-chloro-3-(2-pyridinyl)phenyl)-4-(methylsulfonyl)benzamide and an intermediate of the 2-chloro-N-(4-chloro-3-(2-pyridinyl)phenyl)-4-(methylsulfonyl)benzamide. According to the preparation methods, the intermediate, namely 2-chloro-4-methylsulfonyl-N-(3-(2-pyridinyl)phenyl)benzamide is prepared firstly, and then the 2-chloro-N-(4-chloro-3-(2-pyridinyl)phenyl)-4-(methylsulfonyl)benzamide is prepared through a chlorination reaction. The preparation methods have the characteristics that the steps are short, operation is easy, starting materials are cheap and easy to obtain, no palladium reagent is used, the reaction condition has the low requirements for the anhydrous and oxygen-free condition, and the production cost can be effectively lowered.
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Paragraph 0068-0073
(2020/01/08)
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- ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
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The present invention includes novel heteroleptic/homoleptic iridium complexes containing two tridentate ligands, where at least one of the tridentate ligands comprises of pyridinium-derived N-heterocyclic carbene. The compounds of the present invention may be useful for organic electroluminescent devices.
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Paragraph 0136; 0138
(2019/04/05)
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- Organic metal compounds and organic light emitting diodes comprising the same
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PURPOSE: An organic metal compound is provided to have excellent thermal properties and light emitting efficiency, thereby being useful for a display and lighting device. CONSTITUTION: An organic metal compound is represented by chemical formula 1. In chemical formula 1, each of R and Z is hydrogen, deuterium, cyano, halogen hydroxy, nitro, C1-40 alkyl, C1-40 alkoxy, C1-40 alkylamino, C6-40 arylamino, C3-40 heteroarylamino, C1-40 alkoxy group, C1-40 alkylamino, C6-40 aryl group, C3-40 aryloxy group, germanium, phosphorous, and boron; each of A, B, C, D, and E is a substituted or unsubstituted aromatic cycle, or substituted or unsubstituted hydrocycle, X is carbon or nitrogen, G is chemical bond or C1-4 alkylene which can be substituted by (R-Zi)n.
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Paragraph 0154; 0161; 0164-0166
(2018/12/01)
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- Copper mediated C-H amination with oximes: En route to primary anilines
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Here we report an efficient Cu(i)-mediated C-H amination reaction with oximes as amino donors to introduce NH2 groups directly. Various strongly coordinating heterocycles including quinoline, pyrimidine, pyrazine, pyrazole and triazole were tolerated well. The potential utility was further demonstrated in a late-stage modification of telmisartan (an antagonist for the angiotensin II receptor).
- Xu, Lin-Lin,Wang, Xing,Ma, Biao,Yin, Ming-Xing,Lin, Hai-Xia,Dai, Hui-Xiong,Yu, Jin-Quan
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p. 5160 - 5164
(2018/06/21)
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- Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution
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Allosteric modulators of the cannabinoid CB1 receptor have recently been reported as an alternative approach to modulate the CB1 receptor for therapeutic benefits. In this study, we report the design and synthesis of a series of diarylureas derived from PSNCBAM-1 (2). Similar to 2, these diarylureas dose-dependently inhibited CP55,940-induced intracellular calcium mobilization and [35S]GTP-γ-S binding while enhancing [3H]CP55,940 binding to the CB1 receptor. Structure-activity relationship studies revealed that the pyridinyl ring of 2 could be replaced by other aromatic rings and the pyrrolidinyl ring is not required for CB1 allosteric modulation. 34 (RTICBM-74) had similar potencies as 2 in all in vitro assays but showed significantly improved metabolic stability to rat liver microsomes. More importantly, 34 was more effective than 2 in attenuating the reinstatement of extinguished cocaine-seeking behavior in rats, demonstrating the potential of this diarylurea series as promising candidates for the development of relapse treatment of cocaine addiction.
