- NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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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.
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Paragraph 0396
(2021/11/04)
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- Pyridazine hydrazone derivative and preparation method and application thereof
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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.
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Paragraph 0035-0039
(2020/05/14)
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- Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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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.
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Paragraph 1866; 1868-1870
(2020/08/28)
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- Histone deacetylase inhibitor taking pyridazinone as mother nucleus structure, and preparation method and applications thereof
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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.
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Paragraph 0124-0127
(2019/02/10)
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- Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor
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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.
- 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.
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supporting information
p. 3649 - 3657
(2017/06/13)
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- Intermolecular contacts in the crystal structures of specifically varied halogen and protonic group substituted azines
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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.
- Hübscher, J?rg,Seichter, Wilhelm,Weber, Edwin
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p. 3026 - 3036
(2017/07/10)
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- Selective mono-amination of dichlorodiazines
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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
- Sengmany, Stéphane,Lebre, Julie,Le Gall, Ewan,Léonel, Eric
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p. 4859 - 4867
(2015/08/03)
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- Copper-catalyzed aerobic dehydrogenation of C-C to C=C bonds in the synthesis of pyridazinones
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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.
- Liang, Lei,Yang, Guanyu,Xu, Fengrong,Niu, Yan,Sun, Qi,Xu, Ping
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supporting information
p. 6130 - 6136
(2013/09/24)
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- INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1
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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.
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Page/Page column 26
(2012/05/07)
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- Identification of triazolopyridazinones as potent p38α inhibitors
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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
- 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.
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experimental part
p. 1226 - 1229
(2012/03/26)
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- Efficient and selective demethylation of heteroaryl methyl ethers in the presence of aryl methyl ethers
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A new and efficient method for the demethylation of 6-membered aza-heterocyclic methyl ethers is described using lithium chloride and para-toluenesulfonic acid. This process is chemoselective for aza-heterocyclic methyl ethers in the presence of aryl methyl ethers.
- Soni, Ajay,Dutt, Akhilesh,Sattigeri, Viswajanani,Cliffe, Ian A.
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experimental part
p. 1852 - 1857
(2011/06/20)
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- Synthesis of functionalized pyridazin-3(2 H)-ones via nucleophilic substitution of hydrogen (SNH)
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Reaction of 2-benzyl-5-halopyridazin-3(2H)-ones (3) with Grignard reagents followed by quenching with electrophiles unexpectedly yielded 4,5-disubstituted pyridazin-3(2H)-ones instead of 5-substituted pyridazin-3(2H)-ones. These reactions represent the fi
- Verhelst, Tom,Verbeeck, Stefan,Ryabtsova, Oxana,Depraetere, Stefaan,Maes, Bert U. W.
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supporting information; experimental part
p. 272 - 275
(2011/04/22)
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- DERIVATIVES OF 2H PYRIDAZIN- 3 -ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS
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The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: -R1 represents one or more groups such as: trif luoromethyl, halogen such as F, C1, -when n=m=1, W represents CH then Y represents oxygen, -U represents: ? either - (C=O) CH2NH- and is branched at position 4 of pyridazinone, then R2 represents H, ? or -(C=O)NH- and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, - R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enyzme inhibitors for the treatment of obesitz, tzpe-2 diabetes and lipid disorders.
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Page/Page column 68
(2011/02/24)
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- Concise routes to pyrazolo[1,5-a]pyridin-3-yl pyridazin-3-ones
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Cycloaddition of pyridine N-imine with 6-alkyl-4-oxohex-5-ynoates followed by condensation with hydrazine provides concise access to pharmacologically active 6-(pyrazolo[1,5-a]pyridin-3-yl)pyridazinones. For the first time alkynyl heterocycles are also shown to be effective dipolarophiles for pyridine N-imine, and analogous compounds can be accessed directly in modest yields through the reaction of 6-(alkyn-1-yl)pyridazin-3-one derivatives. The Royal Society of Chemistry 2008.
- Johnston, Karen A.,Allcock, Robert W.,Jiang, Zhong,Collier, Ian D.,Blakli, Haakon,Rosair, Georgina M.,Bailey, Patrick D.,Morgan, Keith M.,Kohno, Yasushi,Adams, David R.
