- Rational engineering of dimeric Dy-based Single-Molecule Magnets for surface grafting
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The deposition of Single-Molecule Magnets (SMMs) on surfaces is a mandatory step toward their possible use as data-storage units or qubits. In this study we report the structural and magnetic characterization of two parent compounds of a well-known SMM called DyPyNO, ([Dy(hfac)3(PyNO)]2 with hfac = hexafluoroacetylacetonate and PyNO = pyridine-N-oxide), that are targeted to be deposited on gold surfaces. Thio-substitution of the pyridine ring of these dimers is expected to provide good anchoring group toward deposition on gold. We have investigated two significantly different geometries of the anchoring groups in dimers 1 and 2. Interestingly, despite these strong differences, SMM behavior is remarkably well-preserved in the polycrystalline material offering possibilities to graft these SMMs on surface.
- Yi, Xiaohui,Pointillart, Fabrice,Le Guennic, Boris,Jung, Julie,Daiguebonne, Carole,Calvez, Guillaume,Guillou, Olivier,Bernot, Kevin
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Read Online
- Synthesis of dicationic carbazole and 4′-amino-(3,3'-bipyridine)-4-ol and the spectral characteristics of carbazoles
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The dicationic carbazole compound, 3,6-dimethyl-3,6-diazacarbazole diiodide (8) was prepared with 3-bromopyridine as a starting material by a six-step synthesis. The intermediates and target compound were confirmed by IR, NMR and MS. Meanwhile, UV-visible and fluorescent characteristics of 3,6-diazacarbazole (7) and 3,6-dimethyl-3,6-diazacarbazole diiodide (8) were investigated. It was found that fluorescence decay over time of dicationic carbazole existed in low ionic strength and high ionic strength could stabilize the fluorescence of dicationic carbazole.
- Wang,Li,Ye,Guo,Jia
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Read Online
- Visible-Light-Induced Decarboxylative Acylation of Pyridine N-Oxides with α-Oxocarboxylic Acids Using Fluorescein Dimethylammonium as a Photocatalyst
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Herein, the development of a visible-light-induced catalytic system to achieve the decarboxylative acylation of pyridine N-oxides with α-oxocarboxylic acids, at room temperature and using the organic dye fluorescein dimethylammonium as a new type of photocatalyst, is reported. A series of 2-arylacylpyridine N-oxides were selectively synthesized in moderate to good yields by controlling the polarity of the reaction solvent. The developed strategy was successfully applied in the synthesis of an important intermediate of the drug, acrivastine, on a gram scale. Notably, this is the first time that fluorescein dimethylammonium has been used to catalyze the Minisci-type C?H decarboxylative acylation reaction. The mechanism of decarboxylative acylation was studied by capturing adducts of acyl radicals and 1,1-diphenylethylene to confirm a radical mechanism. The disclosed catalytic system provides a green synthetic strategy for decarboxylative acylation without the use of additional oxidants or metal catalysts. (Figure presented.).
- Hou, Chuanfu,Sun, Shouneng,Liu, Ziqi,Zhang, Hui,Liu, Yue,An, Qi,Zhao, Jian,Ma, Junjie,Sun, Zhizhong,Chu, Wenyi
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supporting information
p. 2806 - 2812
(2021/04/15)
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- Synthesis method of (3-cyclopropylpyridin-2-yl) methylamine hydrochloride
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The invention provides a synthesis method of (3-cyclopropylpyridin-2-yl) methylamine hydrochloride, and belongs to the technical field of synthesis of organic chemical intermediates. The preparation method comprises the following steps: reacting 3-bromo-2-cyanopyridine with cyclopropylboronic acid, a phosphine ligand, an alkali and a catalyst under the protection of nitrogen, then reacting with hydrogen under the action of the catalyst, reacting with di-tert-butyl dicarbonate and alkali, and finally reacting with an organic solvent solution of hydrogen chloride to obtain a target product (3-cyclopropylpyridin-2-yl) methylamine hydrochloride. The 3-bromo-2-cyanopyridine is prepared by taking 3-bromopyridine as a raw material and carrying out nitrogen oxidation and cyanation. The method is reasonable in process design, simple in experimental operation and easy to control.
