72571-06-3Relevant academic research and scientific papers
INHIBITOR COMPOUNDS
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Page/Page column 188-189, (2021/01/29)
The disclosure relates to heterocyclic compounds and methods for their preparation. The disclosure provides compounds that may have beneficial therapeutic activity in the treatment of a disease or condition mediated by excessive or otherwise undesirable Des1 and/or fibrotic activity.
PISTON FOR AN INTERNAL COMBUSTION ENGINE AND METHOD FOR PRODUCING THE PISTON FOR AN INTERNAL COMBUSTION ENGINE
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, (2018/08/03)
The present invention relates to compounds of general formula (I), wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.
Libraries of C-5 Substituted Imidazoles and Oxazoles by Sequential Van Leusen (VL)–Suzuki, VL–Heck and VL–Sonogashira in Imidazolium-ILs with Piperidine-Appended-IL as Base
Savanur, Hemantkumar M.,Kalkhambkar, Rajesh G.,Laali, Kenneth K.
supporting information, p. 5285 - 5288 (2018/09/06)
Facile access to diverse C5-substituted imidazoles and oxazoles via sequential Van Leusen–Suzuki, Van Leusen–Heck, and Van Leusen–Sonogashira protocols, employing imidazolium-ILs as solvents along with piperidine-appended imidazolium [PAIM][NTf2/sub
COMPOUNDS WITH ANTI-TUMORAL ACTIVITY
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Page/Page column 58; 59; 77, (2016/09/22)
The present invention relates to compounds of general formula (I), wherein A represents an optionally substituted heterocycle group, B represents an aryl or heteroaryl group and wherein X, R1, R2, R3, R4 and R5 are as defined in the description. Compounds of formula (I) are useful to destroy, inhibit, or prevent the growth or spread of cells, especially malignant cells, into surrounding tissues implicated in a variety of human and animal diseases.
Tandem cycloaddition-decarboxylation of α-keto acid and isocyanide under oxidant-free conditions towards monosubstituted oxazoles
Zhang, Ling-Juan,Xu, Mei-Chen,Liu, Jie,Zhang, Xian-Ming
, p. 73450 - 73453 (2016/08/18)
An efficient method, tandem [3 + 2] cycloaddition-decarboxylation of α-keto acid and isocyanide promoted by copper salt, has been developed. Under oxidant-free conditions, a series monosubstituted oxazoles have been constructed. Different from the traditional application of α-oxo acids as acyl surrogates, the elegant approach herein ingeniously avoids consuming excess oxidants.
A One-Pot Tandem Approach for the Synthesis of 5-(Het)aryloxazoles from Substituted (Het)aryl Methyl Alcohols and Benzyl Bromides
Vinay Kumar, Koravangala S.,Swaroop, Toreshettahally R.,Rajeev, Narasimhamurthy,Vinayaka, Ajjampura C.,Lingaraju, Gejjalagere S.,Rangappa, Kanchugarakoppal S.,Sadashiva, Maralinganadoddi P.
supporting information, p. 1363 - 1366 (2016/06/01)
A new modified van Leusen strategy has been developed for the synthesis of biologically significant 5-substituted oxazoles by the reaction of (het)aryl methyl alcohols or benzyl bromides as precursors with tosylmethylisocyanide (TosMIC) under basic conditions. This method is efficient, takes place under mild reaction conditions, and is tolerant of various functional groups with high yield.
Cobalt-Catalyzed Decarboxylative 2-Benzoylation of Oxazoles and Thiazoles with α-Oxocarboxylic Acids
Yang, Ke,Chen, Xinyong,Wang, Yuqi,Li, Wanqing,Kadi, Adnan A.,Fun, Hoong-Kun,Sun, Hao,Zhang, Yan,Li, Guigen,Lu, Hongjian
, p. 11065 - 11072 (2015/11/18)
Cobalt-catalyzed decarboxylative cross-coupling of oxazoles and thiazoles with α-oxocarboxylic acids was developed through an sp2 C-H bond functionalization process. This work represents the first example of cobalt-catalyzed decarboxylative C-H
Nickel-catalyzed decarboxylative acylation of heteroarenes by sp 2 C-H functionalization
Yang, Ke,Zhang, Cheng,Wang, Peng,Zhang, Yan,Ge, Haibo
supporting information, p. 7241 - 7244 (2014/06/23)
Nickel-catalyzed ligand-free decarboxylative cross-coupling of azole derivatives with α-oxoglyoxylic acids has been developed. This work represents the first example of decarboxylative cross-coupling reactions, in a C-H bond functionalization manner, thro
Nickel-catalyzed decarboxylative arylation of heteroarenes through sp2 C-H functionalization
Yang, Ke,Wang, Peng,Zhang, Cheng,Kadi, Adnan A.,Fun, Hoong-Kun,Zhang, Yan,Lu, Hongjian
supporting information, p. 7586 - 7589 (2015/04/22)
The direct decarboxylative arylation of hetereoarenes with benzoic acids through a nickel-catalyzed sp2 C-H functionalization process was developed. This process provides the first examples of decarboxylative cross-coupling reactions with aroma
Discovery and SAR exploration of a novel series of imidazo[4,5-b]pyrazin-2- ones as potent and selective mTOR kinase inhibitors
Mortensen, Deborah S.,Perrin-Ninkovic, Sophie M.,Harris, Roy,Lee, Branden G.S.,Shevlin, Graziella,Hickman, Matt,Khambatta, Gody,Bisonette, Rene R.,Fultz, Kimberly E.,Sankar, Sabita
supporting information; experimental part, p. 6793 - 6799 (2012/01/03)
We report here the discovery of a novel series of selective mTOR kinase inhibitors. A series of imidazo[4,5-b]pyrazin-2-ones, represented by screening hit 1, was developed into lead compounds with excellent mTOR potency and exquisite kinase selectivity. Potent compounds from this series show >1000-fold selectivity over the related PI3Kα lipid kinase. Further, compounds such as 2 achieve mTOR pathway inhibition, blocking both mTORC1 and mTORC2 signaling, in PC3 cancer cells as measured by inhibition of pS6 and pAkt (S473).
