- SUBSTITUTED OXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI
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Substituted oxadiazoles for combating phytopathogenic fungi The present invention relates the use of the compounds of the formula I, or the N-oxides, or the agriculturally acceptable salts thereof for combating phytopathogenic harmful fungi. Further, the present invention relates to novel compounds, to mixtures comprising at least one such compound of the formula I and at least one further pesticidally active substance selected from the group consisting of herbicides, safeners, fungicides, insecticides, and plant growth regulators; and to agrochemical compositions comprising at least one such compound of the formula I and to agrochemical compositions further comprising seeds.
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Page/Page column 68
(2017/09/15)
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- Pyrazolo [3, 4 - c] pyridine - 7 - ketone compound and use thereof
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Belonging to the technical field of medicine, the invention relates to a 4, 5-dihydro-1H-pyrazolo[3, 4-c]pyridine-7-one containing derivative shown as general formula I, and pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein the substituents A, R1 and R2 have meanings given in the specification. The preparation also relates to a preparation method of the general formula I compound and its pharmaceutically acceptable salt or prodrug, medicinal compositions containing the compound and application of the compound as an Xa factor inhibitor, especially application in preparation of drugs for treatment and/or prevention of thromboembolic diseases. (formula I).
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Paragraph 0221; 0252; 0499; 0500
(2017/09/01)
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- Design, synthesis, and structure–activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element
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Four series of novel and potent FXa inhibitors possessing the 1,2,4-triazole moiety and pyrrole moiety as P2 binding element and dihydroimidazole/tetrahydropyrimidine groups as P4 binding element were designed, synthesized, and evaluated for their anticoagulant activity in human and rabbit plasma in vitro. Most compounds showed moderate to excellent activity. Compounds 14a, 16, 18c, 26c, 35a, and 35b were further examined for their inhibition activity against human FXa in vitro and rat venous thrombosis in vivo. The most promising compound 14a, with an IC50(FXa) value of 0.15?μM and 99% inhibition rate, was identified for further evaluation as an FXa inhibitor.
- Wang, Yong,Sun, Xiaoqing,Yang, Di,Guo, Zhuang,Fan, Xuxu,Nie, Minhua,Zhang, Feng,Liu, Yue,Li, Yue,Wang, Yulin,Gong, Ping,Liu, Yajing
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p. 5646 - 5661
(2016/10/24)
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- SULFONYL-AMIDINO CONTAINING AND TETRAHYDROPYRIMIDINO CONTAINING COMPOUNDS AS FACTOR XA INHIBITORS
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The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula (I): P4-P-M-M4 or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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