- Design and synthesis of a novel series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor
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We describe an efficient and convergent synthesis of a series of (1′S,2R,4′S)-3H-4′-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2′-bicyclo[2.2.2]octanes] displaying potency for the α7 nicotinic acetylcholine receptor (nAChR) and good selectivity vs. the re
- Cook, James,Zusi, F. Christopher,Hill, Matthew D.,Fang, Haiquan,Pearce, Bradley,Park, Hyunsoo,Gallagher, Lizbeth,McDonald, Ivar M.,Bristow, Linda,Macor, John E.,Olson, Richard E.
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Read Online
- Regioselective Radical Arene Amination for the Concise Synthesis ofortho-Phenylenediamines
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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.
- Gillespie, James E.,Morrill, Charlotte,Phipps, Robert J.
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supporting information
p. 9355 - 9360
(2021/07/19)
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- SUBSTITUTED BENZIMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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The invention provides substituted benzimidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
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Paragraph 00392
(2021/04/01)
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- CXCR4 INHIBITORS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 00364; 00430; 00431
(2018/04/11)
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- QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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There are disclosed a series of quinuclidines having the Formula (I). which bind to the nicotinic α7 receptor and may be useful for the treatment of disorders of the central nervous system.
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Page/Page column 61
(2016/06/01)
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- INHIBITORS OF HIF PROLYL HYDROXYLASE
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The present invention concerns compounds of formula I or pharmaceutically acceptable salts thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical carrier.
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Page/Page column 219
(2016/04/20)
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- PHENAZINE-BASED COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING THE SAME
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The present invention refers to including and compound phenacy relates to organic light emitting device. (by machine translation)
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Paragraph 0110-0112
(2016/10/08)
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- PRMT5 INHIBITORS AND USES THEREOF
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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
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Paragraph 00419
(2014/07/08)
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- Copolymer comprising anthracene and benzoselenadiazole, preparing method and uses thereof
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A copolymer comprising anthracene and benzoselenadiazole, preparing method and uses thereof are disclosed. The copolymer is represented by formula (I), wherein n is a natural number from 10 to 1000, a is 1 or 2, b is 0, 1 or 2, X, Y are O, S, Se, SO2, N—R4 or R5—Si—R6; R4, R5, R6 are selected from C1-C20 straight-chain, branched-chain or cyclo alkyl or alkoxy; R1, R2 are unsubstituted, monosubstituted or polysubstituted functional group Ar1, and said Ar1 is selected from hydrogen, halogen, cyano, substituted or unsubstituted C1-C40 straight-chain or branched-chain or cyclo alkyl, substituted or unsubstituted aryl or heteroaryl; R3, R7 are unsubstituted, monosubstituted or polysubstituted functional group Ar2, and said Ar2 is selected from hydrogen, cyano, substituted or unsubstituted C1-C40 straight-chain or branched-chain or cyclo alkyl, substituted or unsubstituted C1-C40 alkoxy, substituted or unsubstituted C6-C40 aryl, substituted or unsubstituted C6-C40 aralkyl, substituted or unsubstituted C6-C40 aryl alkoxy.
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Page/Page column
(2014/09/16)
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- L-shaped benzimidazole fluorophores: Synthesis, characterization and optical response to bases, acids and anions
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Nine L-shaped benzimidazole fluorophores have been synthesized, computationally evaluated and spectroscopically characterized. These "half-cruciform" fluorophores respond to bases, acids and anions through changes in fluorescence that vary from moderate t
- Lirag, Rio Carlo,Le, Ha T. M.,Miljanic, Ognjen S.
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p. 4304 - 4306
(2013/06/05)
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- SERINE/THREONINE PAK1 INHIBITORS
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Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
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Page/Page column 108
(2013/03/26)
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- Synthesis and physico-chemical properties in aqueous medium of all possible isomeric bromo analogues of benzo-1H-triazole, potential inhibitors of protein kinases
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In ongoing studies on the role of the individual bromine atoms of 4,5,6,7-tetrabromobenzotriazole (TBBt) in its relatively selective inhibition of protein kinase CK2α, we have prepared all the possible two mono-, four di-, and two tri-bromobenzotriazoles and determined their physicochemical properties in aqueous medium. They exhibited a general trend of a decrease in solubility with an increase in the number of bromines on the benzene ring, significantly modulated by the pattern of substitution. For a given number of attached bromines, this was directly related to the electronic effects resulting from different sites of substitution, leading to marked variations of pK a values for dissociation of the triazole proton. Experimental data (pKa, solubility) and ab initio calculations demonstrated that hydration of halogenated benzotriazoles is driven by a subtle balance of hydrophobic and polar interactions. The combination of QM-derived free energies for solvation and proton dissociations was found to be a reasonably good predictor of inhibitory activity of halogenated benzotriazoles vs CK2α. Since the pattern of halogenation of the benzene ring of benzotriazole has also been shown to be one of the determinants of inhibitory potency vs some viruses and viral enzymes, the present comprehensive description of their physicochemical properties should prove helpful in efforts to elucidate reaction mechanisms, including possible halogen bonding, and the search for more selective and potent inhibitors.
- Wa?sik, Romualda,Wińska, Patrycja,Poznański, Jaros?aw,Shugar, David
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p. 7259 - 7268
(2012/08/28)
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- PHENYLSULFONAMIDE-SUBSTITUTED, PYRAZOLO[1, 5-A]PYRIMIDINES, METHODS FOR PREPARATION AND USES THEREOF
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Phenylsulfonamide substituted, pyrazolo[1,5-a]pyrimidines are described. The compounds of the invention selectively inhibit Raf kinase activity and are useful for treating disorders associated with Raf kinases. Formula (I)
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Page/Page column 31-32
(2009/10/22)
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- BRIDGED, BICYCLIC HETEROCYCLIC OR SPIRO BICYCLIC HETEROCYCLIC DERIVATIVES OF PYRAZOLO[1,5-A]PYRIMIDINES, METHODS FOR PREPARATION AND USES THEREOF
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Compounds of formula A: Formula (1) pharmaceutically acceptable salts thereof are described, which selectively inhibit Raf kinase activity and are useful for treating disorders mediated by Raf kinases.
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Page/Page column 95-96
(2009/10/21)
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- ARYLSULFONYLNAPHTHALENE DERIVATIVES AS 5HT2A ANTAGONISTS
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Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.
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Page/Page column 41
(2008/06/13)
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- DIARYLSULFONES AS 5-HT2A ANTAGONISTS
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Compounds of formula (I) are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
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Page/Page column 76
(2008/06/13)
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- ARYLSULFONYL BENZYL ETHERS AS 5-HT2A ANTAGONISTS
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Compounds of formula (I) are potent and selective antagonists of the 5-HT2A receptor, and hence are useful in treatment of various CNS disorders.
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Page/Page column 23
(2010/11/23)
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