91047-75-5Relevant academic research and scientific papers
Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes
Storer, R. Ian,Pike, Andy,Swain, Nigel A.,Alexandrou, Aristos J.,Bechle, Bruce M.,Blakemore, David C.,Brown, Alan D.,Castle, Neil A.,Corbett, Matthew S.,Flanagan, Neil J.,Fengas, David,Johnson, M. Scott,Jones, Lyn H.,Marron, Brian E.,Payne, C. Elizabeth,Printzenhoff, David,Rawson, David J.,Rose, Colin R.,Ryckmans, Thomas,Sun, Jianmin,Theile, Jonathan W.,Torella, Rubben,Tseng, Elaine,Warmus, Joseph S.
supporting information, p. 4805 - 4811 (2017/10/17)
The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is disclosed. Extensive in vitro pharmacology and ADME profiling followed by in vivo preclinical PK and efficacy model data are discussed. A proposed protein–ligand binding mode for this compound is also provided to rationalise the high levels of potency and selectivity over inhibition of related sodium channels. To further support the proposed binding mode, potent conjugates are described which illustrate the potential for development of chemical probes to enable further target evaluation.
Solid supported palladium(0) nano/microparticle: A ligand-free efficient recyclable heterogeneous catalyst for mono- and β,β-double-Heck reaction
Sharma, Dharminder,Kumar, Sandeep,Shil, Arun K.,Guha, Nitul Ranjan,Bandna,Das, Pralay
supporting information, p. 7044 - 7051 (2013/01/15)
Solid supported palladium nano/microparticles were found to be active catalysts to perform mono- and β,β-double-Heck reactions. Different β-unsubstituted and substituted alkenes including acrylate, methacrylate, crotonate, styrene, acrylonitrile, and acrylamide were investigated successfully for mono- and β,β-double-Heck reactions with aryl iodide under milder reaction condition. One-pot β,β-double-Heck reaction of aryl iodides with α,β-unsaturated ester, amide, nitrile, and styrene derivatives were also performed under standard reaction conditions. Wide functional group tolerance, easy catalyst recovery, and recyclability up to twelve times without significant loss of catalytic activity added extra importance to the present process.
CLASS- AND ISOFORM-SPECIFIC HDAC INHIBITORS AND USES THEREOF
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Page/Page column 95-96, (2011/02/24)
HDAC inhibitors of the general formula (I) and (II) and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and d
CDK INHIBITORS
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Page/Page column 70-71, (2010/07/09)
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.
CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 66, (2009/04/25)
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.
The one-pot Wittig reaction: A facile synthesis of α,β- unsaturated esters and nitriles by using nanocrystalline magnesium oxide
Choudary, Boyapati M.,Mahendar, Koosam,Kantam, M. Lakshmi,Ranganath, Kalluri V. S.,Athar, Taimur
, p. 1977 - 1985 (2007/10/03)
Nanocrystalline magnesium oxide was found to be an effective heterogeneous, solid base catalyst for the one-pot Wittig reaction to afford α,β-unsaturated esters and nitriles in excellent yields with high E-stereoselectivity in the presence of triphenylphosphine under mild conditions.
Ethyl (benzothiazol-2-ylsulfonyl)acetate: A new reagent for the stereoselective synthesis of α,β-unsaturated esters from aldehydes
Blakemore, Paul R.,Ho, Danny K.H.,Nap, W. Mieke
, p. 1365 - 1368 (2007/10/03)
The title reagent engaged in the modified Julia olefination with aldehydes under mild reaction conditions (DBU, CH2Cl2, rt or -78°C) to yield α,β-unsaturated esters; aryl aldehydes and aliphatic aldehydes possessing significant chain branching elements gave trans alkene products with high stereoselectivity (E : Z up to >98 : 2), while straight chain aliphatic aldehydes gave cis products preferentially (Z : E up to 92 : 8). The Royal Society of Chemistry 2095.
Vinylbenzene derivatives
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, (2008/06/13)
The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2and R3, being the same or different, are H, halogen or lower alkyl; R4and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6is carboxyl or phosphono or ester thereof.
HECK REACTIONS IN SOLID PHASE SYNTHESIS
Yu, Kuo-Long,Deshpande, Milind S.,Vyas, Dolatrai M.
, p. 8919 - 8922 (2007/10/02)
Heck reactions of polymer bound aryl iodide (1) or styrene (2) with olefins or aryl halides generally gave good yields of products of high purity.The methodology developed can be applied as a convenient procedure for generating 1,2-disubstituted olefins i
Heck Reaction of Arenediazonium Salts: a Palladium-catalysed Reaction in an Aqueous Medium
Sengupta, Saumitra,Bhattacharya, Sanchita
, p. 1943 - 1944 (2007/10/02)
Heck reaction of arenediazonium salts has been conveniently carried out with 1-2 molpercent Pd(OAc)2 in ethanol.An aqueous one pot procedure starting with anilines is described.
