- Synthesis and characterization of iron(II) quinaldate complexes
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Treatment of iron(II) chloride or iron(II) bromide with 2 equiv of sodium quinaldate (qn=quinaldate or C10H6NO2 -) yields the coordinatively unsaturated mononuclear iron(II) quinaldate complexes Na[FeII(qn)2Cl]-DMF and Na[Fe II(qn)2Br] · DMF (DMF=N,N-dimethylformamide), respectively. When a similar synthesis is carried out using iron(II) triflate, a solvent-derived linear triiron(II) complex, [FeII 3(qn)6(DNF)2], with two five-coordinate iron(II) centers and a single six-coordinate iron(II) center Is obtained. Each of these species has been characterized using X-ray diffraction. The vibrational features of these complexes are consistent with the observed solid-state structures. Each of these compounds exhibits an iron(II)-to-quinaldate (π*) charge-transfer band between 520 and 550 nm. These metalto-ligand charge-transfer bands are sensitive to substitution of the quinaldates as well as alteration of the first coordination sphere ligands. However, the 1H NMR spectra of these paramagnetic high-spin iron(II) complexes are not consistent with retention of the solid-state structures in a DMF solution. The chemical shifts, longitudinal relaxation times (T 1), relative integrations, and substitution of the quinaldate ligands provide a means to fully assign the 1H NMR spectra of the paramagnetic materials. These spectra are consistent with coordination equilibria between five- and sixcoordinate species in a DMF solution. Electrochemical studies are reported to place these oxygen-sensitive compounds in a broader context with other iron(II) compounds. Iron complexes of bidentate quinoline-2-carboxylate-derived ligands are germane to metabolic pathways, environmental remediation, and catalytic applications.
- Houghton, Dylan T.,Arulsamy, Navamoney,Mehn, Mark P.
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Read Online
- Discovery of novel diarylpyrazolylquinoline derivatives as potent anti-dengue virus agents
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A number of diarylpyrazolylquinoline derivatives were synthesized and evaluated for their anti-dengue virus (DENV) activity. Among them, 6-fluoro-2-(1-(4-fluorophenyl)-3- (4-methoxyphenyl)-1H-pyrazol-5-yl)quinoline (11c), 2-[1,3-bis(4-methoxyphenyl)-1H-pyrazol- 5-yl]-6-fluoroquinoline (12c), and 4-[5-(6-fluoroquinolin-2-yl)-3-(4-methoxyphenyl)-1H-pyrazol- 1-yl]benzenesulfonamide (13c) exhibited approximately 10-folds more active anti-DENV-2 activity (IC50 of 1.36, 1.09 and 0.81 μM, respectively) than that of ribavirin (IC50 = 12.61 μM). Compound 13c was also potent inhibited other sero-types of DENV. It reduced DENV replication in both viral protein and mRNA levels, and no significant cell cytotoxicity was detected, with greater than 50% viability of Huh-7-DV-Fluc cells at a concentration of 200 μM. Furthermore, compound 13c can effectively protect mice from DENV infection by reducing disease symptoms and mortality of DENV-infected mice. It represents a potential antiviral agent to block DENV replication in vitro and in vivo. Structural optimization of the initial lead compound, 13c, and the detailed molecular mechanism of action are ongoing.
- Lee, Jin-Ching,Tseng, Chin-Kai,Lin, Chun-Kuang,Tseng, Chih-Hua
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Read Online
- Visible Light-Driven Decarboxylative Alkylation of Aldehydes via Electron Donor–Acceptor Complexes of Active Esters
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There are some synthesis methods from widely available aldehydes to the corresponding ketones, however, they involved in multistep reactions with Grignard’s reagents or transition metal catalysts. In this paper, we have developed photocatalyst-free and visible light-driven decarboxylative alkylation of pyridinaldehydes. The photochemical reactions are initiated via photoinduced single electron transfer from triethylamine to N-hydroxyphthalimide esters in electron donor–acceptor complexes. This photochemical method can achieve to translate 15 pyridinaldehydes and 11 2-quinolinaldehydes to the corresponding ketones. Furthermore, this strategy can also achieve two other transformations, disulfanes to aryl sulfides and a styrene sulfone to the alkyl-substituted alkene.
