cas 86604-79-7, 4-NITRO-2,3,5-TRIMETHYLPYRIDINE-N-OXIDE

Articles about 86604-79-7Total 19 be found

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4-nitro-2,3,5-trimethylpyridine-N-oxide preparation method
The invention belongs to the field of preparation of chemical industry intermediates, and particularly relates to a 4-nitro-2,3,5-trimethylpyridine-N-oxide preparation method, which comprises: obtaining a 2,3,5-trimethylpyridine-N-oxide, and obtaining a 4-nitro-2,3,5-trimethylpyridine-N-oxide. According to the present invention, the preparation method has characteristics of high yield, low raw material cost, simple treatment and good product quality, and is suitable for industrial production.
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Paragraph 0009; 0010; 0011

(2019/07/11)

Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that incorporate a 7-indolizinylamino or 2-naphthylamino substituent on a pyrimidine or 1,3,5-triazine core. The most potent compounds show below 10 nanomolar activity towards wild-type HIV-1 and variants bearing Tyr181Cys and Lys103Asn/Tyr181Cys resistance mutations. The compounds also feature good aqueous solubility. Crystal structures for two complexes enhance the analysis of the structure-activity data.
Lee, Won-Gil,Frey, Kathleen M.,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Chan, Albert H.,Anderson, Karen S.,Jorgensen, William L.
p. 4824 - 4827
(2015/10/28)

BENZIMIDAZOLE COMPOUND HAVING GASTRIC ACID SECRETION INHIBITORY ACTIVITY
The present invention provides a compound that has superior gastric acid secretion inhibitory action, ample long-lasting gastric acid secretion inhibitory action, and is able to maintain intragastric pH at a high level for an extended period of time, making it useful as a therapeutic or prophylactic agent for diseases or symptoms caused by gastric acid, as well as an active form of this compound (form to which the compound is converted in the body following administration thereof) in the form of a compound represented by general formula (1 a) (wherein R2 represents a group represented by formula (I) or the like, and R1, R3, W1 and X- are as defined in the description).
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Page/Page column 19

(2009/06/27)

SALT OF SULFINYLBENZIMIDAZOLE COMPOUND, AND CRYSTAL AND AMORPHOUS FORM THEREOF
Salts of 2-[({4-[(2.2-dimethyl-1,3-dioxan-5-yl)methoxy]-3,5-dimethylpyridin-2-yl}methyl)sulfinyl]-1H-benzimidazole and their crystalline and amorphous forms.
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Page/Page column 15-16

(2009/07/18)

PROCESS FOR THE PRODUCTION OF 2- [ [4- T (2, 2-DIMETHYL-1, 3-DIOXAN-5-YL) METHOXY] PYRIDIN-2-YL] METHYLTHIO] -1H-BENZIMIDAZOLE
It is an object of the present invention to provide a process for the production on an industrial scale of a compound (1) or a salt thereof. There is provided a process for the production of compound (1) represented by the formula or a salt thereof: (wherein R1 and R3 independently represents a hydrogen atom or a methyl group), the process comprising the steps of: (a) reacting together a compound (3T) represented by the formula: (wherein X1 represents a leaving group, and R1 and R3 are defined as above) and (2,2-dimethyl-1,3-dioxan-5-yl)methanol represented by the formula or a salt thereof: so as to produce a compound (2T) represented by the formula (wherein R1 and R3 are defined as above); and (b) reacting the compound represented by above formula (2T) with an oxidizing agent.
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(2008/12/05)

STABILIZED COMPOSITION
It is intended to provide a pharmaceutical composition which contains a proton pump inhibitor and is stable even if it is stored for a long time. It is also intended to provide a pharmaceutical composition which contains a proton pump inhibitor susceptible to acid, and does not dissolve in the stomach but dissolves in the intestine to release a primary drug product promptly. The object could be achieved by the pharmaceutical composition characterized in that a layer containing a proton pump inhibitor and ethyl cellulose, a layer containing an enteric polymer, and if necessary an intermediate layer composed of one or more layers are formed on a pharmacologically inactive core substance. The intermediate layer is composed of a water-insoluble polymer, a water-soluble polymer, a lubricant and the like.
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Page/Page column 7

(2008/06/13)

Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity
Heat shock protein 90 (Hsp90) is a molecular chaperone protein implicated in stabilizing the conformation and maintaining the function of many cell-signaling proteins. Many oncogenic proteins are more dependent on Hsp90 in maintaining their conformation, stability, and maturation than their normal counterparts. Furthermore, recent data show that Hsp90 exists in an activated form in malignant cells but in a latent inactive form in normal tissues, suggesting that inhibitors selective for the activated form could provide a high therapeutic index. Hence, Hsp90 is emerging as an exciting new target for the treatment of cancer. We now report on a novel series of 2-amino-6-halopurine Hsp90 inhibitors exemplified by 2-amino-6-chloro-9-(4-iodo-3,5-dimethylpyridin- 2-ylmethyl)purine (30). These highly potent inhibitors (IC50 of 30 = 0.009 μM in a HER-2 degradation assay) also display excellent antiproliferative activity against various tumor cell lines (IC50 of 30 = 0.03 μM in MCF7 cells). Moreover, this class of inhibitors shows higher affinity for the activated form of Hsp90 compared to our earlier 8-sulfanylpurine Hsp90 inhibitor series. When administered orally to mice, these compounds exhibited potent tumor growth inhibition (>80%) in an N87 xenograft model, similar to that observed with 17-allylamino-17- desmethoxygeldanamycin (17-AAG), which is a compound currently in phase I/II clinical trials.
Kasibhatla, Srinivas R.,Hong, Kevin,Biamonte, Marco A.,Busch, David J.,Karjian, Patricia L.,Sensintaffar, John L.,Kamal, Adeela,Lough, Rachel E.,Brekken, John,Lundgren, Karen,Grecko, Roy,Timony, Gregg A.,Ran, Yingqing,Mansfield, Robert,Fritz, Lawrence C.,Ulm, Edgar,Burrows, Francis J.,Boehm, Marcus F.
p. 2767 - 2778
(2008/02/06)

Benzimidazole compound
An object of the present invention is to provide a novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases, having an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.
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Page/Page column 39; 104

(2008/06/13)

Inhibitors of the gastric H+, K+-atpase with enhanced therapeutic properties
Chemical syntheses and medical uses of novel inhibitors of the gastric H+, K+-ATPase for the treatment and/or management of duodenal ulcers, heartburn, acid reflux, other conditions mediated by gastric acid secretion and/or psoriasis are described.
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(2008/06/13)

NOVEL HETEROCYCLIC COMPOUNDS AS HSP90-INHIBITORS
Novel heterocyclic compounds are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agent. Method of synthesis and use of such compounds are also described.
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Page/Page column 332

(2008/06/13)

NEW METHOD FOR THE PREPARATION OF THE ANTI-ULCER COMPOUNDS OMEPRAZOLE, LANSOPRAZOLE AND PANTOPRAZOLE
The present invention describes a new process for the preparation of omeprazole, lansoprazole and pantoprazole of formula (XXI), (XXXIII), and which involves the formation of pyridines N-oxide using a rhenium compound as a catralyst, followed by nitration of the 4-position with nitric acid fuming in presence of a claycop. The chlorination of the 2-methyl group of pyridine was achieved by using the POCI3/Et3N, which allowed the preparation of the derivates 2-chloromethylpyridines in only one step. These derivates reacted with the mercaptobenzimidazolic derivatives in presence of ultra-sonic radiation, giving the thioethers. The oxidation of these thioethers was done with several oxidizing agents and the required anti-ulcer compounds were obtained after the substitution of nitro group by the corresponding OR groups.
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Page/Page column 11

(2010/02/07)

Structure-activity relationship of 2-[[(2-Pyridyl)methyl]thio]-1H- benzimidazoles as anti Helicobacter pylori agents in vitro and evaluation of their in vivo efficacy
A relationship between the structure of 21 2-[[(2-pyridyl)methyl]thio]- 1H-benzimidazoles (6) and their anti Helicobacter pylori activity expressed as minimum bactericidal concentration (MBC) values is described. Observed MBCs ranged from 256 to 1 μg/mL. The structure - activity relationship (SAR) showed that larger and more lipophilic compounds, especially compounds with such substituents in the 4-position of the pyridyl moiety, generally had lower MBC values. Four new compounds 'that were predicted to be potent by the established SAR model were synthesized and tested. One such compound, i.e., 2-[[(4-[(cyclopropylmethyl)oxy]3-methyl-2-pyridyl)methyl]thio]-1H- benzimidazole (18), was tested for in vivo efficacy in a mouse Helicobacter felis model (125 μmol/kg bid given orally for 4 days, n = 4). Unfortunately, antibacterial activity could not be clearly demonstrated in this model. Instead a potent acid secretion inhibition was observed. This finding was attributed to the methylthio compound being oxidized to the corresponding methyl sulfinyl derivative, i.e., a proton pump inhibitor, in vivo. Although the antibacterial activity had the potential of decreasing H. felis cell counts in vivo the proton pump inhibitory effect became dominant and actually promoted H. felis cell growth. Hence, we conclude that the antibacterial utility of the 2-[[(2-pyridyl)methyl]thio]1H-benzimidazoles (6) as a compound class is compromised by their propensity to become proton pump inhibitors upon metabolic oxidation in vivo.
Kühler, Thomas C.,Swanson, Marianne,Shcherbuchin, Vladimir,Larsson, H?kan,Mellg?rd, Bj?rn,Sj?str?m, Jan-Eric
p. 1777 - 1788
(2007/10/03)

