80019-71-2Relevant academic research and scientific papers
Asymmetric Induction and Enantiodivergence in Catalytic Radical C-H Amination via Enantiodifferentiative H-Atom Abstraction and Stereoretentive Radical Substitution
Lang, Kai,Torker, Sebastian,Wojtas, Lukasz,Zhang, X. Peter
supporting information, p. 12388 - 12396 (2019/08/20)
Control of enantioselectivity remains a major challenge in radical chemistry. The emergence of metalloradical catalysis (MRC) offers a conceptually new strategy for addressing this and other outstanding issues. Through the employment of D2-symmetric chiral amidoporphyrins as the supporting ligands, Co(II)-based MRC has enabled the development of new catalytic systems for asymmetric radical transformations with a unique profile of reactivity and selectivity. With the support of new-generation HuPhyrin chiral ligands whose cavity environment can be fine-tuned, the Co-centered d-radicals enable to address challenging issues that require exquisite control of fundamental radical processes. As showcased with asymmetric 1,5-C-H amination of sulfamoyl azides, the enantiocontrol of which has proven difficult, the judicious use of HuPhyrin ligand by tuning the bridge length and other remote nonchiral elements allows for controlling both the degree and sense of asymmetric induction in a systematic manner. This effort leads to successful development of new Co(II)-based catalytic systems that are highly effective for enantiodivergent radical 1,5-C-H amination, producing both enantiomers of the strained five-membered cyclic sulfamides with excellent enantioselectivities. Detailed deuterium-labeling studies, together with DFT computation, have revealed an unprecedented mode of asymmetric induction that consists of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution.
BICYCLIC HETEROCYCLE DERIVATIVES AS BROMODOMAIN INHIBITORS
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Page/Page column 35; 36, (2017/01/23)
The invention relates to novel bicyclic heterocycle derivatives of formula (I) wherein Cy1,Cy2, R1,R2 and L have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are usefulas bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.
HISTONE DEMETHYLASE INHIBITORS
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Paragraph 00145; 00146, (2017/09/08)
This disclosure relates to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
N-(1-HYDROXY-3-(PYRROLIDINYL)PROPAN-2-YL)PYRROLIDINE-3-CARBOXAMIDE DERIVATIVES AS GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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Paragraph 000455; 000470, (2015/05/19)
Described herein are compounds of Formula I, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and compounds I for use to treat or prevent diseases or conditions associated with the enzyme glucosylceramide synthase (GCS).
SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Paragraph 0246; 0247, (2014/09/30)
Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
Design, synthesis, and biological evaluation of indole derivatives as novel nociceptin/orphanin FQ (N/OFQ) receptor antagonists
Sugimoto, Yuichi,Shimizu, Atsushi,Kato, Tetsuya,Satoh, Atsushi,Ozaki, Satoshi,Ohta, Hisashi,Okamoto, Osamu
, p. 3569 - 3573 (2007/10/03)
A novel series of 2-(1,2,4-oxadiazol-5-yl)-1H-indole derivatives as nociceptin/orphanin FQ (N/OFQ) receptor antagonists was discovered. Systematic modification of our original lead by changing the pendant functional groups, linker, heterocyclic core, and
METHODS OF TREATING OR AMELIORATING THE SYMPTOMS OF COMMON COLD OR ALLERGIC RHINITIS WITH SEROTONIN 5-HT1F
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, (2008/06/13)
This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT 1F agonist.
Use of a serotonin 5-HTlf agonist in the manufacture of a medicament for treating or ameliorating the symptoms of common cold or allergic rhinitis
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, (2008/06/13)
This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT1F agonist.
Use of serotonin 5-HT1F agonists for the prevention of migraine
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, (2008/06/13)
This invention provides methods for the prevention of migraine which comprises administering to a mammal in need thereof a serotonin 5-HT1F agonist.
6-SUBSTITUTED-1,2,3,4-TETRAHYDRO-9H-CARBAZOLES AND 7-SUBSTITUTED-10H-CYCLOHEPTA [7,6-B]INDOLES: NEW 5-HT1F AGONISTS
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, (2008/06/13)
This invention provides novel 6-substituted-1,2,3,4-tetrahydro-9H-carbazoles and 7-substituted-10H-cyclohepta[7,6-b]indoles. These compounds are 5-HT 1F agonists which are useful for the treatment of migraine and associated disorders.