- Cai, Yi-Ping,Nie, Fang-Yuan,Song, Qin-Hua
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supporting information
p. 1262 - 1271
(2022/01/27)
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- Iodine-catalyzed oxidative annulation: Facile synthesis of pyrazolooxepinopyrazolones: Via methyl azaarene sp3C-H functionalization
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An iodine-catalyzed methyl azaarene sp3 C-H functionalization has been developed for the synthesis of a seven-membered O-heterocyclic architecture containing three different heterocyclic aromatic hydrocarbons. This method can be applied to a wide range of substituted methyl azaarenes and diverse 2,4-dihydro-3H-pyrazol-3-ones, and brings about the efficient preparation of 2,9-dihydrooxepino[2,3-c:6,5-c′]dipyrazol-3(7H)-ones in high yields with the merits of low catalyst loading, good functional group tolerance and metal-free conditions.
- Zhang, Xin-Ke,Miao, Xiao-Yu,Zhou, Yu,Wang, Yu-Mei,Song, Ying-Chun,Liu, Hang,Xiong, Yi-Lu,Li, Ling-Yu,Wu, An-Xin,Zhu, Yan-Ping
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supporting information
p. 1236 - 1242
(2022/02/19)
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- Rh-Catalyzed Formal [3+2] Cyclization for the Synthesis of 5-Aryl-2-(quinolin-2-yl)oxazoles and Its Applications in Metal Ions Probes
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A facile and efficient strategy for the synthesis of 5-aryl-2-(quinolin-2-yl)oxazoles via rhodium-catalyzed formal [3+2] cyclization of 4-aryl-1-tosyl-1H-1,2,3-triazoles with quinoline-2-carbaldehydes has been described. The protocol employs mild conditions and offers good yields of diverse 2,5-aryloxazole derivatives with a broad reaction scope. It is amenable to gram-scale synthesis and easily transformation. Moreover, this 5-aryl-2-(quinolin-2-yl)oxazole skeleton is indeed a new fluorophore and its applications in metal ions probes are also investigated and showed fluorescent responses to mercury ion.
- Zhou, Tongtong,He, Xinwei,Zuo, Youpeng,Wu, Yuhao,Hu, Wangcheng,Zhang, Shiwen,Duan, Jiahui,Shang, Yongjia
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p. 621 - 626
(2021/02/12)
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- Iodine-imine Synergistic Promoted Povarov-Type Multicomponent Reaction for the Synthesis of 2,2′-Biquinolines and Their Application to a Copper/Ligand Catalytic System
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An efficient iodine-imine synergistic promoted Povarov-type multicomponent reaction was reported for the synthesis of a practical 2,2′-biquinoline scaffold. The tandem annulation has reconciled iodination, Kornblum oxidation, and Povarov aromatization, where the methyl group of the methyl azaarenes represents uniquely reactive input in the Povarov reaction. This method has broad substrate scope and mild conditions. Furthermore, these 2,2′-biquinoline derivatives had been directly used as bidentate ligands in metal-catalyzed reactions.
- Hu, Qi-Qi,Gao, Yan-Ting,Sun, Jia-Chen,Gao, Jing-Jing,Mu, Hong-Xiao,Li, Yi-Ming,Zheng, Ya-Nan,Yang, Kai-Rui,Zhu, Yan-Ping
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supporting information
p. 9000 - 9005
(2021/11/24)
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- Facile synthesis of 1,3,4-oxadiazoles via iodine promoted oxidative annulation of methyl-azaheteroarenes and hydrazides
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An oxidative sp3 C–H bond of methyl-azaheteroarenes protocol was reported for the synthesis of 1,3,4-oxadiazoles via [4 + 1] annulation with hydrazides. This protocol enables 1,3,4-oxadiazole and quinoline linked diheterocycles via selective oxidation of sp3 C–H bond of methyl-azaheteroarenes in the presence of I2-DMSO. The reaction has a broad substrate scope and good functional group tolerance for methyl-azaheteroarenes and hydrazides.
