57899-62-4Relevant academic research and scientific papers
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists
Lu, Zhonghui,Duan, James J.-W.,Xiao, Haiyun,Neels,Wu, Dauh-Rurng,Weigelt, Carolyn A.,Sack, John S.,Khan,Ruzanov, Max,An, Yongmi,Yarde, Melissa,Karmakar, Ananta,Vishwakrishnan, Sureshbabu,Baratam, Venkata,Shankarappa, Harisha,Vanteru, Sridhar,Babu, Venkatesh,Basha, Mushkin,Kumar Gupta, Arun,Kumaravel, Selvakumar,Mathur, Arvind,Zhao, Qihong,Salter-Cid, Luisa M.,Carter, Percy H.,Murali Dhar
, p. 2265 - 2269 (2019/07/03)
An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that the cyclohexane carboxylic acid group of compound 2 plays a significant role in RORγt binding, forming four hydrog
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents
Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David,Lagrutta, Armando,Bradley, Prudence,Lu, Jun,Patel, Sangita,Rickert, Keith W.,Smith, Robert F.,Soisson, Stephen,Wei, Changqing,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Fukuda, Yasumichi
supporting information, p. 609 - 614 (2014/06/09)
Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit
BRIDGED BICYCLIC COMPOUNDS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page/Page column 67, (2013/03/26)
Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
NOVEL ARYLALKENE DERIVATIVES AND USE THEREOF AS SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Paragraph 0218, (2013/07/19)
The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
Oligo(cyclohexylidene)s and oligo(cyclohexyl) as bridges for photoinduced intramolecular charge separation and recombination
Oosterbaan, Wibren D.,Koper, Carola,Braam, Thijs W.,Hoogesteger, Frans J.,Piet, Jacob J.,Jansen, Bart A. J.,Van Walree, Cornelis A.,Van Ramesdonk, H. Johan,Goes, Marijn,Verhoeven, Jan W.,Schuddeboom, Wouter,Warman, John M.,Jenneskens, Leonardus W.
, p. 3612 - 3624 (2007/10/03)
A series of semirigid donor-bridge-acceptor (D-B-A) molecules was synthesized to study the effect of the position and number of nonconjugated olefinic bonds in the bridge on the photoinduced charge-separation and charge-recombination kinetics. The molecules consist of a phenylpiperidine electron donor, an oligo-(cyclohexylidene) or oligo(cyclohexyl) bridge, and a dicyanovinyl acceptor. Partly saturated ter(cyclohexylidene) bridges were used as well. The edge-to-edge donor-acceptor separation of the compounds under study varies between 2.89 and 15.4 A. The replacement of a C-C single bond by an olefinic bond increases the rate of charge separation with a factor of 3.0 ± 0.8 per replaced bond. For all D-B-A compounds the extended fully charge-separated state folds to a compact charge-transfer (CCT) conformer. The rate of charge recombination (CR) of the CCT state increases with solvent polarity for those compounds having an olefinic bond located three σ bonds from the acceptor. Thus, while in cyclohexane the CR rate is equal for all compounds, in benzene the CR rate in compounds with an olefinic bond near the acceptor is 10 times larger than in compounds with a single bond instead. It is believed that a (virtual) charge-transfer state involving the radical cation of the olefinic bond and the radical anion of the acceptor (D-B;+-A-) is responsible for the enhanced CR process.
Spiro compounds or salts thereof and preventives/remedies for autoimmune diseases and AP-1 inhibitors containing the same
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, (2008/06/13)
The spiro compounds of the present invention represented by the general formula: wherein A, R2, R3, R4, R5, R6and n are as defined in the specification, exhibit an AP-1 activity inhibitory action and, based on the AP-1 inhibitory action, suppresses the expression of a wide variety of genes and are useful as an agent for treating and preventing autoimmune diseases with lessoned side reactions.
Mechanistic Studies of the Palladium(II)-Copper(II)-mediated Demercuriation of Cycloalkyl and Cycloalkylmethyl Systems
Wells, Adam P.,Kitching, William
, p. 527 - 536 (2007/10/02)
The likely events involved in the conversion of cyclohexylmethylmercuric chloride into predominantly trans-4-methylcyclohexyl chloride, on treatment with PdCl2-CuCl2 in acetic acid, have been identified by product and deuterium-labelling studies, as well as by the behaviour of probable intermediates.Extension to related cycloalkyl- and cycloalkylmethyl--mercuric chloride is reported, and mechanistic changes as a function of ring size, with elimination-re-addition of being important in cyclohexyl systems, but carbocation formation dominating in cyclooctyl cases.
FACILE SYNTHESIS OF 4-CARBETHOXYCYCLOHEXANONE
Sanchez, Ignacio H.,Ortega, Armando,Garcia, Gabriel,Larraza, Maria Isabel,Flores, Humberto J.
, p. 141 - 150 (2007/10/02)
A facile decarboalkoxylative route to 4-carbethoxycyclohexanone (1) from the tricarbethoxy derivative 3 is described.
