- NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
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- NOVEL COMPOUNDS AS MODULATORS OF PROTEIN KINASES
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The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
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- Chromenones as potent bradykinin B1 antagonists
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A series of fused 6,6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. These compounds demonstrated favorable pharmacokinetic properties and 5-chlorochromenone 15 was efficacious in a carrageenan-induced mechanical hyperalgesia model for chronic pain.
- Bryan, Marian C.,Biswas, Kaustav,Peterkin, Tanya A.N.,Rzasa, Robert M.,Arik, Leyla,Lehto, Sonya G.,Sun, Hong,Hsieh, Feng-Yin,Xu, Cen,Fremeau, Robert T.,Allen, Jennifer R.
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p. 619 - 622
(2012/02/04)
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- Hydroxylated nebivolol metabolites
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Hydroxylated nebivolol metabolites increase NO release from human endothelial cell preparations in a concentration dependent fashion following acute administration. In addition, hydroxylated nebivolol metabolites, including but not limited to 4-hydroxy-6,6′difluoro-, 4-hydroxy-5-phenol-6,6′difluoro-, and 4-hydroxy-8-pheno-6,6′difluoro-, have the ability to increase the capacity for NO release in human endothelial cells following chronic administration. This invention provides hydroxylated nebivolol metabolites and compositions comprising nebivolol and/or at least one hydroxylated metabolite of nebivolol and/or at least one additional compound used to treat cardiovascular diseases or a pharmaceutically acceptable salt thereof. In addition, this invention provides methods of treating and/or preventing vascular diseases by administering at least one hydroxylated metabolite of nebivolol that is capable of releasing a therapeutically effective amount of nitric oxide to a targeted site affected by the vascular disease. Also, this invention is directed to the treatment and/or prevention of migraine headaches administering at least one hydroxylated metabolite of nebivolol. This invention may also be used in conjunction with or as a single treatment of metabolic syndrome disorders.
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- Use of flavone derivatives for gastroprotection
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The subject invention relates to methods for preventing or treating damage to the mucosal lining of the gastrointestinal tract of a human or lower animal by administering a safe and effective amount of a compound having the structure: STR1 wherein X and Y are each independently selected from O and S; R1, R2 and R3 are each independently selected from hydrogen, hydroxy, halo, unsubstituted or monosubstituted straight or branched C1 -C4 alkanyl, and unsubstituted or substituted straight or branched C1 -C4 alkanoxy; and each of R4, R5, R6 and R7 is hydrogen or, if one or more of R1, R2 and R3 is other than hydrogen, each of R4, R5, R6 and R7 is selected from hydrogen, halo, trifluoromethyl, and unsubstituted straight or branched C1 -C4 alkanyl.
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