- Shang, Zhi-Hao,Sun, Ji-Na,Guo, Jiang-Shan,Sun, Yuan-Yuan,Weng, Wei-Zhao,Zhang, Zhen-Xiao,Li, Zeng-Jing,Zhu, Yan-Ping
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supporting information
(2020/01/08)
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- Metal- and radical-free aerobic oxidation of heteroaromatic methanes: An efficient synthesis of heteroaromatic aldehydes
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A metal-free and radical-free synthesis of heteroaromatic aldehydes was developed through aerobic oxidation of methyl groups in an I2/DMSO/O2 catalytic system. Under the reaction conditions, various functional groups such as methoxy, aldehyde, ester, nitro, amide, and halo (F, Cl, Br) groups were well tolerated. The bioactive compounds like chlorchinaldin derivative and papaverine were also oxidized to the corresponding aldehydes and ketones. This reaction provided an efficient method for preparing the valuable heteroaromatic aldehydes.
- Ye, Rongzi,Cao, Yuanjie,Xi, Xiaoxiang,Liu, Long,Chen, Tieqiao
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supporting information
p. 4220 - 4224
(2019/05/10)
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- Consecutive Intermolecular Reductive Amination/Asymmetric Hydrogenation: Facile Access to Sterically Tunable Chiral Vicinal Diamines and N-Heterocyclic Carbenes
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A highly enantioselective iridium- or ruthenium-catalyzed intermolecular reductive amination/asymmetric hydrogenation relay with 2-quinoline aldehydes and aromatic amines has been developed. A broad range of sterically tunable chiral N,N′-diaryl vicinal diamines were obtained in high yields (up to 95 %) with excellent enantioselectivity (up to >99 % ee). The resulting chiral diamines could be readily transformed into sterically hindered chiral N-heterocyclic carbene (NHC) precursors, which are otherwise difficult to access. The usefulness of this synthetic approach was further demonstrated by the successful application of one of the chiral vicinal diamines and chiral NHC ligands in a transition-metal-catalyzed asymmetric Suzuki–Miyaura cross-coupling reaction and asymmetric ring-opening cross-metathesis, respectively.
- Chen, Ya,Pan, Yixiao,He, Yan-Mei,Fan, Qing-Hua
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supporting information
p. 16831 - 16834
(2019/11/13)
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- Copper-catalyzed three-component reaction of: N-heteroaryl aldehydes, nitriles, and water
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An efficient and straightforward method for the synthesis of N-heteroaroyl imides has been successfully developed involving a copper-catalyzed radical-triggered three-component reaction of N-heteroaryl aldehydes, nitriles, and water. Mechanistic studies indicate that the reaction may undergo a radical-triggered Ritter-type reaction in which water serves as the oxygen source for the formation of the C-O bond. The reaction has advantages such as a broad substrate scope for the N-heteroaryl aldehydes, atom economy, and simple operation.
- Bao, Hanyang,Zhou, Bingwei,Jin, Hongwei,Liu, Yunkui
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p. 5021 - 5028
(2019/06/03)
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- Discovery of fused heterocyclic carboxamide derivatives as novel α7-nAChR agonists: Synthesis, preliminary SAR and biological evaluation
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The α7 nicotinic acetylcholine receptor (α7 nAChR) has emerged as a promising therapeutic target for schizophrenia. In our previous work, a novel series of α7-nAChR agonists bearing scaffold of indolizine were discovered. To explore the effect of aromaticity on the activity and find more active agents, herein, fused heterocyclic carboxamide derivatives were designed and synthesized in this study. Based on the evaluation by two-electrode voltage clamp in Xenopus oocytes, 27 of the synthesized compounds showed obvious agonism of α7 nAChR. Particularly, compounds 10a and 10e showed significantly higher Emax than EVP-6124. The result illustrated the importance of aromaticity to the activity of agonism. Compound 10a, which showed EC50 of 1.88 μM and Emax of 72.4%, was further characterized comprehensively, including co-application with type II positive allosteric modulator PNU-120596, selectivity with other closely related ligand-gated ion channel, etc. The results showed that 10a showed moderate selectivity over other subtypes such as α4β2 and α3β4 nAChR. 10a evoked α7-like currents that were inhibited by MLA and enhanced in the presence of the α7 PAM PNU-120596. The analysis of binding mode and understanding of structure-activity relationship provided insights to develop more potent novel α7-nAChR agonists.
