- 1,5-DIPHENYL-PENTA-1,4-DIEN-3-ONE COMPOUNDS
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This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
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Page/Page column 18-19
(2012/03/10)
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- L -DIHYDRO-2-OXOQUINOLINE COMPOUNDS A 5-HT4 RECEPTOR LIGANDS
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The present invention relates to novel l,2-dihydro-2-oxoquinoline compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. Formula (I) The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The compounds of the present invention are useful in the treatment/prevention of various disorders that are mediated by 5-HT4 receptor activity.
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Page/Page column 35
(2011/04/18)
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- Lightening Agents and/or Dyes that Contain Aldehyde(s)
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Agents for dyeing and/or lightening keratin fibers, in particular human hair, containing, relative to the weight thereof, 0.001 to 15 wt. % of at least one aldehyde of the formula (I): wherein X represents —CH(R2)—SO2—Y—R1, —CR3R4R5, or wherein Y represents —CH(CHO)— or —CH2— or a chemical bond, and wherein each of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 independently represents —H or —CN or —F or —Cl or —Br or —I or —CHO or —NH2 or —NO2 or —CF3 or —CCl3 or —CF2CF3 or —CCl2CCl3 or an optionally substituted (C1-C6) alkyl group or a hydroxyalkyl group or a polyhydroxyalkyl group or an optionally substituted (C1-C6) alkylene group, and wherein the agent contains no oxidation dye precursors of developer and coupler type.
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- (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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p. 2865 - 2874
(2007/10/03)
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- Fused heterocyclic compounds and their use in the treatment of neurodegenerative diseases
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The present invention relates to certain fused heterocyclic compounds and their use in the treatment of neurodegenerative diseases and for the regeneration or prevention of degeneration of lesioned and damaged neurons (I).
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- Indazole derivatives having monocyclic amine
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An indazole compound having the formula (I): wherein: R1 is hydrogen, C1 -C6 alkyl, C3 -C6 alkenyl or C3 -C6 cycloalkyl; Q is carbonyl, thiocarbonyl or methylene; and R2 is a group of the formula (II) or (IV); STR1 wherein R1 is C1 -C6 alkyl, C3 -C6 alkenyl or benzyl, of which a phenyl group thereof is optionally mono- or di-substituted by the same or different halogen or methoxy; m is 0 to 2; n and o is 1 or 2. The compound exhibits 5-HT4 receptor agonist activity.
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- Asymmetric Deprotonations: Lithiation of N-(tert-Butoxycarbonyl)indoline with sec-Butyllithium/ (-)-Sparteine
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The asymmetric lithiation of N-Boc indoline (1) with s-BuLi/(-)-sparteine and subsequent substitution provides the 2-substituted N-Boc indolines 3 and 5-11 with excellent enantiomeric ratios and in variable yields. The asymmetric lithiation-substitution sequence with N-Boc-7-chloroindoline (12) provides products 13-19 with good enantiomeric ratios. Mechanistic investigation establishes that the enantioselectivities arise from an initial asymmetric deprotonation to provide the enantioenriched and configurationally stable organolithium intermediates (S)-28 and (S)-29, which react stereoselectively with electrophiles.
- Bertini Gross, Kathleen M.,Jun, Young M.,Beak, Peter
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p. 7679 - 7689
(2007/10/03)
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- 10-Substituted benzo[b][1,6]naphthyridines as inhibitors of interleukin 1
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There is disclosed a method for the treatment of inflammatory conditions and of collagenase-induced tissue destruction which comprises the administration of a therapeutically effective amount of a compound of the formula STR1 wherein R 1 is lower alkyl or lower alkenyl or any of the foregoing optionally substituted with fluoro, carboxy, lower alkoxycarbonyl, OR 2, N(R 2) 2, SR 2 CON(R 2) 2, SO 2 R 2, cyano, nitro or trifluoromethyl;R 2 is hydrogen, lower alkyl or phenyl;R 3 is halo, morpholino, 4-methylpiperazino, R 4 NNHR 5, NR 4 R 5, OR 5, SR 5, STR2 R 4 is hydrogen or lower alkyl; R 5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR 6 and R 7 are each independently, hydrogen, halo, nitro, lower alkoxy, lower alkyl or trifluoromethyl;which compounds, by virtue of their ability to inhibit interleukin 1, are useful as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and are also intermediates in the preparation of other compounds which possess identical activities.
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- N-Heterocyclic-9-xanthenylamines
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The compounds are N-piperidinyl and pyrrolidinyl-9-xanthenylamines which are inhibitors of gastric acid secretion.
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