1,3,4-oxadiazoles
1,3,4-oxadiazole compounds are disclosed. The subject compounds suppress immune function and have hepatoprotection activity.
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(2008/06/13)

(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate
[(Pyridylmethyl)sulfinyl]benzimidazoles 1 (PSBs) are a class of highly potent antisecretory (H+,K+)-ATPase inhibitors which need to be activated by acid to form their active principle, the cyclic sulfenamide 4. Selective inhibitors of the (H+,K+)-ATPase in vivo give rise to the nonselective thiophile 4 solely at low pH, thus avoiding interaction with other thiol groups in the body. The propensity to undergo the acid-catalyzed transformation is dependent on the nucleophilic/electrophilic properties of the functional groups involved in the formation of 2 since this step is both rate-determining and pH-dependent. The aim of this study was to identify compounds with high (H+,K+)-ATPase inhibitory activity in stimulated gastric glands possessing acidic pH, but low reactivity (high chemical stability) at neutral pH as reflected by in vitro (Na+,K+)-ATPase inhibitory activity. The critical influence of substituents flanking the pyridine 4-methoxy substituent present in all derivatives was carefully studied. The introduction of a 3-methoxy group gave inhibitors possessing a combination of high potency, similar to omeprazole and lansoprazole, but increased stability. As a result of these studies, compound 1a (INN pantoprazole) was selected as a candidate drug and is currently undergoing phase III clinical studies.
Kohl,Sturm,Senn-Bilfinger,Simon,Kruger,Schaefer,Rainer,Figala,Klemm
p. 1049 - 1057
(2007/10/02)

(Bezimidazol-2-yl)-pyridinium compounds
(Benzimidazol-2-yl)-pyridinium compounds of the formula STR1 wherein A is --SR9, --SO3- or --S--SO3- ; R1 and R3 each is hydrogen or (C1 -C7)-alkyl; R2 is hydrogen, (C1 -C7)-alkyl, (C1 -C7)-alkoxy or a negatively charged oxygen atom; R4 is hydrogen or a negative charge; R5, R6, R7 and R8 each is hydrogen, (C1 -C7)-alkyl, aryl, halogen, cyano, nitro, formyl, (C2 -C7)-alkanoyl, arylcarbonyl, carboxy, carboxy-(C1 -C7)-alkyl, (C1 -C7)-alkoxycarbonyl, aryloxycarbonyl, aryl-(C1 -C7)-alkoxycarbonyl, (C1 -C7)-alkoxycarbonyl-(C1 -C7)-alkyl, carbamoyl, mono- or di-(C1 -C7)-alkylcarbamoyl, pyrrolidinocarbonyl, piperidinocarbonyl, carbamoyl-(C1 -C7)-alkyl, mono- or di-(C1 -C7)-alkylcarbamoyl-(C1 -C7)-alkyl, pyrrolidinocarbonyl-(C1 -C7)-alkyl, piperdinocarbonyl-(C1 -C7)-alkyl, hydroxy, (C1 -C7)-alkoxy, (C2 -C7)-alkanoloxy, aryloxy, arylcarbonyloxy, (C1 -C7)-alkoxycarbonyloxy, aryl-(C1 -C7)-alkoxycarbonyloxy, aryloxycarbonyloxy, carbamoyloxy, mono- or di-(C1 -C7)-alkylcarbamoyloxy, pyrrolidinocarbonyloxy, piperidinocarbonyloxy, hydroxy-(C1 -C7)-alkyl, trifluoromethyl, di-(C1 -C7)-alkoxymethyl or (C2 -C3)-alkylenedioxymethyl or two of these substituents which are adjacent jointly and together with the carbon atoms to which they are attached are a 5-, 6- or 7-membered ring; and R9 is (C1 -C20)-alkyl, (C3 -C7)-cycloalkyl, (C3 -C7)-alkenylalkyl, (C3 -C7)-alkynylalkyl, substituted (C3 -C7)- alkenyl-alkyl, aryl, aryl-(C1 -C7)-alkyl, hydroxy- (C2 -C7)-alkyl, (C1 -C7)-alkoxy- (C2 -C7)-alkyl, (C1 -C7)-alkoxycarbonyl- (C1 -C7)-alkyl, carboxy-(C1 -C7)-alkyl, di-(C1 -C7)-alkoxycarbonyl-(C2 -C7)-alkyl, dicarboxy-(C2 -C7)-alkyl, carboxy-(C1 -C7)-alkylcarbamoyl-(C1 -C7)-alkyl, optionally N-substituted amino-(C2 -C7)-alkyl, optionally N-substituted amino-carboxy-(C2 -C7)-alkyl, optionally N-substituted amino-(C1 -C7)-alkoxycarbonyl-(C2 -C7)-alkyl, heteroaryl, heteroaryl-(C1 -C7)-alkyl or a residue derived from a cysteine-containing oligopeptide by elimination of the SH group; provided that when there is a net single positive charge there is an external anion, or a pharmaceutically acceptable acid addition salt thereof.
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(2008/06/13)

