- Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis
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Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite Toxoplasma gondii. The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1H-pyrazolo
- Janetka, James W.,Hopper, Allen T.,Yang, Ziping,Barks, Jennifer,Dhason, Mary Savari,Wang, Qiuling,Sibley, L. David
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supporting information
p. 6144 - 6163
(2020/07/10)
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- CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
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The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
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Page/Page column 298; 299
(2019/10/23)
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- POLYCYCLIC DERIVATIVES, PREPARATION PROCESS AND PHARMACEUTICAL USE THEREOF
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Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutic agents, especially the GPR40 agonist and in preparation of drugs for treating diseases such as diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
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- POLYCYCLIC DERIVATIVES, PREPARATION METHOD AND MEDICAL USES THEREOF
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Disclosed in the present invention are polycyclic derivatives as represented by general formula (I), the preparation method thereof, pharmaceutical compositions containing the derivatives and uses thereof as therapeutical agents, especially the GPR40 agonist and in preparation of drugs for treating diseases like diabetes and metabolic disorders, etc., wherein each substituent in the general formula (I) has the same definition as in the description.
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- SPIROINDOLINONE DERIVATIVES
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There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof wherein W, V, X, Y, A, R and R' are as described herein. The compounds are useful as anticancer agents.
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Page/Page column 102
(2009/07/03)
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- Scope and utility of a new soluble copper catalyst [CuBr-LiSPh-LiBr-THF]: A comparison with other copper catalysts in their ability to couple one equivalent of a Grignard reagent with an alkyl sulfonate
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A mixture of equal amounts of CuBr-SMe2, LiBr, and LiSPh in THF at 0°C furnished a new soluble copper catalyst that was highly efficient at coupling primary, secondary, tertiary, aryl, vinyl, and allylic Grignard reagents to primary tosylates and primary Grignard reagents to secondary tosylates and mesylates, all with the use of only 1 equiv of Grignard reagent. The new catalyst was shown to be much more reactive than copper catalysts CuBr and Li2CuCl4 and more efficient in the transference of secondary and tertiary alkyl groups than lower order cuprates (Gilman reagents) and demonstrated more reactivity than the lower order cuprates with its ability to couple primary Grignard reagents to secondary sulfonates. The Grignard reagent/catalyst system was compatible with an ester functionalized tosylate, thus proving to be more chemoselective than a Grignard reagent without the catalyst. The catalyst exhibited good reactivity below room temperature, and with the addition of 6% v/v of HMPA to the catalyst solution, excellent yields of coupled product were obtained within a 25-67°C temperature range. 1H NMR demonstrated that the catalyst solution consisted of several species that most likely were composed of copper ligated with thiophenol, THF, and LiBr in aggregated forms.
- Burns, Dennis H.,Miller, Jeffrey D.,Chan, Ho-Kit,Delaney, Michael O.
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p. 2125 - 2133
(2007/10/03)
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- Process for the production of aniline derivatives
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Industrial process for the efficient production of aniline derivatives which are important intermediates for the manufacture of oxazolidinedione derivatives and tetrahydrophthalimide derivatives which are useful as active ingredients of herbicides. The process starts from 2,4-dihalo-5-aminophenol or bis(2,4-dihalo-5-aminophenyl)carbonate and selectively cycloalkylates or alkynylates the hydroxy group without protecting the amino group, whereby aniline derivatives having the cycloalkyloxy group or alkynyloxy group can be produced in high yield.
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- TRIETHYL PHOSPHITE IN ORGANIC SYNTHESIS. A FACILE, ONE-POT CONVERSION OF ALCOHOLS INTO AMINES
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General protocols for converting primary, secondary, and tertiary alcohols into the corresponding primary amines are presented.
- Zwierzak, Andrzej
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- Sulphonate Esters as Sources of Sulphonyl Radicals; Ring-closure Reactions of Alk-4- and -5-enesulphonyl Radicals
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Alkyl alkanesulphonates and arenesulphonates were found to be useful sources of sulphonyl radicals, particularly for spectroscopic work, when treated with organotin or organosilyl radicals.Allyl, propynyl and penta-2,4-dienyl methanesulphonates gave, however, allyl, propynyl and pentadienyl radicals, respectively.Sulphonyl radicals generated in this way added efficiently to alk-1-enes with electron-releasing substituents, and the EPR spectra of the adduct radicals were recorded.A variety of radical initiation systems were tried on pent-4-enesulphonyl chloride.The pent-4-enesulphonyl radical cyclised mainly in the endo mode to give the six-membered-ring sulphone.Similarly, the hex-5-enesulphonyl radical cyclised to give thiepane 1,1-dioxide, with a seven-membered ring.The cyclohex-2-enylethanesulphonyl radical cyclised mainly in the exo mode to give 2-chloro-9-thiabicyclononane 9,9-dioxide.The mechanisms of these reactions are discussed.
- Culshaw, Peter N.,Walton, John C.
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p. 1201 - 1208
(2007/10/02)
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- Nuclear Heptylation of Benzene and Naphthalene and Cyclopentylation of Toluene
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Thermal decomposition of 1-, 2-, 3- and 4-heptyltoluene-p-sulphonates in the presence of aromatic substrates like benzene or naphthalene at 130-35 deg, affords differently substituted α- and β-isomers in the case of naphthalene.Skeletal isomerisation of the alkyl group is observed where different isomeric 1-, 2-, 3- and 4-heptyl-aromatics are obtained.Also thermal decomposition of cyclopentylmethane sulphonate in the presence of toluene at 130-35 deg, furnishes the corresponding o-, m- and p-substituted toluenes.The isomers have been identified and estimated quantitatively by GLC.
- Badr, M. Z. A.,El-Naggar, G. M.,Aly, M. M.,Fahmy, A. M.
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p. 961 - 964
(2007/10/02)
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