- Xue, Yu,He, Xiaomeng,Yang, Taoyi,Wang, Yuxi,Liu, Zhenming,Zhang, Guisen,Wang, Yanxing,Wang, Kewei,Zhang, Liangren,Zhang, Lihe
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- PYRAZOLYQUINOLINE COMPOUNDS AND PREPARATION METHODS AND PHARMACEUTICAL COMPOSITIONS THEREOF
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A Pyrazolyquinoline compound is disclosed, comprising: a quinolyl group, its C6 position is connected to a substituent R1, and R1 is a halogen atom a pyrazolyl group a first phenyl group and a second phenyl group, wherein: the C2 position of the quinolyl group is connected to the C3 position or the C5 position of the pyrazolyl group when in the first case, when the C2 position of the quinolyl group is connected to the C3 position of the pyrazolyl group, the C5 position of the pyrazolyl group is connected to the C4 position of the first phenyl group and when in the second case, when the C2 position of the quinolyl group is connected to the C5 position of the pyrazolyl group, the C3 position of the pyrazolyl is connected to the C4 position of the first phenyl group and N1 position of the pyrazolyl group is connected to the C4 position of the second phenyl group.
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Paragraph 0027; 0028
(2018/06/12)
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- Chemical synthesis method of quinoline (oxaline)-2-carboxaldehyde compounds
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The invention relates to a preparation method of quinoline (oxaline)-2-carboxaldehyde compounds. The preparation method comprises the following steps of dissolving 2-methylquinoline(oxaline) shown in a formula (II) into an organic solvent, adding iron salts, and completely reacting under the condition of 100 to 180DEG C with the assistance of microwave; performing after treatment on a reaction solution to obtain the quinoline (oxaline)-2-carboxaldehyde compounds shown in a formula (I), wherein the feed molar ratio of the iron salts to the quinoline (oxaline)-2-carboxaldehyde compounds is (0.5 to 3.5):1. R in the formula (I) and the formula (II) is hydrogen at the same time; or the hydrogen is monosubstituted or polysubstituted by alkyls of C1 to C8, alkoxys of C1 to C8, nitryl or halogen; the number of substituent groups is n; X in the formula (I) and the formula (II) is carbon or nitrogen at the same time. The preparation method disclosed by the invention has the advantages of short reaction time, low reaction temperature, wide application range of reaction, good reaction selectivity, low price and no toxicity of a used catalyst, and simplicity and convenience in operation; the preparation method meets the requirement of green chemistry. (The formulas are shown in the description).
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Paragraph 0060-0062
(2017/04/14)
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- Metal-free C(sp3)–H oxidation of 2-methylquinolines with PIDA under microwave irradiation
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An efficient metal-free protocol has been developed for the sp3C–H bond oxidation of 2-methylquinolines in the presence of PIDA under microwave irradiation, providing 2-quinolinecarboxaldehydes with moderate to high yields and excellent selectivities. A wide range of 2-quinolinecarboxaldehydes with different functional groups have been synthesized. A tentative mechanism has been presented to explain this highly selective oxidation process.
- Jiang, Long,Huang, Yingyi,Yan, Yiyan,Xie, Yuanyuan
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supporting information
p. 4149 - 4151
(2016/08/24)
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- Copper-Catalyzed Aerobic Oxidation of Azinylmethanes for Access to Trifluoromethylazinylols
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A copper-catalyzed oxygenation of methylazaarenes was found to occur in the absence of both ligand and additive, and has been successfully employed for the synthesis of trifluoromethylazinylketols. This synthetic strategy incorporates aerobic oxidation and a trifluoromethylation in one-pot and provides a novel method for the trifluoromethylation of aliphatic C-H bond.
- Zheng, Gang,Liu, Hao,Wang, Mang
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supporting information
p. 519 - 523
(2016/06/01)
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- Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
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Inhibition of HDACs activity has become a promising therapeutic strategy in clinical practice to reverse the abnormal epigenetic states of cancer and other diseases. Therefore, HDAC inhibitors become a relatively new class of anti-cancer agent. In the present study, we reported the design and synthesis of a series of novel HDAC inhibitors using various substituted quinoline rings as the cap group. In vitro studies showed that some compounds have good inhibitory activities against HDACs and potent antiproliferative activities in some tumor cell lines. Especially, compound 9w (IC50 = 85 nM), exhibited better inhibitory effect compared with SAHA (IC50 = 161 nM).
