113520-28-8Relevant articles and documents
Compound with AMPK agonistic activity and preparation and application of prodrug thereof
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Paragraph 0145; 0153-0154, (2021/10/27)
The invention relates to a compound with AMPK agonistic activity and a prodrug thereof, and as well as a preparation method and medical application of a prodrug thereof. The compound has the structure shown in the formula (I), and the prodrug of the compound has the structure shown in the formula (II), wherein each group and the substituent are as defined in the specification. The invention discloses a preparation method of the compound and application of the compound in prevention and treatment AMPK related diseases, and the AMPK related diseases include, but are not limited to, energy metabolism abnormality related diseases. Neurodegenerative diseases and inflammation-related diseases and the like.
HETEROCYCLIC INHIBITORS OF GLUTAMINASE
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Page/Page column 110; 111, (2013/06/06)
The invention relates to the heterocyclic compounds of Formula (I) as defined further herein, and pharmaceutical preparations thereof. The invention further relates to methods of treating cancer, immunological or neurological diseases using the heterocyclic compounds of the invention.
Inhalation by design: Novel ultra-long-acting β2- adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup
Glossop, Paul A.,Lane, Charlotte A. L.,Price, David A.,Bunnage, Mark E.,Lewthwaite, Russell A.,James, Kim,Brown, Alan D.,Yeadon, Michael,Perros-Huguet, Christelle,Trevethick, Michael A.,Clarke, Nicholas P.,Webster, Robert,Jones, Rhys M.,Burrows, Jane L.,Feeder, Neil,Taylor, Stefan C. J.,Spence, Fiona J.
experimental part, p. 6640 - 6652 (2010/11/19)
A novel series of potent and selective sulfonamide derived β2-adrenoreceptor agonists are described that exhibit potential as inhaled ultra-long-acting bronchodilators for the treatment of asthma and chronic obstructive pulmonary disease. Analogues from this series mediate very long-lasting smooth muscle relaxation in guinea pig tracheal strips. The sulfonamide agonist headgroup confers high levels of intrinsic crystallinity that could relate to the acidic sulfonamide motif supporting a zwitterionic form in the solid state. Optimization of pharmacokinetic properties was achieved through targeted introduction of a phenolic moiety to support rapid phase II clearance, thereby minimizing systemic exposure following inhalation and reducing systemically mediated adverse events. Compound 38 (PF-610355) is identified as a clinical candidate from this series, with in vivo duration of action studies confirming its potential for once-daily use in humans. Compound 38 is currently in advanced phase II clinical studies.