70049-77-3Relevant academic research and scientific papers
Impurity generated in production of indapamide as well as synthesis method and application
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Paragraph 0019; 0022, (2020/06/17)
The invention discloses an impurity generated in production of indapamide as well as a synthesis method and application. The synthesis method of the indapamide impurity D comprises the following stepsof: reacting an initial raw material A with thionyl chloride, and carrying out reduced pressure distillation to obtain a compound B, carrying out acylation reaction on the compound B and C, and recrystallizing petroleum ether and ethyl acetate to obtain a compound D. The invention provides a simple synthesis method of the indapamide impurity D. The synthesized indapamide impurity D can provide impurity contrast monitoring for reaction, and the problem of impurity analysis and control of indapamide is solved. And a strong support is provided for large-scale industrial production of indapamide.
A 4 - chloro - N - substituted phenyl -3 - sulfonyl-amino amide compounds and their preparation and anti-tumor application (by machine translation)
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Paragraph 0036; 0040; 0041, (2019/01/08)
The invention discloses a 4 - chloro - N - substituted phenyl - 3 - sulfonyl-amino amide compound and its preparation method and application, the structure of the compound such as formula (I) is shown. According to the results of the anti-tumor activity tests, such compounds have better biological activity, wherein the activity of the most preferred compounds of Soochow 12 to STAT3 high expression of MDA - MB - 231, HCT - 116 and SW - 480 have all demonstrated excellent activity, to the STAT3 non-high expression L3.6 tumor cell inanimate activity, showed very high selectivity; experiments prove that Soochow 12 can inhibit MDA - MB - 231 in the STAT3 phosphorylation; in addition, compared with the Niclosamide has better water-solubility and excellent biological activity, and more easy to synthesize. (by machine translation)
1,4,2-Benzo/pyridodithiazine 1,1-dioxides structurally related to the ATP-sensitive potassium channel openers 1,2,4-Benzo/pyridothiadiazine 1,1-dioxides exert a myorelaxant activity linked to a distinct mechanism of action
Pirotte, Bernard,De Tullio, Pascal,Florence, Xavier,Goffin, Eric,Somers, Fabian,Boverie, Stéphane,Lebrun, Philippe
, p. 3247 - 3256 (2013/06/05)
The synthesis of diversely substituted 3-alkyl/aralkyl/arylamino-1,4,2- benzodithiazine 1,1-dioxides and 3-alkylaminopyrido[4,3-e]-1,4,2-dithiazine 1,1-dioxides is described. Their biological activities on pancreatic β-cells and on smooth muscle cells were compared to those of the reference ATP-sensitive potassium channel (KATP channel) openers diazoxide and 7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide. The aim was to assess the impact on biological activities of the replacement of the 1,2,4-thiadiazine ring by an isosteric 1,4,2-dithiazine ring. Most of the dithiazine analogues were found to be inactive on the pancreatic tissue, although some compounds bearing a 1-phenylethylamino side chain at the 3-position exerted a marked myorelaxant activity. Such an effect did not appear to be related to the opening of KATP channels but rather reflected a mechanism of action similar to that of calcium channel blockers. Tightly related 3-(1-phenylethyl)sulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxides were also found to exert a pronounced myorelaxant activity, resulting from both a K ATP channel activation and a calcium channel blocker mechanism. The present work highlights the critical importance of an intracyclic NH group at the 4-position, as well as an exocyclic NH group linked to the 3-position of the benzo- and pyridothiadiazine dioxides, for activity on KATP channels.
NOVEL PIPERIDINE DERIVATIVE
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Page/Page column 93, (2008/06/13)
The invention provides a compound of the following formula (1): wherein m, n, and p are independently an integer of 0 - 4, provided 3 ≤ m + n ≤ 8; X is nitrogen atom or a group of the formula: C-R15; Y is a substituted or unsubstituted aromatic group, etc.; R15, R1, R2, R3, R4 , R5, R6 and R7 are hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and Z is hydrogen atom, cyano group, etc., or a prodrug thereof, or a pharmaceutically acceptable salt thereof, which exhibits an action for enhancing LDL receptor expression, and is useful as a medicament for treating hyperlipidemia, atherosclerosis, etc.
Benzene-sulphonamide derivatives and their uses
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Page column 9-10, (2010/02/09)
Benzene-sulphonamide derivatives complying with the general formula (I): in which the different symbols have different meanings, their optical isomers and the salts pharmacologically acceptable of these derivatives, as well as their uses for drug manufacture and as radiolabelled pharmacological tools of the thromboxan A2 receptors.
Indanes and analgesic compositions and methods thereof
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, (2008/06/13)
A compound selected from the group consisting of enantiomers and diastereoisomer forms and mixtures thereof of the formula STR1
