60260-49-3Relevant academic research and scientific papers
Regioselective Radical Arene Amination for the Concise Synthesis ofortho-Phenylenediamines
Gillespie, James E.,Morrill, Charlotte,Phipps, Robert J.
, p. 9355 - 9360 (2021/07/19)
The formation of arene C-N bonds directly from C-H bonds is of great importance and there has been rapid recent development of methods for achieving this through radical mechanisms, often involving reactiveN-centered radicals. A major challenge associated with these advances is that of regiocontrol, with mixtures of regioisomeric products obtained in most protocols, limiting broader utility. We have designed a system that utilizes attractive noncovalent interactions between an anionic substrate and an incoming radical cation in order to guide the latter to the areneorthoposition. The anionic substrate takes the form of a sulfamate-protected aniline and telescoped cleavage of the sulfamate group after amination leads directly toortho-phenylenediamines, key building blocks for a range of medicinally relevant diazoles. Our method can deliver both free amines and monoalkyl amines allowing access to unsymmetrical, selectively monoalkylated benzimidazoles and benzotriazoles. As well as providing concise access to valuableortho-phenylenediamines, this work demonstrates the potential for utilizing noncovalent interactions to control positional selectivity in radical reactions.
N-SUBSTITUTED-3-TRICYCLYL PIPERIDINE DERIVATIVES AS ANTICANCER AND NEUROPROTECTIVE AGENTS
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Paragraph 00116-00117, (2021/07/31)
A genus of N-substituted-3-tricyclyl piperidine derivatives is disclosed. The compounds are of the following genus: The compounds induce FOXO1 transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
3-DIARYLMETHYLENES AND USES THEREOF
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Paragraph 0001, (2021/09/26)
3-Diarylmethylenes are disclosed. The compounds activate PP2A, suppress oncogenic kinase signaling, and negatively regulate MYC and MYCN in cancer. The compounds also induce FOXO transcription factor translocation to the nucleus by modulating PP2A and, as a consequence, exhibit anti-proliferative effects. They are useful in the treatment of a variety of disorders, including as a monotherapy in cancer treatment, or used in combination with other drugs to restore sensitivity to chemotherapy where resistance has developed.
PROTEIN KINASE MKK4 INHIBITORS FOR PROMOTING LIVER REGENERATION OR REDUCING OR PREVENTING HEPATOCYTE DEATH
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Page/Page column 88; 89, (2019/08/26)
The invention relates to pyrazolo-pyridine compounds which inhibit mitogen-activated protein kinase kinase 4 (MKK4) and in particular, selectively inhibit MKK4 over protein kinases JNK1 and MKK7. The compounds are useful for promoting liver regeneration or reducing or preventing hepatocyte death. They are further useful for treating osteoarthritis or rheumatoid arthritis, or CNS-related diseases.
MORPHINAN DERIVATIVE AND MEDICAL USAGE THEREOF
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Paragraph 0101, (2018/09/20)
The purpose of the present invention is to provide a compound useful as a prophylactic or therapeutic agent for various diseases and symptoms related to orexin receptors, and a medical usage of the same. The present invention provides a morphinan derivati
HETEROCYCLIC INHIBITORS OF THE SODIUM CHANNEL
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Page/Page column 133, (2015/09/28)
The invention relates to compounds useful in treating conditions associated with voltage-gated ion channel function, particularly conditions associated with sodium channel activity. More specifically, the invention concerns heterocyclic compounds (e.g., compounds according to any of Formulas (l)-(ll l) or Compounds (1 )-(65) of Table 1 ) that are that are useful in treatment of conditions such as epilepsy, cancer, pain, migraine, Parkinson's Disease, mood disorders, schizophrenia, psychosis, tinnitus, amyotropic lateral sclerosis, glaucoma, ischaemia, spasticity disorders, obsessive compulsive disorder, restless leg syndrome and Tourette syndrome.
ANTIBACTERIAL THIAZOLECARBOXYLIC ACIDS
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Page/Page column 106; 107, (2015/01/09)
Compounds of general formula (I), wherein R1, R11, Y, R2, n and A are as defined herein are useful as inhibitors or metallo-β-lactamase (MBL) enzymes and can be used for reducing or removing antibiotic resistance in bacteria.
Directed heterodimerization: Stereocontrolled assembly via solvent-caged unsymmetrical diazene fragmentation
Movassaghi, Mohammad,Ahmad, Omar K.,Lathrop, Stephen P.
supporting information; experimental part, p. 13002 - 13005 (2011/10/12)
A general strategy for the directed and stereocontrolled assembly of carbon-carbon linked heterodimeric hexahydropyrroloindoles is described. The stepwise union of complex amines in the form of mixed diazenes followed by photoexpulsion of dinitrogen in a
AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS
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Page/Page column 68, (2010/02/13)
The present invention provides a novel class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
