18672-04-3Relevant academic research and scientific papers
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 0298-0299, (2019/04/05)
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
PRMT5 INHIBITORS CONTAINING A DIHYDRO- OR TETRAHYDROISOQUINOLINE AND USES THEREOF
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Paragraph 00288, (2014/07/08)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5- mediated disorders are also described.
A novel organic electron donor derived from N-methylisatin
Sword, Ryan,O'Sullivan, Steven,Murphy, John A.
, p. 314 - 322 (2013/05/08)
We report the reactivity of an electron donor derived from N-methylisatin on reduction by sodium amalgam. Transfer of a clear supernatant solution to iodoarenes affords the products of two-electron reduction. Reductions of sulfones, activated arenesulfonamides, and Weinreb amides are also reported.
NOVEL AMIDE AND AMIDINE DERIVATIVES AND USES THEREOF
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Page/Page column 35, (2010/11/03)
The present invention relates to inhibitors of 11-β-hydroxysteroid dehydrogenase type 1 enzyme and their use in treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, central nervous system disorders, and diseases and conditions that are related to excessive glucocorticoids.
Stereospecific synthesis and bio-activity of novel β3-adrenoceptor agonists and inverse agonists
Perrone, Maria Grazia,Santandrea, Ernesto,Bleve, Laura,Vitale, Paola,Colabufo, Nicola Antonio,Jockers, Ralf,Milazzo, Ferdinando Maria,Sciarroni, Anna Floriana,Scilimati, Antonio
, p. 2473 - 2488 (2008/09/21)
Since it is widely distributed into the body, β3-adrenoceptor is becoming an attractive target for the treatment of several pathologies such as obesity, type 2 diabetes, metabolic syndrome, cachexia, overactive bladder, ulcero-inflammatory disorder of the gut, preterm labour, anxiety and depressive disorders, and heart failure. New compounds belonging to the class of arylethanolamines bearing one or two stereogenic centres were prepared in good yields as racemates and optically active forms. They were, then, evaluated for their intrinsic activity towards β3-adrenoceptor and their affinity for β1- and β2-adrenergic receptors. Stereochemical features were found to play a crucial role in determining the behaviour of such compounds. In particular, α-racemic, (αR)- and (αS)-2-{4-[2-(2-hydroxy-2-phenylethylamino)ethyl]phenoxy}-2- methylpropanoic acid, (α-rac, β-rac)-, (αR, βS)- and (αR, βR)- 2-{4-[2-(2-hydroxy-2-phenylethylamino)ethyl]phenoxy}propanoic acid were found to be endowed with β3-adrenoceptor agonistic activity. Whereas, (αS, βS)- and (αS, βR)-2-{4-[2-(2-hydroxy-2-phenylethylamino)ethyl]phenoxy}propanoic acid behaved as β3-adrenoceptor inverse agonists. Such compounds showed no affinity for β1- and β2-adrenergic receptor, respectively. Thus, resulting highly selective β3-adrenoceptor ligands.
One-pot reduction of aryl iodides using 4-DMAP methiodide salt
Garnier, Jean,Murphy, John A.,Zhou, Sheng-Ze,Turner, Andrew T.
scheme or table, p. 2127 - 2131 (2009/05/07)
An efficient one-pot procedure is described for the reduction of aryl iodides to aryl anions using a structurally simple bis-pyridinylidene electron donor, prepared in situ by treating 4-DMAP methiodide salt with base. The results show (i) that pyridinylidene carbenes can be easily used for intermolecular C-C bond formation, (ii) that bis-pyridinylidenes demonstrate superior robustness compared to electron-donor systems based on bis-imidazolylidenes, and (iii) that electron-donor strength is enhanced in the simplified DMAP-based donor. Deuterated analogues of this donor also provide mechanistic information on the source of protons when the aryl anions are quenched in situ. Georg Thieme Verlag Stuttgart.
Super-electron donors: Bis-pyridinylidene formation by base treatment of pyridinium salts
Murphy, John A.,Gamier, Jean,Park, Stuart R.,Schoenebeck, Franziska,Zhou, Sheng-Ze,Turner, Andrew T.
supporting information; experimental part, p. 1227 - 1230 (2009/04/06)
Deprotonation of bispyridinium salt 7b affords bispyridinylidene 10, a very powerful neutral organic two-electron donor [E1/2 (DMF) = -1.13 V vs Ag/AgCI/KCI (sat)], presumably via the pyridinylidene 8. Donor 10 reduces aryl iodides and bromides to aryl anions in excellent yield and also reductively cleaves selected phenylalkylsulfones very efficiently.
The generation of aryl anions by double electron transfer to aryl iodides from a neutral ground-state organic super-electron donor
Murphy, John A.,Zhou, Sheng-Ze,Thomson, Douglas W.,Schoenebeck, Franziska,Mahesh, Mohan,Park, Stuart R.,Tuttle, Tell,Berlouis, Leonard E. A.
, p. 5178 - 5183 (2008/03/27)
(Chemical Equation Presented) It takes two to cyclize: Aryl halides are reduced to aryl anions by double electron transfer from the neutral ground-state electron donor 1 (see scheme), as shown by the formation of a cyclic ketone (2). The reduced compound (3) is also formed. Calculations show that the loss of two electrons from 1 is both thermodynamically and kinetically viable and generates a more planar resonance-stabilized structure.
Amido compounds and their use as pharmaceuticals
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Page/Page column 43, (2010/02/15)
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
Copper(II)-catalyzed O-phenylation of tertiary alcohols with organobismuth(V) reagents
Ikegai, Kazuhiro,Fukumoto, Kentarou,Mukaiyama, Teruaki
, p. 612 - 613 (2007/10/03)
A new method for the Cu(OAc)2-catalyzed phenylation of tertiary alcohols under mild basic conditions is described. Triphenylbismuth(V) diacetate and tetraphenylbismuth reagents undergo cross-coupling reactions with α-hydroxycarbonyl compouds efficiently. For non-chelating tertiary alcohols, tetraphenylbismuth fluoride is found suitable as a phenyl donor. Copyright
