- 5-(BIPHENYL-4-YL)-3-PHENYL-1,2,4-OXADIAZOLYL DERIVATIVES AS LIGANDS ON THE SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTORS
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The present invention provides compounds of Formula (I), as selective S1 P1 inhibitors, as well as their use for treating multiple sclerosis and other diseases.
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Page/Page column 93-94
(2012/02/01)
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- Boronic acid based photoinduced electron transfer (PET) fluorescence sensors for saccharides
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A simple three step synthesis was developed to provide six novel modular sensors, consisting of three para sensors, and three meta sensors with naphthalene, anthracene and pyrene fluorophores. The interaction of the six sensors with the saccharides: d-glu
- Larkin, Joseph D.,Frimat, Karine A.,Fyles, Thomas M.,Flower, Stephen E.,James, Tony D.
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p. 2922 - 2931
(2011/02/27)
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- OXADIAZOLE DERIVATIVES
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The invention relates to compounds of formula (I); wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple
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Page/Page column 67
(2010/11/03)
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- OXADIAZOLE DERIVATIVES
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The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
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Page/Page column 166
(2009/05/29)
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- DERIVATIVES OF 4-(2-AMINO-1-HYDROXIETHYL)PHENOL AS AGONISTS OF THE β2 ADRENERGIC RECEPTOR
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This invention is directed to compounds of formula (I): to pharmaceutical compositions comprising them; to combination products comprising them; and to their use in therapy.
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Page/Page column 44-45
(2008/06/13)
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- ARYLAMINE-SUBSTITUTED QUINAZOLINONE COMPOUNDS
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Compounds represented by Formula (I) which are useful as are alpha-1A/B adrenoceptor antagonists, to methods of treating conditions associated with the activity of alpha-1A/B adrenoceptors, and to methods of making said compounds, wherein Ar, Z, R, R', R
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- Synthesis of N-methyl secondary amines
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A diverse set of N-methyl secondary amines are obtained in high yields by an expedient reductive alkylation of commercially available methanolic methylamine.
- Kumpaty, Hephzibah J.,Williamson, John S.,Bhattacharyya, Sukanta
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p. 1411 - 1416
(2007/10/03)
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- Facile preparation of N-methyl secondary amines by titanium(IV) isopropoxide-mediated reductive animation of carbonyl compounds
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A simple, mild and efficient procedure for obtaining N-methyl secondary amines from aldehydes and ketones is reported. Treatment of carbonyl compounds with methylamine hydrochloride, triethylamine and titanium(IV) isopropoxide, followed by in situ sodium borohydride reduction and straightforward aqueous work-up, affords clean products in good to excellent yields.
- Neidigh, Kurt A.,Avery, Mitchell A.,Williamson, John S.,Bhattacharyya, Sukanta
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p. 2527 - 2531
(2007/10/03)
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- Quantitative structure-activity relationship of the mutagenicity of substituted N-nitroso-N-benzylmethylamines: Possible implications of carcinogenicity
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The relative mutagenicities of substituted N-nitroso-N-benzylmethylamines have been reexamined from a quantitative structure-activity relationship point of view. Most of the compounds were mutagenic toward Salmonella typhimurium TA 1535 with Aroclor-induced male hamster liver S9 activation. The dose-response data were subjected to a multiple linear regression equation calculated in a stepwise manner, which found that the differences in mutagenicities could be explained primarily by differences in the three-bond path molecular connectivity index, with smaller contributions from σ and π. Moreover, a polynomial regression analysis showed that the maximum mutagenicity could be explained by an optimal amount of electron withdrawal by the substituent which could cause a weakening, or activation, of the methylene C-H bond. The possible relevance of these observations to carcinogenesis is discussed.
- Singer,Andrews,Guo
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- Oxidative N-Dealkylation of N,N-Dimethylbenzylamines by Metalloporphyrin-catalysed Model Systems for Cytochrome P450 Mono-oxygenases
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Iodosylbenzene, catalysed by tetraphenylporphyrinato-iron(III) or - manganese(III) chloride, oxidises tertiary amines by an initial one-electron transfer process whereas with t-butyl hydroperoxide with these catalysts the oxidation is initiated by hydrogen atom abstraction.
- Smith, John R. Lindsay,Mortimer, David N.
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- Benzylamines: Synthesis and evaluation of antimycobacterial properties
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The synthesis of benzylamines with various N-alkyl chains and substituents in the aromatic system as well as their evaluation on Mycobacterium tuberculosis H 37 Ra are described. The most active compounds in this test, N-methyl-3-chlorobenzylamine (MIC 10.2 μg/mL), N-methyl-3,5-dichlorobenzylamine (93, MIC 10.2 μg/mL), and N-butyl-3,5-difluorobenzylamine (MIC 6.4 μg/mL), also exhibited a marked inhibitory effect on Mycobacterium marinum and Mycobacterium lufu used for the determination of antileprotic properties. The combination of 93 with aminosalicylic acid, streptomycin, or dapsone exert marked supra-additive effects on M. tuberculosis H 37 Ra.
- Meindl,Von Angerer,Schonenberger,Ruckdeschel
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p. 1111 - 1118
(2007/10/02)
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