53902-76-4Relevant academic research and scientific papers
HETEROCYCLIC COMPOUND AND USE THEREOF
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Paragraph 0574; 0576-0577, (2019/10/17)
The present invention provides a heterocyclic compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and expected to be useful as an agent for the prophylaxis or treatment of major depression, bipolar disorder, migraine, p
Heteroaryl imidazolone derivatives as jak inhibitors
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Page/Page column 98, (2012/01/06)
New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
HETEROARYL IMIDAZOLONE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 162, (2012/01/06)
New heteroaryl imidazolone derivatives having the chemical structure of formula (I) disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
PYRAZOLE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 100, (2011/09/19)
New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
PYRAZOLE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS
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Page/Page column 89, (2010/04/27)
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
Qiao, Lixin,Choi, Sungwoon,Case, April,Gainer, Thomas G.,Seyb, Kathleen,Glicksman, Marcie A.,Lo, Donald C.,Stein, Ross L.,Cuny, Gregory D.
supporting information; experimental part, p. 6122 - 6126 (2010/06/16)
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.
