917474-59-0Relevant academic research and scientific papers
1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase: bioisosteric replacement of the carboxylic acid moiety
Althaus, Jan,Hake, Theresa,Hanekamp, Walburga,Lehr, Matthias
, p. 131 - 140 (2016)
Indazole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent dual inhibitors of cytosolic phospholipase A2α (cPLA2α) and fatty acid amide hydrolase (FAAH). In continuation of our structure-activity studies on cPLA2α and FAAH inhibitors, a number of derivatives of these substances characterized by bioisosteric replacement of the carboxylic acid functionality by inverse amides, sulfonylamides, carbamates and ureas were prepared. The biological evaluation of the obtained compounds showed that the carboxylic acid functionality of the lead compounds is of special importance for a pronounced inhibition of cPLA2α and FAAH.
NOVEL INDAZOLECARBOXAMIDES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL PREPARATIONS COMPRISING THEM AND THEIR USE FOR PRODUCING MEDICAMENTS
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Paragraph 0718; 0719; 0720; 0721; 0722, (2016/11/14)
The present application relates to novel 6-substituted indazoles having a carboxamide side chain, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing me
The discovery of orally bioavailable tyrosine threonine kinase (TTK) inhibitors: 3-(4-(heterocyclyl)phenyl)-1H-indazole-5-carboxamides as anticancer agents
Liu, Yong,Lang, Yunhui,Patel, Narendra Kumar,Ng, Grace,Laufer, Radoslaw,Li, Sze-Wan,Edwards, Louise,Forrest, Bryan,Sampson, Peter B.,Feher, Miklos,Ban, Fuqiang,Awrey, Donald E.,Beletskaya, Irina,Mao, Guodong,Hodgson, Richard,Plotnikova, Olga,Qiu, Wei,Chirgadze, Nickolay Y.,Mason, Jacqueline M.,Wei, Xin,Lin, Dan Chi-Chia,Che, Yi,Kiarash, Reza,Madeira, Brian,Fletcher, Graham C.,Mak, Tak W.,Bray, Mark R.,Pauls, Henry W.
supporting information, p. 3366 - 3392 (2015/05/05)
The acetamido and carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors. However, they display modest ability to attenuate cancer cell growth; their physicochemical properties, and attendant pharmacokinetic parameters, a
Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides
Laufer, Radoslaw,Ng, Grace,Liu, Yong,Patel, Narendra Kumar B.,Edwards, Louise G.,Lang, Yunhui,Li, Sze-Wan,Feher, Miklos,Awrey, Don E.,Leung, Genie,Beletskaya, Irina,Plotnikova, Olga,Mason, Jacqueline M.,Hodgson, Richard,Wei, Xin,Mao, Guodong,Luo, Xunyi,Huang, Ping,Green, Erin,Kiarash, Reza,Lin, Dan Chi-Chia,Harris-Brandts, Marees,Ban, Fuqiang,Nadeem, Vincent,Mak, Tak W.,Pan, Guohua J.,Qiu, Wei,Chirgadze, Nickolay Y.,Pauls, Henry W.
, p. 4968 - 4997 (2014/10/16)
TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.
INDAZOLE COMPOUNDS AS KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 115, (2013/04/25)
The present teaching provide indazole compounds represented by Structural Formulae (I) or (I') or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof as protein kinase inhibitors, such as T
KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME
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Page/Page column 110, (2011/10/31)
The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.
SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Page/Page column 124, (2011/02/24)
Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
A mild and selective method for the N-Boc deprotection by sodium carbonate
El Kazzouli, Sa?d,Koubachi, Jamal,Berteina-Raboin, Sabine,Mouaddib, Abderrahim,Guillaumet, Gérald
, p. 8575 - 8577 (2007/10/03)
A cleavage of N-tert-butyloxycarbonyl protection by Na2CO3 is reported. The N-free products are obtained in excellent yields. The compatibility of the method with the presence of acidic or basic groups is demonstrated. The reactions were performed on indole, azaindole, indazole, pyrazole, indolinone, quinolinone, and oxazolone.
