131748-91-9Relevant academic research and scientific papers
PqsR INVERSE AGONISTS
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Paragraph 52; 54; 55; 58; 59, (2020/01/31)
The present invention relates to a compound according to general formula (I), which acts as an inhibitor of PqsR (the currently only known receptor for the Pseudomonas Quinolone Signal (PQS)); to a pharmaceutical composition containing one or more of the compound(s) of the invention; to a combination preparation containing at least one compound of the invention and at least one further active pharmaceutical ingredient; and to uses of said compound(s), including the use as a medicament, e.g. the use in the treatment or prophylaxis of a bacterial infection, especially a Pseudomonas aeruginosa or Burkholderia infection.
Preparation method of 2-(2-bromo-1,3-thiazol-5-yl) acetonitrile
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Paragraph 0021-0022; 0025-0026; 0030; 0033-0034; 0038-0042, (2019/12/02)
The invention discloses a preparation method of 2-(2-bromo-1,3-thiazol-5-yl) acetonitrile, which comprises the following steps: S1) adding a first organic solvent and methyl 2-bromothiazole-4-carboxylate into a reaction flask, cooling the mixture to 0 DEG C, adding sodium borohydride, reacting the mixture at room temperature, performing concentration and extraction, combining organic phases, and performing concentration and column chromatography separation to obtain 2-bromothiazole-5-methanol; S2) adding a second organic solvent and the 2-bromothiazole-5-methanol into a reaction bottle, cooling the mixture to 0 DEG C, adding phosphorus tribromide, washing a product with mother liquor, and performing concentration to obtain 2-bromo-5-bromomethyl-thiazole; S3) adding acetonitrile, the 2-bromo-5-bromomethyl-thiazole, potassium carbonate, tetrabutylammonium fluoride and TMSCN sequentially into a reaction flask, performing extraction, combining organic phases, and performing concentration and recrystallization to obtain the 2-(2-bromo-1,3-thiazol-5-yl) acetonitrile. The preparation method breaks through the blank at home and abroad, the preparation process and purification steps are safe and simple, and the preparation method is suitable for industrial production.
Thiazole Methylamino Pyridine Compounds and Preparation Method Therefor
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Paragraph 0084, (2015/02/25)
Disclosed are thiazole methylamino pyridine compounds represented by the general formula (I) having fungicidal, insecticidal/acaricidal, and herbicidal activity, the preparation method thereof, the fungicidal, insecticidal/acaricidal, and herbicidal compositions containing the compounds of the present invention, and the use and the method for controlling fungi, insects/acari and weeds of the compounds of the present invention.
BETA-TETRAZOLYL-PROPIONIC ACIDS AS METALLO-BETA-LACTAMASE INHIBITORS
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Page/Page column 63; 64, (2015/11/27)
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
METHODS, COMPOUNDS, AND COMPOSITIONS FOR THE TREATMENT OF ANGIOTENSIN-RELATED DISEASES
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Page/Page column 68; 69, (2014/09/29)
Disclosed are small molecule non-peptidic compounds, as well as methods and compositions for the treatment of angiotensin-related diseases and disorders, including cardiovascular diseases, metabolic diseases, gastrointestinal diseases, renal diseases, inflammatory/autoimmune diseases, neurological diseases, bone marrow diseases and cancer.
HEPATITIS C INHIBITORS AND USES THEREOF
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Page/Page column 126, (2012/07/13)
This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties
Imbriglio, Jason E.,Dirocco, Daniel,Bodner, Rena,Raghavan, Subharekha,Chen, Weichun,Marley, Daria,Esser, Craig,Holt, Tom G.,Wolff, Michael S.,Taggart, Andrew K.P.,Waters, M. Gerard,Tata, James R.,Colletti, Steven L.
supporting information; scheme or table, p. 2721 - 2724 (2011/06/20)
Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties.
Synthesis, herbicidal activities, and 3D-QSAR of 2-cyanoacrylates containing aromatic methylamine moieties
Liu, Yu-Xiu,Wei, Deng-Guo,Zhu, Ye-Rong,Liu, Shao-Hua,Zhang, Yong-Lin,Zhao, Qi-Qi,Cai, Bao-Li,Li, Yong-Hong,Song, Hai-Bin,Liu, Ying,Wang, Yong,Huang, Run-Qiu,Wang, Qing-Min
body text, p. 204 - 212 (2009/04/11)
A series of novel 2-cyanoacrylates containing different aromatic rings were synthesized, and their structures were characterized by 1H NMR, elemental analysis, and single-crystal X-ray diffraction analysis. Their herbicidal activities against four weeds and inhibition of photosynthetic electron transport against isolated chloroplasts (the Hill reaction) were evaluated. Both in vivo and in vitro data showed that the compounds containing benzene, pyridine, and thiazole moieties gave higher activities than those containing pyrimidine, pyridazine, furan, and tetrahedronfuran moieties. To further explore the comprehensive structure-activity relationship on the basis of in vitro data, comparative molecular field analysis (CoMFA) was performed, and the results showed that a bulky and electronegative group around the para-position of the aromatic rings would have the potential for higher activity, which offered important structural insights into designing highly active compounds prior to the next synthesis.
Discovery of biaryl anthranilides as full agonists for the high affinity niacin receptor
Shen, Hong C.,Ding, Fa-Xiang,Luell, Silvi,Forrest, Michael J.,Carballo-Jane, Ester,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Wilsie, Larissa C.,Krsmanovic, Mihajlo L.,Taggart, Andrew K.,Ren, Ning,Cai, Tian-Quan,Deng, Qiaolin,Chen, Qing,Wang, Junying,Wolff, Michael S.,Tong, Xinchun,Holt, Tom G.,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
, p. 6303 - 6306 (2008/04/12)
Biaryl anthranilides are reported as potent and selective full agonists for the high affinity niacin receptor GPR109A. The SAR presented outlines approaches to reduce serum shift and both CYPCYP2C8 and CYP2C9 liabilities, while improving PK and maintainin
NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 25; 37-39, (2008/06/13)
The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.
