- Cu(I)/sucrose-catalyzed hydroxylation of arenes in water: The dual role of sucrose
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A protocol for the hydroxylation of aryl halides catalyzed by copper(I) and sucrose in neat water has been developed. The dual role of sucrose, the reaction pathway, and the high selectivity for hydroxylation were investigated using a combination of experimental and theoretical techniques. This journal is
- Murata, Shigeo,Takagi, Mio,Takita, Ryo,Watanabe, Ayako,Watanabe, Kohei
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supporting information
p. 7827 - 7831
(2020/11/02)
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- AMINO-ISO-INDOLE, AMINO-AZA-ISO-INDOLE, AMINO-DIHYDROISOQUINOLINE AND AMINO-BENZOXAZINE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer?s disease (AD) and related conditions. In one embodiment, t
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Page/Page column 57
(2012/02/15)
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- SPIRO-AMINO-IMIDAZOLONE AND SPIRO-AMINO-DIHYDRO-PYRIMIDINONE COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I), wherein variables A1, A3, A4, A5, A6/su
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Page/Page column 64-65
(2012/06/15)
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- SPIRO-AMINO-IMIDAZO-FUSED HETEROCYCLIC COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined here
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Page/Page column 57-58
(2012/09/10)
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- 5-AMINO-OXAZEPINE AND 5-AMINO-THIAZEPANE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE
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The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula (I); wherein variables A1, A3, A4, A5, A6, As, R2, R7, X and Y of Formula (I) are defined here
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Page/Page column 69
(2012/08/28)
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- CHEMICAL COMPOUNDS
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This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
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Page/Page column 68-69
(2010/11/08)
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- Efficient synthesis of halohydroxypyridines by hydroxydeboronation
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This paper describes a general method for the synthesis of halohydroxypyridines from novel halopyridinylboronic acids and esters recently described by some of us. Halopyridinylboronic acids and esters have been efficiently hydroxydeboronated under mild conditions by employing hydrogen peroxide or meta-chloroperbenzoic acid. These hydroxylations take place regioselectively without other oxidation (N-oxide formation).
- Voisin, Anne Sophie,Bouillon, Alexandre,Lancelot, Jean-Charles,Rault, Sylvain
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p. 1417 - 1421
(2007/10/03)
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- 3-Pyridyl enantiomers and their use as analgesics
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The present invention relates to a method of controlling pain in mammals, including humans, comprising administering to a mammal or patient in need of treatment thereof selected compounds of formula I: STR1 or a pharmaceutically acceptable salt thereof. The invention further relates to selected (R) and (S) compounds of formula I above which are useful as analgesics as well as neuronal cell death preventors and anti-inflammatories.
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- Furopyridine, thienopyridine pyrrolopyridine useful in controlling chemical synaptic transmission
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Novel heterocyclic ether compounds having the formula: STR1 wherein A, m, R, X, Y1, Y2 and Y3 are specifically defined, which are useful in selectively controlling chemical synaptic transmission; therapeutically-effective pharmaceutical compositions thereof; and use of said compositions to selectively control synaptic transmission in mammals.
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- 2-, 5-, and 6-Halo-3-(2(S)-azetidinylmethoxy)pyridines: Synthesis, affinity for nicotinic acetylcholine receptors, and molecular modeling
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3-(2(S)-Azetidinylmethoxy)pyridine (A-85380) has been identified recently as a ligad with high affinity for nicotinic acetylcholine receptors (nAChRs). Here we report the synthesis and in vitro nAChR binding of a series of 10 pyridine-modified analogues of A-85380. The novel compounds feature a halogen substituent at position 2, 5, or 6 of the 3-pyridyl fragment. Those with the substituents at position 5 or 6, as well as the 2-fluoro analogue, possess subnanomolar affinity for nAChRs in membranes from rat brain. For these ligands, K(i) values range from 11 to 210 pM, as measured by competition with (±)-[3H]epibatidine. In contrast, 2-chloro, 2-bromo, and 2-iodo analogues exhibit substantially lower affinity. AM1 quantum chemical calculations demonstrate that the bulky substituents at position 2 cause notable changes in the molecular geometry. The high-affinity members of the series and (+)-epibatidine display a tight fit superposition of low-energy stable conformers. The new ligands with high affinity for nAChRs may be of interest as pharmacological probes, potential medications, and candidates for developing radiohalogenated tracers to study nAChRs.
- Koren, Andrei O.,Horti, Andrew G.,Mukhin, Alexey G.,Gündisch, Daniela,Kimes, Alane S.,Dannals, Robert F.,London, Edythe D.
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p. 3690 - 3698
(2007/10/03)
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