- MTA-Cooperative PRMT5 Inhibitors
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The present invention relates to compounds that inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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Paragraph 0315
(2021/03/19)
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- Furo[3,2-b]pyridine: A Privileged Scaffold for Highly Selective Kinase Inhibitors and Effective Modulators of the Hedgehog Pathway
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Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic sequences based on chemoselective metal-mediated couplings, including assembly of the furo[3,2-b]pyridine scaffold by copper-mediated oxidative cyclization. Optimization of the subseries containing 3,5-disubstituted furo[3,2-b]pyridines afforded potent, cell-active, and highly selective inhibitors of CLKs. Profiling of the kinase-inactive subset of 3,5,7-trisubstituted furo[3,2-b]pyridines revealed sub-micromolar modulators of the Hedgehog pathway.
- Němec, Václav,Hylsová, Michaela,Maier, Luká?,Flegel, Jana,Sievers, Sonja,Ziegler, Slava,Schr?der, Martin,Berger, Benedict-Tilman,Chaikuad, Apirat,Val?íková, Barbora,Uldrijan, Stjepan,Drápela, Stanislav,Sou?ek, Karel,Waldmann, Herbert,Knapp, Stefan,Paruch, Kamil
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supporting information
p. 1062 - 1066
(2019/01/04)
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- BIARYL DERIVATIVE AS GPR120 AGONIST
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The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
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Paragraph 0104; 0329
(2017/11/17)
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- PIPERIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention relates to new piperidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 62-63
(2013/06/27)
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- New piperidine derivatives, pharmaceutical compositions and uses thereof
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The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Paragraph 0337; 0341
(2013/06/26)
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- NEW PIPERIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention relates to new piperidine derivatives of the formula (I) to their use as medicaments, to methods for their therapeutic use as inhibitors of acetyl-CoA carboxylases and to pharmaceutical compositions containing them.
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Page/Page column 67
(2013/07/05)
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- Piperidine Derivatives
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Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
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Paragraph 0374; 0375; 0376; 0377; 0378; 0379
(2013/07/05)
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- NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
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Page/Page column 51-52
(2012/06/30)
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