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Paragraph 0028-0031; 0047-0050; 0066-0069; 0085-0088
(2020/07/08)
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- Synthesis method of (3-cyclopropylpyridin-2-yl) methylamine
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The invention belongs to the technical field of medical intermediates, and particularly relates to a synthesis method of (3-cyclopropylpyridin-2-yl) methylamine. The synthesis method of the (3-cyclopropylpyridin-2-yl) methylamine is provided for the first time, a synthesis route is provided for the synthesis method of the (3-cyclopropylpyridin-2-yl) methylamine, the synthesis method of the (3-cyclopropylpyridin-2-yl) methylamine is short in route, reasonable in design, easy to operate and easy to control, and meanwhile the yield of the obtained product is high.
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Paragraph 0016
(2020/07/28)
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- Method for catalyzing vitamin A isomerization with ruthenium catalyst
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The invention provides a method for catalyzing vitamin A isomer conversion with a ruthenium catalyst. According to the method, a ruthenium compound is used as a catalyst, various vitamin A cis-isomerswith low biological activity can be converted into all-trans-isomers with high biological activity in a high proportion in the presence of an auxiliary agent, and the cis-isomers comprise 9-cis-isomers, 11-cis-isomers and 13-cis-isomers. The method has the characteristics of cheap and easily available catalyst, less catalyst dosage, mild reaction conditions, low reaction cost, high isomerizationefficiency and the like.
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Paragraph 0066; 0069-0070
(2020/04/22)
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- Visible-Light-Induced ortho-Selective Migration on Pyridyl Ring: Trifluoromethylative Pyridylation of Unactivated Alkenes
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The photocatalyzed ortho-selective migration on a pyridyl ring has been achieved for the site-selective trifluoromethylative pyridylation of unactivated alkenes. The overall process is initiated by the selective addition of a CF3 radical to the alkene to provide a nucleophilic alkyl radical intermediate, which enables an intramolecular endo addition exclusively to the ortho-position of the pyridinium salt. Both secondary and tertiary alkyl radicals are well-suited for addition to the C2-position of pyridinium salts to ultimately provide synthetically valuable C2-fluoroalkyl functionalized pyridines. Moreover, the method was successfully applied to the reaction with P-centered radicals. The utility of this transformation was further demonstrated by the late-stage functionalization of complex bioactive molecules.
- Jeon, Jinwon,He, Yu-Tao,Shin, Sanghoon,Hong, Sungwoo
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supporting information
p. 281 - 285
(2019/11/26)
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- Recyclable anhydride catalyst for H2O2 oxidation:: N -oxidation of pyridine derivatives
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The catalytic efficiency and recyclability of poly(maleic anhydride-alt-1-octadecene) (Od-MA) and poly(maleic anhydride-alt-1-isobutylene) (Bu-MA) were evaluated for use in the development of a metal-free, reusable catalyst for the oxidation of pyridines to pyridine N-oxides in the presence of H2O2. The Od-MA catalyst was easily recovered via filtration with recovery yields exceeding 99.8%. The catalyst retained its activity after multiple uses and did not require any treatment for reuse. The Od-MA and H2O2 catalytic system described herein is eco-friendly, operationally simple, and cost-effective; thus, it is industrially applicable. Od-MA and H2O2 could potentially be used in place of percarboxylic acid as an oxidant in a wide range of oxidation reactions.
- Gajeles, Ghellyn,Kim, Se Mi,Lee, Kyung-Koo,Lee, Sang Hee,Yoo, Jong-Cheol
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p. 9165 - 9171
(2020/03/13)
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- Strategic Approach on N-Oxides in Gold Catalysis – A Case Study
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An extensive kinetic study of selected key reactions of (oxidative) gold catalysis concentrates on the decrease of the catalytic activity due to inhibition of the gold(I) catalyst caused by pyridine derivatives that are obtained as by-products if N-oxides are applied as oxygen donors. The choice of the examined pyridine derivatives and their corresponding N-oxides has been made regardless of their commercial availability; particular attention has been paid to the practical benefit which up to now has been neglected in most of the reaction screenings. The test reactions were monitored by GC and 1H NMR spectroscopy. The received reaction constants provide information concerning a correlation between the electronic structure of the heterocycle and the catalytic activity. Based on the collected kinetic data, it was possible to develop a basic set of three N-oxides which have to be taken into account in further oxidative gold(I)-catalyzed reactions. (Figure presented.).
