- COMPOUNDS FOR USING IN IMAGING AND PARTICULARLY FOR THE DIAGNOSIS OF NEURODEGENERATIVE DISEASES
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The invention relates to compounds of formula (II) for using in imaging and particularly for the diagnosis of neurodegenerative diseases
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Paragraph 1040; 1042
(2019/07/23)
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- Discovery of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo signaling pathway inhibitors
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Inhibitors of the Hippo signaling pathway have been demonstrated to have a potential clinical application in cases such as tissue repair and organ regeneration. However, there is a lack of potent Hippo pathway inhibitors at present. Herein we report the discovery of a series of 1,8-disubstituted-[1,2,3]triazolo[4,5-c]quinoline derivatives as a new class of Hippo pathway inhibitors by utilizing a cell line-based screening model (A549-CTGF). Structure-activity relationship (SAR) of these compounds was also discussed. The most potent compound in the A549-CTGF cell assay, 11g, was then evaluated by real-time PCR and immunofluorescence assays. Overall, this study provides a starting point for later drug discovery targeting the Hippo signaling pathway.
- Chen, Pei,Li, L.,Lin, Guifeng,Qiao, Jingxin,Xia, A.,Xiang, Z.,Yang, Shengyong,Zhang, Guo
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supporting information
(2019/08/12)
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- Synthesis, biological evaluation and molecular modeling of a novel series of 7-azaindole based tri-heterocyclic compounds as potent CDK2/Cyclin E inhibitors
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From four molecules, inspired by the structural features of fascaplysin, with an interesting potential to inhibit cyclin-dependent kinases (CDKs), we designed a new series of tri-heterocyclic derivatives based on 1H-pyrrolo[2,3-b]pyridine (7-azaindole) an
- Baltus, Christine B.,Jorda, Radek,Marot, Christophe,Berka, Karel,Bazgier, Václav,Kry?tof, Vladimír,Prié, Gildas,Viaud-Massuard, Marie-Claude
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p. 701 - 719
(2016/01/09)
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- PYRROLOPYRIDINE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing sa
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Page/Page column 30
(2011/02/18)
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- PHTHALAZIN-(2H)-ONE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, Y, Z, n, and m are defined in the description. The present invention relates also to compositions cont
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Page/Page column 21-22
(2011/10/31)
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- PYRROLOPYRAZINONE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, Y, Z, n, and m are defined in the description. The present invention relates also to compositions cont
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Page/Page column 35
(2011/10/31)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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Page/Page column 102
(2008/06/13)
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- PDE4B inhibitors
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Compounds are described that are active on PDE4. Also described are crystal structures of PDE4B determined using X-ray crystallography, the use of PDE4B crystals and strucural information for identifying molecular scaffolds, for developing ligands that bind to and modulate PDE4B, and for identifying improved ligands based on known ligands.
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Page/Page column 52
(2008/06/13)
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- Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors
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A novel series of 2-amino-4-(7-azaindol-3-yl)pyrimidines was discovered as cyclin dependent kinase 1 (CDK1) inhibitors. The core structure was synthesized via Pd(II) catalyzed coupling reaction. A number of analogues showed good potency for CDK1 and exhib
- Huang, Shenlin,Li, Ronghua,Connolly, Peter J.,Emanuel, Stuart,Middleton, Steven A.
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p. 4818 - 4821
(2007/10/03)
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- PYRIMIDINYL SUBSTITUTED FUSED-PYRROLYL COMPOUNDS USEFUL IN TREATING KINASE DISORDERS
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The present invention provides pyrimidinyl substituted fused-pyrrolyl compounds of Formula (I) and pharmaceutical compositions comprising the compounds and methods of synthesis and use thereof. The compounds are kinase inhibitors useful in treating or ameliorating a kinase mediated, angiogenesis-mediated or hyperproliferative disorder. The invention thus also provides a therapeutic or prophylactic method of use for the compounds and/or pharmaceutical compositions to treat such disorders.
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Page/Page column 61
(2010/11/30)
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