cas 124-41-4, Sodium methanolate | Articles data

Articles about 124-41-4Total 109 be found

Article title
Article abstract
Author
Journal number and time
Download

Broensted Acidities of Carbonyl Hydride Complexes of Iron, Ruthenium, and Osmium: pKa Values and Deprotonation Rates in Methanol Solution
Reported are kinetics studies of the reaction of methoxide ion with several mononuclear and polynuclear carbonyl hydride complexes HxMy(CO)z of the iron triad.Deprotonation of the hydrides to give the conjugate base anions occurs with moderate second-order rate constants (ca. 101-104 M-1s-1), considerably smaller than those of oxygen or nitrogen acids of comparable thermodynamic strength under similar conditions.The relative slowness of these reactions is interpreted in terms of possible electronic and structural rearrangements of substrate and solvent occuring as the result of the deprotonation.In addition the kinetics technique allows the measurement of the reverse reacton (protonation of the conjugate base by methanol) rate constants which are also comparatively small (ca. 0.05-25 s-1).The ratio of the forward and reverse rates gives the equilibrium constants from which the pKa's in methanol can be calculated.In several cases pKa's were confirmed by buffer/indicator techniques.From these and other published data are drawn the conclusions that bridging hydrides are more acidic than terminal hydrides and that hydrides of the lighter metals are more acidic than those of homologous heavier metals.Furthermore, it is shown than the substituent effect of replacing CO of a cluster by a trimethyl phosphite is to decrease significantly the acidity of that cluster's hydrides.
Walker, Howard W.,Pearson, Ralph G.,Ford, Peter C.
p. 1179 - 1186
(1983)
Read Online

-
-
Fendler,E.J. et al.
p. 812 - 819
(1972)
Read Online

Kinetic Studies on the Decomposition of Most Typical Meisenheimer Complex of Sodium 1,1-Dimethoxy-2,4,6-trinitrocyclohexadienide in Methanol
The whole decomposition of the Meisenheimer complex formed from 2,4,6-trinitroanisole (TNA) and sodium methoxide proceeds in three steps and obeys the first-order kinetics in each step.The rate of the whole decrease of concentration of the complex is given by -d(+->)/dt=(k1+>+k2)*+(k3+>+k4)*->-k5->*, where k denotes a rate constant.This leads to the modification of the conventional unimolecular mehanism shown by TNA*CH3O- -> TNA +CH3O-.
Abe, Takehiro
p. 1399 - 1405
(1980)
Read Online

Identification of 1, 4-Dihydrothieno[3', 2':5, 6]thiopyrano [4, 3-c]pyrazole derivatives as human 5-lipooxygenase inhibitors
A series of novel 1,4-dihydrothieno[3',2':5,6]thiopyrano [4,3-c]-pyrazole-3-carboxamide derivatives were synthesized and evaluated for their inhibitory activity to human 5-lipo-oxygenase (5-LOX). Compound 7c was found to exhibit significant inhibition to human 5-LOX with IC50 value of 5.7 ± 0.9 μM. Compound 7c was further studied using molecular docking in order to delineate its structure-activity relationship and to gain insight into the design of effective 5-LOX inhibitors.
Hu, Jianshu,Zhu, Wei,Meng, Hu,Liu, Ying,Wang, Xin,Hu, Chun
p. 642 - 647
(2014)
Read Online

Standard molar enthalpies of formation of sodium alkoxides
The molar enthalpies of solution of sodium in methanol, ethanol, and n-propanol and of sodium alkoxides in their corresponding alcohols were measured at T = 298.15 K using an isoperibol solution calorimeter. From these results and other auxiliary data, the standard molar enthalpies of formation Δf Hm{ring operator} (RONa,cr) of sodium methoxide, sodium ethoxide, and sodium n-propoxide were calculated and found to be {(-366.21 ± 1.38), (-413.39 ± 1.45), and (-441.57 ± 1.18)} kJ · mol-1, respectively. A linear correlation has been found between Δf Hm{ring operator} (RONa) and Δf Hm{ring operator} (ROH) for R = n-alkyl, enabling the prediction of data for other sodium alkoxides.
Chandran,Srinivasan,Gopalan,Ganesan
p. 449 - 454
(2007)
Read Online

Synthesis and antimicrobial activities evaluation of some new thiadiazinone and thiadiazepinone derivatives bearing sulfonamide moiety
A new series of novel functionalized 1,3,4-thiadiazin-5-ones and 1,3,4-thiadi-azepin-5-ones bearing sulfonamide moieties were synthesized via 1,3-dipolar cyclocondensation reaction of nitrilimines with α-mercaptoesters and mercaptosuccinic acid respectively. The structures of the prepared compounds were confirmed by spectral methods (IR, 1H-NMR, 13C-NMR and MS spectroscopy) and elemental analysis. The newly synthesized compounds were screened for their in vitro antimicrobial activity. Some of titled compounds exhibited significant antimicrobial activity on several strains of microbes.
Dalloul, Hany M. M.,El-Nwairy, Khaled A.,Shorafa, Ali Z.,Abu Samaha, Ahmed S.
p. 288 - 293
(2018)
Read Online

Synthesis and evaluation of the cytotoxic activity of water-soluble cationic organometallic complexes of the type [Pt(η1-C2H4OMe)(L)(phen)]+ (L = NH3, DMSO; phen = 1,10-phenanthroline)
Starting from the [PtCl(η1-C2H4OMe)(phen)] (phen = 1,10-phenanthroline, 1) platinum(II) precursor, we synthesized and characterized by multinuclear NMR new [Pt(η1-C2H4OMe)(L)(phen)]+ (L = NH3, 2; DMSO, 3) complexes. These organometallic species, potentially able to interact with cell membrane organic cation transporters (OCT), violating some of the classical rules for antitumor activity of cisplatin analogues, were evaluated for their cytotoxicity. Interestingly, despite both complexes 2 and 3 resulting in greater cell uptake than cisplatin in selected tumor cell lines, only 3 showed comparable or higher antitumor activity. General low cytotoxicity of complex 2 in the tested cell lines (SH-SY5Y, SK-OV-3, Hep-G2, Caco-2, HeLa, MCF-7, MG-63, ZL-65) appeared to depend on its stability towards solvolysis in neutral water, as assessed by NMR monitoring. Differently, the [Pt(η1-C2H4OMe)(DMSO)(phen)]+ (3) complex was easily hydrolyzed in neutral water, resulting in a comparable or higher cytotoxicity in cancer cells with respect to cisplatin. Further, both IC50 values and the uptake profiles of the active complex appeared quite different in the used cell lines, suggesting the occurrence of diversified biological effects. Nevertheless, further studies on the metabolism of complex 3 should be performed before planning its possible use in tissue- and tumor-specific drug design.
De Castro, Federica,Stefàno, Erika,Migoni, Danilo,Iaconisi, Giorgia N.,Muscella, Antonella,Marsigliante, Santo,Benedetti, Michele,Fanizzi, Francesco P.
(2021)
Read Online