- Nguyen, Thuy,German, Nadezhda,Decker, Ann M.,Langston, Tiffany L.,Gamage, Thomas F.,Farquhar, Charlotte E.,Li, Jun-Xu,Wiley, Jenny L.,Thomas, Brian F.,Zhang, Yanan
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p. 7410 - 7424
(2017/09/22)
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- Meta-Selective CAr-H Nitration of Arenes through a Ru3(CO)12-Catalyzed Ortho-Metalation Strategy
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The first example of transition metal-catalyzed meta-selective CAr-H nitration of arenes is described. With the use of Ru3(CO)12 as the catalyst and Cu(NO3)2·3H2O as the nitro source, a wide spectrum of arenes bearing diversified N-heterocycles or oximido as the directing groups were nitrated with meta-selectivity exclusively. Mechanism studies have demonstrated the formation of a new 18e-octahedral ruthenium species as a key ortho-CAr-H metalated intermediate, which may be responsible for the subsequent meta-selective electrophilic aromatic substitution (SEAr). Moreover, this approach provides a fast-track strategy for atom/step economical synthesis of many useful pharmaceutical molecules.
- Fan, Zhoulong,Ni, Jiabin,Zhang, Ao
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p. 8470 - 8475
(2016/07/26)
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- Click reaction as a tool to combine pharmacophores: The case of Vismodegib
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Abstract The design and the preparation of a small library of 1,4-diphenyl-1,2,3-triazole derivatives is reported, with the aim to obtain a new class of Hedgehog pathway inhibitors. The smoothened protein is part of the hedgehog signaling pathway that is
- Christodoulou, Michael S.,Mori, Mattia,Pantano, Rebecca,Alfonsi, Romina,Infante, Paola,Botta, Maurizio,Damia, Giovanna,Ricci, Francesca,Sotiropoulou, Panagiota A.,Liekens, Sandra,Botta, Bruno,Passarella, Daniele
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p. 938 - 943
(2015/06/08)
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- Synthesis of new bioorganometallic Ir- and Rh-complexes having β-lactam containing ligands
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The synthesis (and full spectroscopic and crystallographic characterization) of new classes of bioorganometallic Ir- and Rh-complexes having β-lactam containing ligands has been achieved in three steps starting from simple precursors. The procedure for preparing these bioorganometallic compounds uses β-lactams having a phenylpyridyl moiety attached to the C4, N1 or C4 and N1 positions simultaneously, and a directed C-H metal-insertion, in the presence of (MCp*Cl2)2 (M = Ir, Rh). Enantiomerically pure 2-azetidinones can be transformed into diastereomeric (at the metal) mixtures of enantiopure metalla-2-azetidinones. Bimetallic 2-azetidinones are also accessible by this approach. The insertion of electron-poor alkynes into the M-C bond of the bioorganometallic complex occurs regioselectively and in excellent yields. Overall, the sequence imine-β-lactam-metalla-β-lactam is a versatile and efficient full methodology to prepare and functionalize unprecedented, novel Ir- and Rh-complexes having β-lactam containing ligands.
- Muntaner, Jaime G.,Casarrubios, Luis,Sierra, Miguel A.
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supporting information
p. 286 - 297
(2014/01/06)
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- Design, synthesis and biological evaluation of N-arylphenyl-2,2- dichloroacetamide analogues as anti-cancer agents
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Our earlier research has shown that N-phenyl-2,2-dichloroacetamide analogues had much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this current study, a variety of N-arylphenyl-2,2- dichloroacetamide analogues were synthesized via Suzuki coupling reaction and their anti-cancer activity was evaluated. The results showed that N-terphenyl-2,2-dichloroacetamide analogues had satisfactory anti-cancer activity. Among them, N-(3,5-bis(benzo[d][1,3]dioxol-5-yl)phenyl)-2,2- dichloroacetamide (6 k) had an IC50 of 2.40 μM against KB-3-1 cells, 1.04 μM against H460 cells and 1.73 μM against A549 cells.
