283-38-5Relevant articles and documents
Microwave-assisted beckmann rearrangement: Convenient synthesis of 1,3-diaza-bicyclo[3.2.2]nonane
Curtis, Michael P.,Bunnelle, William H.,Pagano, Thomas G.,Gopalakrishnan, Murali,Faghih, Ramin
, p. 321 - 326 (2006)
Small heterocyclic amines such as 1,3-diaza-bicyclo[3.2.2]nonane are known to be key components of biologically active molecules. A convenient synthesis of this compound utilizing a key Beckmann rearrangement of (Z)-1-aza-bicyclo[2.2. 2]octan-3-one oxime (6) with conc. H2SO4 under microwave irradiation was achieved. The desired compound (1) was obtained in 20% yield overall. Copyright Taylor & Francis LLC.
Structure-based design of highly selective 2,4,5-trisubstituted pyrimidine CDK9 inhibitors as anti-cancer agents
Shao, Hao,Foley, David W.,Huang, Shiliang,Abbas, Abdullahi Y.,Lam, Frankie,Gershkovich, Pavel,Bradshaw, Tracey D.,Pepper, Chris,Fischer, Peter M.,Wang, Shudong
supporting information, (2021/02/16)
Cyclin-dependent kinases (CDKs) are a family of Ser/Thr kinases involved in cell cycle and transcriptional regulation. CDK9 regulates transcriptional elongation and this unique property has made it a potential target for several diseases. Due to the conserved ATP binding site, designing selective CDK9 inhibitors has been challenging. Here we report our continued efforts in the optimization of 2,4,5-tri-substituted pyrimidine compounds as potent and selective CDK9 inhibitors. The most selective compound 30m was >100-fold selective for CDK9 over CDK1 and CDK2. These compounds showed broad anti-proliferative activities in various solid tumour cell lines and patient-derived chronic lymphocytic leukaemia (CLL) cells. Decreased phosphorylation of the carboxyl terminal domain (CTD) of RNAPII at Ser-2 and down-regulation of anti-apoptotic protein Mcl-1 were confirmed in both the ovarian cancer model A2780 and patient-derived CLL cells.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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Page/Page column 124; 125, (2015/06/25)
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy.
Glucosylceramide synthase inhibitors
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Page/Page column 51, (2015/09/28)
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.
GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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Page/Page column 167, (2014/04/03)
The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, cystic disease and for the treatment of cancer.
1,4-DIAZABICYCLO[3.2.2]NONANES AS NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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Page/Page column 32, (2013/03/26)
The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using
LABELLED AND UN-LABELLED METHYL-PYRROLYL-OXADIAZOLYL-DIAZABICYCLONONANE DERIVATIVES AND THEIR MEDICAL USE
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Page/Page column 10, (2012/11/06)
The present invention relates to certain labelled or un-labelled pyrrolyl-oxadizolyl-diazabicyclononane derivatives and their medical use. Furthermore, the present invention relates to the use of said derivatives in their labelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).
DIAZABICYCLONONYL OXADIAZOLE COMPOUNDS AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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Page/Page column 14, (2011/07/07)
This invention relates to diazabicyclononyl oxadiazolyl derivatives, which are found to-be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. Ar1 represents a pyrrolyl group, optionally substituted with alkyl or halo-alkyl.
NOVEL DIAZA-BICYCLONONYL-PHENYL DERIVATIVES AND THEIR MEDICAL USE
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Page/Page column 17, (2010/06/20)
This invention relates to novel diazabicyclononyl-phenyl derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulator
N-OXIDES OF DIAZABICYCLONONYL PYRIMIDINE DERIVATIVES AND THEIR MEDICAL USE
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Page/Page column 16, (2010/08/08)
This invention relates to novel N-oxides of certain diazabicyclononyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine