- POLYCYCLIC PYRAZOLINONE DERIVATIVE AND HERBICIDE COMPRISING SAME AS EFFECTIVE COMPONENT THEREOF
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Provided are a polycyclic pyrazolinone derivative indicated by general formula (1) (in the formula, R1, X1, X2, X3, and Y indicate the definitions provided in the Specification) and a herbicide comprising same as effective component thereof.
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Paragraph 0586; 0589
(2016/02/19)
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- PYRAZOLINE-3-ON DERIVATIVE AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT
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PROBLEM TO BE SOLVED: To provide a compound having excellent weed controlling effect and useful as an active ingredient of a herbicide. SOLUTION: There are provided a pyrazoline-3-on derivative represented by the following formula (1), where R1
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Paragraph 0165
(2016/10/08)
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- PYRAZOLINONE DERIVATIVE, MANUFACTURING METHOD THEREFOR AND HERBICIDE CONTAINING THE SAME AS ACTIVE INGREDIENT
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PROBLEM TO BE SOLVED: To provide a compound having excellent weed controlling effect and useful as an active ingredient of a herbicide. SOLUTION: There are provided a pyrazolinone derivative represented by the formula (1), a manufacturing method therefor and herbicide containing the same. (1), where R1 is a halogen atom, R2 and R3 are integrally a trimethylene group (-(CH2)3-), a tetramethylene group (-(CH2)4-), a pentamethylene group (-(CH2)5-) or an oxydiethylene group (-(CH2)2O(CH2)2-), R4 is H or a halogen atom, R5 is a halogen atom, Ar is 3-oxo-1,4-benzoxazine-5-yl group, a 2,2-difluoro-3-oxo-1,4-benzoxazine-5-yl group or a 3,4-dihydro-2-oxo quinoxaline-5-yl group. SELECTED DRAWING: None COPYRIGHT: (C)2016,JPOandINPIT
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Paragraph 0245
(2016/10/09)
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- Isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones as unique, potent and selective inhibitors for Pim-1 and Pim-2 kinases: Chemistry, biological activities, and molecular modeling
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A series of isoxazolo[3,4-b]quinoline-3,4(1H,9H)-diones were synthesized as potent inhibitors against Pim-1 and Pim-2 kinases. The structure-activity-relationship studies started from a high-throughput screening hit and was guided by molecular modeling of inhibitors in the active site of Pim-1 kinase. Installing a hydroxyl group on the benzene ring of the core has the potential to form a key hydrogen bond interaction to the hinge region of the binding pocket and thus resulted in the most potent inhibitor, 19, with Ki values at 2.5 and 43.5 nM against Pim-1 and Pim-2, respectively. Compound 19 also exhibited an activity profile with a high degree of kinase selectivity.
- Tong, Yunsong,Stewart, Kent D.,Thomas, Sheela,Przytulinska, Magdalena,Johnson, Eric F.,Klinghofer, Vered,Leverson, Joel,McCall, Owen,Soni, Niru B.,Luo, Yan,Lin, Nan-horng,Sowin, Thomas J.,Giranda, Vincent L.,Penning, Thomas D.
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scheme or table
p. 5206 - 5208
(2009/05/07)
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- 2-(POLY-SUBSTITUTED ARYL)-6-AMINO-5-HALO-4-PYRIMIDINECARBOXYLIC ACIDS AND THEIR USE AS HERBICIDES
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6-Amino-5-halo-4-pyrirnidinecarboxylic acids having poly-substituted aryl substituents in the 2-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
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Page/Page column 26
(2008/06/13)
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- 6-(Poly-substituted aryl)-4-aminopicolinates and their use as herbicides
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4-Aminopicolinic acids having tri- and tetra-substituted aryl substituents in the 6-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.
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Page/Page column 8
(2008/06/13)
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- Substituted piperazines
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Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
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