5418-10-0Relevant academic research and scientific papers
FUSED BICYCLIC PYRIMIDINE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 45, (2011/06/19)
The present invention relates to Fused Bicyclic Pyrimidine Derivatives, compositions comprising a Fused Bicyclic Pyrimidine Derivative, and methods of using the Fused Bicyclic Pyrimidine Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.
NITROGENOUS FUSED BICYCLIC COMPOUND
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Page/Page column 61, (2010/11/26)
A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R 0 represents hydrogen, halogeno, etc.; R 1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D 1 , D 2 and D 3 each represents N or CH; R 2 represents halogeno or optionally halogenated lower alkyl, etc.; R 3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)
Tricyclic base analogues
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, (2008/06/13)
Nucleoside analogues have structure (2) wherein Q is H or a sugar moiety or sugar analogue or a modified sugar or a nucleic backbone or backbone analogue, W is an alkylene or alkenylene chain of 0-5 carbon atoms, any of which may carry a substituent R8, X is O or N or NR12or CR10, X′ is O or S or N, provided that when X′ is O or S, then X is C, Y is CH or N, R6is NH2or SMe or SO2Me or NHNH2, each of R7and R8is independently H or F or alkyl or alkenyl or aryl or acyl or a reporter moiety, R12is independently H or alkyl or alkenyl or aryl or acyl or a reporter moiety, and R10is H or ═O or F or alkyl or aryl or a reporter moiety.
Synthesis and biological activity of 4-substituted 1-[1-(2-hydroxyethoxy)-methyl-1,2,3-triazol-(4 & 5)-Ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines
Moukha-Chafiq,Taha,Lazrek,Pannecouque,Witvrouw,De Clercq,Barascut,Imbach
, p. 1797 - 1810 (2007/10/03)
The chemical synthesis of some 4-substituted 1-[1-(2-hydroxyethoxy)-methyl-1,2,3-triazol-(4 and 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines 12a,b, 13a,b and 14-23 as acyclic nucleosides is described. Treatment of (2-acetoxyethoxy)methylbromide with sodium azide afforded (2-acetoxyethoxy)methylazide 9. The heterocycles 6a,b were alkylated, separately, with propargyl bromide to obtain, regioselectively, 4-(methyl and benzyl)thio-1-(prop-2-ynyl)-1H-pyrazolo[3,4-d] pyrimidines 7a,b. These N1alkylated products were condensed with compound 9 via a 1,3-dipolar cycloaddition reaction to obtain, after separation and deprotection, 1,4-and 1,5-regioisomers 12a,b and 13a,b. The deprotected acyclic nucleosides 12a and 13a served as precursors for the preparation of 4-amino (14 and 15), 4-methylamino (16 and 17), 4-benzylamino (18 and 19), 4-methoxy (20 and 21) and 4-hydroxy (22 and 23) analogues. Compounds 7a,b and all deprotected acyclic nucleosides were evaluated for their inhibitory effects against the replication of HIV-1(IIIB) and HIV-2(ROD) in MT-4 cells and for their anti-tumor activity. No marked activity was found. However, initial evaluation of 6a,b, 7a,b, 12a,b, 13a,b and 14-23 showed that compound 7b has marked activity against M. tuberculosis.