- Schie?l, Jasmin,Stein, Philipp M.,Stirn, Judith,Emler, Kirsten,Rudolph, Matthias,Rominger, Frank,Hashmi, A. Stephen K.
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supporting information
p. 725 - 738
(2018/10/20)
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- An one-pot two-step automated synthesis of [18F]T807 injection, its biodistribution in mice and monkeys, and a preliminary study in humans
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[18F]T807 is a potent tau protein imaging agent. In order to fulfill the demand from preclinical and clinical studies, we developed an automated one-pot two-step synthesis of this potent tau imaging agent and studied its stability, and dosimetr
- Huang, Ya-Yao,Chiu, Ming-Jang,Yen, Ruoh-Fang,Tsai, Chia-Ling,Hsieh, Hao-Yu,Chiu, Ching-Hung,Wu, Chi-Han,Hsin, Ling-Wei,Tzen, Kai-Yuan,Cheng, Cheng-Yi,Ma, Kuo-Hsing,Shiue, Chyng-Yann
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- Synthesis method of heterocyclic compound 3-methoxypyridine
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The invention discloses a synthesis method of a heterocyclic compound 3-methoxypyridine. The method comprises the following steps: putting raw materials, i.e., 3-halogenated pyridine, hydrogen peroxide and acetic acid into a three-mouth flask, carrying out reaction for 4-8h at the temperature of 40-80 DEG C under the condition of stirring, recovering the acetic acid, adding a saturated sodium carbonate solution and stirring to enable a system to be alkaline, evaporating to remove water, then adding chloroform for washing, and carrying out vacuum distillation to obtain N-oxide-3-halogenated pyridine; respectively adding the N-oxide-3-halogenated pyridine, metal salt of alkyl alcohol, a catalyst A and alcohol into the three-mouth flask, carrying out reflux reaction for 5-8h under the condition of stirring, then cooling, neutralizing a product to be neutral, and carrying out distillation to obtain N-oxide-3-alkyloxypyridine; respectively adding the N-oxide-3-alkyloxypyridine, ferric trichloride, hydrazine hydrate, activated carbon and ethanol into the three-mouth flask, carrying out reaction at the temperature of 70 DEG C for 3h, cooling to room temperature, and carrying out vacuum distillation to obtain the 3-methoxypyridine. The synthesis method is high in intermediate conversion rate, mild in reaction conditions, safe in operation, low in price of raw materials and easy in raw material obtaining, thus being suitable for industrial production.
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Paragraph 0028
(2017/08/17)
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- C2-Alkenylation of N-heteroaromatic compounds: Via Br?nsted acid catalysis
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Substituted heteroaromatic compounds, especially those based on pyridine, hold a privileged position within drug discovery and medicinal chemistry. However, functionalisation of the C2 position of 6-membered heteroarenes is challenging because of (a) the difficulties of installing a halogen at this site and (b) the instability of C2 heteroaryl-metal reagents. Here we show that C2-alkenylated heteroaromatics can be accessed by simple Br?nsted acid catalysed union of diverse heteroarene N-oxides with alkenes. The approach is notable because (a) it is operationally simple, (b) the Br?nsted acid catalyst is cheap, non-toxic and sustainable, (c) the N-oxide activator disappears during the reaction, and (d) water is the sole stoichiometric byproduct of the process. The new protocol offers orthogonal functional group tolerance to metal-catalysed methods and can be integrated easily into synthetic sequences to provide polyfunctionalised targets. In broader terms, this study demonstrates how classical organic reactivity can still be used to provide solutions to contemporary synthetic challenges that might otherwise be approached using transition metal catalysis.
- Crisenza, Giacomo E. M.,Dauncey, Elizabeth M.,Bower, John F.
