- Organic electroluminescent device
-
The present invention relates to electronic devices, in particular organic electroluminescent devices, comprising compounds of the formula (1), to the corresponding compounds, and to a process for the preparation of these compounds.
- -
-
Page/Page column 117
(2016/06/01)
-
- NOVEL COMPOUNDS AS CHLORIDE CHANNEL BLOCKING AGENT
-
Disclosed is a novel compound to function as a calcium-dependent chloride channel blocking agent.
- -
-
Paragraph 0167; 0168; 0169; 0170; 0171; 0172
(2015/06/03)
-
- EBNA1 INHIBITORS AND THEIR METHOD OF USE
-
Pharmaceutical compositions of the invention comprise EBNA1 inhibitors useful for the treatment of diseases caused by EBNA1 activity such as cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and rheumatoid arthritis. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection. Pharmaceutical compositions of the invention also comprise EBNA1 inhibitors useful for the treatment of diseases caused by lytic Epstein-Barr Virus (EBV) infection.
- -
-
Paragraph 0585-0586
(2015/06/03)
-
- ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
-
This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
- -
-
Page/Page column 157
(2015/01/06)
-
- Monna, a potent and selective blocker for transmembrane protein with unknown function 16/anoctamin-1
-
Transmembrane protein with unknown function 16/anoctamin-1 (ANO1) is a protein widely expressed in mammalian tissues, and it has the properties of the classic calcium-activated chloride channel (CaCC). This protein has been implicated in numerous major physiological functions. However, the lack of effective and selective blockers has hindered a detailed study of the physiological functions of this channel. In this study, we have developed a potent and selective blocker for endogenous ANO1 in Xenopus laevis oocytes (xANO1) using a drug screening method we previously established (Oh et al., 2008). We have synthesized a number of anthranilic acid derivatives and have determined the correlation between biological activity and the nature and position of substituents in these derived compounds. A structure-activity relationship revealed novel chemical classes of xANO1 blockers. The derivatives contain a-NO2 group on position 5 of a naphthyl group-substituted anthranilic acid, and they fully blocked xANO1 chloride currents with an IC 5050 of 0.08 μM for xANO1. Selectivity tests revealed that other chloride channels such as bestrophin-1, chloride channel protein 2, and cystic fibrosis transmembrane conductance regulator were not appreciably blocked by 10～30 μM MONNA. The potent and selective blockers for ANO1 identified here should permit pharmacological dissection of ANO1/CaCC function and serve as potential candidates for drug therapy of related diseases such as hypertension, cystic fibrosis, bronchitis, asthma, and hyperalgesia.
- Oh, Soo-Jin,Hwang, Seok Jin,Jung, Jonghoon,Yu, Kuai,Kim, Jeongyeon,Choi, Jung Yoon,Hartzell, H. Criss,Roh, Eun Joo,Justin Lee
-
p. 726 - 735
(2013/11/06)
-
- SUBSTITUTED BENZENE COMPOUNDS
-
The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
- -
-
Page/Page column 351
(2012/11/06)
-
- Synthesis of cyclic selenenate/seleninate esters stabilized by ortho-nitro coordination: Their glutathione peroxidase-like activities
-
The syntheses of selenenate/seleninate esters and related derivatives by aromatic nucleophilic substitution (SNAr) reactions of 2-bromo-3-nitrobenzylalcohol (13) and 2-bromo-3-nitrobenzaldehyde (17) with Na2Se2/nBuSeNa are
- Singh, Vijay P.,Singh, Harkesh B.,Butcher, Ray J.
-
p. 1431 - 1442
(2013/01/11)
-
- A noveland practical synthesis of substituted 2-ethoxy benzimidazole: Candesartan cilexetil
-
A novel and practical synthetic route for the preparation of candesartan cilexetil from methyl 2-amino-3-nitrobenzoate is described.The key steps are the reaction of methyl 2-bromo-3-(diethoxy-methyleneamino)benzoate with (2-(1-trityl-1H-tetrazol-5-yl) biphenyl-4-yl) methanamine and the final formation of 2-ethoxy benzimidazole ring via intramolecular N-arylation.The final ring closure process could be utilized to prepare other 2-substituted benzimidazoles.The method is simple for operation and suitable for industrial production.
- Wang, Ping,Zheng, Guo-Jun,Wang, Ya-Ping,Wang, Xiang-Jing,Li, Yan,Xiang, Wen-Sheng
-
experimental part
p. 5402 - 5406
(2010/08/19)
-
- Substituted tricyclics
-
A class of novel tricyclics is disclosed together with the use of such compounds for inhibiting sPLA2mediated release of fatty acids for treatment of conditions such as septic shock.