Anti-Helicobacter pylori activity of some newly synthesized derivatives of xanthone
A series of 20 xanthone derivatives was synthesized and evaluated for anti-Helicobacter pylori (H. pylori) activity. Qualitative and quantitative in vitro tests using the Kirby-Bauer method (agar disc-diffusion method) were performed. The tested compounds were screened against clarithromycin- and/or metronidazole-resistant strains of H. pylori. As a reference, Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli) bacterial strains were examined. On the basis of microbiological assays, xanthones can be considered as potential anti-H. pylori agents. They displayed significant activity against the examined strains, which was higher against the bacteria resistant to metronidazole than clarithromycin. The lowest MIC values ranging up to 20 mg l-1 were observed for the following compounds: 3, 4, 8, 9, 12, 19 (against the metronidazole-resistant strains) and the compound 10 (against the clarithromycin-resistant strain). These preliminary results for screening of xanthone derivatives form a part of an ongoing study of the structure-activity relationships of a large group of compounds. Microbiological assays will be conducted afterwards to determine the mechanism of xanthones' action against H. pylori.
Klesiewicz, Karolina,Karczewska, Elzbieta,Budak, Alicja,Marona, Henryk,Szkaradek, Natalia
p. 825 - 834
(2016)
Read Online

Investigation of the crystal structures and magnetic features of two bis(dithiolato)nickelate salts with flexible organic cations
Two bis(dithiolato)nickel salts with different flexible ammonium counterions, [Et3MeN][Ni(dmit)2] (1) and [(i-Bu)Et3N][Ni(dmit)2] (2) (dmit2? = 2-thioxo-1,3-dithiole-4,5-dithiolate, Et3MeN+ = triethylmethylammonium, (i-Bu)Et3N+ = triethylisobutylammonium), are prepared and identified by powder X-ray diffraction (PXRD) patterns and single-crystal X-ray diffraction. Salt 1 crystallizes in the triclinic space group P???1 at 293?K. The anions and cations in 1 form alternating layered arrangements along the a-axis direction. Salt 2 belongs to the monoclinic crystal system and space group P21/n. The anions and cations in 2 form separate columnar stacks along bc-plane direction. The neighboring anions are stacked as dimers in the anion columnar stacks of 2. The magnetic features of salts 1 and 2 show 1D alternating spin chain magnetic exchange behavior, and the magnetic experimental data are well fitted through a spin chain magnetic model. The difference in the crystal structures and magnetic properties between the two new salts 1 and 2 fully demonstrates that the magnetic properties are dependent on the alignment of the [Ni(dmit)2]? anions, which are related to the flexible organic cations. Graphical abstract: [Figure not available: see fulltext.]
Chen, Xuan-Rong,Zhang, Zhen-Min,Luo, Min,Liu, Hang,Yuan, Jia-Yi
p. 353 - 362
(2021)
Read Online

Near-infrared light-controlled circularly polarized luminescence of self-organized emissive helical superstructures assisted by upconversion nanoparticles
A near-infrared light-driven self-organized emissive helical superstructure was constructed by doping a new chiral fluorescent photoswitch and upconversion nanoparticles (UCNPs) into a nematic LC. The reversible switching of circularly polarized luminescence (CPL) can be achieved by modulating the power intensity of the 980 nm NIR excitation light.
Juan, Ao,Sun, Hao,Qiao, Jinghui,Guo, Jinbao
p. 13649 - 13652
(2020)
Read Online

-
-
Crampton,M.R. et al.
p. 825 - 826
(1975)
Read Online

Synthesis and herbicidal activities of novel 3-(α-hydroxymethylene) pyrrolidine-2,4-dione derivatives containing a cyclopropane moiety
A variety of novel 3-(α-hydroxymethylene)pyrrolidine-2,4-dione derivatives containing a cyclopropane moiety were designed and synthesized in satisfactory yields. Their structures were confirmed by 1H NMR and HRMS. The bioassays indicated that most of the title compounds displayed some extent herbicidal activities at 100 mg/mL.
Zhu, You-Quan,Zhang, Jin,Yuan, Yan-Wei,Xie, Li-Fen,Xu, Hai-Zhen,Zou, Xiao-Mao,Yang, Hua-Zheng
p. 202 - 205
(2013)
Read Online

Chemical transformations and biological studies of terpenoids isolated from essential oil of Cyperus scariosus
Cyperus scariosus is a potential medicinal herb belonging to the family Cyperaceae. The GC-MS analysis of the oil showed cyprene (18.57 %) as the major terpene present in it. Cyprene was isolated from the non-polar fraction of the oil using hexane as solvent and characterized using TLC and spectral techniques (IR and 1H NMR). Cyprene was derivatized to cyprene epoxide by two methods i.e. using perbenzoic acid and epichlorohydrin. Further, the oil, it's polar fraction (dichloromethane), non-polar fraction (hexane), cyprene and cyprene epoxide were screened for their plant growth regulating property in case of wheat seedlings (HD 2967 and PBW 621). Complete germination was observed above 2.5 μg/mL of all the test fractions in both the cultivars. Moreover, cyprene epoxide was found to be the most effective in enhancing the length of roots and shoots. Seedling vigour index was calculated in order to analyze the enhancement shown by the oil and its various components on the seedlings.
Sharma,Utreja,Bedi
p. 2153 - 2158
(2016)
Read Online