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supporting information
p. 5820 - 5825
(2016/07/06)
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- Metal-Free, Phosphonium Salt-Mediated Sulfoximination of Azine N-Oxides: Approach for the Synthesis of N-Azine Sulfoximines
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Herein, we report a simple and metal-free method for the synthesis of N-azine sulfoximines by the nucleophilic substitution of azine N-oxides with NH-sulfoximines. The present method works at room temperature with wide functional group compatibility and gives several unprecedented N-azine sulfoximines. The reaction conditions were also found suitable with enantiopure substrates and furnished products without any racemization. It also finds an application in the sulfoximination of azine-based functional molecules such as 2,2′-bipyridine, 1,10-phenanthroline, and quinine.
- Aithagani, Sravan Kumar,Kumar, Mukesh,Yadav, Mahipal,Vishwakarma, Ram A.,Singh, Parvinder Pal
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p. 5886 - 5894
(2016/07/23)
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- 2,2,2-Trifluoroacetophenone as an organocatalyst for the oxidation of tertiary amines and azines to N-oxides
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A cheap, mild and environmentally friendly oxidation of tertiary amines and azines to the corresponding Noxides is reported by using polyfluoroalkyl ketones as efficient organocatalysts. 2,2,2-Trifluoroacetophenone was identified as the optimum catalyst for the oxidation of aliphatic tertiary amines and azines. This oxidation is chemoselective and proceeds in high-to-quantitative yields utilizing 10 mol% of the catalyst and H2O2 as the oxidant.
- Limnios, Dimitris,Kokotos, Christoforos G.
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supporting information
p. 559 - 563
(2014/04/03)
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- N-(3-Arylaminopyridin-4-yl)alkanesulfonamides as pyridine analogs of nimesulide: Cyclooxygenases inhibition, anti-inflammatory studies and insight on metabolism
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Nimesulide, a COX-2 preferential inhibitor with a favorable gastric and cardiovascular safety profile, was responsible for some cases of acute liver failure attributed to the nitrobenzene ring. A series of analogs of nimesulide resulting from isosteric replacement of the nitrobenzene ring by the pyridine nucleus, was synthesized and their ability to inhibit both cyclooxygenases (COXs) isoforms was evaluated in vitro using a human whole blood model. Compounds 19c, 23b and 23c displayed an important inhibitory activity associated to a COX-2/COX-1 selectivity ratio similar to or higher than that of celecoxib. The anti-inflammatory activity and the ability of several compounds to decrease leukocyte infiltration were further evaluated in vivo in a model of a λ carrageenan-induced pleurisy. Plasma assays were performed on blood samples collected from rats and allowed us to identify the 4-position of the phenyl ring as a major metabolism site explaining the occasionally observed lack of correlation between in vitro and in vivo results.
- Renard, Jean-Fran?ois,Lecomte, Frédéric,Hubert, Philippe,De Leval, Xavier,Pirotte, Bernard
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- SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS AS mPGES-1 INHIBITORS
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The present invention relates to bicyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (m PGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
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Page/Page column 36
(2013/03/28)
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- Synthesis of N-heterocyclic ligands for use in affinity and mixed mode chromatography
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A set of heterocyclic ligands have been synthesised for use in the preparation of mixed mode affinity chromatographic adsorbents for application in the purification of proteins, including antibodies. The ligand structures were designed to consist of a pyridinyl or related aza-heterocyclic nucleus bearing a pendant arm containing either an alkylamine, alkylthiol or hydroxyalkyl nucleophilic group to allow their facile immobilisation onto an activated support matrix. Ligand diversity was achieved by altering the length of the alkyl chain between the heterocyclic nucleus and nucleophilic group, varying the position of alkyl chain attachment to the heterocycle, and incorporating extra substituents into the pyridinyl or related aza-heterocyclic ring. This diversity in ligand structure was intended to enable key structural features of the ligand, required for efficient protein binding, to be determined. In contrast to the previously used multi-step procedures for the preparation of analogous substituted pyridine or aza-heterocyclic compounds, the synthesis routes for the ligands described here have generally utilized very mild, one-step reactions with readily available heterocyclic precursors. Copyright
- Mountford, Simon J.,Campi, Eva M.,Robinson, Andrea J.,Hearn, Milton T.W.