- Li, Tianwen,Yang, Yongchong,Cheng, Changmei,Tiwari, Amit K.,Sodani, Kamlesh,Zhao, Yufen,Abraham, Ioana,Chen, Zhe-Sheng
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supporting information
p. 7268 - 7271
(2013/01/15)
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- Investigations on the 1-(2-biphenyl)piperazine motif: Identification of new potent and selective ligands for the serotonin7 (5-HT7) receptor with agonist or antagonist action in vitro or ex vivo
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Here we report the design, synthesis, and 5-HT7 receptor affinity of a set of 1-(3-biphenyl)- and 1-(2-biphenyl)piperazines. The effect on 5-HT7 affinity of various substituents on the second (distal) phenyl ring was analyzed. Several compounds showed 5-HT7 affinities in the nanomolar range and >100-fold selectivity over 5-HT1A and adrenergic α1 receptors. 1-[2-(4-Methoxyphenyl)phenyl] piperazine (9a) showed 5-HT7 agonist properties in a guinea pig ileum assay but blocked 5-HT-mediated cAMP accumulation in 5-HT7- expressing HeLa cells.
- Lacivita, Enza,Patarnello, Daniela,Stroth, Nikolas,Caroli, Antonia,Niso, Mauro,Contino, Marialessandra,De Giorgio, Paola,Di Pilato, Pantaleo,Colabufo, Nicola A.,Berardi, Francesco,Perrone, Roberto,Svenningsson, Per,Hedlund, Peter B.,Leopoldo, Marcello
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supporting information; experimental part
p. 6375 - 6380
(2012/10/08)
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- INHIBITOR OF PLASMINOGEN ACTIVATOR INHIBITOR-1
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The present invention relates to a novel compound having plasminogen activator inhibitor-1 (PAI-1) inhibitory activity, and a PAI-1 inhibitor comprising the compound as an active ingredient. The present invention further relates to a pharmaceutical compos
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Page/Page column 53
(2011/02/17)
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- PdCl2(dppf)-catalyzed in situ coupling of 2-hydroxypyridines with aryl boronic acids mediated by PyBroP and the one-pot chemo- and regioselective construction of two distinct aryl-aryl bonds
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We present a PdCl2(dppf)-catalyzed synthesis of 2-arylated pyridine derivatives via the in situ coupling of 2-OH pyridines and boronic acids mediated by PyBroP. In addition, the highly chemo- and regioselective construction of two different aryl-aryl bonds via a one-pot operation has also been demonstrated by the orthogonal use of this method with the Ni-catalyzed Suzuki-Miyaura coupling of phenols.
- Li, Shui-Ming,Huang, Jie,Chen, Guo-Jun,Han, Fu-She
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supporting information; experimental part
p. 12840 - 12842
(2012/01/05)
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- 2-Pyridyl and 3-pyridylzinc bromides: direct preparation and coupling reaction
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A facile synthetic approach to the direct preparation of 2-pyridyl and 3-pyridylzinc bromides has been demonstrated using Rieke zinc with 2-bromopyridine and 3-bromopyridine, respectively. A variety of different electrophiles have been coupled with the resulting organozinc reagents to give the corresponding cross-coupling products in moderate to good yields.
- Kim, Seung-Hoi,Rieke, Reuben D.
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scheme or table
p. 3135 - 3146
(2010/06/13)
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- Coupling reactions with haloaromatic amines and alcohols for a practical synthetic route to 2-substituted aminophenyl and hydroxyphenyl pyridines
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A practical synthetic route to 2-substituted aminophenyl and hydroxyphenyl pyridines has been developed. It has been accomplished by the cross-coupling reactions of readily available 2-pyridylzinc bromides with haloaromatic amines and alcohols under mild
- Kim, Seung-Hoi,Rieke, Reuben D.
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supporting information; experimental part
p. 6985 - 6988
(2010/02/27)
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- BICYCLIC DERIVATIVES AS P38 KINASE INHIBITORS
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New bicyclic derivatives of formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.
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Page/Page column 52
(2008/06/13)
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- CAPREOMYCIN DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
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The present invention relates to phenylurea derivatives of capreomycin I, IIB, IIA, or IB, and metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are useful as antibacterial agents for treating b
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Page/Page column 64
(2008/06/13)
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- Scope and selectivity in palladium-catalyzed directed C-H bond halogenation reactions
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Palladium-catalyzed ligand directed C-H activation/halogenation reactions have been extensively explored. Both the nature of the?directing group and the substitution pattern on the arene ring of the substrate lead to different reactivity profiles, and often different and complementary products, in the presence and absence of the catalyst.
