- An optimized synthesis of the potent and selective Pak1 inhibitor FRAX-1036
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FRAX-1036 is a p21-activated kinase I inhibitor of significant interest to cancer biologists yet no commercial providers or detailed procedures are available. In this Letter, we chronicle the optimized synthesis of FRAX-1036, one of the most specific Pak1
- Koval, Alexander B.,Wuest, William M.
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p. 449 - 451
(2016/01/12)
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- 2- PYRIDONE COMPOUND
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PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT
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- 8-ETHYL-6-(ARYL)PYRIDO [2,3-D]PYRIMIDIN-7(8H) -ONES FOR THE TREATMENT OF NERVOUS SYSTEM DISORDERS AND CANCER
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Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.
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- 2-AMINOBUTANOL COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
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The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect. The present invention provides a 2-aminobutanol compound represented by the following formula (I) wherein R1 is a hydrogen atom or P(=O)(OH)2, R2 is an alkyl having 1 to 4 carbon atoms optionally substituted by hydroxyl group(s) or optionally substituted by halogen atom(s), R3 is a hydrogen atom; a halogen atom; cyano; an alkyl having 1 to 4 carbon atoms optionally substituted by halogen atom(s); or an acyl having 2 to 5 carbon atoms optionally substituted by halogen atom(s), X is an oxygen atom, a sulfur atom, carbonyl or NR4 wherein R4 is a hydrogen atom or an alkyl having 1 to 4 carbon atoms, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, and Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl, provided that when X is an oxygen atom, Ar1 is phenylene and Ar2 is phenyl, then the phenyl for Ar2 should be substituted, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, as well as a production method of the above-mentioned 2-aminobutanol compound.
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Page/Page column 21-22
(2009/02/10)
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