53360-89-7Relevant academic research and scientific papers
PYRAZOLO PYRIMIDINES
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, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
PYRIDO PYRIMIDINES
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, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
CARBOXYLIC ACID ARYL AMIDES
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, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer.
1,6- AND 1,8-NAPHTHYRIDINES
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, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
IMIDAZO PYRAZINES
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, (2012/09/25)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositio
PYRAZOLO PYRIMIDINES AS DYRK1A AND DYRK1B INHIBITORS
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, (2012/08/07)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase
Wittman, Mark D.,Balasubramanian, Balu,Stoffan, Karen,Velaparthi, Upender,Liu, Pieying,Krishnanathan, Subramaniam,Carboni, Joan,Li, Aixin,Greer, Ann,Attar, Ricardo,Gottardis, Marco,Chang, Chiehying,Jacobson, Bruce,Sun, Yax,Hansel, Steven,Zoeckler, Mary,Vyas, Dolatrai M.
, p. 974 - 977 (2007/10/03)
A novel class of 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase is described. This report discusses the SAR of 4-(2-hydroxy-2-phenylethylamino)-substituted pyridones with improved IGF-1R potency.
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route
Blagg, Julian,Allerton, Charlotte M.N.,Batchelor, David V.J.,Baxter, Andrew D.,Burring, Denise J.,Carr, Christopher L.,Cook, Andrew S.,Nichols, Carly L.,Phipps, Joanne,Sanderson, Vivienne G.,Verrier, Hugh,Wong, Stephen
, p. 6691 - 6696 (2008/03/14)
This paper reports the synthesis and biological activity of a novel series of aryl-morpholine dopamine receptor agonists. Several compounds show high levels of functional selectivity for the D3 over the D2 dopamine receptor. Compound 26 has >1000-fold functional selectivity and has been successfully progressed in vivo using an intranasal delivery route.
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Jarvest, Richard L.,Erskine, Symon G.,Forrest, Andrew K.,Fosberry, Andrew P.,Hibbs, Martin J.,Jones, Joanna J.,O'Hanlon, Peter J.,Sheppard, Robert J.,Worby, Angela
, p. 2305 - 2309 (2007/10/03)
High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.
1,4-benzodioxin derivatives
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, (2008/06/13)
PCT No. PCT/JP96/01252 Sec. 371 Date Nov. 12, 1997 Sec. 102(e) Date Nov. 12, 1997 PCT Filed May 13, 1996 PCT Pub. No. WO96/35685 PCT Pub. Date Nov. 14, 1996A 1,4-benzodioxin derivative represented by formula (I) wherein A is an aryl group or a (C3-C8)cycloalkyl group, R1 and R2 individually are a hydrogen atom, a halogen atom, an alkyl group, a trifluoromethyl group, an alkoxy group, an aryl group, an aryloxy group, or R1 and R2 together form a methylenedioxy group, R3 is a hydrogen atom or an alkyl group, R4 is a hydrogen atom or CO2R5, R5 is a hydrogen atom or an alkyl group, X is a radical of formula (II) or (III) wherein n is 1 or 2. The compounds are useful for a prophylactic or therapeutic agent for diabetes, hyperglycemia and obesity.