- Wang, Lei,Hou, Xuben,Fu, Huansheng,Pan, Xiaole,Xu, Wenfang,Tang, Weiping,Fang, Hao
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p. 4364 - 4374
(2015/08/03)
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- Synthesis of fluorine-containing phosphodiesterase 10A (PDE10A) inhibitors and the in vivo evaluation of F-18 labeled PDE10A PET tracers in rodent and nonhuman primate
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A series of fluorine-containing PDE10A inhibitors were designed and synthesized to improve the metabolic stability of [11C]MP-10. Twenty of the 22 new analogues had high potency and selectivity for PDE10A: 18a-j, 19d-j, 20a-b, and 21b had IC50 values 18F]18a-e, [18F]18g, and [18F]20a were radiosynthesized by 18F-introduction onto the quinoline rather than the pyrazole moiety of the MP-10 pharmacophore and performed in vivo evaluation. Biodistribution studies in rats showed ~2-fold higher activity in the PDE10A-enriched striatum than nontarget brain regions; this ratio increased from 5 to 30 min postinjection, particularly for [18F]18a-d and [18F]20a. MicroPET studies of [18F]18d and [18F]20a in nonhuman primates provided clear visualization of striatum with suitable equilibrium kinetics and favorable metabolic stability. These results suggest this strategy may identify a 18F-labeled PET tracer for quantifying the levels of PDE10A in patients with CNS disorders including Huntington's disease and schizophrenia.
- Li, Junfeng,Zhang, Xiang,Jin, Hongjun,Fan, Jinda,Flores, Hubert,Perlmutter, Joel S.,Tu, Zhude
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supporting information
p. 8584 - 8600
(2015/11/25)
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- Iron-catalyzed C-H bond functionalization for the exclusive synthesis of pyrido[1,2-a]indoles or triarylmethanols
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The efficient and selective iron-catalyzed C-H activation of 2-benzhydrylpyridine derivatives was employed for the preparation of pyrido[1,2-a]indoles through an intramolecular C-H amination reaction. In the presence of molecular oxygen as the sole oxidant, the same 2-benzhydrylpyridines were also used for the synthesis of the corresponding tertiary alcohols. In these approaches, the iron catalyst was used to selectively activate the C(sp2)-H bond of 2-benzhydrylpyridine, in the case of the intramolecular ring-closing C-H amination reaction in which the pyridine nitrogen atom was a directing group as well as a nucleophile, and the C(sp3)-H bond of the same compound, in the case of the oxidation reaction to give the corresponding triaryl carbinol.
- Karthikeyan, Iyyanar,Sekar, Govindasamy
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supporting information
p. 8055 - 8063
(2015/01/09)
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- Design, synthesis and biological evaluation of 2-substituted quinolines as potential antileishmanial agents
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An analogous library of 2-substituted quinoline compounds was synthesized with the aim to identify a potential drug candidate to treat visceral leishmaniasis. These molecules were tested for their in vitro and in vivo biological activity against Leishmania donovani. Metabolic stability of these compounds was also improved through the introduction of halogen substituents. Compound (26g), found to be the most active; exhibited an IC50 value of 0.2 μM and >180 fold selectivity. The hydrochloride salt of (26g) showed 84.26 ± 4.44 percent inhibition at 50 mg/kg × 5 days (twice daily, oral route) dose in L. donovani/hamster model. The efficacy was well correlated with the PK data observed which indicating that the compound is well distributed.
- Gopinath, Vadiraj S.,Pinjari, Jakir,Dere, Ravindra T.,Verma, Aditya,Vishwakarma, Preeti,Shivahare, Rahul,Moger, Manjunath,Kumar Goud, Palusa Sanath,Ramanathan, Vikram,Bose, Prosenjit,Rao,Gupta, Suman,Puri, Sunil K.,Launay, Delphine,Martin, Denis
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supporting information
p. 527 - 536
(2013/10/22)
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- HETEROARYL COMPOUNDS AS PDE10A INHIBITORS
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The present invention provides heteroaryl compounds as Phosphodiesterase 10A (PDE I OA) inhibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders by inhibiting Phosphodiesterase 10A enzyme. Also provided herein are processes for preparing compounds described herein, Formula (I), intermediates used in their synthesis, pharmaceutical compositions thereof.
