cas 603288-22-8, LY2090314 | Articles data

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Pictet-Spengler based synthesis of a bisarylmaleimide glycogen synthase kinase-3 inhibitor
A practical synthesis of the glycogen synthase kinase-3 (GSK3) inhibitor bisarylmaleimide 1 has been accomplished employing Pictet-Spengler methodology to access the indole 7-position in preparing the benzodiazepine tricyclic fragment. A seven-step linear sequence that starts with commercially available 5-fluoroindole 7 affords the bisarylmaleimide 1 in 33% overall yield.
Magnus, Nicholas A.,Ley, Christopher P.,Pollock, Patrick M.,Wepsiec, James P.
p. 3700 - 3703
(2010)
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POTENTIATION OF CANCER CHEMOTHERAPY
An improved method for treating gastric cancer, ovarian cancer, non-small cell lung cancer, or colorectal cancer in a patient is described, as well as pharmaceutical compositions useful for the method and a process for preparing said compositions.
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Paragraph 0048

(2015/12/19)

HEMATOPOIETIC NEOPLASM CHEMOTHERAPY
A method and medicament for treating mixed lineage leukemia; translocated mixed lineage leukemia; translocated mixed lineage leukemia based acute myelogenous leukemia; translocated mixed lineage leukemia based acute lymphoid leukemia; a non-MLL based chronic myeloproliferative disorder, or non-MLL based acute lymphoid leukemia is provided.
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(2010/11/03)

Substituted 3-imidazo[1,2-a]pyridin-3-yl-4-(1,2,3,4-tetrahydro-[1,4] diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3
Glycogen synthase kinase-3 (GSK3) is involved in signaling from the insulin receptor. Inhibitors of GSK3 are expected to effect lowering of plasma glucose similar to insulin, making GSK3 an attractive target for the treatment of type 2 diabetes. Herein we report the discovery of a series of potent and selective GSK3 inhibitors. Compounds 7-12 show oral activity in an in vivo model of type II diabetes, and 9 and 12 have desirable PK properties.
Engler, Thomas A.,Henry, James R.,Malhotra, Sushant,Cunningham, Brian,Furness, Kelly,Brozinick, Joseph,Burkholder, Timothy P.,Clay, Michael P.,Clayton, Joshua,Diefenbacher, Clive,Hawkins, Eric,Iversen, Philip W.,Li, Yihong,Lindstrom, Terry D.,Marquart, Angela L.,McLean, Johnathan,Mendel, David,Misener, Elizabeth,Briere, Daniel,O'Toole, John C.,Porter, Warren J.,Queener, Steven,Reel, Jon K.,Owens, Rebecca A.,Brier, Richard A.,Eessalu, Thomas E.,Wagner, Jill R.,Campbell, Robert M.,Vaughn, Renee
p. 3934 - 3937
(2007/10/03)

Chemical Properties

Density: 1.55±0.1 g/cm3(Predicted)
Solubility:insoluble in H2O; ≥91 mg/mL in DMSO; ≥4.27 mg/mL in EtOH with gentle warming and ultrasonic
Storage Temp.:-20°C
PKA: 7.41±0.60(Predicted)
PSA: 95.44000
LogP: 3.56850

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Chemical Properties

Density: 1.55±0.1 g/cm3(Predicted)

Solubility:insoluble in H2O; ≥91 mg/mL in DMSO; ≥4.27 mg/mL in EtOH with gentle warming and ultrasonic

Storage Temp.:-20°C

PKA: 7.41±0.60(Predicted)

PSA: 95.44000

LogP: 3.56850

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