Synthesis and structure of hypercoordinated germanate complexes with naphthalene-2,3-dialkoxide ligands
The synthesis of six-coordinated germanate complexes with naphthalene-2,3-dialkoxide ligands with alkali metals (Li, Na, and K) as counter ions are described. The molecular structures of lithium and potassium germanate complexes were clarified by X-ray diffraction analysis. Each germanium center atom is coordinated by six oxygen atoms to form slightly distorted octahedral configuration. All the compounds were thermally stable up to 300 °C determined by thermogravimetric analysis under air-flow conditions.
Goto, Mitsuki,Nakashima, Yuta,Nanjo, Masato
(2021)
Read Online

Synthesis, monoamine oxidase inhibition activity and molecular docking studies of novel 4-hydroxy-N′-[benzylidene or 1-phenylethylidene]-2-H/methyl/benzyl-1,2-benzothiazine-3-carbohydrazide 1,1-dioxides
Three series of 4-hydroxy-N′-[benzylidene/1-phenylethylidene]-2-H/methyl/benzyl-1,2-benzothiazine-3-carbohydrazide 1,1-dioxides (9–11)a-l were synthesized and unraveled to be highly potent dual inhibitors of monoamine oxidases (MAO-A and MAO-B). All the examined compounds demonstrated IC50 values in lower micro-molar range for both MAO-A as well as MAO-B. The most active MAO-A inhibitor was 4-hydroxy-N′-(1-phenylethylidene)-2H-benzo[e][1,2]thiazine-3-carbohydrazide 1,1-dioxide (9i) with an IC50 value of 0.11 ± 0.005 μM, whereas, methyl 4-hydroxy-2H-benzo[e][1,2]thiazine-3-carboxylate 1,1-dioxide (3) was the most active MAO-B inhibitor with an IC50 value of 0.21 ± 0.01 μM. Enzyme kinetics studies revealed that the most potent compounds inhibited both MAO enzymes (A & B) in a competitive fashion. Molecular docking studies were also performed to obtain an intuitive picture of inhibition potential for potent inhibitors. The high potency of these compounds is optimally combined with highly favorable ADME profile with predicted good oral bioavailability.
Saddique, Furqan Ahmad,Zaib, Sumera,Jalil, Saquib,Aslam, Sana,Ahmad, Matloob,Sultan, Sadia,Naz, Humera,Iqbal, Mazhar,Iqbal, Jamshed
p. 1373 - 1386
(2018)
Read Online

Evolution of the Synthesis of AMPK Activators for the Treatment of Diabetic Nephropathy: From Three Preclinical Candidates to the Investigational New Drug PF-06409577
Indole acids 1, 2, and 3 are potent 5′-adenosine monophosphate-activated protein kinase (AMPK) activators for the potential treatment of diabetic nephropathy. Compounds 1-3 were scaled to supply material for preclinical studies, and indole 3 was selected for advancement to first-in-human clinical trials and scaled to kilogram quantities. The progression of the synthesis strategy for these AMPK activators is described, as routes were selected for efficient structure-activity relationship generation and then improved for larger scales. The developed sequences employed practical isolations of intermediates and APIs, reproducible cross-coupling, hydrolysis, and other transformations, and enhanced safety and purity profiles and led to the production of 40-50 g of 1 and 2 and 2.4 kg of 3. Multiple polymorphs of 3 were observed, and conditions for the reproducible formation of crystalline material suitable for clinical development were identified.
Smith, Aaron C.,Kung, Daniel W.,Shavnya, Andre,Brandt, Thomas A.,Dent, Philip D.,Genung, Nathan E.,Cabral, Shawn,Panteleev, Jane,Herr, Michael,Yip, Ka Ning,Aspnes, Gary E.,Conn, Edward L.,Dowling, Matthew S.,Edmonds, David J.,Edmonds, Ian D.,Fernando, Dilinie P.,Herrinton, Paul M.,Keene, Nandell F.,Lavergne, Sophie Y.,Li, Qifang,Polivkova, Jana,Rose, Colin R.,Thuma, Benjamin A.,Vetelino, Michael G.,Wang, Guoqiang,Weaver, John D.,Widlicka, Daniel W.,Price Wiglesworth, Kristin E.,Xiao, Jun,Zahn, Todd,Zhang, Yingxin
p. 681 - 696
(2018)
Read Online

Ni-Catalyzed 1,2-Diarylation of Alkenyl Ketones: A Comparative Study of Carbonyl-Directed Reaction Systems
A nickel-catalyzed 1,2-diarylation of alkenyl ketones with aryl iodides and arylboronic esters is reported. Ketones with a variety of substituents serve as effective directing groups, offering high levels of regiocontrol. A representative product is diversified into a wide range of useful products that are not readily accessible via existing 1,2-diarylation reactions. Preliminary mechanistic studies shed light on the binding mode of the substrate, and Hammett analysis reveals the effect of electronic factors on initial rates.
Apolinar, Omar,Derosa, Joseph,Engle, Keary M.,Karunananda, Malkanthi K.,Kleinmans, Roman,Li, Zi-Qi,Tran, Van T.,Wisniewski, Steven R.
supporting information
p. 5311 - 5316
(2021/07/26)

Bithiazole Inhibitors of Phosphatidylinositol 4-Kinase (PI4KIIIβ) as Broad-Spectrum Antivirals Blocking the Replication of SARS-CoV-2, Zika Virus, and Human Rhinoviruses
Over half a century since the description of the first antiviral drug, “old” re-emerging viruses and “new” emerging viruses still represent a serious threat to global health. Their high mutation rate and rapid selection of resistance toward common antiviral drugs, together with the increasing number of co-infections, make the war against viruses quite challenging. Herein we report a host-targeted approach, based on the inhibition of the lipid kinase PI4KIIIβ, as a promising strategy for inhibiting the replication of multiple viruses hijacking this protein. We show that bithiazole inhibitors of PI4KIIIβ block the replication of human rhinoviruses (hRV), Zika virus (ZIKV) and SARS-CoV-2 at low micromolar and sub-micromolar concentrations. However, while the anti-hRV/ZIKV activity can be directly linked to PI4KIIIβ inhibition, the role of PI4KIIIβ in SARS-CoV-2 entry/replication is debated.
Grazia Martina, Maria,Vicenti, Ilaria,Bauer, Lisa,Crespan, Emmanuele,Rango, Enrico,Boccuto, Adele,Olivieri, Noemi,Incerti, Matteo,Zwaagstra, Marleen,Allodi, Marika,Bertoni, Simona,Dreassi, Elena,Zazzi, Maurizio,van Kuppeveld, Frank J. M.,Maga, Giovanni,Radi, Marco
supporting information
p. 3548 - 3552
(2021/09/09)

