- Neutral hosts for the complexation of creatinine
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Three hydrogen bonds are formed between creatinine and derivatives of 2-amino-4(3H)pyrimidone. Changes in the tautomer ratio of the latter upon complexation can be observed by UV spectroscopy. The formation of a further hydrogen bond between creatinine and a 4-aminoacridin-5-yl-amino-substituted 4(3H)pyrimidone seems to be sterically prevented. The properties of three other, quite different compounds assumed to form three hydrogen bonds with creatinine have also been investigated. Dodecyl 4-octadecylallophanate and 2,6-bis(dodecylamino)-pyridine do not associate appreciably with creatinine, which can be explained by the formation of an intramolecular hydrogen bond in the former compound and the lack of tautomerization of the latter. With 6-(1-heptyloctylamino)-2(1H)-pyridone, however, creatinine forms a complex that is almost as stable as those with 2-amino-4(3H)-pyrimidone derivatives.
- Buhlmann,Simon
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Read Online
- A nitrogen oxide C2 - bit hydroxylated method (by machine translation)
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The present invention relates to nitrogen oxide C2 - bit hydroxylated method, in particular under reflux conditions in dichloroethane, three pyrrole alkyl bromide (PyBrop) [...] phosphate, sodium acetate, water and nitrogen oxides produced by the reaction of hydroxyl-substituted product. The process has simple operation, mild condition, high reaction selectivity, substrate wide applicability, high yield and the like. The application for the first time using this method to synthesize a series of 2 - hydroxyquinoline, 2 - hydroxy pyridine and 1 - hydroxy isoquinoline compound, in the establishment of the compounds of the library synthesis application have broad prospects. (by machine translation)
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Paragraph 0031; 0032; 0033; 0034; 0035; 0036-0038; 0135-0150
(2017/05/19)
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- A catalytic oxidation fragrant boron class compound preparing phenol method (by machine translation)
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The invention discloses a method for catalytic oxidation of phenolic compounds fragrant boron class compound synthesis method, the flux in the solvent in the aqueous solution, under the action of alkali, adding hydrazine hydrate or acid hydrazides catalyst, catalytic oxidation fragrant boron class compound directly for the preparation of phenolic compound. The invention of the method of preparation of the phenol compound, the catalyst is a cheap hydrazine hydrate or hydrazine compound, the oxidizing agent is atmospheric pressure of air or oxygen, the reaction does not need good and activeness metal catalyst, is extensive and stable substrate, substrate-sensitive functional group compatibility good and wide range of application. In the optimized under the reaction conditions, the yield of the target product separation up to 99%. (by machine translation)
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Paragraph 0073; 0079; 0080
(2017/08/08)
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- Structure-activity relationships of small molecule autotaxin inhibitors with a discrete binding mode
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Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others. Many of the developed synthetic inhibitors for ATX have resembled the lipid chemotype of the native ligand; however, a small number of inhibitors have been described that deviate from this common scaffold. Herein, we report the structure-activity relationships (SAR) of a previously reported small molecule ATX inhibitor. We show through enzyme kinetics studies that analogues of this chemotype are noncompetitive inhibitors, and by using a crystal structure with ATX we confirm the discrete binding mode.
- Miller, Lisa M.,Keune, Willem-Jan,Castagna, Diana,Young, Louise C.,Duffy, Emma L.,Potjewyd, Frances,Salgado-Polo, Fernando,García, Paloma Engel,Semaan, Dima,Pritchard, John M.,Perrakis, Anastassis,MacDonald, Simon J. F.,Jamieson, Craig,Watson, Allan J. B.
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supporting information
p. 722 - 748
(2017/02/05)
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- Solution and Solid-Phase Stereocontrolled Synthesis of 1,2-cis-Glycopyranosides with Minimally Protected Glycopyranosyl Donors Catalyzed by BF3-N,N-Dimethylformamide Complex
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Methods are described for the stereoselective synthesis of 1,2-cis glycopyranosides in the d-galacto, d-gluco, and 2-azido-2-deoxy-d-glucopyranoside series utilizing minimally protected (3-bromo-2-pyridyloxy) β-d-glycopyranosyl donors in the presence of BF3-N,N-dimethylformamide (DMF) as a catalyst and a variety of alcohol acceptors relying on the "remote activation concept". Precursors to antifreeze glycopeptide components are synthesized in excellent yields and high α/β ratios. The method is adaptable to one-pot sequential glycosidation as well as to solid-supported synthesis giving access to diverse sets of minimally protected α-d-glycopyranosides as major products.