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body text
p. 471 - 485
(2011/03/18)
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- C-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS
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The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
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Page/Page column 33
(2011/05/05)
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- Efficient synthesis of 1,3,5-trisubstituted benzenes via three Pd-mediated carbon-sulfur, carbon-nitrogen and carbon-carbon bond formation reactions
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An efficient synthesis of 1,3,5-trisubstituted benzenes via a sequential Pd-mediated carbon-sulfur, carbon-nitrogen, and carbon-carbon bond formation reactions is reported. Selective amidation and sulfonamidation reactions are accomplished via Pd-catalyze
- Liu, Bin,Shetty, Rupa S.,Moffett, Kristofer K.,Kelly, Martha J.
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body text
p. 1680 - 1684
(2011/04/26)
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- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem -lactam antibiotics having structure (I) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar1, Ar2, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 76-77
(2010/04/06)
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- GLUCOCORTICOID RECEPTOR MODULATOR AND METHODS OF USE
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The present invention provides Compound (I): Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and methods for the treatment of inflammatory and immune disorders comprising administering to a patient in need thereof an effective amount of Compound (I) or a pharmaceutically acceptable salt thereof.
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Page/Page column 12
(2010/04/23)
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- 3-OXO-2, 3-DIHYDRO- [1,2, 4] TRIAZOLO [4, 3-A]PYRIDINES AS SOLUBLE EPOXIDE HYDROLASE (SEH) INHIBITORS
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Claimed are intermediates in the synthesis of N-Arylmethyl-3-Oxo-2,3-dihydro- [1,2,4]triazolo[4,3-a]pyridine-6-carboxamides as well as a process (A) to arrive at 3-Oxo-2, 3-dihydro-[1,2,4]triazolo[4,3-a]pyridine-6-carboxylic acid. The triazolo[4,3-a]pyridine-6-carboxamides of formula (I) are used as soluble epoxide hydrolase inhibitors (sEH) having therapeutic effect in pathologic conditions such as hypertension, stroke, inflammatory processes, diabetes and a variety of cardiovascular diseases.
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Page/Page column 57-58
(2010/09/17)
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- CARBACEPHEM β-LACTAM ANTIBIOTICS
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Carbacephem β-lactam antibiotics having the following chemical structures (I) and (II) are disclosed, including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, R1, R2 and R3 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
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Page/Page column 90-91
(2009/05/30)
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- (E)-N-{3- [1-(8-FLUORO-11H-10-OXA-1-AZA-DIBENZO [A,D] CYCL0HEPTEN-5YLIDENE)-PROPYL]-PHENYL }-METHYNSULFON AMIDE AS GLUCOCORTICOID RECEPTOR MODULATOR FOR THE TREATMENT OF RHEUMATOID
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The present invention provides Compound (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising Compound (I) in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents; and discloses met
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Page/Page column 22
(2009/09/04)
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- Magnesiation of pyridine N-oxides via iodine or bromine-magnesium exchange: A useful tool for functionalizing pyridine N-oxides
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Iodo- or 2-bromopyridine N-oxides were readily magnesiated with i-PrMgCl ? LiCl via the iodine or bromine-magnesium exchange. The bromine adjacent to pyridine N-oxide (at the 2- or 6-position) can be regioselectively magnesiated in the presence of other position substituted halogens. This method was tested in various substituted pyridine N-oxide systems, and has been successfully applied to the total synthesis of caerulomycins E and A.
- Duan, Xin-Fang,Zi-Qian, Ma.,Zhang, Fang,Zhang, Zhan-Bin
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supporting information; experimental part
p. 939 - 942
(2009/06/20)
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- Pyridine analogues of nimesulide: Design, synthesis, and in vitro and in vivo pharmacological evaluation as promising cyclooxygenase 1 and 2 inhibitors
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Nonsteroidal anti-inflammatory drugs (NSAIDs) represent one of the most prescribed medications, although the chronic use of such pharmacological agents is commonly associated with numerous side effects. The demonstration that the use of COX-2 selective or
- Renard, Jean-Fran?ois,Arslan, Deniz,Garbacki, Nancy,Pirotte, Bernard,De Leval, Xavier
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supporting information; experimental part
p. 5864 - 5871
(2010/02/28)
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- A safe, convenient and efficient method for the preparation of heterocyclic N-oxides using urea·hydrogen peroxide
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A novel, convenient, and high-yielding method has been developed for the preparation of heterocyclic N-oxides. The reaction uses the urea·hydrogen peroxide addition complex as a peroxide source for the in situ generation of trifluoroperacetic acid. The advantages of this method are easy handling of a stable, solid oxidant; high yields and simple removal of excess reagents and by-products.