NHC-CDI Betaine Adducts and Their Cationic Derivatives as Catalyst Precursors for Dichloromethane Valorization
Zwitterionic adducts of N-heterocyclic carbene and carbodiimide (NHC-CDI) are an emerging class of organic compounds with promising properties for applications in various fields. Herein, we report the use of the ICyCDI(p-Tol) betaine adduct (1a) and its cationic derivatives2aand3aas catalyst precursors for the dichloromethane valorization via transformation into high added value products CH2Z2(Z = OR, SR or NR2). This process implies selective chloride substitution of dichloromethane by a range of nucleophiles Na+Z-(preformed or generatedin situfrom HZ and an inorganic base) to yield formaldehyde-derived acetals, dithioacetals, or aminals with full selectivity. The reactions are conducted in a multigram-scale under very mild conditions, using dichloromethane both as a reagent and solvent, and very low catalyst loading (0.01 mol %). The CH2Z2derivatives were isolated in quantitative yields after filtration and evaporation, which facilitates recycling the dichloromethane excess. Mechanistic studies for the synthesis of methylal CH2(OMe)2rule out organocatalysis as being responsible for the CH2transfer, and a phase-transfer catalysis mechanism is proposed instead. Furthermore, we observed that1aand2areact with NaOMe to form unusual isoureate ethers, which are the actual phase-transfer catalysts, with a strong preference for sodium over other alkali metal nucleophiles.
Sánchez-Roa, David,Mosquera, Marta E. G.,Cámpora, Juan
p. 16725 - 16735
(2021/11/18)

Application of myrtle ketone compound in preparation of novel coronavirus SARS-CoV-2 medicine
The invention discloses application of myrtle ketone compounds in preparation of novel coronavirus SARS-CoV-2 medicaments. The myrtle ketone compound has obvious inhibition effect on novel coronavirus SARS-CoV-2. Mechanisms include, but are not limited to, inhibition of new coronavirus SARS-CoV-2 into cells, preventing the replication of new coronavirus SARS-CoV-2 in the host cell, and timely modulating apoptosis of infected cells. To the myrtle ketone compound provided by the invention, the novel coronavirus SARS-CoV-2 has a remarkable inhibiting effect, and the cytotoxicity is relatively small. It can therefore be used for the prophylaxis or treatment of neoplastic pneumonitis. The invention is expected to provide new candidate drug molecules for clinic treatment of nebrodensis.
-
Paragraph 0045; 0048; 0051-0052

(2021/12/07)

Mechanistic Studies on the Base-Promoted Ring Opening of Glycal-Derived gem-Dibromocyclopropanes
In the presence of a nucleophilic base, ring-fused gem-dibromocyclopropanes derived from d-glycals undergo ring opening to give 2-deoxy-2-(E-bromomethylene)glycosides. Such cleavage of an exocyclic cyclopropane bond contrasts with the more usual silver-promoted ring-expansion reactions in which endocyclic bond cleavage occurs. Experimental and theoretical studies are reported which provide insights into the reaction mechanism and the origin of its kinetic selectivity for E-configured bromoalkene products. Density functional theory computations (M06-2X) predict that the reaction commences with alkoxide-induced HBr elimination from the dibromocyclopropane to form a bromocyclopropene. Ring opening then gives a configurationally stable zwitterionic (oxocarbenium cation/vinyl carbanion) intermediate, which undergoes nucleophilic addition and protonation to give the bromoalkene. There are two competing sources of the proton in the final step: One is the alcohol (co)solvent, and the other is the molecule of alcohol produced during the initial deprotonation step. The roles of the formed alcohol molecule and the bulk (co)solvent are demonstrated by isotope-labeling studies performed with deuterated solvents. The acid-promoted isomerization of the E-bromoalkene product into the corresponding Z-bromoalkene is also described. The mechanistic knowledge gained in this investigation sheds light on the unusual chemistry of this system and facilitates its future application in new settings.
Harvey, Joanne E.,Hewitt, Russell J.,Krenske, Elizabeth H.,Lepage, Romain J.,Moore, Peter W.,Teesdale-Spittle, Paul H.
supporting information

(2022/01/03)

Accessing dihydro-1,2-oxazine via cloke-wilson-type annulation of cyclopropyl carbonyls: application toward the diastereoselective synthesis of pyrrolo[1,2- b][1,2]oxazine
A convenient additive-free synthesis of dihydro-4H-1,2-oxazines via a Cloke-Wilson-type ring expansion of the aryl-substituted cyclopropane carbaldehydes with the hydroxylamine salt is introduced. Comparatively less active cyclopropyl ketones also follow a similar protocol if supplemented by catalytic p-toluene sulfonic acid monohydrate. The transformation is performed in an open-to-air flask as it shows negligible sensitivity toward air/moisture. Dihydro-4H-1,2-oxazines when subjected to cycloaddition with the cyclopropane diester afford a trouble-free formulation of the valued hexahydro-2H-pyrrolo[1,2-b][1,2]oxazine derivatives. A cascade one-pot variant of this two-step strategy offers a comparable overall yield of the final product.
Banerjee, Prabal,Kumar, Pankaj,Kumar, Rakesh
p. 6535 - 6550
(2020/06/09)

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Provided herein are compounds of Formula (I-I): and pharmaceutically acceptable salts thereof; wherein p, R1, R3a, R2a, R11a, R11b, R6a, and R6b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-X) and methods of using the compounds, e.g., in the treatment of CNS-related disorders.
-
Paragraph 0554; 0559; 0585; 0683

(2019/07/13)

