37972-69-3Relevant articles and documents
Synthesis of 3-chloropyridazine-6-carboxylic acid hydrazide and selective hydrazinolysis of 3,6-substituted pyridazines
Morishita,Kobayashi,Yamada,Yajima
, p. 371 - 372 (1994)
3-Chloropyridazine-6-carboxylic acid hydrazide (5) was synthesized by employing hydrazine monohydrate and methyl levalinate as starting materials through five steps, including hydrazinolysis. Selective hydrazinolysis of 3,6-substituted pyridazines was investigated.
METHODS OF MANUFACTURING A BIFUNCTIONAL COMPOUND, ULTRAPURE FORMS OF THE BIFUNCTIONAL COMPOUND, AND DOSAGE FORMS COMPRISING THE SAME
-
, (2021/11/20)
The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A: The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.
VINYL COMPOUNDS AS FGFR AND VEGFR INHIBITORS
-
, (2018/06/23)
FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies
Qian, Hai-Yan,Wang, Zhi-Long,Xie, Xiao-Yu,Pan, You-Lu,Li, Gang-Jian,Xie, Xin,Chen, Jian-Zhong
, p. 598 - 611 (2017/06/29)
Herein, we described the design and synthesis of a series of pyridazine-3-carboxamides to be CB2-selective agonists via a combination of scaffold hopping and bioisosterism strategies. The compounds were subjected to assessment of their potential activities through calcium mobilization assays. Among the tested derivatives, more than half of these compounds exhibited moderate to potent CB2 agonist activity. Six compounds showed EC50 values below 35 nM, and several derivatives also exhibited significantly enhanced potency and high selectivity at the CB2 receptor over the CB1 receptor. Specifically, compound 26 showed the highest CB2 agonist activity (EC50 = 3.665 ± 0.553 nM) and remarkable selectivity (Selectivity Index > 2729) against CB1. In addition, logPs of some representative compounds were measured to display significantly decreased values in comparison with GW842166X. Furthermore, docking simulations were conducted to explain the interaction mode of this series.
Pyridazine derivative and preparation method and application thereof
-
, (2017/02/17)
The invention provides a pyridazine derivative and a pharmaceutically acceptable salt or hydrate of the pyridazine derivative. The compound is an active ligand of a novel cannabinoid II type receptor CB2. The compound and the pharmaceutically acceptable salt or hydrate of the compound generally have high calcium current activity and quite good selectivity for anthropogenic marijuana receptors CB2. The compound is a specificity agonist of the cannabinoid receptor CB2, and can be used for treating, preventing and inhibiting diseases mediated by CB2 receptors. The compound I has the general formula shown in the description.
TBK/IKK INHIBITOR COMPOUNDS AND USES THEREOF
-
Paragraph 1225; 1226, (2017/01/23)
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TBK/IKKε inhibitors.
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.
