- Purine compound containing bicyclic group, and preparation method thereof
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The invention provides a purine compound containing a bicyclic group which is shown as a formula (I) and a formula (II) and a pharmaceutically acceptable salt, and a preparation method thereof. The compound is an inhibitor of histone methyltransferase DOT1L, and can be used for treating diseases caused by the abnormity of enzyme activity, such as tumor.
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Paragraph 0123; 0129; 0130
(2019/10/01)
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- Triazolopyridine ethers as potent, orally active mGlu2positive allosteric modulators for treating schizophrenia
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Triazolopyridine ethers with mGlu2positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted in the discovery of a potent, selective, and brain penetrant lead molecule BMT-133218 ((+)-7m). After oral administration at 10 mg/kg, BMT-133218 demonstrated full reversal of PCP-stimulated locomotor activity and prevented MK-801-induced working memory deficits in separate mouse models. Also, reversal of impairments in executive function were observed in rat set-shifting studies at 3 and 10 mg/kg (p.o.). Extensive plasma protein binding as the result of high lipophilicity likely limited activity at lower doses. Optimized triazolopyridine ethers offer utility as mGlu2PAMs for the treatment of schizophrenia and merit further preclinical investigation.
- Higgins, Mendi A.,Marcin, Lawrence R.,Christopher Zusi,Gentles, Robert,Ding, Min,Pearce, Bradley C.,Easton, Amy,Kostich, Walter A.,Seager, Matthew A.,Bourin, Clotilde,Bristow, Linda J.,Johnson, Kim A.,Miller, Regina,Hogan, John,Whiterock, Valerie,Gulianello, Michael,Ferrante, Meredith,Huang, Yanling,Hendricson, Adam,Alt, Andrew,Macor, John E.,Bronson, Joanne J.
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p. 496 - 513
(2016/12/30)
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- Br?nsted Acid-Catalyzed Intramolecular Hydroarylation of β-Benzylstyrenes
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Using triphenylmethylium tetrakis(pentafluorophenyl)borate as a convenient Br?nsted acid precatalyst, β-(α,α-dimethylbenzyl)styrenes are shown to cyclize efficiently to afford a variety of new indanes that possess a benzylic quaternary center. The geminal dimethyl-containing quaternary center is proposed to be necessary to arm the substrate for cyclization through steric biasing.
- Cai, Xiao,Keshavarz, Amir,Omaque, Justin D.,Stokes, Benjamin J.
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supporting information
p. 2626 - 2629
(2017/05/24)
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- PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION
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The disclosure generally relates to compounds of formula I, II, III and IV, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.
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Paragraph 0114
(2015/09/22)
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- TRIAZOLOPYRIDINE ETHER DERIVATIVES AND THEIR USE IN NEUROLOGICAL AND PYSCHIATRIC DISORDERS
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The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
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Page/Page column 25
(2015/04/15)
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- SUBSTITUTED PURINE AND 7 - DEAZAPURINE COMPOUNDS AS MODULATORS OF EPIGENETIC ENZYMES
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The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOTl -mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
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Page/Page column 304
(2012/06/16)
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- INDOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
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Compound of formula (I) are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
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Page/Page column 50
(2010/09/17)
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- HETEROSUBSTITUTED PYRIDINE DERIVATIVES AS PDE 4 INHIBITORS
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The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE 4)
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