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Page/Page column 37-38
(2011/11/06)
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- Discovery of 2-(6-{[(6-Fluoroquinolin-2-yl)methyl]amino}bicyclo[3.1.0]hex- 3-yl)- N -hydroxypyrimidine-5-carboxamide (CHR-3996), a class i selective orally active histone deacetylase inhibitor
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A novel series of HDAC inhibitors demonstrating class I subtype selectivity and good oral bioavailability is described. The compounds are potent enzyme inhibitors (IC50 values less than 100 nM), and improved activity in cell proliferation assays was achieved by modulation of polar surface area (PSA) through the introduction of novel linking groups. Employing oral pharmacokinetic studies in mice, comparing drug levels in spleen to plasma, we selected compounds that were tested for efficacy in human tumor xenograft studies based on their potential to distribute into tumor. One compound, 21r (CHR-3996), showed good oral activity in these models, including dose-related activity in a LoVo xenograft. In addition 21r showed good activity in combination with other anticancer agents in in vitro studies. On the basis of these results, 21r was nominated for clinical development.
- Moffat, David,Patel, Sanjay,Day, Francesca,Belfield, Andrew,Donald, Alastair,Rowlands, Martin,Wibawa, Judata,Brotherton, Deborah,Stimson, Lindsay,Clark, Vanessa,Owen, Jo,Bawden, Lindsay,Box, Gary,Bone, Elisabeth,Mortenson, Paul,Hardcastle, Anthea,Van Meurs, Sandra,Eccles, Suzanne,Raynaud, Florence,Aherne, Wynne
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experimental part
p. 8663 - 8678
(2011/03/19)
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- Chromanylurea compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor and uses thereof
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Compounds that are antagonists of the VR1 receptor, having formula (I) [image] or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.
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Page/Page column 38
(2008/06/13)
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- 3-Thio-1,2,4-triazoles, novel somatostatin sst2/sst5 agonists
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Novel 3-thio-1,2,4-triazoles have been obtained via a solution-phase parallel synthesis strategy, affording potent non-peptidic human somatostatin receptor subtypes 2 and 5 agonists.
- Contour-Galcera, Marie-Odile,Sidhu, Alban,Plas, Pascale,Roubert, Pierre
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p. 3555 - 3559
(2007/10/03)
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- CARBAMIC ACID COMPOUNDS COMPRISING A BICYCLIC HETEROARYL GROUP AS HDAC INHIBITORS
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This invention pertains to certain carbamic acid compounds of the following formula, which inhibit HDAC (histone deacetylase) activity wherein: A is independently an unsubstituted or substituted bicyclic C9-10heteroaryl group (e.g., quinolinyl; quinoxalinyl; benzoxazolyl; benzothiazolyl); Q is an acid leader group, and is independently an unsubstituted or substituted, saturated or unsaturated C1 7alkylene group having a backbone length of 4 or less; with the proviso that if A is unsubstituted benzothiazol-2-yl, then Q is an unsaturated group; and with the proviso that if A is unsubstituted quinolin-6-yl, then Q is unsubstituted at the α-position; and with the proviso that A is not benzimidazol-2-yl; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both invitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
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- Novel N-acylated heterocycles
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Described are compositions comprising a muscarinic receptor antagonist and an N-acylated heterocycle derivative having affinity for serotonergic receptors, and enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts thereof. The combination of a muscarinic receptor antagonist and an N-acylated heterocycle, or an enantiomer, diastereoisomer, N-oxide, polymorph, solvate or pharmaceutically acceptable salt thereof, is useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptors.
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- Preparation of lavendamycin analogues
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A Pictet-Spengler type reaction conducted under modified conditions using a catalytic amount of pyridinium p-toluenesulfonate was used to prepare several lavendamycin (1) analogues.
- Barbier, Christine,Joissains, Arnaud,Commercon, Alain,Riou, Jean-Francois,Huet, Francois
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