- N-Difluoromethylation of imidazoles and pyrazoles using BrCF2PO(OEt)2 under mild condition
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A simple and efficient protocol for the direct N-difluoromethylation of imidazoles and pyrazoles has been developed. The reaction makes use of commercially available, non-ozone-depleting and easy handling BrCF2PO(OEt)2 as difluorocarbene precursor, and provides a cost-efficient and environmentally benign access to some difluoromethylated biologically relevant molecules.
- Mao, Ting,Zhao, Liang,Huang, Yang,Lou, Yue-Guang,Yao, Qiuli,Li, Xiao-Fei,He, Chun-Yang
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Read Online
- [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
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Page/Page column 343-344
(2021/02/19)
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- COMPOUNDS USEFUL AS CSF1 MODULATORS
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This invention relates to novel compounds and to pharmaceutical compositions comprising the novel compounds. More specifically, the invention relates to compounds useful as Colony Stimulating Factor 1 Receptor (cFMS) modulators (e.g. cFMS inhibitors). This invention also relates to processes for preparing the compounds, uses of the compounds in treatment and methods of treatment employing the compounds. Specifically, the invention relates to the use of the compounds for the treatment of cancer and autoimmune diseases.
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Paragraph 00578; 00579; 00580
(2016/04/26)
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- Herbicide compositions
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A herbicidal composition which comprises i) an isoxazoline derivative represented by the following general formula (I) or its salt and ii) at least one compound selected from the Group A: Formula (I) wherein R1, R2, R3, R4, R5 and R6 are defined in the specification.
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Page/Page column 37
(2010/02/14)
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- ISOXAZOLINE DERIVATIVE AND HERBICIDE COMPRISING THE SAME AS ACTIVE INGREDIENT
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An isoxazoline derivative represented by the following general formula [I]: wherein R1 and R2 may be the same or different and are each an alkyl group; ???R3, R4, R5 and R6 are each a hydrogen atom; ???Y is an optionally substituted 5- to 6-membered aromatic heterocyclic group or fused aromatic heterocyclic group having a hetero atom selected from a nitrogen atom, a oxygen atom and a sulfur atom; and ???n is an integer of 0 to 2. The isoxazoline derivative has an excellent herbicidal effect and an excellent selectivity between crop and weed.
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Page/Page column 204
(2010/02/07)
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- Synthesis of Fluoromethyl, Difluoromethyl and Trifluoromethyl Analogues of Pyrazosulfuron-ethyl as Herbicides
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Ethyl 1-fluoromethyl-5-(4,6-dimethoxypyrimidin-2-ylcarbamoylsulfamoyl)pyrazole-4-carboxylate 1b, a new fluoromethyl analogue of the herbicide pyrazosulfuron-ethyl 1a, was prepared from ethyl 1-fluoromethylpyrazole-4-carboxylate 4b.The difluoromethyl and trifluoromethyl analogues 1c,d were also synthesized from ethyl pyrazole-4-carboxylate 2 via difluorocarbene reaction.
- Morimoto, Katsushi,Makino, Kenzi,Yamamoto, Susumu,Sakata, Gozyo
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p. 807 - 810
(2007/10/02)
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