19064-67-6Relevant articles and documents
NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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Paragraph 0396, (2021/11/04)
The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
Pyridazine hydrazone derivative and preparation method and application thereof
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Paragraph 0035-0039, (2020/05/14)
The invention relates to a pyridazine hydrazone derivative shown as a chemical structural formula I and a pharmaceutically acceptable salt thereof, a pharmaceutical composition and application thereofin preparation of an influenza virus neuraminidase inhibitor, wherein Y is selected from the group consisting of: hydroxyl, dihydroxyl, 2-hydroxyl-3-methoxy, 2-hydroxyl-4-methoxy, 2-hydroxyl-5-methoxy, 2-hydroxyl-6-methoxy, 3-hydroxyl-2-methoxy, 3-hydroxyl-4-methoxy, 3-hydroxyl-5-methoxy, 3-hydroxyl-6-methoxy, 4-hydroxyl-2-methoxy, 4-hydroxyl-3-methoxy, 4-hydroxyl-3, 5-dimethoxy, 2-hydroxyl-3-ethoxy, 2-hydroxy-4-ethyoxyl, 2-hydroxy-5-ethyoxyl, 2-hydroxy-6-ethyoxyl, 3-hydroxy-2-ethyoxyl, 3-hydroxy-4-ethyoxyl, 3-hydroxy-5-ethyoxyl, 3-hydroxy-6-ethyoxyl, 4-hydroxy-2-ethyoxyl, 4-hydroxy-3-ethyoxyl, 4-hydroxy-3, 5-diethyoxyl, trihydroxy or 4-hydroxy-3, 5-dimethyl.
Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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Paragraph 1866; 1868-1870, (2020/08/28)
The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
Histone deacetylase inhibitor taking pyridazinone as mother nucleus structure, and preparation method and applications thereof
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Paragraph 0124-0127, (2019/02/10)
The invention discloses a histone deacetylase inhibitor taking pyridazinone as a mother nucleus structure, and a preparation method and applications thereof. The structure of the inhibitor is shown asa formula I; and the compound shown as the formula I has good histone deacetylase inhibitory activity and anti-tumor cell proliferation effects, and can be used for treating cancers. The structure ofthe inhibitor is shown as the formula I.
Intermolecular contacts in the crystal structures of specifically varied halogen and protonic group substituted azines
Hübscher, J?rg,Seichter, Wilhelm,Weber, Edwin
, p. 3026 - 3036 (2017/07/10)
A series of azines featuring differently halogen and protic group substituted pyridine, pyrimidine and pyridazine compounds have been synthesized and studied in terms of their crystal structures in order to develop a better understanding of the links between structural conditions and molecular packing behavior. Complemented by the structure results of related compounds known from the literature, intermolecular contact relationships connected to the present substance types were found, having potential use in future crystal engineering of similar compounds. This primarily involves the formation of N?I contacts aside from specific halogen?halogen and hydrogen bond type interactions.
Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor
Zhuang, Linghang,Tice, Colin M.,Xu, Zhenrong,Zhao, Wei,Cacatian, Salvacion,Ye, Yuan-Jie,Singh, Suresh B.,Lindblom, Peter,McKeever, Brian M.,Krosky, Paula M.,Zhao, Yi,Lala, Deepak,Kruk, Barbara A.,Meng, Shi,Howard, Lamont,Johnson, Judith A.,Bukhtiyarov, Yuri,Panemangalore, Reshma,Guo, Joan,Guo, Rong,Himmelsbach, Frank,Hamilton, Bradford,Schuler-Metz, Annette,Schauerte, Heike,Gregg, Richard,McGeehan, Gerard M.,Leftheris, Katerina,Claremon, David A.
supporting information, p. 3649 - 3657 (2017/06/13)
A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (11j) has been identified. Compound 11j inhibited 11β HSD1 activity in human adipocytes with an IC50 of 4.3?nM and in primary human adipose tissue with an IC80 of 53?nM. Oral administration of 11j to cynomolgus monkey inhibited 11β HSD1 activity in adipose tissue. Compound 11j exhibited >1000× selectivity over other hydroxysteroid dehydrogenases, displays desirable pharmacodynamic properties and entered human clinical trials in 2011.
Selective mono-amination of dichlorodiazines
Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
, p. 4859 - 4867 (2015/08/03)
A mild, easy-to-perform, and versatile method for the formation of aminochlorodiazines from reaction of several types of dichlorodiazines (i.e., pyridazines, pyrimidines, and pyrazines) with primary or secondary amines in ethanol in the presence of trieth
Copper-catalyzed aerobic dehydrogenation of C-C to C=C bonds in the synthesis of pyridazinones
Liang, Lei,Yang, Guanyu,Xu, Fengrong,Niu, Yan,Sun, Qi,Xu, Ping
supporting information, p. 6130 - 6136 (2013/09/24)
A simple and efficient procedure for the synthesis of pyridazin-3(2H)-ones through copper-catalyzed dehydrogenation of a single C-C bond of 4,5-dihydropyridazin-3(2H)-ones to a C=C bond with oxygen as the terminal oxidant is described. Functional groups including hydroxy, carboxylic, bromo, chloro, cyano, nitro and alkoxy were all tolerated under the reaction conditions. Moreover, this methodology was applied to the preparation of a series of structurally similar N-substituted 6-phenylpyridazinone compounds containing fluorine. The dehydrogenation reactions exhibit good yields and selectivity. Copper-catalyzed dehydrogenation of a C-C bond of 4,5-dihydropyridazinones to a C=C bond with oxygen as the terminal oxidant is described. Various functional groups were tolerated under the reaction conditions. The method was also applied to the preparation of a series of N-substituted 6-phenylpyridazinones containing fluoride. The dehydrogenation reactions exhibit good yields and selectivity.
INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 26, (2012/05/07)
This invention relates to novel compounds of the Formula (I), (Ia1-10), (Ib1-10), (Ic1-10), (Id1-7), (Ie1-5) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
Identification of triazolopyridazinones as potent p38α inhibitors
Herberich, Brad,Jackson, Claire,Wurz, Ryan P.,Pettus, Liping H.,Sherman, Lisa,Liu, Qiurong,Henkle, Bradley,Saris, Christiaan J.M.,Wong, Lu Min,Chmait, Samer,Lee, Matthew R.,Mohr, Christopher,Hsieh, Faye,Tasker, Andrew S.
experimental part, p. 1226 - 1229 (2012/03/26)
Structure-activity relationship (SAR) investigations of a novel class of triazolopyridazinone p38α mitogen activated protein kinase (MAPK) inhibitors are disclosed. From these studies, increased in vitro potency was observed for 2,6-disubstituted phenyl m