Water/Alkali-Catalyzed Reactions of Azides with 2-Cyanothioacetamides. Eco-Friendly Synthesis of Monocyclic and Bicyclic 1,2,3-Thiadiazole-4-carbimidamides and 5-Amino-1,2,3-triazole-4-carbothioamides
The reactions of thioamides with azides in water were studied. It was reliably shown that the reaction of 2-cyanothioacetamides 1 with various types of azides 2 in water in the presence of alkali presents an efficient, general, one-step, atom-economic, and eco-friendly method for the synthesis of 1,2,3-thiadiazol-4-carbimidamides 5 and 1,2,3-triazole-4-carbothioamides 4. This method can be extended to the one-pot reaction of sulfonyl chlorides and 6-chloropyrimidines 2′o with sodium azide, leading to final products in higher yields, that is, avoiding the isolation of unsafe sulfonyl azides. The method was furthermore applied to the reaction of N,N′-bis-(2-cyanothiocarbonyl)pyrazine 1h with sulfonyl azides to afford bicyclic 1,2,3-thiadiazoles 8 and 1,2,3-triazoles 9 connected via a 1,1′-piperazinyl linker. 2-Cyanothioacetamides 1 were also shown to react with aromatic azides in water in the presence of alkali to afford 1-aryl-5-amino-1,2,3-triazole-4-carbothioamides 11. In contrast to aromatic azides and similarly to sulfonyl azides, 6-azidopyrimidine-2,4-diones 2o-q react with cyanothioacetamides to form N-pyrimidin-6-yl-5-dialkylamino-1,2,3-thiadiazole-4-N-l-carbimidamides 12. A mechanism was proposed to rationalize the role of water in changing the reactivity of azides toward 2-cyanothioacetamides.
Filimonov, Valeriy O.,Dianova, Lidia N.,Beryozkina, Tetyana V.,Mazur, Dmitrii,Beliaev, Nikolai A.,Volkova, Natalia N.,Ilkin, Vladimir G.,Dehaen, Wim,Lebedev, Albert T.,Bakulev, Vasiliy A.
p. 13430 - 13446
(2019/10/16)

Synthesis of Isoxazole- And Oxazole-4-carboxylic Acids Derivatives by Controlled Isoxazole-Azirine-Isoxazole/Oxazole Isomerization
The first synthesis of isoxazole-4-carboxylic acid derivatives by domino isoxazole-isoxazole isomerization is reported. Fe(II)-catalyzed isomerization of 4-acyl-5-methoxy-/5-aminoisoxazoles (dioxane, 105 °C) leads to the formation of isoxazole-4-carboxylic esters and amides in good yields. 4-Formyl-5-methoxyisoxazoles give methyl oxazole-4-carboxylates under the same reaction conditions. Fe(II)-catalyzed isomerization of 4-acyl-5-methoxyisoxazoles under milder conditions (MeCN, 50 °C) allows the preparation of transient 2-acyl-2-(methoxycarbonyl)-2H-azirines. The azirines isomerize quantitatively either into isoxazoles under catalytic conditions (dioxane, 105 °C) or into oxazoles under noncatalytic thermolysis (o-dichlorobenzene, 170 °C). The mechanism of the isomerization and dependence of the reaction routes on substituents at starting isoxazole core and reaction conditions are discussed on the basis of DFT calculations.
Serebryannikova, Anna V.,Galenko, Ekaterina E.,Novikov, Mikhail S.,Khlebnikov, Alexander F.
p. 15567 - 15577
(2019/11/16)

Rare earth complex with benzoyl trifluoroacetone derivative as ligand and high light emission efficiency and preparation and application of rare earth complex
The invention provides a rare earth complex with a benzoyl trifluoroacetone derivative as ligand and high light emission efficiency and preparation and application of the rare earth complex. A benzoyltrifluoroacetone derivative is designed and synthesized as the ligand, the ligand and europium chloride form the rare earth complex, infrared spectrums, ultraviolet spectrums, fluorescent spectrums and the like of the complex are represented, in addition, structures and properties of the complex are specially studied, results show that the designed and synthesized ligand with rare earth metal europium ions is successfully coordinated, and the prepared rare earth complex has high light emission efficiency; due to design and synthesis of beta-diketone ligand, a function of instructing regulation and control on the light emission effect of rare earth metal ions can be achieved, and the application values of a europium metallic rare earth light emission material can be greatly increased.
-
Paragraph 0103-0109

(2019/01/16)

Efficient Synthesis of N-Substituted 2,4-Azepandione Ring System as an Active Intermediate for Heterocyclic Syntheses
An improved efficient synthesis for 2,4-azepandiones (3, 8, and 14) could be achieved by a careful control of the reaction conditions to cyclize ethyl 4-(N-acetylarylamino) butanoate (1, 7, and 13), respectively. The ethyl 4-arylamino butanoate (9 or 12) was prepared by stirring the ethyl 4-bromobutanoate and substituted anilines at room temperature. Then, they were acetylated with acetyl chloride and triethylamine under the conditions that avoid the formation of 2-pyrrolidinone derivatives 10. Due to the rapid decomposition of the acetylated product (7 or 13) to its starting material (9 or 12), the reaction mixture is directly transferred without workup to the next cyclization step. The azepandione synthesis is favored by using a weak base at low temperature, where it is in a competition with the other modes of ring closure. The structures of the new compounds were supported by correct analytical and spectral data.
Waly, Mohamed A.,Yossif, Shiam A.,Ibrahim, Ismail T.,Sofan, Mamdouh A.
p. 1318 - 1326
(2017/03/27)