- -
-
-
- Preparation and NMR analysis of 2,6-heterodifunctional halobenzenes as precursors for substituted biphenyls
-
Preparation and complete characterization of 16 2,6-disubstituted halobenzenes, including nine new compounds, from two common starting materials is described. Seven of the new compounds contain one or two propylthio groups, which have been introduced in two ways. Direct reaction of arenediazonium salts with 1-propanethiolate gives yields comparable to those obtained in a three-step method through sulfonyl chlorides. The 1H- and 13C NMR chemical shifts of 17 1,2,3-trisubstituted benzenes have been correlated with the predicted values and the observed trends explained using commonly available modeling packages.
- Sienkowska, Monika,Benin, Vladimir,Kaszynski, Piotr
-
p. 165 - 173
(2007/10/03)
-
- Substituted carbazoles, process for their preparation and their use as sPLA2 inhibitors
-
Novel tricyclics are disclosed together with the use of such compounds for inhibiting SPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.
- -
-
-
- N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3- methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide; one of a class of novel benzenesulphonamides which are orally-active, ET(A)-seIective endothelin antagonists
-
A series of novel sulphonamides have been discovered which show high affinity and selectivity for the endothelin ET(A) receptor. N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(-3-methoxy-5-methylpyrazin-2 -ylsulfamoyl)benzamide (18) is the most widely investigated compound and is a potent antagonist in vivo when dosed either i.v. or orally, and has prolonged oral duration of action.
- Mortlock, Andrew A.,Bath, Colin,Butlin, Roger J.,Heys, Christine,Hunt, Sarah J.,Reid, Alan C.,Sumner, Neil F.,Tang, Eric K.,Whiting, Elaine,Wilson, Campbell,Wright, Nicola D.
-
p. 1399 - 1402
(2007/10/03)
-
- Synthesis and Anti-HIV-1 Activity of 4,5,6,7-Tetrahydro-5-methylimidazobenzodiazepin-2(1H)-one (TIBO) Derivatives
-
A series of 6-substituted 4,5,6,7-tetrahydro-5-methylimidazobenzodiazepin-2(1H)-ones (9) have been synthesized and tested for their ability to inhibit the replication of the HIV-1 virus in MT-4 cells.Two synthetic methods are described, one of which allows the synthesis of single enantiomers of the final products.A structure-activity study was done within the series of compounds to determine the optimum group for the 6-position substitution and to determine whether the activity was enantiospecific at the 5-position, which was substituted with a methyl group.The best analogue, 9jj, inhibited HIV-1 with an IC50 of 4 μM, which is comparable to the activity level of DDI, a 2',3'-dideoxynucleoside-type structure undergoing clinical trials as an anti-AIDS therapy.
- Kukla, Michael J.,Breslin, Henry J.,Pauwels, Rudi,Fedde, Cynthia L.,Miranda, Milton,et al.
-
p. 746 - 751
(2007/10/02)
-
- Antifolate and Antibacterial Activities of 5-Substituted 2,4-Diaminoquinazolines
-
A series of 5-substituted 2,4-diaminoquinazolines (3) has been synthesized and evaluated as inhibitors of the enzyme dihydrofolate reductase (DHFR) from both bacterial and mammalian sources.The best compounds (e.g. 53) show good activity against Escherichia coli DHFR, but there is no significant selectivity for the bacterial over the mammalian enzyme.The structure-activity relationships for enzyme inhibition appear to be complex and not amenable to simple analysis; a hypotesis to explain the observed qualitative structure-activity relationships is proposed.The inhibitory activities of the compounds against the growth of intact bacterial cells in vitro closely parallel those for the inhibition of the isolated bacterial enzymes, suggesting that their antifolate action is responsible for their antibacterial effects.Five of the compounds were tested for their ability to cure a systemic E. coli infection in the mouse, but they showed no therapeutic effects at their maximum tolerated doses.
- Harris, Neil V.,Smith, Christopher,Bowden, Keith
-
p. 434 - 444
(2007/10/02)
-
- Palladium-Catalyzed Coupling of 2-Bromoanilines with Vinylstannanes. A Regiocontrolled Synthesis of Substituted Indoles
-
The palladium-catalyzed cross-coupling reaction of aryl halides and triflates with vinylstannane reagents has been used to produce a variety of substituted indoles.The mild reaction conditions and selectivity inherent in the coupling reaction have been utilized to produce regiochemically pure 4-, 5-, and 6-substituted indoles.
- Krolski, Michael E.,Renaldo, Alfred F.,Rudisill, Duane E.,Stille, J. K.
-
p. 1170 - 1176
(2007/10/02)
-
