91065-17-7Relevant articles and documents
Novel amidrazone derivatives: Design, synthesis and activity evaluation
Zhou, Hua,Wang, Zhi Sen,Liu, Xin Hua,Chen, Fei Hu
, p. 3158 - 3165 (2018/05/05)
A series of new 6-styryl-naphthalene-2-amidrazone derivatives were synthesized and evaluated as potential ASIC1a inhibitors. Among them, compound 5e showed the most activity to inhibit [Ca2+]i. elevation in acid-induced articular chondrocytes. Together with the important role of ASIC1a in the pathogenesis of tissue acidification diseases including rheumatoid arthritis, these results might provide a meaningful hint or inspiration in developing drugs targeting at tissue acidification diseases.
Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase
Lee, Won-Gil,Frey, Kathleen M.,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Chan, Albert H.,Anderson, Karen S.,Jorgensen, William L.
, p. 4824 - 4827 (2015/10/28)
Non-nucleoside inhibitors of HIV-1 reverse transcriptase (HIV-RT) are reported that incorporate a 7-indolizinylamino or 2-naphthylamino substituent on a pyrimidine or 1,3,5-triazine core. The most potent compounds show below 10 nanomolar activity towards wild-type HIV-1 and variants bearing Tyr181Cys and Lys103Asn/Tyr181Cys resistance mutations. The compounds also feature good aqueous solubility. Crystal structures for two complexes enhance the analysis of the structure-activity data.
Nickel-catalyzed cross-couplings of benzylic pivalates with arylboroxines: Stereospecific formation of diarylalkanes and triarylmethanes
Zhou, Qi,Srinivas, Harathi D.,Dasgupta, Srimoyee,Watson, Mary P.
, p. 3307 - 3310 (2013/04/23)
We have developed a stereospecific nickel-catalyzed cross-coupling of benzylic pivalates with arylboroxines. The success of this reaction relies on the use of Ni(cod)2 as the catalyst and NaOMe as a uniquely effective base. This reaction has broad scope with respect to the arylboroxine and benzylic pivalate, enabling the synthesis of a variety of diarylalkanes and triarylmethanes in good to excellent yields and ee's.
ARYL-PYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
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, (2011/06/19)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
ARYL PYRIDINE AS ALDOSTERONE SYNTHASE INHIBITORS
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, (2012/04/23)
The present invention provides a compound of Formula (I); a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Urokinase inhibitors
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, (2008/06/13)
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
Ukokinase inhibitors
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, (2008/06/13)
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
SRN1 SYNTHESES OF BIS(PHENYLTHIO)- AND DICYANO-NAPHTHALENES VIA DIAZOSULFIDES
Novi, M.,Garbarino, G.,Petrillo, G.,Dell'Erba, C.
, p. 2205 - 2212 (2007/10/02)
The reactions of bromonaphthalenediazonium tetrafluoroborates (6a,b and 11a,b) with sodium benzenethiolate in DMSO give, through the preliminary formation of the corresponding diazosulfides (7a,b and 12a,b) bis(phenylthio)naphthalenes (8a,b and 13a,b) deriving from substitution of both the diazo group and the bromine.Isolated diazosulfides (7a,b and 12a,b) likewise furnish satisfactory yields of dinitriles (9a,b and 14a,b) by reaction with excess tetrabutylammonium cyanide in DMSO under photostimulation by a sunlamp.The intervention of an SRN1 process accounting for the formation of the disubstitution products is postulated.