- Fragment-based lead discovery to identify novel inhibitors that target the ATP binding site of pyruvate dehydrogenase kinases
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A fragment-based lead discovery approach was applied to Pyruvate Dehydrogenase Kinases (PDHKs) to discover inhibitors against the ATP binding site with novel chemotypes. X-ray fragment screening toward PDHK4 provided a fragment hit 1 with a characteristic
- Akaki, Tatsuo,Bessho, Yuki,Ito, Takashi,Fujioka, Shingo,Ubukata, Minoru,Mori, Genki,Yamanaka, Kenji,Orita, Takuya,Doi, Satoki,Iwanaga, Tomoko,Ikegashira, Kazutaka,Hantani, Yoshiji,Nakanishi, Isao,Adachi, Tsuyoshi
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- Preparation method for catalyzing pyrimidine cyclic hydroxyl chlorination by tetraethylammonium chloride
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The invention discloses a preparation method for catalyzing pyrimidine cyclic hydroxyl chlorination by tetraethylammonium chloride, which comprises the following steps: (1) adding phosphorus oxychloride into a container, adding tetraethylammonium chloride as a catalyst, adding a pyrimidine cyclic hydroxyl compound, and heating to react; (2) preparing an alkali liquor, cooling to 0 DEG C, and slowly dropwise adding an obtained reaction liquid into the alkali liquor for quenching to obtain a target product. The method has the advantages that the provided pyrimidine cyclic hydroxyl chlorination catalysis method is small in environmental pollution, the obtained product is light in color, the catalysis efficiency is high, and the phosphorus oxychloride recovery pressure is small.
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Paragraph 0031-0034
(2020/04/17)
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- SUBSTITUTED CARBONUCLEOSIDE DERIVATIVES USEFUL AS ANTICANCER AGENTS
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Compounds of the general formula:processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Page/Page column 220; 221
(2018/05/29)
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- PYRIMIDINE COMPOUNDS AND PYRIMIDO INDOLE COMPOUNDS AND METHODS OF USE
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The present invention discloses substituted pyrimidine and pyrimido indole compounds and optionally pharmaceutically acceptable salts, hydrates or solvates thereof. A method of treating a patient having cancer or a disease comprising administering to a patient an effective amount of the compound or pharmaceutically acceptable salt, hydrate, or solvate thereof.
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Page/Page column 50
(2016/03/19)
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- PIPERIDINE SUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES WITH INHIBITORY ACTIVITY ON THE REPLICATION OF THE RESPIRATORY SYNCYTIAL VIRUS (RSV)
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The invention concerns novel substituted bicyclic pyrazolo pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further conce
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Page/Page column 36
(2016/11/07)
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- Synthesis, cytostatic, antimicrobial, and anti-HCV activity of 6-substituted 7-(het)aryl-7-deazapurine ribonucleosides
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A series of 80 7-(het)aryl- and 7-ethynyl-7-deazapurine ribonucleosides bearing a methoxy, methylsulfanyl, methylamino, dimethylamino, methyl, or oxo group at position 6, or 2,6-disubstituted derivatives bearing a methyl or amino group at position 2, were
- Nau?, Petr,Caletková, Olga,Kone?ny, Petr,D?ubák, Petr,Bogdanová, Kate?ina,Kolá?, Milan,Vrbková, Jana,Slavětínská, Lenka,Tlou?t'Ová, Eva,Perlíková, Pavla,Hajdúch, Marián,Hocek, Michal
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supporting information
p. 1097 - 1110
(2014/03/21)
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- Synthesis and discovery of water-soluble microtubule targeting agents that bind to the colchicine site on tubulin and circumvent Pgp mediated resistance
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Two classes of molecules were designed and synthesized based on a 6-CH 3 cyclopenta[d]pyrimidine scaffold and a pyrrolo[2,3-d]pyrimidine scaffold. The pyrrolo[2,3-d]pyrimidines were synthesized by reacting ethyl 2-cyano-4,4-diethoxybutanoate an
- Gangjee, Aleem,Zhao, Ying,Lin, Lu,Raghavan, Sudhir,Roberts, Elizabeth G.,Risinger, April L.,Hamel, Ernest,Mooberry, Susan L.
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experimental part
p. 8116 - 8128
(2011/02/26)
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- BICYCLIC COMPOUNDS HAVING ANTIMITOTIC AND/OR ANTITUMOR ACTIVITY AND METHODS OF USE THEREOF
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The present invention provides bicyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor a
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Page/Page column 15-16
(2010/02/17)
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- FUSED HETEROARYL PYRIDYL AND PHENYL BENZENESUFLONAMIDES AS CCR2 MODULATORS FOR THE TREAMENT OF INFLAMMATION
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Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2- mediated diseases and as controls in assays for the identification of CCR2 antagonists. A compound of the formula (I) or a salt thereof: where: R1 and R2 are each independently hydrogen, halogen, C1-8alkyl, -CN. or C1-8 haloalkyl, provided that at least one of R11or R2 is other than hydrogen; each R3 is independently hydrogen; R4 is hydrogen; R5 is halogen or C1-8 alkyl; R6 is hydrogen; X1 is CR7, N or NO; X2 and X4 are N or NO; X3 is CR7; X6 and X7 are each independently selected from CR7, N, and NO; each R7 is independently selected from the group consisting of hydrogen, halogen, substituted or unsubstituted C2-8 alkyl, substituted or unsubstituted C2-8 alkeπyl, substituted or unsubstituted C2-8 alkynyl, -CN. =O, -NO2, -OR6, -OC(O)R8, -CO2R8, -C(O)R8, -C(O)NR0R8, -OC(O)NR9R8, -NR10C(O)R8, -NR10C(O)NR9R8, -NR9R8, -NR10CO2R8, -SR8, -S(O)R8, -S(O)2R8, -S(O)2NR9R8, -NR10S(O)2R8, substituted or unsubstituted C6-10 aryl, substituted or unsubstituted 5- to 10-membered heteroaryl and substituted or unsubstituted 3- to 10-membered heterocyclyl;
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Page/Page column 71; 72
(2009/03/07)
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