- St-Pierre, Gabrielle,Hanessian, Stephen
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p. 3106 - 3109
(2016/07/14)
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- Asymmetric Homogeneous Hydrogenation of 2-Pyridones
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An asymmetric homogeneous hydrogenation of 2(1H)-pyridones has been developed, using a ruthenium complex bearing two chiral N-heterocyclic carbene (NHC) ligands. To the best of our knowledge, the presented reaction is the first example of a homogeneous asymmetric conversion of 2-pyridones into the corresponding enantioenriched 2-piperidones.
- Wysocki, Jedrzej,Schlepphorst, Christoph,Glorius, Frank
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supporting information
p. 1557 - 1562
(2015/06/30)
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- INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES
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Inhibitors of viral replication of formula (I), their process of preparation and their therapeutical uses. The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.
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Page/Page column 174
(2014/05/07)
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- CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1
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This invention relates to novel compounds of the Formula Ik, Im1, Im2, Im5, In1, In2, In5, Io1, Io2, Io5, Ip1, Ip3, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
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Page/Page column 69
(2011/01/05)
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- COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
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Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
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Page/Page column 82
(2009/12/28)
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- SELECTIVE ESTROGEN RECEPTOR MODULATORS
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The present invention provides a compound represented by the following formula (I); [wherein T represents a single bond, a C1-C4 alkylene group which may have a substituent and the like; formula (I-1) represents a single bond or a double bond; A represents a single bond, a bivalent 5- to 14-membered heterocyclic group which may have a substituent and the like; Y represents a single bond and the like; Z represents a methylene group and the like; ring G represents a phenylene group and the like which may condense with a 5- to 6-membered ring and may have a heteroatom; Ra and Rb are the same as or different from each other and represent a hydrogen atom and the like; W represents a single bond and the like; R' represents 1 to 4 independent hydrogen atoms and the like; and R" represents 1 to 4 independent hydrogen atoms and the like] or a salt thereof, or a hydrate thereof.
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Page/Page column 110
(2008/06/13)
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- Efficient synthesis of halohydroxypyridines by hydroxydeboronation
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This paper describes a general method for the synthesis of halohydroxypyridines from novel halopyridinylboronic acids and esters recently described by some of us. Halopyridinylboronic acids and esters have been efficiently hydroxydeboronated under mild conditions by employing hydrogen peroxide or meta-chloroperbenzoic acid. These hydroxylations take place regioselectively without other oxidation (N-oxide formation).
- Voisin, Anne Sophie,Bouillon, Alexandre,Lancelot, Jean-Charles,Rault, Sylvain
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p. 1417 - 1421
(2007/10/03)
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- Tandem radical reactions of isonitriles with 2-pyridonyl and other aryl radicals: Scope and limitations, and a first generation synthesis of (±)-camptothecin
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Photolysis of N-propargyl-6-halo-2-pyridones and related aromatic halides in the presence of aryl isonitriles provides tetra- and penta-cyclic products in a single step by a sequence of radical addition to the isonitrile followed by two cyclizations. The scope and limitations of the process are described along with a first generation synthesis of racemic camptothecin.
- Curran, Dennis P.,Liu, Hui,Josien, Hubert,Ko, Sung-Bo
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p. 11385 - 11404
(2007/10/03)
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- EQUILIBRE LACTIME-LACTAME DES HYDROXY-PYRIDINES ET DES HYDROXY-PYRIMIDINES (URACILES) EN MILIEU APOLAIRE: ETUDE INFRA-ROUGE
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In contrast to what observed with mono hydroxy-pyridines and -pyrimidines the lactim-lactam equilibrium of uracils is not found to be markedly influenced by solvent polarity.
- Chevrier, Marianne,Bensaude, Olivier,Guillerez, Jean,Dubois, Jacques-Emile
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p. 3359 - 3362
(2007/10/02)
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