- ISO-CITRATE DEHYDROGENASE (IDH) INHIBITOR
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Disclosed are compounds inhibiting the conversion of α–KG to D-2-HG, pharmaceutically acceptable salts, hydrates, solvates or stereoisomers thereof and pharmaceutical compositions comprising the compounds. The compound and the pharmaceutical composition c
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Page/Page column 81; 83-84
(2021/04/17)
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- 18F LABELLED THIAZOLYLHYDRAZONE DERIVATIVES
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The present invention relates to compounds of Formula (I) wherein R1 and R2 are independently selected from 19F and 18F having selective binding for MAO-B as compared with MAO-A. The invention also provides radi
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Page/Page column 8-9
(2016/07/05)
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- PYRIDINE DERIVATIVES AND THEIR USE AS HERBICIDES
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The invention relates to the use of amide derivatives of the formula (I) wherein X1, X2, X3, X4, Z1 and Y are as defined in the specification as herbicides. Furthermore, the present invention relates
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Page/Page column 32
(2014/09/03)
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- Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: New multimodal fluorinated and iodinated radiotracers
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This study reports a series of 14 new iodinated and fluorinated compounds offering both early imaging (123I, 124I, 18F) and systemic treatment (131I) of melanoma potentialities. The biodistribution of each 125I-labeled tracer was evaluated in a model of melanoma B16F0-bearing mice, using in vivo serial γ scintigraphic imaging. Among this series, [125I]56 emerged as the most promising compound in terms of specific tumoral uptake and in vivo kinetic profile. To validate our multimodality concept, the radiosynthesis of [18F]56 was then optimized and this radiotracer has been successfully investigated for in vivo PET imaging of melanoma in B16F0- and B16F10-bearing mouse model. The therapeutic efficacy of [131I]56 was then evaluated in mice bearing subcutaneous B16F0 melanoma, and a significant slow down in tumoral growth was demonstrated. These data support further development of 56 for PET imaging (18F, 124I) and targeted radionuclide therapy ( 131I) of melanoma using a single chemical structure.
- Maisonial, Aurélie,Kuhnast, Bertrand,Papon, Janine,Boisgard, Rapha?l,Bayle, Martine,Vidal, Aurélien,Auzeloux, Philippe,Rbah, Latifa,Bonnet-Duquennoy, Mathilde,Miot-Noirault, Elisabeth,Galmier, Marie-Josèphe,Borel, Michèle,Askienazy, Serge,Dollé, Frédéric,Tavitian, Bertrand,Madelmont, Jean-Claude,Moins, Nicole,Chezal, Jean-Michel
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experimental part
p. 2745 - 2766
(2011/06/24)
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- Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
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In an attempt to simplify nucleophilic radiofluorination reactions to be amenable for automation, a series of [18F]fluoronicotinamides, [ 18F]fluoroisonicotinamides and [18F]fluorobenzamides were synthesized using one-step
- Al Jammaz,Al-Otaibi,Okarvi,Amartey
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experimental part
p. 312 - 317
(2012/06/04)
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- AMIDE COMPOUND AND METHOD FOR CONTROLLING PLANT DISEASE USING THE SAME
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Disclosed is a plant disease control agent containing an amide compound represented by formula (1) below which has an excellent plant disease controlling effect as an active ingredient. (In the formula, X1, X2, Z1 and Esu
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Page/Page column 32-33
(2010/04/30)
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- SUBSTITUTED PYRAZOLE COMPOUNDS USEFUL AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS
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Disclosed are compounds active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same.
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Page/Page column 100-101
(2008/06/13)
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- N-PHENYL-(2R,5S)DIMETHYLPIPERADINE DERIVATIVE
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The present invention relates to a novel N-phenyl-(2R,5S)dimethylpiperazine derivatives useful as antiandrogenic agent which exhibits a sufficient prostate gland reducing effect as compared with conventional compounds and are excellent in oral activity. The compound of the present application is useful in preventing or treating prostate cancer, benign prostatic hyperplasia, and the like. The present invention also provides a novel intermediate useful in producing the compound of the present invention.
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Page/Page column 18
(2010/02/12)
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- Bis-acyloxymethyl derivatives
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This invention relates to new pyridyl, quinoline and acridine bis-acyloxymethyl compounds; to compositions comprising these compounds; and to processes for their utility as fungicides, bactericides and as inhibitors of the growth of cancer in warm-blooded animals. In accordance with this invention, new bis-acyloxymethyl derivatives are provided of the formula: STR1 wherein B is selected from substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl and alkynyl; A is selected from hydrogen and B; or, A and B together comprise a pyrrolizine; L is selected from STR2 wherein Y is selected from hydrogen or STR3 each R and Z is independently selected from hydrogen or substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl, alkynyl, amine group, each Z' is independently selected from hydrogen and substituted or unsubstituted alkyl; M is Z or is selected from halogen, nitro, hydroxyl, nitrile and substituted or unsubstituted, carboxylic acid group, carboxylic acid ester group, carboxylic acid amide group, sulfonic acid group and sulfonic acid amide group; ether group, thioether group, acylated hydroxyl, sulfonylamide, sulfonylurea, sulfoxide group, sulfone group and mixtures thereof; each n is the same and is 0 or 1; q is from 0-4; and, X is the anion of an acid.
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- Synthesis, Chemistry, and Antineoplastic Activity of α-Halopyridinium Salts: Potential Pyridone Prodrugs of Acylated Vinylogous Carbinolamine Tumor Inhibitors
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A series of 4- and 5-methyl>-1H-pyrrolizin-5-yl>-2-halopyridinium iodides were synthesized.The rates of hydrolysis of the α-halopyridinium salts to the corresponding pyridones, and the reactivities of the carbamate moieties were studied as a function of pH, buffer composition, and ionic strength.The 4- and 5-pyrrolizinyl-2-halopyridinium iodides and the corresponding pyridones were evaluated against P388 lymphocytic leukemia in vivo.The α-fluoropyridinium compounds were active but the α-chloro compounds were not.This activity was correlated with the rates of hydrolysis of the α-halopyridinium compounds to the active pyridone.Compounds that were active in the P388 screen were evaluated in L1210 leukemia, M5076 carcinoma, and MX-1 mammary xenograft assays in mice.
- Anderson, Wayne K.,Dean, Dennis C.,Endo, Toshiyasu
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p. 1667 - 1675
(2007/10/02)
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