146679-66-5Relevant articles and documents
Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties
Charles, Mark D.,Brookfield, Joanna L.,Ekwuru, Tennyson C.,Stockley, Martin,Dunn, John,Riddick, Michelle,Hammonds, Tim,Trivier, Elisabeth,Greenland, Gavin,Wong, Ai Ching,Cheasty, Anne,Boyd, Susan,Crighton, Diane,Olson, Michael F.
, p. 8309 - 8313 (2015)
As part of a program to develop a small molecule inhibitor of LIMK, a series of aminothiazole inhibitors were discovered by high throughput screening. Scaffold hopping and subsequent SAR directed development led to a series of low nanomolar inhibitors of LIMK1 and LIMK2 that also inhibited the direct biomarker p-cofilin in cells and inhibited the invasion of MDA MB-231-luc cells in a matrigel inverse invasion assay.
SUBSTITUTED HETEROARYL ALDEHYDE COMPOUNDS AND METHODS FOR THEIR USE IN INCREASING TISSUE OXYGENATION
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Paragraph 0522; 0523, (2015/12/25)
Provided are substituted heteroaryl aldehydes and derivatives thereof that act as allosteric modulators of hemoglobin, methods and intermediates for their preparation, pharmaceutical compositions comprising the modulators, and methods for their use in treating disorders mediate by hemoglobin and disorders that would benefit from increased tissue oxygenation.
Oxidisable pyridine derivatives, their preparation and use as anti-Alzheimer agents
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Paragraph 0067; 0068, (2014/08/06)
A compound of the formula (I) in which the dotted lines indicate the presence of at least one double bond; n = 0 to 4; R3 and R4 are H, or when n = 1, R3 and R4 can also form together a double bond between the carbon atoms, and m = 0, 1 or 2, Z is CH or N or Z is C and -CHR3- is =CH- linked by the double bond to the cyclopentanone; or -(-)m- is absent, and Z is NH, >N-alkyl, >N-phenyl, >N-benzyl or >N-heteroaryl; R8 is alkyl, aryl or heteroaryl which can be optionally substituted; EWG represents an electron withdrawing group selected from the group comprising COOR, COSR, CONRR', CN, COR, CF3, SOR, SO2R, SONRR', SO2NRR', NO2, halogen, heteroaryl; and the pharmaceutical salts or tautomers thereof. The compounds of formula (I) are potent in the treatment of neurodegenerative diseases such as Alzheimer's disease.