- Rong, Dawen,Phillips, Victoria A.,Rubio, Ramón Sánchez,ángeles Castro, Ma,Wheelhouse, Richard T.
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experimental part
p. 6933 - 6935
(2009/04/07)
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- An intra/intermolecular suzuki sequence to benzopyridyloxepines containing geometrically pure exocyclic tetrasubstituted alkenes
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(Chemical Equation Presented) A route to enable the preparation of 5-benzylidenyl-benzopyridyloxepine analogues was developed to continue our research in the field of nuclear hormone receptor modulators. The key steps are1) a syn-stereoselective diboratio
- Carson, Matthew W.,Giese, Matthew W.,Coghlan, Michael J.
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supporting information; experimental part
p. 2701 - 2704
(2009/05/26)
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- NOVEL INHIBITORS
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Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoisomers and polymorphs thereof wherein: R1 represents C2-8alkyl; C2-8alkenyl; —(C1-6alkyl)-aryl; —(C1-6alkyl)-heteroaryl; —(C1-6alkyl)-carbocyclyl; —(C1-6alkyl)-heterocyclyl; -aryl; -heteroaryl; -carbocyclyl or -heterocyclyl; wherein said aryl or heteroaryl groups may be optionally substituted by one or more substituents selected from, C1-4alkyl, C1-4-fluoroalkyl, C1-4alkoxy, C1-4-fluoroalkoxy, hydroxy, —SO2(C1-4alkyl), —SO2N(C1-4alkyl)(C1-4alkyl), —SOC1-4alkyl, —SOC3-6cycloalkyl —C(O)O(C1-4alkyl), benzyloxy and phenyl; and wherein said carbocyclyl and heterocyclyl groups may be optionally substituted by one or more substituents selected from —C1-4 alkyl, —C1-4 alkoxy, hydroxyl, halogen and oxo; R2 represents H; C1-4alkyl or halogen; R3 represents H; C1-4alkyl or halogen; and R4 represents H; C1-4alkyl or halogen.
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Page/Page column 27
(2008/12/08)
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- Aluminum-catalyzed asymmetric alkylations of pyridyl-substituted alkynyl ketones with dialkylzinc reagents
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Alkylations of pyridyl-substituted ynones with Et2Zn and Me 2Zn, promoted by amino acid-based chiral ligands in the presence of Al-based alkoxides, afford tertiary propargyl alcohols efficiently in 57% to >98% ee. Two easily accessib
- Friel, Donna K.,Snapper, Marc L.,Hoveyda, Amir H.
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supporting information; experimental part
p. 9942 - 9951
(2009/02/04)
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- C-FMS KINASE INHIBITORS
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The invention is directed to compounds of Formula II: wherein A, R1, R2, R3, R4, X, Y and W are set forth in the specification, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase.
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Page/Page column 52-53
(2008/06/13)
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- A COMPOSITION FOR TREATING OR PREVENTING A CANCER COMPRISING PYRROLOPYRIDINE DERIVATIVES
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The present invention provides a composition for treating or preventing a cancer comprising a pyrrolopyridine derivative or its salt and a pharmaceutically acceptable carrier.
