61363-66-4Relevant academic research and scientific papers
HETERO-1,5,6,7-TETRAHYDRO-4H-INDOL-4-ONES
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Page/Page column 118; 119, (2017/07/14)
Compounds of formula (I) as described herein, processes for their production and their use as pharmaceuticals.
THIA-TRIAZA-AS-INDACENES AS PI3-KINASES INHIBITORS FOR THE TREATMENT OF CANCER
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Page/Page column 37, (2010/11/05)
The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the
An improved synthesis of Pyran-3,5-dione: Application to the synthesis of ABT-598, a potassium channel opener, via Hantzsch reaction
Li, Wenke,Wayne, Gregory S.,Lallaman, John E.,Chang, Sou-Jen,Wittenberger, Steven J.
, p. 1725 - 1727 (2007/10/03)
Ketoester 1 is cyclized to give pyran-3,5-dione 2 in 78% yield using a parallel addition of ketoester 1 and base NaOtBu in refluxing THF. Compared to the previously reported procedures, these optimized conditions have significantly increased the yield of this transformation and the quality of pyran 2 and prove to be suitable for large-scale preparation. An application of 2 to the synthesis of ABT-598, a potassium channel opener, is demonstrated.
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2, 6-dioxa-4-azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener
Altenbach, Robert J.,Brune, Michael E.,Buckner, Steven A.,Coghlan, Michael J.,Daza, Anthony V.,Fabiyi, Adebola,Gopalakrishnan, Murali,Henry, Rodger F.,Khilevich, Albert,Kort, Michael E.,Milicic, Ivan,Scott, Victoria E.,Smith, Jamie C.,Whiteaker, Kristi L.,Carroll, William A.
, p. 6869 - 6887 (2007/10/03)
Structure-activity relationships were investigated on the tricyclic dihydropyridine (DHP) KATP openers 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H- 2,6-dioxa-4-azacyclopenta[b]naphthalene-1,8-dione (6) and 10-(3-bromo-4- fluorophenyl)-9,10-dihydro-1H,8H-2,7-dioxa-9-azaanthracene-4,5-dione (65). Substitution off the core of the DHP, absolute stereochemistry, and aromatic substitution were evaluated for KATP channel activity using Ltk- cells stably transfected with the Kir6.2/SUR2B exon 17- splice variant and in an electrically stimulated pig bladder strip assay. A select group of compounds was evaluated for in vitro inhibition of spontaneous bladder contractions. Several compounds were found to have the unique characteristic of partial efficacy in both the cell-based and electrically stimulated bladder strip assays but full efficacy in inhibiting spontaneous bladder strip contractions. For compound 23b, this profile was mirrored in vivo where it was fully efficacious in inhibiting spontaneous myogenic bladder contractions but only partially able to reduce neurogenically mediated reflex bladder contractions.
5-Amino-2H-pyran-3(6H)-one, 1, a Convenient Intermediate in the Synthesis of Pyran Containing 1,4-Dihydropyridines
Altenbach, Robert J.,Agrios, Konstantinos,Drizin, Irene,Carroll, William A.
, p. 557 - 565 (2007/10/03)
5-Amino-2H-pyran-3(6H)-one, 1, is a novel intermediate that is useful in the synthesis of pyran containing dihydropyridines. The synthesis and use of 1 will be discussed.
Pyrano, piperidino, and thiopyrano compounds and methods of use
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, (2008/06/13)
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
Novel radioligands and their use for identifying potassium channel modulators
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, (2008/06/13)
The present invention relates to novel radioligands and test methods using those radioligands in screening compounds.
Pyrano, piperidino, and thiopyrano compounds and methods of use
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, (2008/06/13)
The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.
Morpholino derivatives of daunorubicin and doxorubicin
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, (2008/06/13)
Anthracycline glycosides of the general formula (A): STR1 wherein X is hydrogen or hydroxy and R is hydrogen or a methyl or a hydroxymethyl group; and their pharmaceutically acceptable salts; are useful as antitumor agents.
