- HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Compounds of formula I' and formula II' and their pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity for the treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity.
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Paragraph 00625
(2016/04/26)
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- 2-(Substituted ethynyl)quinoline Derivatives as mGLUr5 Antagonists
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Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor
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Paragraph 0085-0086
(2014/08/06)
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- Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain
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We described here the synthesis and biological evaluation of mGluR5 antagonists containing a quinoline ring structure. Using intracellular calcium mobilization assay (FDSS assay), we identified compound 5n, showing high inhibitory activity against mGluR5. In addition, it was found that compound 5n has excellent stability profile. Finally, this compound exhibited favorable analgesic effects in spinal nerve ligation model of neuropathic pain, which is comparable to gabapentin.
- Son, Myung-Hee,Kim, Ji Young,Lim, Eun Jeong,Baek, Du-Jong,Choi, Kihang,Lee, Jae Kyun,Pae, Ae Nim,Min, Sun-Joon,Cho, Yong Seo
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supporting information
p. 1472 - 1476
(2013/03/28)
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- Molecular recognition via triplex formation of mixed purine/pyrimidine DNA sequences using oligoTRIPs
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Stable DNA triple-helical structures are normally restricted to homopurine sequences. We have described a system of four heterocyclic bases (TRIPsides) that, when incorporated into oligomers (oligoTRIPs), can recognize and bind in the major groove to any
- Li, Jian-Sen,Chen, Fa-Xian,Shikiya, Ronald,Marky, Luis A.,Gold, Barry
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p. 12657 - 12665
(2007/10/03)
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- Synthesis of a fluorine-18-labelled derivative of 6-nitroquipazine, as a radioligand for the in vivo serotonin transporter imaging with PET.
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Considerable efforts have been engaged in the design, synthesis and pharmacological characterization of radioligands for imaging the serotonin transporter, based on its implication in several neuropsychiatric diseases, such as depression, anxiety and schizophrenia. In the 5-halo-6-nitroquipazine series, the fluoro derivative has been designed for positron emission tomography (PET). The corresponding 5-iodo-, 5-bromo- and 5-chloro N-Boc-protected quipazines as labelling precursors, as well as 5-fluoro-6-nitroquipazine as a reference compound have been synthesized. 5-[(18)F]Fluoro-6-nitroquipazine has been radiolabelled with fluorine-18 (positron-emitting isotope, 109.8 min half-life) by nucleophilic aromatic substitution from the corresponding N-Boc protected 5-bromo- and 5-chloro-precursors using K[(18)F]F-K(222) complex in DMSO by conventional heating (145 degrees C, 2 min) or microwave activation (50 W, 30-45 s), followed by removal of the protective group with TFA. Typically, 15-25 mCi (5.5-9.2 GBq) of 5-[(18)F]fluoro-6-nitroquipazine (1-2 Ci/micromol or 37-72 GBq/micromol) could be obtained in 70-80 min starting from a 550-650 mCi (20.3-24.0 GBq) aliquot of a cyclotron [(18)F]F(-) production batch (2.7-3.8% non decay-corrected yield based on the starting [(18)F]fluoride). Ex vivo studies (biodistribution in rat), as well as PET imaging (in monkey) demonstrated that 5-[(18)F]fluoro-6-nitroquipazine ([(18)F]-1d) readily crossed the blood brain barrier and accumulated in the regions rich in 5-HT transporter (frontal- and posterial cortex, striata). However, the low accumulation of the tracer in the thalamus (rat and monkey) as well as the comparable displacement of the tracer observed with both citalopram, a -HT re-uptake inhibitor and maprotiline, a norepinephrine re-uptake inhibitor (rat), indicate that 5-[(18)F]fluoro-6-nitroquipazine ([(18)F]-1d) does not have the suggested potential for PET imaging of the serotin transporter (SERT).
- Karramkam, Mylene,Dolle, Frederic,Valette, Heric,Besret, Laurent,Bramoulle, Yann,Hinnen, Francoise,Vaufrey, Francoise,Franklin, Carine,Bourg, Sebastien,Coulon, Christine,Ottaviani, Michele,Delaforge, Marcel,Loc'h, Christian,Bottlaender, Michel,Crouzel, Christian
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p. 2611 - 2623
(2007/10/03)
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- II. Synthesis and biological evaluation of some bioisosteres and congeners of the antitumor agent, 2-{4-[(7-chloro-2-quinoxalinyl)oxylphenoxy}propionic acid (XK469)
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XK469 (1) is among the most highly and broadly active antitumor agents to have been evaluated in our laboratories. Subsequent developmental studies led to the entry of (R)-(+) 1 (NSC 698215) into phase 1 clinical trials (NIH UO1-CA62487). The antitumor me
- Hazeldine, Stuart T.,Polin, Lisa,Kushner, Juiwanna,White, Kathryn,Bouregeois, Nicole M.,Crantz, Brianna,Palomino, Eduardo,Corbett, Thomas H.,Horwitz, Jerome P.
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p. 3130 - 3137
(2007/10/03)
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