136709-51-8Relevant academic research and scientific papers
TRICYCLIC DEGRADERS OF IKAROS AND AIOLOS
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Page/Page column 490-491, (2020/10/21)
Tricyclic cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway for therapeutic applications are described.
FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0360; 0361, (2018/06/26)
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.
FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0358; 0360; 0361, (2014/11/13)
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands
Jenkins,Wadsworth,Bromidge,Orlek,Wyman,Riley,Hawkins
, p. 2392 - 2406 (2007/10/02)
The effect of variation of the 1-azabicyclic substituent on the novel 1,2,3-triazol-4-yl-, 1,2,4-triazol-1-yl-, tetrazol-5-yl-, and tetrazol-2-yl- based muscarinic receptor ligands has been studied, and the exo- azabicyclic[2.2.1]hept-3-yl substituent was found to give the most potent and efficacious compounds. In addition, variation of the second substituent on 1,2,4-triazol-1-yl- and tetrazol-2-yl-based muscarinic receptor ligands has yielded a series of novel compounds with high potencies and efficacies, ranging from full agonists to antagonists. Small lipophilic electron withdrawing substituents give potent but low efficacy compounds, while small polar electron donating substituents give potent and efficacious compounds. The activity of these compounds is described in terms of a model of the receptor involving lipophilic and hydrogen bonding interactions. These compounds provide muscarinic ligands with high potency and a range of efficacies suitable for testing as candidate drugs in the treatment of Alzheimer's disease.
