- 4-(ORTHO)-FLUOROPHENYL-5-FLUOROPYRIMIDIN-2-YL AMINES CONTAINING A SULFOXIMINE GROUP
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The present invention relates to 4-(ortho)-fluorophenyl-5-fluoropyrimidin-2-yl amine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or p
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Page/Page column 97
(2014/06/11)
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- DISUBSTITUTED 5-FLUORO PYRIMIDINE DERIVATIVES CONTAINING A SULFOXIMINE GROUP
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The present invention relates to disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of diso
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Page/Page column 104; 134
(2013/03/28)
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- PYRROLE DERIVATIVES WITH CRTH2 RECEPTOR MODULATOR ACTIVITY
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There are provided according to the invention compounds of formula (I) in free or salt form, wherein R3, R 4, R5, R6a, R6b, Q and W are as described in the specification, process for preparing them, a
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Page/Page column 38
(2008/06/13)
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- Synthesis and structure-activity relationships of 3-aminobenzophenones as antimitotic agents
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A new series of 3-aminobenzophenone compounds as potent inhibitors of tubulin polymerization was discovered based on the mimic of the aminocombretastatin molecular skeleton. Lead compounds 5 and 11, with alkoxy groups at the C-4 position of B-ring, were p
- Liou, Jing-Ping,Chang, Jang-Yang,Chang, Chun-Wei,Chang, Chi-Yen,Mahindroo, Neeraj,Kuo, Fu-Ming,Hsieh, Hsing-Pang
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p. 2897 - 2905
(2007/10/03)
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- Enzymatic resolution of substituted mandelic acids
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A series of substituted mandelic acids were prepared and subjected to enzymatic resolution utilizing Lipase PS 'Amano'.
- Campbell, Robert F.,Fitzpatrick, Kevin,Inghardt, Tord,Karlsson, Olle,Nilsson, Kristina,Reilly, John E.,Yet, Larry
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p. 5477 - 5481
(2007/10/03)
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- New amidino derivatives and their use as thormbin inhibitors
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There is provided compounds of formula I, wherein Y and R1 have meanings given in the description, and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
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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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