Tricyclic imidazole derivatives
Tricyclic imidazole derivatives of formula I STR1 wherein one of R1 and R3 is lower alkyl and the other is hydrogen or lower alkyl, R2 is lower alkyl, n is the number 0 or 1, A is STR2 R4, R5, R6 and R7 each is lower alkyl and R8 is hydrogen or lower alkyl, and their acid addition salts are described. These compounds are useful as agents for control or prevention of ulcers and of increased gastric acid secretion.
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(2008/06/13)

Fluoroalkoxy substituted benzimidazoles useful as gastric acid secretion inhibitors
Fluoroalkoxy compounds of the general formula I STR1 wherein R1 represents a 1-3C-alkyl radical which is completely or predominantly substituted by fluorine, or a chlorodifluoromethyl radical, R1' represents hydrogen, halogen, trifluoromethyl, a 1-3C-alkyl radical, or a 1-3C-alkoxy radical which is optionally completely or predominantly substituted by fluorine, R2 represents hydrogen or a 1-3C-alkyl radical, R3 represents hydrogen or a 1-3C-alkyl or 1-3C-alkoxy radical, R4 represents hydrogen or a 1-3C-alkyl radical and n represents the number 0 or 1, and their salts are new compounds with a marked protective effect on the stomach.
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(2008/06/13)

[1,3]-Dioxolo[4,5-f]benzimidazoles and [1,4]-dioxino[2,3-f]benzimidazoles
Tricyclic ethers of the general formula I STR1 wherein R represents a bond and R1 represents a 1-2C-alkylene radical which is completely or partly substituted by fluorine, or a chlorotrifluoroethylene radical, or R and R1 each represent a difluoromethylene radical, R2 represents hydrogen or a 1-3C-alkyl radical, R3 represents hydrogen or a 1-3C-alkyl or 1-3C-alkoxy radical, R4 represents hydrogen or a 1-3C-alkyl radical and n represents the number 0 or 1, and their salts are new compounds with a marked protective effect on the stomach.
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(2008/06/13)

2-Pyridylmethyl thio(sulfinyl)benzimidazoles with gastric acid secretion inhibiting effects
4- or 5-Trifluoromethyl-2-[(4-methoxy-2-pyridylmethyl)thio or sulfinyl]-(-benzimidazoles are useful as such or in medicament compositions for protecting the stomach and intestines and for inhibiting gastric acid secretion of warm-blooded animals to which they are administered.
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(2008/06/13)

Chemical Properties

Melting Point: 73-74 °C
Boiling Point: 397.8 °C at 760 mmHg
Flash Point:194.4 °C
Density: 1.26 g/cm³
Storage Temp.:Keep in dark place,Inert atmosphere,Room temperature
Vapor Pressure: 3.54E-06mmHg at 25°C
Refractive Index: 1.564
PKA: -0.89±0.10(Predicted)
PSA: 71.28000
LogP: 2.47170

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86604-79-7

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Chemical Properties

Melting Point: 73-74 °C

Boiling Point: 397.8 °C at 760 mmHg

Flash Point:194.4 °C

Density: 1.26 g/cm³

Storage Temp.:Keep in dark place,Inert atmosphere,Room temperature

Vapor Pressure: 3.54E-06mmHg at 25°C

Refractive Index: 1.564

PKA: -0.89±0.10(Predicted)

PSA: 71.28000

LogP: 2.47170

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Article Database

86604-79-7

Articles about 86604-79-7Total 19 be found

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Chemical Properties

Melting Point: 73-74 °C

Boiling Point: 397.8 °C at 760 mmHg

Flash Point:194.4 °C

Density: 1.26 g/cm3

Storage Temp.:Keep in dark place,Inert atmosphere,Room temperature

Vapor Pressure: 3.54E-06mmHg at 25°C

Refractive Index: 1.564

PKA: -0.89±0.10(Predicted)

PSA: 71.28000

LogP: 2.47170

Global suppliers and manufacturers of 86604-79-7total 41 suppliers on LookChem

Density: 1.26 g/cm³