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Relevant academic research and scientific papers

PYRAZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS

The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10- alkenyl, C2-C10-alkynyl, etc.; n is 0 to 4; or two radicals Rpx bound to the same ring- member may form an oxo substituent, or two radicals Rpx bound to adjacent ring- members may form a 3- to 7-membered fused cyclic radical; B is N or CR4, wherein R4 is H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkyl, etc.; X2 is O2a, NR2bR2c or S(O)mR2d, wherein m is 0, 1 or 2; R2a is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2b, R2c are H, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R2d is C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, etc.; R1 is H, CN, C1-C10-alkyl, C1-C10-haloalkyl, C3-C10-cycloalkyl, etc.; R2, R3 and R5 are H, halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, etc.; to a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material comprising at least one compound of formulae I or II, to a method for treating or protecting an animal from infestation or infection by parasites, to novel pyrazole compounds of formulae I or Il and agricultural composition containing those compounds.

Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors

A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a phenyl or small electron donating substituents to the 5-position of the pyrazolo[1,5-a]pyridine. In addition, replacement of the pyrazolo[1,5-a]pyridine with imidazo[1,2-a]pyridine was well tolerated and resulted in enhanced mouse liver microsome stability. The structure-activity relationship for EphB3 inhibition of both heterocyclic series was similar. Kinase inhibitory activity was also demonstrated for representative analogs in cell culture. An analog (32, LDN-211904) was also profiled for inhibitory activity against a panel of 288 kinases and found to be quite selective for tyrosine kinases. Overall, these studies provide useful molecular probes for examining the in vitro, cellular and potentially in vivo kinase-dependent function of EphB3 receptor.