Technology for producing sodium methoxide from metallic sodium
The invention discloses a technology for producing sodium methoxide from metallic sodium. The technology comprises the following steps: 1, charging: conveying industrial methanol to a methanol metering tank through using a pump, and adding 120g of the metallic sodium to a reaction kettle; 2, carrying out nitrogen displacement: stopping charging and closing an emptying valve, introducing nitrogen to the reaction kettle to make the index of a pressure meter reach 0.1mpa, opening the emptying valve to release pressure, repeating closing and opening three times, and keeping a reflux emptying valve to be in an open state in order to continuously introduce nitrogen; 3, reacting: introducing cooling water to a condense, immediately adding methanol through the methanol metering tank, reacting for 5-10min, stopping introduction of nitrogen, continuously adding methanol to realize metered addition of 820kg of methanol within 2-3h, closing a methanol charging valve, and continuously reacting for 2-3h until no bubbles are generated in a reaction solution; and 4, blending: putting a product obtained in step 3 in a blending storage tank, sampling the product, analyzing the sampled product, blending the product to obtain a required concentration, and barreling the product with the required concentration. An industrial product of sodium methoxide is successfully prepared through adopting the sodium method production technology, and the content, the free alkali and other indexes of the product are better than normal standards. The production technology adopting the sodium method has the advantages of simplification, device investment reduction, meeting of special needs of the medicine industry and other industries, and provision of great economic benefits for enterprises.
-
Paragraph 0007

(2016/11/17)

Preparation method for low residual granular sodium alkoxide or potassium alcoholate
The invention provides a preparation method for low residual granular sodium alkoxide or potassium alcoholate. The method includes using sodium or potassium and alcohol as raw materials, mixing the mixture with a solvent, reacting in inert gas atmosphere by using a microwave heating method, and removing the residual alcohol and solvent in the presence of microwave after the reaction to get the granular sodium alkoxide or potassium alcoholate. The microwave frequency is 2450 +/- 50 MHz. The method can prepare sodium alkoxide or potassium alcoholate with low residual solvent, and the prepared sodium alkoxide or potassium alcoholate is large granular solid, so that the development from powdered product to granular product can be realized, and the problems of residual solvent and potential risk troubled human for a long time can be overcome.
-
Paragraph 0022-0023

(2017/01/17)

Tuning the Reactivity of Terminal Nickel(III)-Oxygen Adducts for C-H Bond Activation
Two metastable NiIII complexes, [NiIII(OAc)(L)] and [NiIII(ONO2)(L)] (L = N,N′-(2,6-dimethylphenyl)-2,6-pyridinedicarboxamidate, OAc = acetate), were prepared, adding to the previously prepared [NiIII(OCO2H)(L)], with the purpose of probing the properties of terminal late-transition metal oxidants. These high-valent oxidants were prepared by the one-electron oxidation of their NiII precursors ([NiII(OAc)(L)]- and [NiII(ONO2)(L)]-) with tris(4-bromophenyl)ammoniumyl hexachloroantimonate. Fascinatingly, the reaction between any [NiII(X)(L)]- and NaOCl/acetic acid (AcOH) or cerium ammonium nitrate ((NH4)2[CeIV(NO3)6], CAN), yielded [NiIII(OAc)(L)] and [NiIII(ONO2)(L)], respectively. An array of spectroscopic characterizations (electronic absorption, electron paramagnetic resonance, X-ray absorption spectroscopies), electrochemical methods, and computational predictions (density functional theory) have been used to determine the structural, electronic, and magnetic properties of these highly reactive metastable oxidants. The NiIII-oxidants proved competent in the oxidation of phenols (weak O-H bonds) and a series of hydrocarbon substrates (some with strong C-H bonds). Kinetic investigation of the reactions with di-tert-butylphenols showed a 15-fold enhanced reaction rate for [NiIII(ONO2)(L)] compared to [NiIII(OCO2H)(L)] and [NiIII(OAc)(L)], demonstrating the effect of electron-deficiency of the O-ligand on oxidizing power. The oxidation of a series of hydrocarbons by [NiIII(OAc)(L)] was further examined. A linear correlation between the rate constant and the bond dissociation energy of the C-H bonds in the substrates was indicative of a hydrogen atom transfer mechanism. The reaction rate with dihydroanthracene (k2 = 8.1 M-1 s-1) compared favorably with the most reactive high-valent metal-oxidants, and showcases the exceptional reactivity of late transition metal-oxygen adducts.
Pirovano, Paolo,Farquhar, Erik R.,Swart, Marcel,McDonald, Aidan R.
supporting information
p. 14362 - 14370
(2016/11/13)

Synthesis of functional isoxazole derivatives proceeding from (5-arylisoxazol-3-yl)chloromethanes
Reaction of 3-chloromethyl-5-phenyl(p-tolyl)isoxazoles with substituted phenols under the conditions of Williamson reaction afforded the corresponding 3-aryloxymethyl-5-phenyl(p-tolyl)isoxazoles. Treating the latter with sodium methylate, sodium phenyl(benzyl, furfuryl)thiolates and morpholine in methanol resulted in the replacement of the chlorine atom in 3-chloromethyl-5-phenyl(p-tolyl)isoxazoles by methoxy-, phenyl-(benzyl, furfuryl)sulfanyl groups and morpholine residue.
Potkin,Bumagin,Petkevich,Dikusar,Semenova,Kurman,Zolotar',Pashkevich,Gurinovich,Kul'Chitskii
p. 1119 - 1130
(2015/10/12)

2-(HETERO)ARYL-BENZIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF ASPARAGIME EMETHYL TRANSFERASE
Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from:, a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are β to one another; L1 is selected from: (i)A1-O-CH2-A2; (ii)A1-CH2-O-A2; (iii)A1-C(=O)-NH-A2; (iv)A1-CH(OH)-A2; (v)A1-CH2-NH-C(=O)-A2; (vi) A1-S-CH2-A2; (vii)A1- CH2-S-A2; (viii)A1-CH2-A2; and (ix)A1-CH(CH3)-O-A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.
-
Page/Page column 136

(2014/09/03)

Synthesis of a series of carbon-14 labeled tetrahydropyrido[4,3-d] pyrimidin-4(3H)-ones
A series of tetrahydropyrido[4,3-d]pyrimidin-4(3H)-ones labeled with carbon-14 in the 2-position of pyrimidinone moiety were prepared as part of a 3-step sequence from benz[amidino-14C]amidine hydrochloride as a key synthetic intermediate. Copyright
Arjomandi, Omid Khalili,Saemian, Nader,McGeary, Ross P.,Shirvani, Gholamhossein
p. 722 - 725
(2014/01/06)

