- ADENINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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The present invention relates to a compound suitable for use as a kinase inhibitor according to general formula (I) [compound (C), herein after], or the N- oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof, formula (I) wherein A, R1, R2, R3, R3', R4, R4', X, Y, Z, T are as defined in the claims. The invention further relates to an in vitro method of inhibiting protein kinase activity which comprises contacting a protein kinase with a compound of formula (I), or the N-oxide, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or stereoisomer thereof. The invention further relates to the compounds of formula (I) per se, as well as to their use as a medicament, and for use or in a method of treatment of a disease mediated by a protein kinase selected from cancer, inflammatory disorders, cardiovascular diseases, viral induced diseases, circulatory diseases, fibro-proliferative diseases and pain sensitization disorders.
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Page/Page column 130; 131
(2017/12/14)
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- Aurora isoform selectivity: Design and synthesis of imidazo[4,5- B ]pyridine derivatives as highly selective inhibitors of aurora-A kinase in cells
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Aurora-A differs from Aurora-B/C at three positions in the ATP-binding pocket (L215, T217, and R220). Exploiting these differences, crystal structures of ligand-Aurora protein interactions formed the basis of a design principle for imidazo[4,5-b]pyridine-
- Bavetsias, Vassilios,Faisal, Amir,Crumpler, Simon,Brown, Nathan,Kosmopoulou, Magda,Joshi, Amar,Atrash, Butrus,Pérez-Fuertes, Yolanda,Schmitt, Jessica A.,Boxall, Katherine J.,Burke, Rosemary,Sun, Chongbo,Avery, Sian,Bush, Katherine,Henley, Alan,Raynaud, Florence I.,Workman, Paul,Bayliss, Richard,Linardopoulos, Spiros,Blagg, Julian
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supporting information
p. 9122 - 9135
(2014/01/06)
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- NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF
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The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.
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Paragraph 1332; 1333
(2013/07/25)
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- Trisubstituted ureas as potent and selective mPGES-1 inhibitors
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A novel series of trisubstituted ureas has been identified as potent and selective mPGES-1 inhibitors. These compounds are selective over other prostanoid enzymes such as PGF synthase and TX synthase. This series of inhibitors was developed by lead optimi
- Chiasson, Jean-Franois,Boulet, Louise,Brideau, Christine,Chau, Anh,Claveau, David,C?té, Bernard,Ethier, Diane,Giroux, André,Guay, Jocelyne,Guiral, Sébastien,Mancini, Joseph,Massé, Frédéric,Méthot, Nathalie,Riendeau, Denis,Roy, Patrick,Rubin, Joel,Xu, Daigen,Yu, Hongping,Ducharme, Yves,Friesen, Richard W.
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scheme or table
p. 1488 - 1492
(2011/04/23)
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- NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF
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The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.
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Page/Page column 241
(2010/04/30)
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- Synthesis and application of a new fluorous-tagged ammonia equivalent
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A novel fluorous-tagged ammonia equivalent has been developed. It is based on a nitrogen-oxygen bond, which can be cleaved in a traceless manner by a molybdenum complex or samarium diiodide. The application in the synthesis of ureas, amides, sulfonamides, and carbamates is described. The scope of the fluo-rous N-O linker is exemplified by the synthesis of itopride, a drug used for the treatment of functional dyspepsia. Itopride was synthesized with the aid of fluorous purification methods and the product was isolated in good overall yield, with high purity.
- Nielsen, Simon D.,Smith, Garrick,Begtrup, Mikael,Kristensen, Jesper L.
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supporting information; experimental part
p. 4557 - 4566
(2010/08/20)
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- UREA DERIVATIVES AS ANTIBACTERIAL AGENTS
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This invention relates to compounds of the Formula (I):or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which is useful for the treatment of diseases or conditions mediated by LpxC.
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Page/Page column 33
(2010/04/03)
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- PHTHALAZINE DERIVATIVES
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The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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Page/Page column 115
(2008/12/05)
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- CHEMICAL COMPOUNDS
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The present invention discloses pyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such pyrimidine derivatives are useful in the treat
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Page/Page column 74
(2010/02/10)
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- FORMAMIDE DERIVATIVES USEFUL AS ADRENOCEPTOR
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 73
(2008/06/13)
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- Sulfonamide derivatives for the treatment of diseases
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
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Page/Page column 31-32
(2008/06/13)
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- Compounds for the treatment of diseases
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
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Page/Page column 47
(2008/06/13)
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- 2-(6-AMINO-PYRIDIN-3-YL)-2-HYDROXYETHYLAMINE DERIVATIVES AS BETA 2-ADRENOCEPTORS AGONISTS
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The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
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