850233-82-8Relevant academic research and scientific papers
PYRIMIDINE COMPOUNDS CONTAINING ACIDIC GROUPS
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Paragraph 1276; 1277, (2018/06/15)
The present disclosure relates to a class of pyrimidine derivatives having immunomodulating properties that act via TLR7 which are useful in the treatment of viral infections and cancers.
Different products in the reaction of the alcohols with cyclic and acyclic 1,3-dicarbonyl compounds: K5CoW12O40 as an electron transfer nano catalyst
Rafiee, Ezzat,Kahrizi, Masoud,Joshaghani, Mohammad
, p. 1363 - 1366 (2013/02/22)
K5CoW12O40 was used as a highly effective catalyst for the benzylation of 1,3-dicarbonyl compounds. β-Keto enol ethers were obtained when cyclic 1,3-dicarbonyl compounds used in this conditions instead of linear ones. The present methodology offers a practical, simple, mild, environmentally friendly, and time-saving method for etherification. Very low loading of catalyst, ease of workup, ease of handling, and reusability of catalyst are other advantages of this catalyst.
4H- [1, 2, 4] TRIAZOLO [5, 1 -B] PYRIMIDIN-7 -ONE DERIVATIVES AS CCR2B RECEPTOR ANTAGONISTS
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Page/Page column 103, (2011/10/10)
The present invention relates to novel compounds for use in the compositions, to processes for their preparation, to intermediates useful in their preparation and to their use as therapeutic agents. The present invention also relates to pharmaceutical com
NOVEL PYRIMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CANCER AND FURTHER DISEASES
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Page/Page column 48-49, (2010/12/18)
The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compoun
2-OXO-2H-CHROMENE COMPOUNDS
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Page/Page column 34, (2010/11/29)
Compounds of structural formula (1) modulate CRTH2 activity and are of utility in, for example, respiratory diseases formula (1): in which: A represents a direct bond, an optionally substituted alkylene or alkenylene group, or a group of formula Z-(optionally substituted)alkylene; B represents a direct bond, an optionally substituted alkylene or alkenylene group, or a group of formula Z-(optionally substituted)alkylene or (optionally substituted)alkylene-Z; Z represents an oxygen atom, an NH or N-alkyl group, or a group of formula S(O)n, in which n = 0 to 2; X represents a carboxylic acid, tetrazole, 3-hydroxyisoxazole, hydroxamic acid, phosphinate, phosphonate, phosphonamide, sulfonic acid or a group of formula C(=O)NHSO2W or SO2NHC(=O)W; W represents an optionally substituted aryl or heteroaryl group or an optionally substituted alkyl or cycloalkyl group; Y represents an optionally substituted phenyl or 5- or 6-membered heteroaryl group, Ra, Rb, and Rc independently represent hydrogen, acyl, alkoxy, alkoxycarbonyl, alkylamino, alkylsulfinyl, alkylsulfonyl, alkylthio, -NH2, aminoalkyl, hydroxyalkyl, alkoxyalkyl, arylalkyl, cyano, dialkylamino, halo, haloalkoxy, haloalkyl, alkyl, alkenyl, -OH, optionally substituted aryl, optionally substituted heteroaryl, heterocycloalkyl, aminoacyl, aminosulfonyl, acylamino, sulfonylamino, heteroarylalkyl, cyclic amino, aryloxy, heteroaryloxy, arylalkyloxy or heteroarylalkyloxy.
Design, synthesis, and antifolate activity of new analogues of piritrexim and other diaminopyrimidine dihydrofolate reductase inhibitors with ω-carboxyalkoxy or ω-carboxy-1-alkynyl substitution in the side chain
Chan, David C. M.,Fu, Hongning,Forsch, Ronald A.,Queener, Sherry F.,Rosowsky, Andre
, p. 4420 - 4431 (2007/10/03)
As part of a search for dihydrofolate reductase (DHFR) inhibitors combining the high potency of piritrexim (PTX) with the high antiparasitic vs mammalian selectivity of trimethoprim (TMP), the heretofore undescribed 2,4-diamino-6-(2′,5′-disubstituted benzyl)pyrido[2,3-d]pyrimidines 6-14 with O-(ω-carboxyalkyl) or ω-carboxy-1-alkynyl groups on the benzyl moiety were synthesized and tested against Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium DHFR vs rat DHFR. Three N-(2,4-diaminopteridin-6-yl)methyl)-2′-(ω-carboxy-1-alkynyl) -dibenz[b,f]azepines (19-21) were also synthesized and tested. The pyridopyrimidine with the best combination of potency and selectivity was 2,4-diamino-5-methyl-6-[2′-(5-carboxy-1-butynyl)-5′-methoxy]benzyl] pyrimidine (13), with an IC50 value of 0.65 nM against P. carinii DHFR, 0.57 nM against M. avium DHFR, and 55 nM against rat DHFR. The potency of 13 against P. carinii DHFR was 20-fold greater than that of PTX (IC50 = 13 nM), and its selectivity index (SI) relative to rat DHFR was 85, whereas PTX was nonselective. The activity of 13 against P. carinii DHFR was 20 000 times greater than that of TMP, with an SI of 96, whereas that of TMP was only 14. However 13 was no more potent than PTX against M. avium DHFR, and its SI was no better than that of TMP. Molecular modeling dynamics studies using compounds 10 and 13 indicated a slight binding preference for the latter, in qualitative agreement with the IC50 data. Among the pteridines, the most potent against P. carinii DHFR and M. avium DHFR was the 2′-(5-carboxy-1-butynyl) dibenz[b,f]azepinyl derivative 20 (IC50 = 2.9 nM), whereas the most selective was the 2′-(5-carboxy-1-pentynyl) analogue 21, with SI values of > 100 against both P. carinii and M. avium DHFR relative to rat DHFR. The final compound, 2,4-diamino-5-[3′-(4-carboxy-1-butynyl)-4′-bromo- 5′-methoxybenzyl]pyrimidine (22), was both potent and selective against M. avium DHFR (IC50 = 0.47 nM, SI = 1300) but was not potent or selective against either P. carinii or T. gondii DHFR.
