- (l)-Proline-catalysed novel tandem reactions of 1-substituted piperidin-4-ones with (E)-4-arylbut-3-en-2-ones: N-substituent mediated product selectivity and synthesis of novel nitrogen heterocycles
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(l)-Proline-catalysed reaction of 1-alkyl/aralkylpiperidin-4-ones with (E)-4-arylbut-3-en-2-ones furnishes novel isoquinoline derivatives, with two or three rings, in good yields via tandem Robinson annulation-Michael addition(s) sequences, while the reaction of 1-arylpiperidin-4-ones with (E)-4-arylbut-3-en-2-ones affords 3-azabicyclo[3.3.1]nonan-9-ones via a tandem Michael addition-aldol reaction sequence.
- Srinivasan, Murugesan,Perumal, Subbu
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- PHTHALAZINE DERIVATIVES OF FORMULA (I) AS PCAF AND GCN5 INHIBITORS FOR USE IN THE TREATMENT OF CANCER
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The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein ring A, R1, R3, R4, R5, and each Re have any of the values defined in the specification. Also included are novel compounds of Formula (I) and salts thereof, as well as pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.
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Page/Page column 71-72
(2016/03/19)
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- NOVEL TETRAHYDROPYRIDOPYRIMIDINES AND TETRAHYDROPYRIDOPYRIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
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The invention provides novel compounds having the general formula (I): wherein R1, R2, R3, Q, U,W, Z, X and Y are as described herein, compositions including the compounds and methods of using the compounds. These compounds are HbsAg inhibitors and are useful as medicaments for the treatment or prophylaxis of HBV infection.
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Page/Page column 86
(2016/07/27)
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- NIROGENOUS HETEROCYCLIC DERIVATIVES SUBSTITUTED WITH CYCLIC GROUPS
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It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is -(CR3R4)m-, -CO(CR3R4)n-, -CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.
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Page/Page column 66
(2008/12/08)
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- Some observations relating to the use of 1-aryl-4-alkoxypiperidin-4-yl groups for the protection of the 2′-hydroxy functions in the chemical synthesis of oligoribonucleotides
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The comparative rates of acid-catalysed removal often 1-aryl-4-methoxypiperidin-4-yl 8 (R = Me) [including the previously reported Ctmp 5 and Fpmp 6] protecting groups for the 2′-hydroxy functions in oligoribonucleotide synthesis are discussed. These studies have led to the development of the 1-(4-chlorophenyl)-4-ethoxypiperidin-4-yl (Cpep) protecting group 8 (R = Et, R1 = R2 = H, R3 = Cl) which is both more stable than the Ctmp and Fpmp groups at pH 0.5 and more labile at pH 3.75. The influence of the ribonucleoside aglycone on the stability of the 2′-O-Fpmp and 2′-O-Ctmp protecting groups both at low and high pH is examined. The Royal Society of Chemistry 2000.
- Lloyd, Wayne,Reese, Colin B.,Song, Quanlai,Vandersteen, Anthony M.,Visintin, Cristina,Zhang, Pei-Zhou
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p. 165 - 176
(2007/10/03)
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- Facile preparation of acetals and enol ethers derived from 1-arylpiperidin-4-ones
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When primary aromatic amines 6 are heated under reflux with slight excesses each of crude 1,5-dichloro-pentan-3-one 4 and toluene-4-sulfonic acid monohydrate in dry methanol solution, and an excess of trimethyl orthoformate is then added to the reactants,
- Faja, Montserrat,Reese, Colin B.,Song, Quanlai,Zhang, Pei-Zhuo
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p. 191 - 194
(2007/10/03)
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- Synthesis and exploratory photophysical investigation of donor-bridge-acceptor systems derived from N-substituted 4-piperidones
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We report a two-step synthesis for N-aryl- and N-alkyl-substituted 4-piperidones, in which the N substituent can easily be varied.A number of intramolecular donor-acceptor systems was synthesized from these piperidones by conversion of the carbonyl functionality.The influence of the N-aryl donor on the electronic absorption and fluorescence spectra was investigated systematically.It was concluded that some systems can be used as efficient fluorescent probes with a high sensitivity for solvent polarity.
- Scherer, T.,Hielkema, W.,Krijnen, B.,Hermant, R. M.,Eijckelhoff, C.,et al.
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p. 535 - 548
(2007/10/02)
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- A New Synthesis of 1-Arylpiperidin-4-ols
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1,5-Dichloropentan-3-ol (8), which is readily prepared from the corresponding ketone (7), reacts with 2-fluoro-, 4-methyl-, 2-chloro-, 3-chloro-, 4-chloro-, and 3-chloro-4-methyl-anilines in the presence of potassium carbonate and sodium iodide in dimethy
- Reese, Colin B.,Thompson, Elizabeth A.
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p. 2881 - 2886
(2007/10/02)
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