2271-72-9Relevant academic research and scientific papers
Novel 1,4-benzoxazine and 1,4-benzodioxine inhibitors of angiogenesis
Ili?, Milo?,Ila?, Janez,Dunkel, Petra,Mátyus, Péter,Bohá?, Andrej,Liekens, Sandra,Kikelj, Danijel
, p. 160 - 170 (2013/02/23)
Esters of 1,4-benzoxazine and 1,4-benzodioxine compounds 1 and 10, which combine thrombin inhibitory and GPIIb/IIIa antagonistic activity in one molecule are shown to inhibit endothelial cell migration and tube formation in vitro and angiogenesis in the c
Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Page/Page column 55, (2008/06/13)
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
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Page/Page column 31-32, (2010/11/23)
Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.
Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1
Tavares, Francis X.,Al-Barazanji, Kamal A.,Bigham, Eric C.,Bishop, Michael J.,Britt, Christy S.,Carlton, David L.,Feldman, Paul L.,Goetz, Aaron S.,Grizzle, Mary K.,Guo, Yu C.,Handlon, Anthony L.,Hertzog, Donald L.,Ignar, Diane M.,Lang, Daniel G.,Ott, Ronda J.,Peat, Andrew J.,Zhou, Hui-Qiang
, p. 7095 - 7107 (2008/04/18)
The high expression of MCH in the hypothalamus with the lean hypophagic phenotype coupled with increased resting metabolic rate and resistance to high fat diet-induced obesity of MCH KO mice has spurred considerable efforts to develop small molecule MCHR1 antagonists. Starting from a lead thienopyrimidinone series, structure-activity studies at the 3- and 6-positions of the thienopyrimidinone core afforded potent and selective MCHR1 antagonists with representative examples having suitable pharmacokinetic properties. Based on structure-activity relationships, a structural model for MCHR1 was constructed to explain the binding mode of these antagonists. In general, a good correlation was observed between pKas and activity in the right-hand side of the template, with Asp123 playing an important role in the enhancement of binding affinity. A representative example when evaluated chronically in diet-induced obese mice resulted in good weight loss effects. These antagonists provide a viable lead series in the discovery of new therapies for the treatment of obesity.
Melanin concentrating hormone antagonist
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Page/Page column 86-87, (2010/11/23)
A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms;Y is a bond or a spacer having a main chain of 1
Amino-substituted dihydropyrimido[4,5-D]pyrimidinone derivatives
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Page 16, (2010/11/30)
Compounds of formula I are described. These compounds are protein kinase inhibitors, in particular they inhibit the src family tyrosine kinases. Thus, these compounds are useful for the treatment of diseases mediated by src tyrosine kinases, including cel