GABAERGIC RECEPTOR SUBTYPE SELECTIVE LIGANDS AND THEIR USES
Described herein are α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands, pharmaceutical compositions, and methods of use of such ligands and compositions in treatment of anxiety disorders, epilepsy and schizophrenia with reduced sedative and ataxic side effects. In embodiments, such as α3 or α2 or α2/α3 GABAergic receptor subtype selective ligands lack ester linkages and may be thus relatively insensitive to hydrolysis by esterases.
-
Page/Page column 26

(2012/12/13)

Novel Platensimycin Derivatives, Their Intermediates, and Process for Preparing the Same, and New Process for Preparing Platensimycin
The present invention relates to novel platensimycin derivatives, their intermediates and preparing methods of the same. Platensimycin is known as an effective antibiotic material having a broad antimicrobial spectrum and its derivatives are also expected to be effective antibiotic candidates. The present invention also relates to a novel preparing method of platensimycin. The intermediates used for the production of platensimycin and its derivatives of the present invention are tricyclo ketone derivatives and tetracyclo derivatives. Tetracyclo derivatives are prepared from tricyclo ketone derivatives prepared by carbonyl ylide [3+2] cycloaddition of dia-zoketone derivative.
-
Page/Page column 19

(2011/02/25)

POLYMERIZABLE PHOTOINITIATORS AND RADIATION CURABLE COMPOSITIONS
A new type of polymerizable Norrish Type II photoinitiators having an optionally substituted benzophenone group or an optionally substituted thioxanthone group is disclosed exhibiting improved compatibility with and solubility in radiation curable compositions. Radiation curable compositions and inkjet inks containing these polymerizable Norrish Type Il photoinitiators, exhibiting low extractable amounts of the photoinitiators and their residues after curing, are also disclosed.
-
Page/Page column 36

(2010/04/06)

AZA PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
MCHR1 antagonists are provided having the following Formula (I): A 1 and A 2 are independently C or N, E is C or N, Q 1 , Q 2 , and Q 3 are independently C or N provided that at least one of Q 1 , Q 2 , and Q 3 is N but not more than one of Q 1 , Q 2 , and Q 3 is N, D 1 is a bond, -CR 8 R 9 X-, -XCR 8 R 9 -, -CHR 8 CHR 9 -, -CR 10 =CR 10' -, -C-C-, or 1,2-cyclopropyl; X is O, S or NR 11, R 1 , R 2 , and R 3 are ,independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF 3 , -OCF 3 , -OR 12 and -SR 12, G is O, S or -NR 15, D 2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkylcycloalkoxy or when G is NR 15 , G and D 2 together may optionally form an azetidine, pyrrolidine or piperidine ring; Z 1 and Z 2 are independently hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF 3 , -OCONR 14 R 14' , -CN, -CONR 14 R 14' , -SOR 12 , -SO 2 R 12 , -NR 14 COR 14' , -NR 14 CO 2 R 14' , -CO 2 R 12 , NR 14 SO 2 R 12 or COR 12 ; R 5 , R 6 , and R 7 are independently selected from the group consisting of hydrogen lower alkyl, lower cycloalkyl, -CF 3 , -SR 12 , lower alkoxy, lower cycloalkoxy, -CN, -CONR 14 R 14' , SOR 12 , SO 2 R 12 , NR 14 COR 14' , NR 14 CO 2 R 12 , CO 2 R 12 , NR 14 SO 2 R 12 and -COR 12 ; R 8 , R 9 , R 10 , R 10' , R 11 are independently hydrogen or lower alkyl; R 12 is lower alkyl or lower cycloalkyl; R 14 and R 14' are independently H, lower alkyl, lower cycloalkyl or R 14 and R 14' together with the N to which they are attached form a ring having 4 to 7 atoms; and R 15 is independently selected from the group consisting of hydrogen and lower alkyl. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety
-
Page/Page column 62

(2010/10/03)

Solubility of sodium sulfide in alcohols
The solubility of sodium sulfide in methanol, ethanol, 2-propanol, 2-methyl-1-propanol, and benzyl alcohol and the acid-base interaction of these compounds have been determined at (20 and 35) °C. The reactions result in the formation of sodium alkoxide and hydrosulfide. The reported values on the solubility of sodium sulfide in alcohols differ essentially from the data described in the literature.
Kurzin, Alexander V.,Evdokimov, Andrey N.,Golikova, Valerija S.,Pavlova, Olesja S.
experimental part
p. 4080 - 4081
(2011/05/28)

Amide acetals in the synthesis of pyridothienopyrimidines
Methyl 3-amino-4-arylaminothieno[2,3-b]pyridine-2-carboxylates containing various substituents in the benzene ring were synthesized by the Thorpe-Ziegler reaction of 4-arylamino-2-chloropyridine-3-carbonitriles with methyl thioglycolates. The influence of the substituent in the benzene ring, acetal structure, the solvent and the process temperature on the reactions of obtained compounds with amide acetals was studied. It was established that reactions with dimethylacetamide dimethylacetal in toluene smoothly results in amidine derivatives, viz., methyl 4-arylamino-3-[1-(dimethylamino)ethylidene] aminothieno[2,3-b]pyridine-2-carboxylates, regardless of the substituent in the benzene ring. Analogous reaction of p-fluoroderivative with dimethylacetamide dimethylacetal in refluxing anhydrous ethanol leads to intramolecular cyclocondensation to produce substituted pyridothienopyrimidines, viz., 5H-1-thia-3,5,8-triazaacenaphthenes, in good yields. Amidine derivatives were the major products in the case of the coupling of aminothienopyridines with dimethylformamide dimethylacetal under the same conditions. A new approach to the synthesis of substituted pyridothienopyrimidines, viz., 3H-1-thia-3,5,8- triazaacenaphthylenes, based on the prolonged heating of methyl 4-arylamino-3-[1-(dimethylamino)ethylidene]aminothieno[2,3-b] pyridine-2-carboxylates in the excess of acetic anhydride was elaborated. Putative mechanisms of the processes concerned are given.
Medvedeva,Tugusheva,Alekseeva,Chernyshev,Avramenko,Granik
experimental part
p. 1946 - 1958
(2011/07/29)