- Kalyani, Dipannita,Dick, Allison R.,Anani, Waseem Q.,Sanford, Melanie S.
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p. 11483 - 11498
(2007/10/03)
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- Capreomycin derivatives and their use as antibacterials
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The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial
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Page/Page column 23
(2008/06/13)
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- HETEROYCLYLPHENYL-AND HETEROCYCLYLPYRIDYL-SUBSTITUTED AZOLECARBOXAMIDES AS HERBICIDES
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Compounds of Formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation : wherein (J) is (J-1), (J-2), (J-3), (J-4), (J-5), (J-6), (J-7), (J-8), or (J-9) ; R5 is a phenyl ring or a 5- or 6-membered heteroaromatic ring which includes at least one heteroatom selected from N, O and S, each ring optionally substituted with one or more substituents selected from R15; or R5 is a 5- or 6-membered partially unsaturated heterocyclic ring which includes at least one heteroatom selected form N, O and S, the ring connected through a nitrogen atom or an sp2 carbon atom to the remainder of Formula (I) and optionally substituted by one or more substituents selected from R16; and R1a, R1b, R2a, R2b, R3, R4, R15, R16, T, U, W, Y and Z are as defined in the disclosure.
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Page/Page column 56
(2010/02/11)
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- Novel compounds and their use as positive AMPA receptor modulators
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The invention provides novel compounds represented by the general formula 5 compound represented by the formula: wherein the bond represented by the broken line may be a single, a double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R2; X represents SO2 or C═O or CH2; Y represents —CH(R4)—, —N(R4)— or —N(R4)—CH2—, O; and the meaning of R2, R3, R4, R5, R6, R7, and R8 are as defined in the application The compounds are useful as positive modulators of the AMPA-receptor.
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- Method for treating neoplasia with amino or pyridylamino cyclobutene derivatives
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A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to amino or pyridylamino cyclobutane derivatives.
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- Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: Identification of 5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent
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The evolution, synthesis, and biological activity of a novel series of 5-HT(2C) receptor inverse agonists are reported. Biarylcarbamoylindolines have been identified with excellent 5-HT(2C) affinity and selectivity over 5- HT(2A) receptors. In addition, (pyridyloxypyridyl)carbamoylindolines have been discovered with additional selectivity over the closely related 5-HT(2B) receptor. Compounds from this series are inverse agonists at the human cloned 5-HT(2C) receptor, completely abolishing basal activity in a functional assay. The new series have reduced P450 inhibitory liability compared to a previously described series of 1-(3-pyridylcarbamoyl)indolines (Bromidge et al. J. Med. Chem. 1998, 41, 1598) from which they evolved. Compounds from this series showed excellent oral activity in a rat mCPP hypolocomotion model and in animal models of anxiety. On the basis of their favorable biological profile, 32 (SB-228357) and 40 (SB-243213) have been selected for further evaluation to determine their therapeutic potential for the treatment of CNS disorders such as depression and anxiety.
- Bromidge, Steven M.,Dabbs, Steven,Davies, David T.,Davies, Susannah,Duckworth, D. Malcolm,Forbes, Ian T.,Gaster, Laramie M.,Ham, Peter,Jones, Graham E.,King, Frank D.,Mulholland, Keith R.,Saunders, Damian V.,Wyman, Paul A.,Blaney, Frank E.,Clarke, Stephen E.,Blackburn, Thomas P.,Holland, Vicky,Kennett, Guy A.,Lightowler, Sean,Middlemiss, Derek N.,Trail, Brenda,Riley, Graham J.,Wood, Martyn D.
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p. 1123 - 1134
(2007/10/03)
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- Benzimidazole compounds, pharmaceutical compositions containing the compounds and their use
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The present patent application discloses compounds having the formula STR1 or a pharmaceutically acceptable salt thereof or an oxide thereof wherein R 3 is STR2 wherein A, B and D each is CH, or one or two of A, B and D is N and the others are CH;R 11 is
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