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p. 175 - 186
(2008/09/20)
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- HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA
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The invention relates to compounds of formula (I), Chemical formula should be inserted here. Please see paper copy wherein R1 is hydrogen, C1-3alkyl, R5R6 aminoC1-5alkyl, where R5 and R6 are each independently selected from hydrogen and C1-3alkyl, or R5 and R6 may, together with the nitrogen to which they are attached, form a five- or six-membered heterocyclic ring, where said heterocyclic ring has 0 or 1 additional heteroatom; n is 1 or 2; each R2 are independently selected from hydrogen, oxo and C1-3alkyl, R3 is an indolyl, and R4 a hydrogen or a halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
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Page/Page column 31
(2010/11/25)
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- NEW DERIVATIVES OF 6-4{4-[1H-INDOLE-2-SULPHONYL)-PIPERAZIN-1-CARBONYL-PHENYL]}PYRADIZIN-3-ONE
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The invention relates to heterocyclic derivatives of formula (I), wherein R2 is amino, a group OR4 or a group -Y-R5 where R4 is hydrogen or C1-4alkyl, Y is C1-4alkylene, R5 is hy
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Page/Page column 20
(2010/02/12)
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- Polymorph-specific chlorination of maleic-hydrazide
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The reaction of chlorination of maleic-hydrazide (1) with POC13 is specific to the substrate polymorph. Chlorination of either the triclinic polymorph of maleic-hydrazide (1), denoted MH1, or the monoclinic polymorph MH2 leads to a single product of 3,6-dichloropyridazine (2), while chlorination of the monoclinic polymorph MH3 under the same conditions results in two products: 3,6-dichloropyridazine (2) and 6-chloro-3-pyridazinone (3). The structural differences between polymorphs and their topochemical chlorination in phosphorus oxychloride are discussed. The crystal structure of 6-chloro-3-pyridazinone (3) monohydrate, determined in this study by X-ray diffraction, is built of ribbons of hydrogen-bonded 3 and water molecules. It has been established that the chlorination of ground crystals of polymorph MH3 yields exclusively the dichloropyridazine, which suggests that the crystal habit of MH3, the size of crystallites and the lower solubility of MH3 than MH1 and MH2 are the main reasons for the different course of the reaction.
- Katrusiak, Andrzej,Katrusiak, Anna
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p. 203 - 210
(2007/10/03)
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- The Mechanism of Thermal Eliminations. Part 18. Relative Rates of Pyrolysis of 2-Ethoxypyrazine, 3-Ethoxypyridazine, 2-and 4-Ethoxypyrimidine, 3-Chloro-6-ethoxypyridazine, and 2-Chloro-4-ethoxypyrimidine : the Effect of the Aza 'Substituent' and ?-Bond Order on the Elimination Rate
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A kinetic study has been made of the first-order thermal decomposition of the title compounds into ethylene and the corresponding aza-substituted pyridines, between 650 and 713 K.The relative elimination rates at 650 K are (2-ethoxypyridine = 1): 0.545, 10.0, 1.03, 1.12, 9.68, and 3.28, respectively.The electronic effects of the aza 'substituent' are small, and a more important factor appears to be the C-N ?-bond order; this latter accounts for the high reactivity of the pyridazines.The effects of the chloro substituent and of the aza 'substituent' are explicable in terms of a balance between electron withdrawal from the C-O bond (producing deactivation) and from the nitrogen involved in the cyclic transition state (producing deactivation).The effects of the chloro substituents confirm that the most important step of the reaction is breaking of the C-O bond.The statistically corrected rate (per ring nitrogen) of 2-ethoxypyrimidine is unexpectedly low.This may reflect difficulty in achieving the coplanar transition state in which the lone pairs in the s-orbitals of oxygen and the nitrogen not involved in the elimination are brought into close proximity.
- Al-Awadi, Nouria,Taylor, Roger
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p. 1255 - 1258
(2007/10/02)
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- 7-[α-(2-Aminomethyl-1-cyclohexenyl)-acetamido]-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acids
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7-[α-(2-Aminomethyl-1-cyclohexyl)-acetamido]-3-heterocyclic thiomethyl-3-cephem-4-carboxylic acids, and their nontoxic, pharmaceutically acceptable salts and their Schiff bases, as made by reaction of salicylaldehyde with the free amino group, are valuable as antibacterial agents and are particularly valuable as therapeutic agents in poultry and animals, including man, in the treatment of infectious diseases caused by many Gram-positive and Gram-negative bacteria.
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