- PYRIDIN-2-ONE DERIVATIVES OF FORMULA (II) USEFUL AS EP3 RECEPTOR ANTAGONISTS
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The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
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- PYRIDIN-2-ONE DERIVATIVES OF FORMULA (III) USEFUL AS EP3 RECEPTOR ANTAGONISTS
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The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
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- PYRIDIN-2-ONE DERIVATIVES OF FORMULA (I) USEFUL AS EP3 RECEPTOR ANTAGONISTS
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The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
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- Structure-Guided Design of Group i Selective p21-Activated Kinase Inhibitors
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The p21-activated kinases (PAKs) play important roles in cytoskeletal organization, cellular morphogenesis, and survival and have generated significant attention as potential therapeutic targets for cancer. Following a high-throughput screen, we identified an aminopyrazole scaffold-based series that was optimized to yield group I selective PAK inhibitors. A structure-based design effort aimed at targeting the ribose pocket for both potency and selectivity led to much-improved group I vs II selectivity. Early lead compounds contained a basic primary amine, which was found to be a major metabolic soft spot with in vivo clearance proceeding predominantly via N-acetylation. We succeeded in identifying replacements with improved metabolic stability, leading to compounds with lower in vivo rodent clearance and excellent group I PAK selectivity.
- Crawford, James J.,Lee, Wendy,Aliagas, Ignacio,Mathieu, Simon,Hoeflich, Klaus P.,Zhou, Wei,Wang, Weiru,Rouge, Lionel,Murray, Lesley,La, Hank,Liu, Ning,Fan, Peter W.,Cheong, Jonathan,Heise, Christopher E.,Ramaswamy, Sreemathy,Mintzer, Robert,Liu, Yanzhou,Chao, Qi,Rudolph, Joachim
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p. 5121 - 5136
(2015/07/02)
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- SERINE/THREONINE PAK1 INHIBITORS
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Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.
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- NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS FOR OPIOID RECEPTORS
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This invention relates to novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy.
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Page/Page column 90; 91
(2010/09/07)
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