- SUBSTITUTED PYRROLOPYRIDINES AS JAK INHIBITORS
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The present invention relates to new pyrrolopyridine compounds having the structures of Formula (I)-(IV), wherein the R groups, A, B, C, D and n are as defined in the detailed description, and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis.
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Paragraph 0467; 0468
(2020/11/12)
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- INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
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Page/Page column 67
(2015/02/25)
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- ALKYLSULFINYL-SUBSTITUTED THIAZOLIDE COMPOUNDS
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A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses
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Page/Page column 32
(2012/05/07)
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- Thiazolides as novel antiviral agents. 1. Inhibition of hepatitis B virus replication
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We report the syntheses and activities of a wide range of thiazolides [viz., 2-hydroxyaroyl-N-(thiazol-2-yl)amides] against hepatitis B virus replication, with QSAR analysis of our results. The prototypical thiazolide, nitazoxanide [2-hydroxybenzoyl-N-(5-
- Stachulski, Andrew V.,Pidathala, Chandrakala,Row, Eleanor C.,Sharma, Raman,Berry, Neil G.,Iqbal, Mazhar,Bentley, Joanne,Allman, Sarah A.,Edwards, Geoffrey,Helm, Alison,Hellier, Jennifer,Korba, Brent E.,Semple, J. Edward,Rossignol, Jean-Francois
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supporting information; experimental part
p. 4119 - 4132
(2011/08/05)
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- Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of Type-2 diabetes
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Sulfonylureido thiazoles were identified from a HTS campaign and optimized through a combination of structure-activity studies, X-ray crystallography and molecular modeling to yield potent inhibitors of fructose-1,6-bisphosphatase. Compound 12 showed favo
- Kitas, Eric,Mohr, Peter,Kuhn, Bernd,Hebeisen, Paul,Wessel, Hans Peter,Haap, Wolfgang,Ruf, Armin,Benz, Joerg,Joseph, Catherine,Huber, Walter,Sanchez, Ruben Alvarez,Paehler, Axel,Benardeau, Agnes,Gubler, Marcel,Schott, Brigitte,Tozzo, Effie
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scheme or table
p. 594 - 599
(2010/05/19)
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- ALKYLSULFONYL-SUBSTITUTED THIAZOLIDE COMPOUNDS
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A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.
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Page/Page column 66; 77
(2009/04/24)
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- Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer's disease
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High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide (1). This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320 nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved.
- Helal, Christopher J.,Sanner, Mark A.,Cooper, Christopher B.,Gant, Thomas,Adam, Mavis,Lucas, John C.,Kang, Zhijun,Kupchinsky, Stanley,Ahlijanian, Michael K.,Tate, Bonnie,Menniti, Frank S.,Kelly, Kristin,Peterson, Marcia
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p. 5521 - 5525
(2007/10/03)
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