- Synthesis of thieno[2,3-c]pyridine derived GRK2 inhibitors
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Bicyclic heteroaromatic motifs with hydrogen bond donor–acceptor hinge binder motifs are frequently used as ATP-mimetic kinase inhibitors. Althought the thieno[2,3-c]pyridine scaffold also meets these criteria its use was limited so far by the availability of synthetic building blocks. Inspired by two X-ray structures of kinase bound thieno[2,3-c]pyridines we prepared a diverse collection of simple thieno[2,3-c]pyridine derivatives that could serve as starting points for future drug discovery programs. In our search for inhibitors of the GRK2 kinase we also identified a hit compound bearing the thieno[2,3-c]pyridine moiety. Following a structure-driven optimization process a collection of potent and highly ligand efficient inhibitors were prepared and characterized, which could form the basis of a future drug discovery program. Graphical abstract: [Figure not available: see fulltext.]
- Balo, Timea,Berger, Sylvie,Cattin, Marie-Elodie,Faucher, Nicolas,Kiss, Arpad,Kotschy, Andras,Paysant, Jérome,Raimbaud, Eric,Sapi, Attila
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- Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof
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The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.
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Paragraph 0814-0818
(2021/05/01)
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- AMPK INHIBITORS
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The 5'-AMP-activated protein kinase AMPK functions as a master switch to maintain cellular and whole-body energy homeostasis and abnormal activity profiles of AMPK may cause pathological disorders. The present invention relates to a series of compounds (I
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Page/Page column 58
(2019/06/17)
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- PYRAZOLE DERIVATIVES AS MALT1 INHIBITORS
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Disclosed are compounds, compositions and methods for treating of diseases, syndromes, conditions, and disorders that are affected by the modulation of MALT1. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, R4, R5, R6, R5, G1, and G2 are defined herein.
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Paragraph 2528; 2529
(2018/07/05)
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- AMIDO-BENZYL SULFONE AND SULFOXIDE DERIVATIVES
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The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
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Page/Page column 135
(2013/09/12)
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- PYRIDINYL AND PYRIMIDINYL SULFOXIDE AND SULFONE DERIVATIVES
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Disclosed are certain pyridinyl and pyrimidinyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds and methods of treatment using such compounds.
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Page/Page column 86; 87
(2013/09/12)
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- AMIDO-BENZYL SULFONE AND SULFONAMIDE DERIVATIVES
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Disclosed are certain amido-benzyl sulfone and sulfonamide compounds, pharmaceutical compositions comprising such compounds, land methods of treatment using such compounds.
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Page/Page column 64; 65
(2013/09/12)
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- AMIDO-BENZYL SULFOXIDE DERIVATIVES
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The present invention relates to certain amido-benzyl sulfoxide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment of an NAMPT-mediated disease or condition in a subject, selected from solid or liquid tumor, rheumat
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Paragraph 0188
(2013/09/12)
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- ALKYL-AND DI-SUBSTITUTED AMIDO-BENZYL SULFONAMIDE DERIVATIVES
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The present invention relates to certain alkyl- and di-substituted amido-benzyl sulfonamide compounds, pharmaceutical compositions comprising such compounds, and to methods of treatment of NAMPT-mediated disorders, such as diabetes, rheumatoid arthritis,
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Paragraph 0196
(2013/09/12)
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- A facile and general synthesis of 2,4-di- and 2,4,7-trisubstituted thieno[2,3-c]pyridines
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(Chemical Equation Presented) Treatment of 3,5-dibromo- or 3,5-dichloro-pyridine-4-carboxaldehyde 2 with one equivalent of methyl thioglycolate, followed by exposure to base, provided 4-bromo- or 4-chloro-thieno[2,3-c]pyridine-2-carboxylate 4 in good yiel
- Zhu, Gui-Dong,Gunawardana, Indrani W.,Boyd, Steven A.,Melcher, Laura M.
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- Discovery of thieno[2,3-c]pyridines as potent COT inhibitors
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Evaluation of hit chemotypes from high throughput screening identified a novel series of 2,4-disubstituted thieno[2,3-c]pyridines as COT kinase inhibitors. Structural modifications exploring SAR at the 2- and 4-positions resulting in inhibitors with improved enzyme potency and cellular activity are disclosed.
- George, Dawn,Friedman, Michael,Allen, Hamish,Argiriadi, Maria,Barberis, Claude,Bischoff, Agnieszka,Clabbers, Anca,Cusack, Kevin,Dixon, Richard,Fix-Stenzel, Shannon,Gordon, Thomas,Janssen, Bernd,Jia, Yong,Moskey, Maria,Quinn, Christopher,Salmeron, Jose-Andres,Wishart, Neil,Woller, Kevin,Yu, Zhengtian
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scheme or table
p. 4952 - 4955
(2009/05/30)
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- KINASE INHIBITORS AS THERAPEUTIC AGENTS
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A compound or pharmaceutically acceptable salts thereof of Formula (I) wherein the substituents are as defined herein, which are useful as kinase inhibitors.
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Page/Page column 80-81
(2010/02/14)
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- Cell adhesion-inhibiting antiinflammatory compounds
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Compounds having Formula I are useful for treating inflammation. Also disclosed are pharmaceutical compositions comprising compounds of Formula I, and methods of inhibiting/treating inflammatory diseases in a mammal.
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- Novel Thienopyridines
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A number of novel thienopyridines were prepared from the reaction of 1 with unsaturated haloalkanes, and by the reaction of the amino ketones 9 and 10 with DMF dimethylacetal or triethyl orthoformate.The synthesis of novel thieno and
- Dunn, A. D.,Norrie, R.
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p. 483 - 486
(2007/10/02)
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