- Deuterated acetylene derivatives, its pharmaceutical composition and application
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The invention discloses a deuterated acetylenic derivative, a pharmaceutical composition and application thereof. The deuterated acetylenic derivative comprises one or more of the deuterated acetylenic derivative (I) with curative effective dose, pharmace
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Paragraph 0169; 0171; 0174; 0175
(2018/11/22)
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- Synthesis of 5-bromo-6-methyl imidazopyrazine, 5-bromo and 5-chloro-6-methyl imidazopyridine using electron density surface maps to guide synthetic strategy
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Small heteroaromatic rings are valuable monomers in drug discovery that can enable rapid access to novel and desirable chemical space. Installation of a synthetic handle on a heteroaromatic core may be difficult if steric and electronic factors are not in alignment with the desired transformation. Described are practical routes for the construction of 5-bromo-6-methyl imidazopyrazine (1) as well as 5-bromo and 5-chloro-6-methyl imidazopyridines (2a and 2b), which were developed using electron density surface maps encoded with ionization potential to guide synthetic strategy.
- Harris, Anthony R.,Nason, Deane M.,Collantes, Elizabeth M.,Xu, Wenjian,Chi, Yushi,Wang, Zhihan,Zhang, Bingzhi,Zhang, Qingjian,Gray, David L.,Davoren, Jennifer E.
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scheme or table
p. 9063 - 9066
(2011/12/03)
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- 5,6,7,8-TETRAHYDROIMIDAZO[1,2-A]PYRAZINE DERIVATIVES AS P2X7 MODULATORS
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The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2/s
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Page/Page column 50
(2010/11/17)
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- Imidazo-pyrazine derivatives as ligands for gaba receptors
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A class of imidazo[1,2-α]pyrazine analogues substituted in the 3-position by a substituted phenyl ring, being selective ligands for GABAA receptors which interact more favourably with the α2 and/or α3 subunit than with the α1 subunit, are accordingly of b
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Page/Page column 9
(2008/06/13)
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- Synthesis of imidazo[1,2-a]pyrazine derivatives with uterine-relaxing, antibronchospastic, and cardiac-stimulating properties
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A series of imidazo[1,2-a]pyrazine derivatives was synthesized by condensation of α-halogenocarbonyl compounds and aminopyrazines. Various compounds resulted from competitive reactions or reagent isomerization and demonstrated in vitro uterine-relaxing and in vivo antibronchospastic activities. On isolated atria, 5-bromoimidazo[1,2-a]pyrazine showed positive chronotropic and inotropic properties; the latter was associated with an increase in the cyclic AMP tissue concentration. Potentiation of the isoproterenol positive inotropic effect of 5-bromoimidazo[1,2-a]pyrazine and the lack of blockade of the 5-bromoimidazo[1,2-a]pyrazine positive inotropic effect by propranolol suggested phosphodiesterase-inhibiting properties.
- Sablayrolles,Cros,Milhavet,Rechenq,Chapat,Boucard,Serrano,McNeill
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p. 206 - 212
(2007/10/02)
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