- Tetrabutylammonium fluoride-assisted rapid N9-alkylation on purine ring: Application to combinatorial reactions in microtiter plates for the discovery of potent sulfotransferase inhibitors in situ
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Tremendous efforts have been invested in the synthesis of purine libraries due to their importance in targeting various enzymes involved in different diseases and cellular processes. The synthesis of N9-alkylated purine scaffolds relied mostly
- Brik, Ashraf,Wu, Chung-Yi,Best, Michael D.,Wong, Chi-Huey
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Read Online
- Regioselective alkylation reaction of purines under microwave irradiation
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The alkylation of purines which is generally carried out after anion formation by treatment with a base and alkyl halide is complicated and in the best cases, mixtures of N-alkylated compounds are obtained. Purine derivatives can be acquired from alkylati
- Vinuesa, Arturo,Vi?as, Miquel,Jahani, Daniel,Ginard, Jaume,Mur, Nuria,Pujol, Maria Dolors
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p. 597 - 602
(2021/12/22)
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- HYPOXANTHINE COMPOUND
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PROBLEM TO BE SOLVED: To provide a novel compound having an inhibitory action of prolyl hydroxylase (PHDs) and useful as a therapeutic agent of an inflammatory bowel disease such as ulcerative colitis. SOLUTION: The present invention relates to a hypoxanthine compound represented by the following formula (I) or a pharmacologically acceptable salt thereof. The compound of the present invention or its pharmaceutically acceptable salt has an inhibitory effect of prolyl hydroxylase and is useful as a therapeutic agent for inflammatory bowel disease such as ulcerative colitis. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
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Paragraph 0216
(2021/07/17)
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- SUBSTITUTED BICYCLIC PYRIMIDINE-BASED COMPOUNDS AND COMPOSITIONS AND USES THEREOF
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Novel C-2-substituted bicyclic compounds of Formula I have been prepared and found to be useful as potent inhibitors of hGGPPS by inhibiting geranylgeranylation of proteins and inhibiting the biosynthesis of GGPP. The application is directed to these compounds, to compositions comprising these compounds, and to their use, in particular as medicaments for use in the treatment of cancer and other conditions which are treatable by inhibiting human geranylgeranylation pyrophosphate hGGPPS activity.
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Paragraph 00231; 00232
(2018/08/20)
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- Direct, Regioselective N-Alkylation of 1,3-Azoles
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Regioselective N-alkylation of 1,3-azoles is a valuable transformation. Organomagnesium reagents were discovered to be competent bases to affect regioselective alkylation of various 1,3-azoles. Counterintuitively, substitution selectively occurred at the more sterically hindered nitrogen atom. Numerous examples are provided, on varying 1,3-azole scaffolds, with yields ranging from 25 to 95%.
- Chen, Shuai,Graceffa, Russell F.,Boezio, Alessandro A.
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supporting information
p. 16 - 19
(2016/01/15)
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- COMPOUNDS FOR IMPROVING MRNA SPLICING
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Provided herein are compounds useful for improving mRNA splicing in a cell. Exemplary compounds provided herein are useful for improving mRNA splicing in genes comprising at least one exon ending in the nucleotide sequence CAA. Methods for preparing the compounds and methods of treating diseases of the central nervous system are also provided.
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Page/Page column 222; 223
(2016/08/10)
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- HETEROCYCLIC HYDROXAMIC ACIDS AS PROTEIN DEACETYLASE INHIBITORS AND DUAL PROTEIN DEACETYLASE-PROTEIN KINASE INHIBITORS AND METHODS OF USE THEREOF
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The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mpsl kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mpsl k
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Paragraph 00425; 00426
(2016/04/26)
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- A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors
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A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines also show potent mTOR inhibition with selectivity toward both PI3α and δ kinases. The most potent compound synthesized is pyrazolo[4,3-d]pyrimidine 21c. Compound 21c shows a Ki of 2 nM against mTOR inhibition, remarkable selectivity (>2900×) over PI3 kinases, and excellent potency in cell-based assays.
- Lee, Wendy,Ortwine, Daniel F.,Bergeron, Philippe,Lau, Kevin,Lin, Lichuan,Malek, Shiva,Nonomiya, Jim,Pei, Zhonghua,Robarge, Kirk D.,Schmidt, Stephen,Sideris, Steve,Lyssikatos, Joseph P.
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p. 5097 - 5104
(2013/09/12)
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- N-9 SUBSTITUTED PURINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4 and D have the meaning described herein. The present invention also relates to pharmac
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Page/Page column 25
(2011/04/25)
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- SUBSTITUTED PURINYL-PYRAZOL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
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This invention relates to novel substituted purinyl-pyrazol derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of disea
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Page/Page column 6-7
(2011/10/19)
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- N-7 SUBSTITUTED PURINE AND PYRAZOLOPYRIMINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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The present invention relates to compounds of Formula I: wherein R1, R2, R3, A1, A2, A3, A4, Y1 and Y2 and D have the meaning described herein. The present invention also relates to pharmaceutical compositions comprising such compounds and therapeutic uses thereof.
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Page/Page column 29
(2011/04/25)
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- SUBSTITUTED PURINYL-PYRAZOL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
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This invention relates to novel substituted purinyl-pyrazol derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of disea
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Page/Page column 15
(2010/04/27)
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- SUBSTITUTED PURINYL-PYRAZOL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
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This invention relates to novel substituted purinyl-pyrazol derivatives (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
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Page/Page column 15
(2010/04/27)
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- PURINYL DERIVATIVES AND THEIR USE AS POTASSIUM CHANNEL MODULATORS
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This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
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Page/Page column 22
(2008/12/04)
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- HIV REPLICATION INHIBITING PURINE DERIVATIVES
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The present invention relates to the use of a compound of formula (I) for the manufacture of a medicament for the prevention or the treatment of HIV infection wherein the compound of formula (I) is a compound of formula (I) a N-oxide, a pharmaceutically a
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Page/Page column 58
(2010/02/11)
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- Products of the reaction of 2-chloro-6-thio-7-methylpurine with amines
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Treatment of 2-chloro-6-thio-7-methylpurine with aniline, piperidine, or morpholine with heating in DMF gives 2-phenylamino(piperidino or morpholino)-6-thio-7-methylpurine. The scheme for the formation of the side products 2.6-dithio- and 2,6-dipiperidino-7-methylpurine is discussed.
- Kochergin,Aleksandrova,Korsunskii
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