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Page/Page column 13
(2010/11/25)
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- PYRROLO[3,2-C]PYRIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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The present invention provides novel pyrrolo[3,2-c]pyridine derivatives or pharmaceutically acceptable salts thereof, processes for the preparation thereof, and compositions comprising the same. The pyrrolo[3,2-c]pyridine derivatives or pharmaceutically a
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Page/Page column 10
(2008/06/13)
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- Oxidation of substituted pyridines by dimethyldioxirane: Kinetics and solvent effects
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The second order rate constants for the oxidation of substituted pyridines by dimethyldioxirane at 23°C in dried acetone were found to correlate with sigma values (ρ = -2.91). The reaction was shown to be very sensitive to protic, polar solvents. The oxidation of a series of substituted pyridines by dimethyldioxirane (1) produced the expected N-oxides in quantitative yields. The second order rate constants (k2) for the oxidation of a series of substituted pyridines (2a-g) by dimethyldioxirane were determined in dried acetone at 23°C. An excellent correlation with Hammett sigma values was found (ρ = -2.91, r = 0.995). Kinetic studies for the oxidation of 4-trifluoromethylpyridine by 1 were carried out in the following dried solvent systems: acetone (k2 = 0.017 M-1 s-1), carbon tetrachloride/acetone (7:3; k2 = 0.014 M-1 s -1), acetonitrile/acetone (7:3; k2 = 0.047 M-1 s-1), and methanol/acetone (7:3; k2 = 0.68 M-1 s-1). Kinetic studies of the oxidation of pyridine by 1 versus mole fraction of water in acetone [k2 = 0.78 M-1 s-1 (χ = 0) to k2 = 11.1 M-1 s-1 (χ = 0.52)] were carried out. The results showed the reaction to be very sensitive to protic, polar solvents.
- Winkeljohn, W. Rucks,Vasquez, Pedro C.,Strekowski, Lucjan,Baumstark, Alfons L.
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p. 8295 - 8297
(2007/10/03)
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- Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function
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Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.
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- Spectral and crystallographic study of pyridinic analogues of nimesulide: Determination of the active form of methanesulfonamides as COX-2 selective inhibitors
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Compound 7, N-(3-phenoxy-4-pyridinyl)trifluoromethanesulfonamide, showed in vitro (whole blood assay) a strong inhibitory activity on the two cyclooxygenase (COX) enzymes (IC50(COX1) = 2.2 μM and IC50(COX-2) = 0.4 μM), being more act
- Julémont, Fabien,De Leval, Xavier,Michaux, Catherine,Damas, Jacques,Charlier, Caroline,Durant, Fran?ois,Pirotte, Bernard,Dogné, Jean-Michel
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p. 5182 - 5185
(2007/10/03)
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- Pyrazinone thrombin inhibitors
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein A is
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- Synthesis and pharmacological evaluation of derivatives structuraily related to nimesulide
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The present work reports the synthesis of a series of compounds structurally related to the antiinflammatory and antihistaminic agent nimesulide (I), in which the p-nitrophenyl moiety has been replaced by pyridine (1a-c) and pyridine N-oxide (2a-c). In addition, two compounds (3a, 4a) have been synthesized in which the p-nitro group of I was substituted by a cyano and a 1H-tetrazol-5-yl group, respectively. Representative 1a and 2a were also modified by replacing the methanesulfonamido group with an acetamido group (5a, 6a). The pharmacological evaluation of compounds 1-6 in comparison to I, indicates that such modifications are detrimental to the activity. Moreover 3a and 4a caused bronchoconstriction and hypotension, thus behaving as histaminic-like rather then antihistaminic agents.
- Cignarella,Vianello,Berti,Rossoni
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p. 359 - 364
(2007/10/03)
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- SUBSTITUTED 2-ARYLCARBONYLOXYMETHYL-1,2,5-THIADIAZOLIDIN-3-ONE 1,1-DIOXIDE DERIVATIVES AND COMPOSITIONS AND METHOD OF USE THEREOF
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Substituted 2-arylcarbonyloxymethyl-1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
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- Biphenylmethyl-substituted pyridones
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Biphenylmethyl-substituted pyridones are prepared by reaction of pyridones with appropriate biphenylmethyl compounds. The biphenylmethyl-substituted pyridones can be employed as active compounds in medicaments, in particular for the treatment of arter
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- Sulfonylbenzyl-substituted benzo- and pyridopyridones
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Sulfonylbenzyl-substituted benzo- and pyridopyridones are prepared by reacting corresponding benzo- and pyridopyridones with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted benzo- and pyridopyridones can be employed as active compounds in medicaments, in particular for the treatment of arterial hyper tension and atherosclerosis.
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