Triazolophthalazines
The compounds of formula I in which R1 and R2 have the meanings as given in the description are novel effective PDE2 inhibitors.
-
Page/Page column 11

(2009/01/24)

PROCESSES FOR PREPARING HIV REVERSE TRANSCRIPTASE INHIBITORS
Compounds of Formula (I): can be prepared by a multi-step process from compounds of Formula (II): wherein G is Cl, Br or I.
-
Page/Page column 14

(2009/07/10)

Amide-containing diketoacids as HIV-1 integrase inhibitors: Synthesis, structure-activity relationship analysis, and biological activity
HIV-1 integrase, which catalyzes the integration of the viral genome into the cellular chromosome, is an essential enzyme for retroviral replication, and represents an attractive and validated target in the development of therapeutics against AIDS. In this paper, 17 amide-containing novel diketoacids were designed and synthesized, and their ability to inhibit HIV-1 integrase was tested. The structure-activity relationships were also analyzed.
Li, Hongcai,Wang, Chao,Sanchez, Tino,Tan, Yanmei,Jiang, Chunying,Neamati, Nouri,Zhao, Guisen
experimental part
p. 2913 - 2919
(2009/09/06)

Process for Synthesis of (3R,3'R,6'R)-Lutein and its Stereoisomers
(3R,3′R,6′R)-Lutein and (3R,3′R)-zeaxanthin are two dietary carotenoids that are present in most fruits and vegetables commonly consumed in the US. These carotenoids accumulate in the human plasma, major organs, and ocular tissues. In the past decade, numerous epidemiological and experimental studies have shown that lutein and zeaxanthin play an important role in the prevention of age-related macular degeneration (AMD) that is the leading cause of blindness in the U.S. and Western World. The invention provides a process for the synthesis of (3R,3′R,6′R)-lutein and its stereoisomers from commercially available (rac)-α-ionone by a C15+C10+C15 coupling strategy. In addition, the present invention also provides access to the precursors of optically active carotenoids with 3-hydroxy-ε-end group that are otherwise difficult to synthesize. The process developed for the synthesis of lutein and its stereoisomers is straightforward and has potential for commercialization.
-
Page/Page column 19

(2009/10/30)

NOVEL PLATENSIMYCIN DERIVATIVES, THEIR INTERMEDIATES, AND PROCESS FOR PREPARARING THE SAME, AND NEW PROCESS FOR PREPARING PLATENSIMYCIN
The present invention relates to novel platensimycin derivatives, their intermediates and preparing methods of the same. Platensimycin is known as an effective antibiotic material having a broad antimicrobial spectrum and its derivatives are also expected to be effective antibiotic candidates. The present invention also relates to a novel preparing method of platensimycin. The intermediates used for the production of platensimycin and its derivatives of the present invention are tricyclo ketone derivatives and tetracyclo derivatives. Tetracyclo derivatives are prepared from tricyclo ketone derivatives prepared by carbonyl ylide [3+2] cycloaddition of dia- zoketone derivative
-
Page/Page column 30

(2009/11/29)

Process for Obtaining Alkoxides
Alkoxides are isolated by crystallization of an alcohol from a solution in the corresponding alcohol, with the alkoxide being crystallized out at a pressure of at least 3 bar abs. and a temperature of at least 120° C.
-
Page/Page column 3

(2009/01/20)

5-SULFANYLMETHYL-[1,2,4] TRIAZOL[l,5-A] PYRIMIDIN-7-OL DERIVATIVES AS CXCR2 ANTAGONISTS
The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.
-
Page/Page column 20

(2008/12/05)

5-SULFANYLMETHYL-PYRAZOLO [1,5-A] PYRIMIDIN-7-OL DERIVATIVES AS CXCR2 ANTAGONISTS
The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.
-
Page/Page column 28; 29

(2008/12/05)

Process for preparing alkali metal alkoxides
The invention relates to a process for preparing an alcoholic solution of an alkali metal alkoxide from alkali metal hydroxide and alcohol in a reaction column, the alcohol and the alkali metal hydroxide being conducted in countercurrent, which is characterized in that a reflux ratio of at least is established in the reaction column.
-
Page/Page column 3; 4; 5

(2009/01/20)

Pyrazole glucokinase activators
Disclosed herein are pyrazole glucokinase activators of the formula (I) useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.
-
Page/Page column 88-89

(2008/06/13)

SUBSTITUTED PIPERIDINES FOR USE IN THE TREATMENT OF BACTERIAL INFECTIONS
The present invention relates compounds of Formula (I) or pharmaceutically acceptable salts thereof, which are believed to possess antibacterial activity.
-
Page/Page column 52

(2008/12/04)

AZABENZIMIDAZOLYL COMPOUNDS
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I), as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
-
Page/Page column 56

(2008/06/13)

Substituted heteroaryl pyridopyrimidone derivatives
A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof : wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom, a sulphur atom, a methylene group optionally substituted by one or two groups chosen from a C1-6 alkyl group, a hydroxyl group, a C1-6 alkoxy group, a C1-2 perhalogenated alkyl group or an amino group; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring; R2 represents a 4-15 membered heterocyclic group , R3 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R4 and R5 represent, each independently, a hydrogen atom, a C1-6 alkyl group, optionally substituted by 1 to 4 substituents selected from a halogen atom, a phenyl group, a hydroxyl group or a C1-6 alkoxy group; R6 represents a hydrogen atom, a C1-6 alkyl group ; a cycloalkyl group, or a halogen atom; R7 represents a hydrogen atom or a C1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2; in the form of a free base or of an addition salt with an acid. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.
-
Page/Page column 17

(2008/12/06)

AURORA KINASE MODULATORS AND METHOD OF USE
The present invention relates to chemical compounds having a general formula I {INSERT STRUCTURE HERE} wherein A1-8, D,, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
-
Page/Page column 48-49

(2008/12/04)

INDAZOLE DERIVATIVES AND THEIR USE AS VANILLOID RECEPTOR LIGANDS
The present invention relates to indazole derivatives of the following formula I, which can be used as vanilloid receptor ligands, processes for their preparation, and their use in treating diseases, conditions and/or disorders modulated by vanilloid receptors. (I)
-
Page/Page column 30-31

(2008/12/07)