- PYRIDAZINONE DERIVATIVES
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The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as medicaments
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Page/Page column 109; 110; 117-118; 119
(2010/06/20)
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- Design, synthesis, and biological evaluation of novel 2-pyridinyl-[1,2,4] triazoles as inhibitors of transforming growth factor β1 type 1 receptor
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A series of 2-pyridinyl-[1,2,4]triazoles have been synthesized and evaluated for their ALK5 inhibitory activity in the luciferase reporter assays. Compound 12b showed significant ALK5 inhibition (SBE-Luciferase, 73%; p3TP-Luciferase, 85%) at a concentration of 5μM that is comparable to that of SB-431542 (SBE-Luciferase, 79%; p3TP-Luciferase, 88%), but weak p38α MAP kinase inhibition (4%) at a concentration of 10μM that is much lower than that of SB-431542 (54%). The binding mode of 12b generated by flexible docking studies revealed that the structure of 12b is a good fit into the (NPC-30345)-binding cavity of ALK5.
- Kim, Dae-Kee,Kim, Joonseop,Park, Hyun-Ju
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p. 2013 - 2020
(2007/10/03)
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- Thrombopoietin mimetics
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Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
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