81561-66-2Relevant articles and documents
RORγ ANTAGONIST AND APPLICATION THEREOF IN MEDICINE
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Paragraph 00556, (2020/02/06)
Provided herein are compounds as RORγ antagonist having Formula (I). The compounds or pharmaceutical composition thereof can be used for regulating Retinoid-related orphan receptor gamma t (RORγt). Also provided herein are methods of preparation of the compounds and composition thereof, and uses thereof in treating or preventing RORγt mediated inflammation or autoimmune diseases in mammals, particularly humans.
DOPAMINE D3 RECEPTOR ANTAGONISTS HAVING A MORPHOLINE MOIETY
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Paragraph 0256, (2018/11/21)
The disclosure provides compounds of formula (I) or pharmaceutically acceptable salts thereof: The disclosure also provides processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them, and their use
NOVEL NON-SYSTEMIC TGR5 AGONISTS
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Page/Page column 79, (2018/02/28)
The present invention relates to tricyclic compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present tricyclic compounds are useful non-sytemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing tricyclic compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.
Synthesis, molecular modelling and CYP24A1 inhibitory activity of novel of (E)-N-(2-(1H-imidazol-1-yl)-2-(phenylethyl)-3/4-styrylbenzamides
Taban, Ismail M.,Zhu, Jinge,DeLuca, Hector F.,Simons, Claire
supporting information, p. 4076 - 4087 (2017/07/05)
CYP24A1 (25-hydroxyvitamin D-24-hydroxylase) is a useful enzyme target for a range of medical conditions including cancer, cardiovascular and autoimmune disease, which show elevated CYP24A1 levels and corresponding reduction of calcitriol (the biologically active form of vitamin D). A series of (E)-N-(2-(1H-imidazol-1-yl)-2-(phenylethyl)-3/4-styrylbenzamides have been synthesised using an efficient synthetic route and shown to be potent inhibitors of CYP24A1 (IC50 0.11–0.35?μM) compared with the standard ketoconazole. Molecular modelling using our CYP24A1 homology model showed the inhibitors to fill the hydrophobic binding site, forming key transition metal interaction between the imidazole nitrogen and the haem Fe3+ and multiple interactions with the active site amino acid residues.
Direct catalytic synthesis of unprotected 2-amino-1-phenylethanols from alkenes by using iron(II) phthalocyanine
Legnani, Luca,Morandi, Bill
supporting information, p. 2248 - 2251 (2016/02/18)
Aryl-substituted amino alcohols are privileged scaffolds in medicinal chemistry and natural products. Herein, we report that an exceptionally simple and inexpensive FeII complex efficiently catalyzes the direct transformation of simple alkenes into unprotected amino alcohols in good yield and perfect regioselectivity. This new catalytic method was applied in the expedient synthesis of bioactive molecules and could be extended to aminoetherification.
Novel morpholine scaffolds as selective dopamine (DA) D3 receptor antagonists
Micheli, Fabrizio,Cremonesi, Susanna,Semeraro, Teresa,Tarsi, Luca,Tomelleri, Silvia,Cavanni, Paolo,Oliosi, Beatrice,Perdon, Elisabetta,Sava, Anna,Zonzini, Laura,Feriani, Aldo,Braggio, Simone,Heidbreder, Christian
, p. 1329 - 1332 (2016/02/23)
A new series of morpholine derivatives has been identified as selective DA D3 receptor antagonists; their in vitro profile and pharmacokinetic data are provided.
Catalyst development for organocatalytic hydrosilylation of aromatic ketones and ketimines
Malkov, Andrei V.,Stewart-Liddon, Angus J. P.,McGeoch, Grant D.,Ramirez-Lopez, Pedro,Kocovsky, Pavel
experimental part, p. 4864 - 4877 (2012/07/28)
A new family of Lewis basic 2-pyridyl oxazolines have been developed, which can act as efficient organocatalysts for the enantioselective reduction of prochiral aromatic ketones and ketimines with trichlorosilane, a readily available and inexpensive reagent. 1-Isoquinolyl oxazoline, derived from mandelic acid, was identified as the most efficient catalyst of the series, capable of delivering high enantioselectivities in the reduction of both ketones (up to 94% ee) and ketimines (up to 89% ee).
PYRIMDINE COMPOUNDS USEFUL AS KINASE INHIBITORS
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Page/Page column 45, (2010/11/30)
A compound of formula (I) or a salt or solvate thereof: Formula (1) compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such mono-anilino pyrimidine derivative
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Jarvest, Richard L.,Erskine, Symon G.,Forrest, Andrew K.,Fosberry, Andrew P.,Hibbs, Martin J.,Jones, Joanna J.,O'Hanlon, Peter J.,Sheppard, Robert J.,Worby, Angela
, p. 2305 - 2309 (2007/10/03)
High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.
