- AROMATIC HETEROCYCLIC COMPOUND WITH KINASE INHIBITORY ACTIVITY
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Provided are a JAK kinase inhibitor, preparation and use thereof. In particular, provided is a compound of Formula I, wherein each group is as described in the specification. The compound has an excellent JAK inhibitory activity, and therefore can be used to prepare pharmaceutical compositions for the treatment of cancer and other diseases related to JAK activity.
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Paragraph 0207-0209
(2021/07/29)
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- Synthesis and preliminary pharmacological evaluation of 4′-arylalkyl analogues of clozapine. II. Effect of the nature and length of the linker
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We report the synthesis of a second generation of tricyclic analogues of clozapine, investigating the length and nature of the chain between an ionizable nitrogen atom at physiological pH and the introduced aryl moiety. The chemistry, structural characterization, and pharmacological evaluation of this series of 4′-arylalkyl analogues of clozapine are described. Preliminary findings on the effects on activity of the nature and length of the linker, degree of unsaturation, and type of aryl moiety on blockade of dopamine D4 and serotonin 5-HT2A receptors are discussed and animal behavioural data for key compounds presented.
- Capuano, Ben,Crosby, Ian T.,Lloyd, Edward J.,Podloucka, Anna,Taylor, David A.
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p. 875 - 886
(2007/10/03)
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- Synthesis and psychoanaleptic properties of new compounds structurally related to diphenhydramine
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A new series of benzhydryloxyalkylpiperazines carrying a trivalent function has been synthesized and studied for its effects on the central nervous system. Most of the compounds exhibit unexpected nonamphetaminic psychoanaleptic properties. The structure-
- Buzas,Champagnac,Dehnel,Lavielle,Pommier
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p. 149 - 153
(2007/10/02)
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